SK4032003A3 - Association of the CB1 receptor antagonist and sibutramin, for treating obesity - Google Patents

Association of the CB1 receptor antagonist and sibutramin, for treating obesity Download PDF

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SK4032003A3
SK4032003A3 SK403-2003A SK4032003A SK4032003A3 SK 4032003 A3 SK4032003 A3 SK 4032003A3 SK 4032003 A SK4032003 A SK 4032003A SK 4032003 A3 SK4032003 A3 SK 4032003A3
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methyl
chlorophenyl
bis
methylsulfonyl
azetidine
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Odile Piot-Grosjean
Philippe Picaut
Francois Petitet
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Aventis Pharma Sa
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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Abstract

The invention concerns the association of the CB1 receptor antagonist and a sibutramin, pharmaceutical compositions containing same and use thereof for treating obesity.

Description

Kombinácia antagonistu receptora CBl a sibutramínu, farmaceutická kompozícia, ktorá ju obsahuje, a jej použitie pri liečbe obezityCombination of CB1 receptor antagonist and sibutramine, pharmaceutical composition containing it, and its use in the treatment of obesity

Oblasť technikyTechnical field

Predkladaný vynález sa týka kombinácie antagonistu receptora CBl a sibutramínu, farmaceutických prostriedkov, ktoré ju obsahujú, a jej použitia pri liečbe obezity.The present invention relates to a combination of a CB1 receptor antagonist and sibutramine, pharmaceutical compositions containing it, and its use in the treatment of obesity.

Doterajší stav technikyBACKGROUND OF THE INVENTION

Antagonisty receptora CBl sú známe pre svoj účinok na príjem potravy a ich použitie ako anorexigénne činidlá (G. Colombo a kol., Life Sciences, 63 (8), 113-117 (1998); J. Siamand a kol., Behavioural Pharmacol., 9, 179-181 (1998)).CB1 receptor antagonists are known for their effect on food intake and their use as anorexigenic agents (G. Colombo et al., Life Sciences, 63 (8), 113-117 (1998); J. Siamand et al., Behavioral Pharmacol. 9: 179-181 (1998)).

Sibutramín (BTS 54524; N-{1-[1-(4-chlórfenyl)cyklobutyl]-3-metylbutyl}-N,N-dimetylamín; Meridia®, Reductil®), jeho hydrát a jeho farmaceutický pŕijatelné soli a najmä jeho hydrochlorid, znižuje príjem potravy a používa sa pri liečbe obezity (WO 90/061110; D. H. Ryan a kol., Obesity Research, 3 (4), 553 (1995); H. C. Jackson a kol., British Journal of Pharmacology, 121, 1758 (1997); G. Fanghanel a kol., Inter. J. Obes., 24 (2), 144 (2000); G. A. Bray a kol., Obes. Res., 7 (2), 189 (1999)).Sibutramine (BTS 54524; N- {1- [1- (4-chlorophenyl) cyclobutyl] -3-methylbutyl} -N, N-dimethylamine; Meridia®, Reductil®), its hydrate and its pharmaceutically acceptable salts, and in particular its hydrochloride , decreases food intake and is used in the treatment of obesity (WO 90/061110; DH Ryan et al., Obesity Research, 3 (4), 553 (1995); HC Jackson et al., British Journal of Pharmacology, 121, 1758 ( G. Fanghanel et al., Inter J. Obes., 24 (2), 144 (2000); GA Bray et al., Obes. Res., 7 (2), 189 (1999)).

Podstata vynálezuSUMMARY OF THE INVENTION

Teraz sa zistilo, že kombinácia sibutramínu, jeho hydrátu a jeho farmaceutický prijateľných solí a antagonistu receptora CBl sa vyznačuje synergickým účinkom v znížení príjmu potravy, a preto sa používa pri liečbe obezity.It has now been found that the combination of sibutramine, its hydrate and its pharmaceutically acceptable salts and a CB1 receptor antagonist has a synergistic effect in reducing food intake and is therefore used in the treatment of obesity.

Kombinácia môže obsahovať aj niekolko antagonistov receptoraThe combination may also contain several receptor antagonists

CB1.CB1.

Z antagonistov CB1 sa môžu použiť najmä deriváty azetidinu sané vo WO 00/15609, WO 01/64633 a WO 01/64634 všeobecného opísané v< vzorca (I)Among the CB1 antagonists, in particular, the azetidine derivatives disclosed in WO 00/15609, WO 01/64633 and WO 01/64634 of general formula (I) may be used.

R (I) kde každá skupina R znamená reťazec A alebo BR (I) wherein each R is A or B

C = CH so2r‘ aleboC = CH with 2 r ';

II

C-CH (A)C-CH

R1 R 1

R2 R 2

R1 R 1

R2 znamená metylovú skupinu alebo etylovú skupinu, znamená buď aromatickú skupinu vybranú z fenylovej skupiny, naftylovej skupiny alebo indenylovej skupiny, pričom tieto aromatické skupiny môžu byť nesubstituovaná alebo substituované jedným alebo viacerými atómami halogénu, alkylovými skupinami, alkoxyskupinami, skupinami -CO-alk, hydroxylovými skupinami, skupinami -COOR5, formylovými skupinami, trifluórmetylovými skupinami, trifluórmetylsulfanylovými skupinami, trifluórmetoxyskupinami, nitroskupinami, skupinami -WR6R7, skupinami -CO-NH-NR6R7, skupinami -N (alk) COORC, kyanoskupinami, skupinami -CONHR9, skupinami -CO-NR16R17, alkylsulfanylovými skupinami, hydroxyalkylovými skupinami, skupinami -O-alk-NR12R13 alebo alkyltioaikylovými skupinami, alebo heteroaromatickú skupinu, vybranú z benzofurylovej skupiny, benzotiazolylovej skupiny, benzotienylovej skupiny, benzoxazolylovej skupiny, chromanylovej skupiny, 2,3-dihydroxybenzofurylovej skupiny, 2,3-dihydrobenzotienylovej skupiny, in3 zofurylovej skupiny, 2,3-dihydrobenzotienylovej skupiny, indolinylovej skupiny, indolylovej skupiny, izochromanylovej skupiny, izochinolylovej skupiny, pyridylovej skupiny, chinolylovej skupiny, 1,2,3,4-tetrahydroizochinolylovej skupiny, I,2,3,4-tetrahydrochinolylovej skupiny, tiazoiylovej skupiny alebo tienylovej skupiny, pričom tieto heteroaromatické skupiny môžu byť nesubstituovaná alebo substituované atómom halogénu, alkylovou skupinou, alkoxyskupinou, skupinou -COOR5, trifluórmetylovou skupinou, trifluórmetylsulfanylovou skupinou, trifluórmetoxyskupinou, nitroskupinou, skupinou -NR6R7, skupinou -CO-NH-NR5R7, kyanoskupinou, skupinou -CONHR9, alkylsulfanylovou skupinou, hydroxyalkylovou skupinou alebo alkyltioalkylovou skupinou,R 2 represents a methyl or ethyl radical, means either an aromatic group selected from phenyl, naphthyl and indenyl, these aromatic groups may be unsubstituted or substituted by one or more halogen, alkyl, alkoxy, -CO-alk, hydroxyl groups, -COOR 5 groups, formyl groups, trifluoromethyl groups, trifluoromethylsulfanyl groups, trifluoromethoxy groups, nitro groups, -WR 6 R 7 groups, -CO-NH-NR 6 R 7 groups, -N (alk) COOR C groups, cyano groups, -CONHR 9 groups, -CO-NR 16 R 17 groups, alkylsulfanyl groups, hydroxyalkyl groups, -O-alk-NR 12 R 13 groups or alkylthioalkyl groups, or a heteroaromatic group selected from benzofuryl, benzothiazolyl, benzothienyl, benzoxazolyl 2,3-dihydroxybenzofuryl j, 2,3-dihydrobenzothienyl, 3-isofuryl, 2,3-dihydrobenzothienyl, indolinyl, indolyl, isochromanyl, isoquinolyl, pyridyl, quinolyl, 1,2,3,4-tetrahydroisoquinolyl, 1,2,3,4-tetrahydroquinolyl, thiazolyl or thienyl, wherein the heteroaromatic groups may be unsubstituted or substituted by a halogen atom, an alkyl group, an alkoxy group, -COOR 5 , a trifluoromethyl group, a trifluoromethylsulfanyl group, a trifluoromethoxy group, a nitro group, a nitro group, a nitro group, -NR 6 R 7 , -CO-NH-NR 5 R 7 , cyano, -CONHR 9 , alkylsulfanyl, hydroxyalkyl or alkylthioalkyl,

R3 a R4, ktoré sú rovnaké alebo rôzne predstavujú buď aromatickú skupinu vybranú z fenylovej skupiny, naftylovej skupiny alebo indenylovej skupiny, pričom tieto aromatické skupiny môžu byť nesubstituovaná alebo substituované jedným alebo viacerými atómami halogénu, alkylovými skupinami, alkoxyskupinami, formylovými skupinami, hydroxylovými skupinami, trifluórmetylovými skupinami, trifluórmetoxyskupinami, skupinami -CO-alk, kyanoskupinami, skupinami -COOR5, skupinami -CONR10Rn, skupinami -CO-NH-NR6R7, alkylsulfanylovými skupinami, hydroxyalkýlovými skupinami, skupinami -alk-NR6R7 alebo alkyltioalkylovými skupinami, alebo heteroaromatickú skupinu vybranú z benzofurylovej skupiny, benzotiazolylovej skupiny, benzotienylovej skupiny, benzoxazolylovej skupiny, chromanylovej skupiny, 2,3-dihydrobenzofurylovej skupiny, 2,3-dihydrobenzotienylovej skupiny, furylovej skupiny, izochromanylove j skupiny, izochinolylovej skupiny, pyrolylovej skupiny, chinolylovej skupiny, 1,2,3,4-tetrahydroizochinolylovej skupiny, tiazoiylovej skupiny alebo tienylovej skupiny, pričom tieto heteroaromatické skupiny môžu byť nesubstituované alebo substituované jedným alebo viacerými atómami halogénu, alkylovými skupinami, alkoxyskupinami, hy4 droxylovými skupinami, trifluórmetylovými skupinami, trifluórmetoxyskupinami, kyanoskupinami, skupinami -COOR5, skupinami -CO-NH-NR6R7, skupinami -CONR10RU, skupinami -alk-NR6R7, alkylsulfanylovými skupinami, hydroxyalkylovými skupinami alebo alkyltioalkylovými skupinami,R 3 and R 4 which are the same or different represent either an aromatic group selected from phenyl, naphthyl or indenyl, which aromatic groups may be unsubstituted or substituted by one or more halogen atoms, alkyl groups, alkoxy groups, formyl groups, hydroxyl groups groups, trifluoromethyl, trifluoromethoxy, -CO-alk, cyano, -COOR 5, -CONR 10 R n, -CO-NH-NR 6 R 7, alkylmercapto, hydroxyalkyl, -alk-NR 6 R 7 or alkylthioalkyl, or a heteroaromatic group selected from benzofuryl, benzothiazolyl, benzothienyl, benzoxazolyl, chromanyl, 2,3-dihydrobenzofuryl, 2,3-dihydrobenzothienyl, furyl, isoquinromyl, pyrrolyl, ch inolyl, 1,2,3,4-tetrahydroisoquinolyl, thiazolyl or thienyl, wherein the heteroaromatic groups may be unsubstituted or substituted by one or more halogen atoms, alkyl groups, alkoxy groups, hydroxy groups, trifluoromethyl groups, trifluoromethoxy groups, trifluoromethoxy groups, trifluoromethoxy groups , -COOR 5 group, a -CO-NH-NR 6 R 7, -CONR 10 R U, -alk-NR 6 R 7, alkylmercapto, hydroxyalkyl or alkylthioalkyl,

R3 je alkylová skupina alebo fenylová skupina pripadne substituovaná jedným alebo viacerými atómami halogénu,R 3 is an alkyl or phenyl optionally substituted with one or more halogen atoms,

R6 a R7, ktoré sú rovnaké alebo rôzne, predstavujú atóm vodíka, alkylovú skupinu, skupinu -COOalk, cykloalkylovú skupinu, alkylcykloalkylovú skupinu, skupinu -alk-O-alk alebo hydroxyalkylovú skupinu, alebo R6 a R7 spoločne s atómom dusíka, na ktorý sa viažu, tvoria nasýtenú alebo nenasýtenú monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 členov, prípadne obsahujúcu ďalší heteroatóm vybraný z atómu kyslíka, atómu síry alebo atómu dusíka a prípadne substituovanú jednou alebo viacerými alkylovými skupinami, skupinami -CO-alk, skupinami -COOalk, skupinami -CONHalk, skupinami -CSNHalk, skupinami -CO-alk-NR14Rl3, oxoskupinami, hydroxyalkylovými skupinami, skupinami -alk-O-alk alebo skupinami -CO-NH2,R 6 and R 7 , which are the same or different, represent a hydrogen atom, an alkyl group, a -COOalk group, a cycloalkyl group, an alkylcycloalkyl group, an -alk-O-alk group or a hydroxyalkyl group, or R 6 and R 7 together with a nitrogen atom to which they are attached form a saturated or unsaturated monocyclic or bicyclic heterocyclic group containing from 3 to 10 members, optionally containing another heteroatom selected from oxygen, sulfur or nitrogen and optionally substituted by one or more alkyl, -CO-alk, -COOalk groups, -CONHalk groups, -CSNHalk groups, -CO-alk-NR 14 R 13 groups, oxo groups, hydroxyalkyl groups, -alk-O-alk groups, or -CO-NH 2 groups,

R8 znamená alkylovú skupinu,R 8 represents an alkyl group,

R9 znamená atóm vodíka, alkylovú skupinu alebo alkylovú skupinu substituovanú dialkylaminoalkylovou skupinou, fenylovou skupinou, cykloalkylovou skupinou (prípadne substituovanou skupinou -COOalk) alebo nasýtenou alebo nenasýtenou monocyklickou alebo bicyklickou heterocyklickou skupinou obsahujúcou 3 až 10 členov, prípadne obsahujúcou jeden alebo viacero heteroatómov vybraných z atómu kyslíka, atómu síry a atómu dusíka a prípadne substituovanou jedným alebo viacerými alkylovými skupinami,R 9 represents a hydrogen atom, an alkyl group or an alkyl group substituted with a dialkylaminoalkyl group, a phenyl group, a cycloalkyl group (optionally substituted with -COOalk group) or a saturated or unsaturated monocyclic or bicyclic heterocyclic group containing 3 to 10 members, optionally containing one or more heteroatoms selected from an oxygen atom, a sulfur atom and a nitrogen atom and optionally substituted by one or more alkyl groups,

Rl0 a R11, ktoré sú rovnaké alebo rôzne, predstavujú atóm vodíka alebo alkylovú skupinu, alebo R10 a R11 tvoria spoločne s atómom dusíka, na ktorý sa viažu, nasýtenú monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 členov, prípadne obsahujúcu ďalší heteroatóm vybraný z atómu kyslíka, atómu síry a atómu dusíka a prípadne substituovanú jedným alebo viacerými alkylovými skupinami,R 10 and R 11 , which are the same or different, represent a hydrogen atom or an alkyl group, or R 10 and R 11 together with the nitrogen atom to which they are attached form a saturated monocyclic or bicyclic heterocyclic group containing from 3 to 10 members, optionally containing another heteroatom selected from oxygen, sulfur and nitrogen and optionally substituted with one or more alkyl groups,

R12 a R13, ktoré sú rovnaké alebo rôzne, predstavujú atóm vodíka, alkylovú skupinu alebo cykloalkylovú skupinu, alebo Ri2 a R13 tvoria spoločne s atómom dusíka, na ktorý sa viažu, nasýtenú monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 členov, prípadne obsahujúcu ďalší heteroatóm vybraný z atómu kyslíka, atómu síry a atómu dusíka a prípadne substituovanú alkylovou skupinou, skupinou -CO-alk, skupinou -COOalk, skupinou -CONHalk, skupinou -CSNHalk, skupinou -CO-alk-NR14R15 alebo nasýtenou monocyklickou alebo bicyklickou heterocyklickou skupinou obsahujúcou 3 až 10 členov a obsahujúcou heteroatóm vybraný z atómu kyslíka, atómu síry a atómu dusíka,R 12 and R 13 , which are the same or different, represent a hydrogen atom, an alkyl group or a cycloalkyl group, or R 12 and R 13 together with the nitrogen atom to which they are attached form a saturated monocyclic or bicyclic heterocyclic group containing 3 to 10 members , optionally containing a further heteroatom selected from oxygen, sulfur and nitrogen and optionally substituted with alkyl, -CO-alk, -COOalk, -CONHalk, -CSNHalk, -CO-alk-NR 14 R 15 or a saturated monocyclic or bicyclic heterocyclic group containing 3 to 10 members and containing a heteroatom selected from oxygen, sulfur and nitrogen,

R14 a R15, ktoré sú rovnaké alebo rôzne, predstavujú atóm vodíka, alkylovú skupinu alebo skupinu -COOalk,R 14 and R 15 , which are the same or different, represent a hydrogen atom, an alkyl group or a -COOalk group,

R16 a R17 tvoria spoločne s atómom dusíka, na ktorý sa viažu, nasýtenú monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 členov, prípadne obsahujúcu ďalšie heteroatómy vybrané z atómu kyslíka, atómu síry a atómu dusíka,R 16 and R 17 together with the nitrogen atom to which they are attached form a saturated monocyclic or bicyclic heterocyclic group containing from 3 to 10 members, optionally containing further heteroatoms selected from oxygen, sulfur and nitrogen,

R' znamená atóm vodíka alebo skupinu -CO-alk, alebo R znamená skupinu CHR18, aR 'is H or -CO-alk, or R represents a CHR 18 radical, and

R18 znamená skupinu -NHCOR19 alebo skupinu -N (R20)-Y-R21,R 18 represents a radical -NHCOR 19 or -N (R 20) -YR 21,

Y je skupina CO alebo skupina SO2,Y is CO or SO 2 ,

R4 a R3, ktoré sú rovnaké alebo rôzne, predstavujú buď aromatickú skupinu vybranú z fenylovej skupiny, naftylovej skupiny alebo indenylovej skupiny, pričom tieto aromatické skupiny môžu byť nesubstituované alebo substituované jedným alebo viacerými atómami halogénu, alkylovými skupinami, alkoxyskupinami, formylovými skupinami, hydroxylovými skupinami, trifluórmetylovými skupinami, trifluórmetoxyskupinami, skupinami -CO-alk, kyanoskupinami, skupinami -COOH, skupinami -COOalk, skupinami -CONR22R23, skupinami -CO-NH-NR24R25, alkylsulfanylovými skupinami, alkylsulfinylovými skupinami, alkylsulfonylovými skupinami, alkylsulfanylalkylovými skupinami, alkylsulfinylalkylovými skupinami, alkylsulfonylalkylovými skupinami, hydroxyalkylovými skupinami alebo skupinami -alk-NR22R23, alebo heteroaromatickú skupinu vybranú z benzofurylovej skupiny, benzotiazolylovej skupiny, benzotienylovej skupiny, benzoxazolylovej skupiny, chromanylovej skupiny, 2,3-dihydroxybenzofurylovej skupiny, 2,3-dihydrobenzotienylovej skupiny, pyrimidinylovej skupiny, furylovej skupiny, imidazolylovej skupiny, izochromanylovej skupiny, izochinolylovej skupiny, pyrolylovej skupiny, pyridylovej skupiny, chinolylovej skupiny, 1,2,3,4-tetrahydroizochinoiylovej skupiny, tiazolylovej skupiny alebo tienylovej skupiny, pričom tieto heteroaromatické skupiny môžu byt nesubstituované alebo substituované atómom halogénu, alkylovou skupinou, alkoxyskupinou, hydroxylovou skupinou, trifluórmetylovou skupinou, trifluórmetoxyskupinou, kyanoskupinou, skupinou -COOH, skupinou -COOalk, skupinou -CO-NH-NR24R25, skupinou -CONR22R23, skupinou-alk-NR24R25, alkylsulfanylovou skupinou, alkylsulfinylovou skupinou, alkylsulfonylovou skupinou, alkylsulfanylalkyiovou skupinou, alkylsulfinylakylovou skupinou, alkylsulfonylalkylovou skupinou alebo hydroxyalkylovou skupinou,R 4 and R 3 , which are the same or different, represent either an aromatic group selected from phenyl, naphthyl or indenyl, which aromatic groups may be unsubstituted or substituted by one or more halogen atoms, alkyl groups, alkoxy groups, formyl groups, hydroxyl groups, trifluoromethyl groups, trifluoromethoxy groups, -CO-alk groups, cyano groups, -COOH groups, -COOalk groups, -CONR 22 R 23 groups, -CO-NH-NR 24 R 25 groups, alkylsulfanyl groups, alkylsulfinyl groups, alkylsulfonyl groups , alkylsulfanylalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, hydroxyalkyl or -alk-NR 22 R 23 groups, or a heteroaromatic group selected from benzofuryl, benzothiazolyl, benzothienyl, benzoxazolyl, chromanyl, 2,3- dihydroxybenzofuryl, 2,3-dihydrobenzothienyl, pyrimidinyl, furyl, imidazolyl, isochromanyl, isoquinolyl, pyrrolyl, pyridyl, quinolyl, 1,2,3,4-tetrahydroisoquinolyl, thiazolyl wherein the heteroaromatic groups may be unsubstituted or substituted by halogen, alkyl, alkoxy, hydroxyl, trifluoromethyl, trifluoromethoxy, cyano, -COOH, -COOalk, -CO-NH-NR 24 R 25 , -CONR 22 R 23, the group-alk-NR 24 R 25, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, alkylsulfanylalkyiovou group, alkylsulfinylakylovou group, alkylsulfonylalkyl or hydroxyalkyl,

R19 znamená skupinu -alk-SO2R26, skupinu -alk-SO2-CH=CH-R26, skupinu Het1 substituovanú skupinou -SO2-R26 alebo fenylovú skupinu substituovanú skupinou -SO2-R26 alebo skupinou -alk-SO2-R26,R 19 represents an -alk-SO 2 R 26, -alk-SO 2 -CH = CH-R 26, Het 1 is substituted by -SO 2 R 26 or phenyl substituted by -SO 2 R 26 or -alk-SO 2 R 26 ,

R20 znamená atóm vodíka alebo alkylovú skupinu,R 20 represents a hydrogen atom or an alkyl group,

R21 znamená fenylalkylovú skupinu, skupinu Het1 alebo skupinuR 21 represents a phenylalkyl group, a Het 1 group or a group

Ar1,Ar 1 ,

R22 a R23, ktoré sú rovnaké alebo rôzne, predstavujú atóm vodíka alebo alkylovú skupinu, alebo R22 a R23 tvoria spoločne s atómom dusíka, na ktorý sa viažu, nasýtenú monocyklickú alebo bicyklickú skupinu obsahujúcu 3 až 10 členov, prípadne obsahujúcu ďalší heteroatóm vybraný z atómu kyslíka, atómu i síry a atómu dusíka a prípadne substituovanú jedným alebo viacerými alkylovými skupinami,R 22 and R 23 , which are the same or different, represent a hydrogen atom or an alkyl group, or R 22 and R 23 together with the nitrogen atom to which they are attached form a saturated monocyclic or bicyclic group containing 3 to 10 members, optionally containing further a heteroatom selected from oxygen, sulfur and nitrogen, and optionally substituted with one or more alkyl groups,

R24 a R25, ktoré sú rovnaké alebo rôzne, predstavujú atóm vodíka, alkylovú skupinu, skupinu -COOalk, cykloalkylovú skupinu, alkylcykloalkylovú skupinu, skupinu -alk-O-alk alebo hydroxyalkylovú skupinu, alebo R24 a R25 spoločne s atómom uhlíka, na ktorý sa viažu, tvoria nasýtenú alebo nenasýtenú monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 členov, prípadne obsahujúcu ďalší heteroatóm vybraný z atómu kyslíka, atómu síry alebo atómu dusíka a prípadne substituovanú jednou alebo viacerými alkylovými skupinami, skupinami -CO-alk, skupinami -COOalk, skupinami -CONHalk, skupinami -CSNHalk, oxoskupinami, hydroxyalkylovými skupinami, skupinami -alk-O-alk alebo skupinami -CO-NH2,R 24 and R 25 , which are the same or different, represent a hydrogen atom, an alkyl group, a -COOalk group, a cycloalkyl group, an alkylcycloalkyl group, an -alk-O-alk group or a hydroxyalkyl group, or R 24 and R 25 together with a carbon atom to which they are attached form a saturated or unsaturated monocyclic or bicyclic heterocyclic group containing from 3 to 10 members, optionally containing another heteroatom selected from oxygen, sulfur or nitrogen and optionally substituted by one or more alkyl, -CO-alk, -COOalk groups, -CONHalk groups, -CSNHalk groups, oxo groups, hydroxyalkyl groups, -alk-O-alk groups or -CO-NH 2 groups,

R25 znamená alkylovú skupinu, skupinu Ar1 alebo skupinu Het1,R 25 represents an alkyl group, an Ar 1 group or a Het 1 group,

Ar1 znamená fenylovú skupinu, naftylovú skupinu alebo indenylovú skupinu, pričom tieto skupiny sú prípadne substituované jedným alebo viacerými atómami halogénu, alkylovými skupinami, alkoxyskupinami, kyanoskupinami, skupinami -CO-alk, skupinami -COOH, skupinami -COOalk, skupinami -CONR27R28, skupinami -CO-NH-NR29R30, alkylsulfanylovými skupinami, alkylsulfinylovými skupinami, alkylsulfonylovými skupinami, skupinami -alk-NR29R30, skupinami -NR29R30, alkyltioalkylovými skupinami, formylovými skupinami, hydroxylovými skupinami, hydroxyalkylovými skupinami, skupinami Het, skupinami -O-alk-NH-cykloalkyl, trifluórmetoxyskupinami, trifluórmetylovými skupinami, skupinami -NH-CO-alk, skupinami -SO2NH2, skupinami -NH-COCH3, skupinami -NH-COOalk, skupinami Het alebo ešte dve susedné skupiny môžu tvoriť dioxymetylénovú skupinu,Ar 1 is phenyl, naphthyl or indenyl, these groups being optionally substituted by one or more halogen atoms, alkyl groups, alkoxy groups, cyano groups, -CO-alk groups, -COOH groups, -COOalk groups, -CONR 27 R groups 28 , -CO-NH-NR 29 R 30 , alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, -alk-NR 29 R 30 , -NR 29 R 30 , alkylthioalkyl, formyl, hydroxyl, hydroxyalkyl, Het groups, -O-alk-NH-cycloalkyl groups, trifluoromethoxy groups, trifluoromethyl groups, -NH-CO-alk groups, -SO 2 NH 2 groups, -NH-COCH 3 groups, -NH-COOalk groups, Het groups or two more adjacent groups may form a dioxymethylene group,

Het1 znamená nenasýtenú alebo nasýtenú monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 kruhových členov, obsahujúcu jeden alebo viacero heteroatómov vybraných z atómu kyslíka, atómu síry a atómu dusíka, ktorá je prípadne substituovaná jednou alebo viacerými alkylovými skupinami, alkoxyskupinami, vinylovými skupinami, stornami halogénu, alkoxykarbonylovými skupinami, oxoskupinami, hydroxylovými skupinami trifluórmetoxyskupinami alebo trifluórmetyiovými skupinami, pričom atómy dusíka heterccyklov sú prípadne v N-oxidovanej forme,Het 1 means an unsaturated or saturated monocyclic or bicyclic heterocyclic group containing 3 to 10 ring members, containing one or more heteroatoms selected from oxygen, sulfur and nitrogen, optionally substituted by one or more alkyl, alkoxy, vinyl, vinyl halogen, alkoxycarbonyl, oxo, hydroxyl, trifluoromethoxy or trifluoromethyl groups, the nitrogen atoms of the heterocycles optionally being in the N-oxidized form,

R27 a R28, ktoré sú rovnaké alebo rôzne, predstavujú atóm vodíka, alkylovú skupinu, alebo R27 a R28 spoločne s atómom uhlíka, na ktorý sa viažu, tvoria nasýtenú monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 členov, prípadne obsahujúcu ďalší heteroatóm vybraný z atómu kyslíka, atómu síry alebo atómu dusíka a prípadne substituovanú jednou alebo viacerými alkylovými skupinami,R 27 and R 28 , which are the same or different, represent a hydrogen atom, an alkyl group, or R 27 and R 28 together with the carbon atom to which they are attached form a saturated monocyclic or bicyclic heterocyclic group containing from 3 to 10 members, optionally containing another heteroatom selected from oxygen, sulfur or nitrogen and optionally substituted with one or more alkyl groups,

R29 a R30, ktoré sú rovnaké alebo rôzne, predstavújú atóm vodíka, alkylovú skupinu, skupinu -COOalk, cykloalkylovú skupinu, alkylcykloalkylovú skupinu, skupinu -alk-O-alk alebo hydroxyalkylovú skupinu, alebo R29 a R30 spoločne s atómom uhlíka, na ktorý sa viažu, tvoria nasýtenú alebo nenasýtenú monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 členov, prípadne obsahujúcu ďalší heteroatóm vybraný z atómu kyslíka, atómu síry alebo atómu dusíka a prípadne substituovanú jednou alebo viacerými alkylovými skupinami, skupinami -CO-alk, skupinami -COOalk, skupinami -CONHalk, skupinami -CSNHalk, oxoskupinami, hydroxyalkylovými skupinami, skupinami -alk-O-alk alebo skupinami -CO-NH2, alebo R znamená skupinu CHR31, aR 29 and R 30 , which are the same or different, represent a hydrogen atom, an alkyl group, a -COOalk group, a cycloalkyl group, an alkylcycloalkyl group, an -alk-O-alk group or a hydroxyalkyl group, or R 29 and R 30 together with a carbon atom to which they are attached form a saturated or unsaturated monocyclic or bicyclic heterocyclic group containing from 3 to 10 members, optionally containing another heteroatom selected from oxygen, sulfur or nitrogen and optionally substituted by one or more alkyl, -CO-alk, -COOalk groups, -CONHalk groups, -CSNHalk groups, oxo groups, hydroxyalkyl groups, -alk-O-alk groups or -CO-NH 2 groups, or R represents CHR 31 , and

R31 znamená skupinu -NR32R33, skupinu -NR32-CO-R33 alebo skupinu -NR32-SO2R3\ r4 a R3, ktoré sú rovnaké alebo rôzne, predstavujú buď aromatickú skupinu vybranú z fenylovej skupiny, naftylovej skupiny alebo indenylovej skupiny, pričom tieto aromatické skupiny môžu byť nesubstituované alebo substituované jedným alebo viacerými atómami halogénu, alkylovými skupinami, alkoxyskupinami, formylovými skupinami, hydroxylovými skupinami, trifluórmetylovými skupinami, trifluórmetoxyskupinami, skupinami -CO-alk, kyanoskupinami, skupinami -COOH, skupinami -COOalk, skupinami -CONR22R23, skupinami -CO-NH-NR24R25, aikylsulfanylovými skupinami, alkyisulfinylovými skupinami, alkylsulfonyiovými skupinami, alkylsulfanylalkylovými skupinami, alkyisulfinylalkylovými skupinami, alkyisulfonylalkylovými skupinami, hydroxyalkylovými skupinami alebo skupinami -alk-NR7R8, alebo heteroaromatickú skupinu vybranú z benzofurylovej skupiny, benzotiazolylovej skupiny, benzotienylovej skupiny, benzoxazolylovej skupiny, chromanylove j skupiny, 2,3-dihydroxybenzofurylovej skupiny, 2,3-dihydrobenzotienylovej skupiny, furylovej skupiny, imidazolylovej skupiny, izochromanylovej skupiny, izochinoiylovej skupiny, pyrolylovej skupiny, pyridylovej skupiny, pyrimidinylovej skupiny, chinolylovej skupiny, 1,2,3,4-tetrahydroizochinolylovej skupiny, tiazolylovej skupiny alebo tienylovej skupiny, pričom tieto heteroaromatické skupiny môžu byť nesubstituované alebo substituované atómom halogénu, alkylovou skupinou, alkoxyskupinou, hydroxylovou skupinou, trifluórmetylovou skupinou, trifluórmetoxyskupinou, kyanoskupinou, skupinou -COOH, skupinou -COOalk, skupinou -CO-NH-NR24R25, skupinou -CONR22R23, skupinou-alk-NR24R25, alkyisulf anylovou skupinou, alkyisulfinylovou skupinou, alkylsulfonylovou skupinou, alkylsulfanylalkylovou skupinou, alkyisulfinylakylovou skupinou, alkyisulfonylalkyiovou skupinou alebo hydroxy10 alkylovou skupinou,R 31 represents -NR 32 R 33 , -NR 32 -CO-R 33, or -NR 32 -SO 2 R 3, R 4 and R 3 , which may be the same or different, represent either an aromatic group selected from a phenyl group , naphthyl or indenyl, which aromatic groups may be unsubstituted or substituted by one or more halogen atoms, alkyl groups, alkoxy groups, formyl groups, hydroxyl groups, trifluoromethyl groups, trifluoromethoxy groups, -CO-alk groups, cyano groups, -COOH groups, -COOalk groups, -CONR 22 R 23 groups, -CO-NH-NR 24 R 25 groups, alkylsulfanyl groups, alkyisulfinyl groups, alkylsulfonyl groups, alkylsulfanylalkyl groups, alkyisulfinylalkyl groups, alkyisulfonylalkyl groups, hydroxyalkyl groups or -alk-NR 7 groups 8 , or a heteroaromatic group selected from benzofuryl, benzothiazolylo benzothenyl, benzoxazolyl, chromanyl, 2,3-dihydroxybenzofuryl, 2,3-dihydrobenzothienyl, furyl, imidazolyl, isochromanyl, isoquinolyl, pyrrolyl, pyridyl, pyrimidinolyl , 1,2,3,4-tetrahydroisoquinolyl, thiazolyl or thienyl, wherein the heteroaromatic groups may be unsubstituted or substituted by a halogen atom, an alkyl group, an alkoxy group, a hydroxyl group, a trifluoromethyl group, a trifluoromethoxy group, a cyano group, a -COOH group, -COOalk, -CO-NH-NR 24 R 25 , -CONR 22 R 23 , -alk-NR 24 R 25 , alkyisulfanyl, alkyisulfinyl, alkylsulfonyl, alkylsulfanylalkyl, alkyisulfinylalkyl, alkyisulfonylalkyl, or hydroxy 10 an alkyl group u.

R32 znamená skupinu -C (R35) (R36)-Het2, skupinu -Het2, skupinu -C (R35) (R36)-Ar2, skupinu Ar2, cykloalkylovú skupinu alebo norbornylovú skupinu,R 32 is -C (R 35 ) (R 36 ) -Het 2 , -Het 2 , -C (R 35 ) (R 36 ) -Ar 2 , Ar 2 , cycloalkyl or norbornyl,

R33 znamená atóm vodíka, hydroxyalkylovú skupinu, skupinu -alk-COOalk, skupinu -alk-CONR22R23, skupinu -alk-NR22R23, alkoxyskupinu, skupinu Ar2, skupinu Het2, skupinu -CH2Ar2, skupinu -CH2Het2 alebo alkylovú skupinu prípadne substituovanú jedným alebo viacerými atómami halogénu,R 33 is hydrogen, hydroxyalkyl, -alk-COOalk, -alk-CONR 22 R 23 , -alk-NR 22 R 23 , alkoxy, Ar 2 , Het 2 , -CH 2 Ar 2 , - CH 2 Het 2 or an alkyl group optionally substituted by one or more halogen atoms,

R34 znamená hydroxyalkylovú skupinu, skupinu -alk-COOalk, skupinu -alk-CONR22R23, skupinu -alk-NR22R23, alkoxyskupinu, skupinu Ar2, skupinu Het2, skupinu -CH2Ar2, skupinu -CH2Het2 alebo alkylovú skupinu prípadne substituovanú jedným alebo viacerými atómami halogénu,R 34 represents a hydroxyalkyl, -alk-COOalk, -alk-CONR 22 R 23, -alk-NR 22 R 23, alkoxy, Ar 2, Het 2, -CH 2 Ar 2 group, or a group -CH2Het 2 an alkyl group optionally substituted by one or more halogen atoms,

R35 znamená atóm vodíka, hydroxyalkylovú skupinu, skupinu -alk-COOalk, skupinu -alk-CONR22R23, skupinu -alk-NR22R23, alkoxyalkylovú skupinu, skupinu Ar2, skupinu Het2, skupinu -CH2Ar2, skupinu -CH2Het2 alebo alkylovú skupinu prípadne substituovanú jedným alebo viacerými atómami halogénu,R 35 is hydrogen, hydroxyalkyl, -alk-COOalk, -alk-CONR 22 R 23 , -alk-NR 22 R 23 , alkoxyalkyl, Ar 2 , Het 2 , -CH 2 Ar 2 , -CH 2 Het 2 or an alkyl group optionally substituted by one or more halogen atoms,

R36 znamená atóm vodíka, hydroxyalkylovú skupinu, skupinu -alk-COOalk, skupinu -alk-CONR22R23, skupinu -alk-NR22R23, alkoxyalkylovú skupinu alebo alkylovú skupinu prípadne substituovanú jedným alebo viacerými atómami halogénu, alebo ešte R35 a R36 tvoria spoločne s atómom uhlíka, na ktorý sa viažu, nasýtený monocyklický alebo bicyklický kruh obsahujúci 3 až 10 členov, prípadne obsahujúci ďalší heteroatóm vybraný z atómu kyslíka, atómu síry a atómu dusíka a prípadne substituovaný jedným alebo viacerými alkylovými skupinami,R 36 is hydrogen, hydroxyalkyl, -alk-COOalk, -alk-CONR 22 R 23 , -alk-NR 22 R 23 , alkoxyalkyl or alkyl optionally substituted by one or more halogen atoms, or R 35 and R 36 together with the carbon atom to which they are attached form a saturated monocyclic or bicyclic ring containing from 3 to 10 members, optionally containing another heteroatom selected from oxygen, sulfur and nitrogen and optionally substituted with one or more alkyl groups,

Ar2 znamená fenylovú skupinu, naftylovú skupinu alebo indenylovú skupinu, pričom tieto skupiny sú prípadne substituované jed11 ným alebo viacerými atómami halogénu, alkylovými skupinami, alkoxyskupinami, kyanoskupinami, skupinami -CO-alk, skupinami -COOH, skupinami -COOalk, skupinami -CONR37R38, skupinami -CO-NH-NR39R40, alkylsulfanylovými skupinami, alkylsulfinylovými skupinami, alkylsulfonylovými skupinami, skupinami -alk-NR39R40, skupinami -NR39R40, alkyltioalkylovými skupinami, formylovými skupinami, trifluórmetylovými skupinami, trifluórmetoxyskupinami, skupinami Het, skupinami -O-alk-NH-cykloalkyl, skupinami -SO2NH2, hydroxylovými skupinami, hydroxyalkylovými skupinami, skupinami -NHCOalk, skupinami -NH-COOalk alebo na dvoch susedných atómoch uhlíka dioxymetylénovou skupinou,Ar 2 represents a phenyl group, a naphthyl group or an indenyl group, these groups being optionally substituted by one or more halogen atoms, alkyl groups, alkoxy groups, cyano groups, -CO-alk groups, -COOH groups, -COOalk groups, -CONR 37 groups R 38 , -CO-NH-NR 39 R 40 groups, alkylsulfanyl groups, alkylsulfinyl groups, alkylsulfonyl groups, -alk-NR 39 R 40 groups, -NR 39 R 40 groups, alkylthioalkyl groups, formyl groups, trifluoromethyl groups, trifluoromethoxy groups, Het groups, -O-alk-NH-cycloalkyl groups, -SO2NH2 groups, hydroxyl groups, hydroxyalkyl groups, -NHCOalk groups, -NH-COOalk groups or two adjacent carbon atoms with a dioxymethylene group,

Het2 znamená nenasýtenú alebo nasýtenú monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 kruhových členov, obsahujúcu jeden alebo viacero heteroatómov vybraných z atómu kyslíka, atómu síry a atómu dusíka, ktorá je prípadne substituovaná jednou alebo viacerými alkylovými skupinami, alkoxyskupinami, atómami halogénu, alkoxykarbonylovými skupinami, oxoskupinami alebo hydroxylovými skupinami, pričom atómy dusíka heterocyklov sú prípadne v N-oxidovanej forme,Het 2 means an unsaturated or saturated monocyclic or bicyclic heterocyclic group containing 3 to 10 ring members, containing one or more heteroatoms selected from oxygen, sulfur and nitrogen, optionally substituted by one or more alkyl, alkoxy, halogen, alkoxycarbonyl groups, oxo or hydroxyl groups, the nitrogen atoms of the heterocycles optionally being in the N-oxidized form,

R37 a R38, ktoré sú rovnaké alebo rôzne, predstavujú atóm vodíka alebo alkylovú skupinu, alebo R37 a R38 spoločne s atómom uhlíka, na ktorý sa viažu, tvoria nasýtenú monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 členov, prípadne obsahujúcu ďalší heteroatóm vybraný z atómu kyslíka, atómu síry alebo atómu dusíka a prípadne substituovanú jednou alebo viacerými alkylovými skupinami,R 37 and R 38 , which are the same or different, represent a hydrogen atom or an alkyl group, or R 37 and R 38 together with the carbon atom to which they are attached form a saturated monocyclic or bicyclic heterocyclic group containing from 3 to 10 members, optionally containing another heteroatom selected from oxygen, sulfur or nitrogen and optionally substituted with one or more alkyl groups,

R39 a R40, ktoré sú rovnaké alebo rôzne, predstavujú atóm vodíka alebo alkylovú skupinu, alebo R39 a R40 spoločne s atómom uhlíka, na ktorý sa viažu, tvoria nasýtenú monocyklickú alebo ‘bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 členov, prípadne obsahujúcu ďalší heteroatóm vybraný z atómu kyslíka, atómu síry alebo atómu dusíka a prípadne substituovanú jednou alebo viacerými alkylovými skupinami, alk znamená alkylovú skupinu alebo alkylénovú skupinu, pričom alkylové, alkylénové a alkoxylové časti sú s priamym alebo rozvetveným reťazcom obsahujúcim 1 až 6 atómov uhlíka, a cykloalkylové skupiny obsahujú 3 až 10 atómov uhlíka, optické izoméry týchto zlúčenín a ich farmaceutický prijatelné soli s anorganickou alebo organickou kyselinou.R 39 and R 40 , which are the same or different, represent a hydrogen atom or an alkyl group, or R 39 and R 40 together with the carbon atom to which they are attached form a saturated monocyclic or bicyclic heterocyclic group containing 3 to 10 members, optionally containing another heteroatom selected from oxygen, sulfur or nitrogen and optionally substituted by one or more alkyl groups, alk represents an alkyl group or an alkylene group, wherein the alkyl, alkylene and alkoxy groups are straight or branched chain containing 1 to 6 carbon atoms, and cycloalkyl groups contain 3 to 10 carbon atoms, the optical isomers of these compounds, and their pharmaceutically acceptable salts with an inorganic or organic acid.

Výhodnými azetidínovými derivátmi sú nasledovné zlúčeniny:Preferred azetidine derivatives are the following compounds:

l-benzhydryl-3-[(metylsulfonyl)(fenyl)metylén]azetidín, l-benzhydryl-3-[(3-metylfenyl) (metylsulfonyl) metylén]azetidín, l-benzhydryl-3-[(3-chlórfenyl)(metylsulfonyl)metylén]azetidín, l-benzhydryl-3-[(3,5-dichlórfenyl)(metylsulfonyl)metylén]-azetidín, l-benzhydryl-3-[(2,5-dichlórfenyl)(metylsulfonyl)metylén]-azetidín, l-benzhydryl-3-[(2,3-dichlórfenyl)(metylsulfonyl)metylén]-azetidín, l-benzhydryl-3-[(3-fluórfenyl)(metylsulfonyl)metylén]azetidín, l-benzhydryl-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]-azetidín, l-benzhydryl-3-[(3-brómfenyl)(metylsulfonyl)metylén]azetidín, l-benzhydryl-3-[(3-jódfenyl)(metylsulfonyl)metylén]azetidín, l-benzhydryl-3-[(metylsulfonyl)(3-trifluórmetoxyfenyl)metylén]-azetidín, l-benzhydryl-3-[(metylsulfonyl)(3-trifluórmetylfenyl)metylén]-azetidín, l-benzhydryl-3-{ [3,.5-bis (trifluórmetyl) fenyl] (metylsulfonyl) -metylén]azetidín, l-benzhydryl-3-[(3,5-dibrómfenyl)(metylsulfonyl)metylén]-azetidín, l-benzhydryl-3-[(3-metoxykarbonylfenyl)(metylsulfonyl)metylén]-azetidín, l-benzhydryl-3-[(3-kyanofenyl)(metylsulfonyl)metylén]azetidín, l-benzhydryl-3-[(3-karbamoylfenyl)(metylsulfonyl)metylén]-azetidín, l-benzhydryl-3-[(metylsulfonyl)(naft-l-yl)(metylsulfonyl)-metylén]azetidín,1-benzhydryl-3 - [(methylsulfonyl) (phenyl) methylene] azetidine, 1-benzhydryl-3 - [(3-methylphenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-chlorophenyl) (methylsulfonyl) ) methylene] azetidine, 1-benzhydryl-3 - [(3,5-dichlorophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(2,5-dichlorophenyl) (methylsulfonyl) methylene] azetidine, 1 -benzhydryl-3 - [(2,3-dichlorophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-fluorophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3, 5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-bromophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-iodophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(methylsulfonyl) (3-trifluoromethoxyphenyl) methylene] azetidine, 1-benzhydryl-3 - [(methylsulfonyl) (3-trifluoromethylphenyl) methylene] azetidine, 1-benzhydryl-3 - {[3, .5-bis (trifluoromethyl) phenyl] (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3,5-dibromophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-mee) 1-benzhydryl-3 - [(3-cyanophenyl) (methylsulfonyl) methylene] azetidine; 1-benzhydryl-3 - [(3-carbamoylphenyl) (methylsulfonyl) methylene] azetidine; 1-benzhydryl-3 - [(3-cyanophenyl) (methylsulfonyl) methylene] benzhydryl-3 - [(methylsulphonyl) (naphth-l-yl) (methylsulfonyl) methylene] azetidine,

1-[bis(4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyl) -metylén]azetidín,1- [bis (4-chlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine,

1-[bis(4-metoxyfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1- [Bis (4-methoxyphenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine,

1-[bis(4-metylfenyl)metyl]-3-[(3, 5-difluórfenyl) (metylsulfonyl) -metylén]azetidín, {RS}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]-1-[(4-metoxyfenyl)(fenyl)metyl]azetidín, (í?) — 3 — [(3,5-difluórfenyl)(metylsulfonyl)metylén]-1-[(4-metoxyfenyl)(fenyl)metyl]azetídín, (S)-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]-1-[(4-metoxyfenyl)(fenyl)metyl]azetidín,1- [bis (4-methylphenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, {RS} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] - 1 - [(4-methoxyphenyl) (phenyl) methyl] azetidine, (R) -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] -1 - [(4-methoxyphenyl) (phenyl) methyl] azetidine (S) -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] -1 - [(4-methoxyphenyl) (phenyl) methyl] azetidine,

1-[bis(4-trifluórmetoxyfenyl)metyl]-3-[(3,5-difluórfenyl)-(metylsulfonyl)metylén]azetidín,1- [bis (4-trifluoromethoxyphenyl) methyl] -3 - [(3,5-difluorophenyl) - (methylsulphonyl) methylene] azetidine,

1-[bis(4-trifluórmetylfenyl)metyl]-3-[(3,5-difluórfenyl) -(metylsulfonyl)metylén]azetidín,1- [bis (4-trifluoromethylphenyl) methyl] -3 - [(3,5-difluorophenyl) - (methylsulfonyl) methylene] azetidine,

1-[bis(4-chlórfenyi)metyl·]-3-{[3,5-bis(trifluórmetyl)fenyl]-metylsulfonylmetylén}azetidín, (RS)-1-[(4-chlórfenyl)(2,4-dichlórfenyl)metyl]-3-[(3,5-difluór fenyl)(metylsulfonyl)metylén]azetidín, (í?) -1- [ (4-chlórfenyl) (2,4-dichlórfenyl)metyl] -3- [ (3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, (S)-1-[(4-chlórfenyl)(2,4-dichlórfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, (FS)-1-{(4-chlórfenyl)[4-(hydroxymetyl)fenyl]metyl}-3-[(3,5-di fluórfenyl)(metylsulfonyl)metylén]azetidín, (Ä)-l-{(4-chlórfenyl) [4-(hydroxymetyl)fenyl]metyl)-3-[(3, 5-difluórfenyl)(metylsulfonyl)metylén]azetidín, (S)-l-{(4-chlórfenyl) [4-(hydroxymetyl)fenyl]metyl}-3-[(3, 5-difluórfenyl)(metylsulfonyl)metylén]azetidín, (FS)-l-{(4-chlórfenyl)[4-(pyrolidinylmetyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, (F)-l-{(4-chlórfenyl)[4-(pyrolidinylmetyl)fenyl]metyl]-3- [ (3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, (S)-1{(4-chlórfenyl)[4-(pyrolidinylmetyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1- [bis (4-chlorophenyl) methyl] -3 - {[3,5-bis (trifluoromethyl) phenyl] methylsulfonylmethylene} azetidine, (RS) -1 - [(4-chlorophenyl) (2,4-dichlorophenyl) methyl] -3 - [(3,5-difluoro phenyl) (methylsulfonyl) methylene] azetidine, (R) -1 - [(4-chlorophenyl) (2,4-dichlorophenyl) methyl] -3 - [(3) 5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (S) -1 - [(4-chlorophenyl) (2,4-dichlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine (FS) -1 - {(4-chlorophenyl) [4- (hydroxymethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (R) -1 - {( 4-chlorophenyl) [4- (hydroxymethyl) phenyl] methyl) -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (S) -1 - {(4-chlorophenyl) [4- (hydroxymethyl)] phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (FS) -1 - {(4-chlorophenyl) [4- (pyrrolidinylmethyl) phenyl] methyl} -3 - [(3 (5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (F) -1 - {(4-chlorophenyl) [4- (pyrrolidinylmethyl) phenyl] methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (S) -1 {(4-chloro r phenyl) [4- (pyrrolidinylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine,

1-(RS)-(4-chlórfenyl) [4-(3, 3-dimetylpiperid-l-ylmetyl)fenyl]-metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1- (RS) - (4-Chlorophenyl) [4- (3,3-dimethylpiperid-1-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine,

1-((Ä)-(4-chlórfenyl) [4-(3, 3-dimetylpiperid-l-ylmetyl)fenyl]-metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-((S)-(4-chlórfenyl·) [4-(3,3-dimetylpiperid-l-ylmetyl)fenyl]151 - ((R) - (4-chlorophenyl) [4- (3,3-dimethylpiperid-1-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - ((S) - (4-chlorophenyl) - [4- (3,3-dimethylpiperid-1-ylmethyl) phenyl] 15

-metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine,

1—{(RS)-(4-chlórfenyl)[4-(tíomorfolín-4-ylmetyl)fenyljmetyl}-[(3, 5-difluórfenyl) (metylsulfonyl)metylén]azetidín, l-((F)-(4-chlórfenyl)[4-(tiomorfolin-4-ylmetyl)fenyl]metyl·}-3-[(3, 5-difluórfenyl) (metylsulfonyl)metylén]azetidín, l-{(S)-(4-chlórfenyl) [4-(tiomorfolin-4-ylmetyl)fenyl]metyl}-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, l-{(RS) -(4-chlórfenyl) [4-(N-etyl-N-cyklohexylaminometyl)fenyl] -metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-((F)-(4-chlórfenyl)[4-(N-etyl-N-cyklohexylaminometyl)fenyl]-metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(S) -(4-chlórfenyl) [4- (N-etyl-N-cyklohexylaminometyl)fenyl]-metyl}-3-[(3, 5-difluórfenyl) (metylsulfonyl)metylén]azetidín,1 - {(RS) - (4-chlorophenyl) [4- (thiomorpholin-4-ylmethyl) phenyl] methyl} - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - ((F) - (4- chlorophenyl) [4- (thiomorpholin-4-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(S) - (4-chlorophenyl) [4- (thiomorpholin-4-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(RS) - (4-chlorophenyl) [4- (N-ethyl-N) -cyclohexylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - ((F) - (4-chlorophenyl) [4- (N-ethyl-N-cyclohexylaminomethyl)) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(S) - (4-chlorophenyl) [4- (N-ethyl-N-cyclohexylaminomethyl) phenyl] - methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine,

1-{{(FS) -(4-chlórfenyl){4-[(4-etoxykarbonylpiperaziny1)metyl]-fenylJmetyl}}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]-azetidín, l-{{(R) ~(4-chlórfenyl) (4-[ (4-etoxykarbonylpiperazinyl)metyl]-fenylJmetyl)}}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]-azetidín, l-({(S)-(4-chlórfenyl){4-[(4-etoxykarbonylpiperazinyl)metyl]-fenylJmetyl}}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]-azetidín, l-{(FS)-(4-chlórfenyl)[4-(N-cyklopropyl-N-propylaminometyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]-azetidín, l-{(F)-(4-chlórfenyl)[4-(N-cyklopropyl-N-propylaminometyl)-fenyl]metyl}-3-[(3, 5-difluórfenyl) (metylsulfonyl)metylén]-azetidín,1 - {{(FS) - (4-chlorophenyl) {4 - [(4-ethoxycarbonylpiperazinyl) methyl] phenyl] methyl}} - 3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - { {(R) - (4-chlorophenyl) (4 - [(4-ethoxycarbonylpiperazinyl) methyl] phenyl] methyl}} - 3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - ({( S) - (4-chlorophenyl) {4 - [(4-ethoxycarbonylpiperazinyl) methyl] phenyl] methyl}} - 3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(FS) - ( 4-chlorophenyl) [4- (N-cyclopropyl-N-propylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(F) - (4-chlorophenyl) ) [4- (N-Cyclopropyl-N-propylaminomethyl) -phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine,

1-((S)-(4-chlórfenyl)[4-(N-cyklopropyl-N-propylaminometyl)-fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]-azetidín, l-{(RS)-(4-chlórfenyl)[4-(diizopropylaminometyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1 - ((S) - (4-chlorophenyl) [4- (N-cyclopropyl-N-propylaminomethyl) -phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1- {(R) - (4-chlorophenyl) [4- (diisopropylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine,

1-{(R) -(4-chlórfenyl)-[4-(diizopropylaminometyl)fenyl]metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(S)-(4-chlórfenyl)[4-(diizopropylaminometyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén)azetidín,1 - {(R) - (4-chlorophenyl) - [4- (diisopropylaminomethyl) phenyl] methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(S) - (4 chlorophenyl) [4- (diisopropylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene) azetidine,

1-{{ (RS) - (4-chlórfenyl){4-[bis(2-metoxyetyl·)aminometyl]fenyl}-metyl}}-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín,1 - {{(RS) - (4-chlorophenyl) {4- [bis (2-methoxyethyl) aminomethyl] phenyl} methyl}} - 3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine,

1-({(R)-(4-chlórfenyl){4-[bis(2-metoxyetyl)aminometyl]fenyl}-metyl]}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1 - ({(R) - (4-chlorophenyl) {4- [bis (2-methoxyethyl) aminomethyl] -phenyl} -methyl]} - 3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine,

1-{{(S)-(4-chlórfenyl)(4-[bis(2-metoxyetyl)aminometyl]fenyl}-metyl}}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(RS)-(4-chlórfenyl)[4-[di-n-propylaminometyl)fenyl]metyl}-3- [ (3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín,1 - {{(S) - (4-chlorophenyl) (4- [bis (2-methoxyethyl) aminomethyl] phenyl} methyl}} - 3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(RS) - (4-Chlorophenyl) [4- [di-n-propylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine,

1—{(R)-(4-chlórfenyl)[4-(di-n-propylaminometyl)fenyljmetyl)-3- [ (3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, l-{(S)-(4-chlórfenyl)[4-(di-n-propylaminometyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(RS)-(4-chlórfenyl)[4-(piperid-l-ylmetyl)fenyl]metyl}-3- [ (3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, l-{ (R) - (4-chlórfenyl)[4-(piperid-l-ylmetyl)fenyl]metyl}-3- [ (3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín,1 - {(R) - (4-chlorophenyl) [4- (di-n-propylaminomethyl) phenyl] methyl) -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(S) - ( 4-chlorophenyl) [4- (di-n-propylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(RS) - (4-chlorophenyl) [4 - (piperid-1-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(R) - (4-chlorophenyl) [4- (piperid-1- ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine,

1-{(S)-(4-chlórfenyl) [4-(piperid-l-ylmetyl)fenyl]metyl)-3 - [ (3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín,1 - {(S) - (4-Chlorophenyl) [4- (piperid-1-ylmethyl) phenyl] methyl) -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine,

1-((RS)-(4-chlórfenyl)[4-(4-metylpiperazin-l-ylmetyl)fenyl]-meťyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidin, l-{ (í?) - (4-chlórfenyl) [4 - (4-metylpiperazin-l-ylmetyl) fenyl] -metyl}-3-[(3, 5-difluórfenyl) (metylsulfonyl)metylén]azetidin, l-{(S)-(4-chlórfenyl)[4-(4-metylpiperazin-l-ylmetyl)fenyl]-metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidin,1 - ((RS) - (4-chlorophenyl) [4- (4-methylpiperazin-1-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1- { (R) - (4-Chlorophenyl) [4- (4-methylpiperazin-1-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(S) ) - (4-chlorophenyl) [4- (4-methylpiperazin-l-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine,

1-{(RS) -(4-chlórfenyl)[4-(morfolin-4-ylmetyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidin, l-{(F)-(4-chlórfenyl)[4-(morfolin-4-ylmetyl)fenyl]metyl}-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidin, l-{(S)-(4-chlórfenyl)[4-(morfolin-4-ylmetyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidin, l-{(RS)-(4-chlórfenyl)(4-(dietylaminometyl)fenyl·]metyl}-3-[(3,5-difiuórfenyl)(metylsulfonyl)metylén]azetidin, l-{ (i?) - (4-chlórfenyl) [4- (dietylaminometyl) fenyl]metyl}-3- [ (3,5-difluórfenyl)(metylsulfonyl)metylén]azetidin, l-{(S)-(4-chlórfenyl)[4-(dietylaminometyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidin, l-{((RS)-(4-chlórfenyl)[4-(piperazin-2-on-4-ylmetyl)fenyl]-metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidin, l-{(Ä)-(4-chlórfenyl)[4-(piperazin-2-on-4-ylmetyl)fenyl]-metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidin, l-((S)-(4-chlórfenyl)[4-(piperazin-2-on-4-ylmetyl)fenyl]-metyl}-3—[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidin, l-{(RS)-(4-chlórfenyl)[4-(imidazol-l-ylmetyl)fenyl]metyl}-3- [ (3>, 5-difluórfenyl) (metylsulfonyl) metylén] azetidin,1 - {(RS) - (4-chlorophenyl) [4- (morpholin-4-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(F) - (4-chlorophenyl) [4- (morpholin-4-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(S) - (4-chlorophenyl) [4- (morpholin-4-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(RS) - (4-chlorophenyl) (4- (diethylaminomethyl)) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(R) - (4-chlorophenyl) [4- (diethylaminomethyl) phenyl] methyl} -3- [ (3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(S) - (4-chlorophenyl) [4- (diethylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {((RS) - (4-chlorophenyl) [4- (piperazin-2-one-4-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(R) - (4-chlorophenyl) [4- (piperazin-2-one-4-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene ] azetidine, 1 - ((S) - (4-chlorophenyl) [4- (piperazin-2-one-4-ylmethyl) phenyl] methyl 1} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(RS) - (4-chlorophenyl) [4- (imidazol-1-ylmethyl) phenyl] methyl} -3- [ (3,5,5-Difluorophenyl) (methylsulfonyl) methylene] azetidine,

1- { (jR) — (4-chlórfenyl) [4 - (imidazol-l-ylmetyl) fenyl] metyl} -3181 - {(R) - (4-chlorophenyl) [4- (imidazol-1-ylmethyl) phenyl] methyl} -318

-[(3,5-difluórfenyl) (metylsulfonyl·)metylén]azetidin, l-{(S)-(4-chlórfenyl)[4-(imidazol-1-ylmetyl)fenyl]metyl}-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidin, (RS)-1-((4-chlórfenyl)[ 4-(N,N-dimetylkarbamoyl·)fenyl]metyl}-3-[(3, 5-difluórfenyl) (metylsulfonyl)metylén]azetidin, (R) -1-((4-chlórfenyl)[4-(N,N-dimetylkarbamoyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidin, (S) -l-{(4-chlórfenyl) [4- (N,N-dimetylkarbamoyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidin, (RS) — 1—{(4-chlórfenyl)[4-(N-etylkarbamoyl)fenyl]metyl)}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidin, (R) —1—{(4-chlórfenyl)[4-(N-etylkarbamoyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidin, (S) -1-{(4-chlórfenyl)[4-(N-etylkarbamoyl)fenyl]mety]-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidin, (RS)-1-[(4-karbamoylfenyl)(4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidin, (R) -1-[(4-karbamoylfenyl)(4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidin, (S) -1-[(4-karbamoylfenyl)(4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidin,- [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(S) - (4-chlorophenyl) [4- (imidazol-1-ylmethyl) phenyl] methyl} -3 - [(3, 5-Difluorophenyl) (methylsulfonyl) methylene] azetidine, (RS) -1 - ((4-chlorophenyl) [4- (N, N-dimethylcarbamoyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) ( methylsulfonyl) methylene] azetidine, (R) -1 - ((4-chlorophenyl) [4- (N, N-dimethylcarbamoyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (S) -1 - {(4-Chlorophenyl) [4- (N, N-dimethylcarbamoyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (RS) -1- {(4-chlorophenyl) [4- (N-ethylcarbamoyl) phenyl] methyl)} - 3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (R) -1 - {(4-chlorophenyl) [ 4- (N-ethylcarbamoyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (S) -1 - {(4-chlorophenyl) [4- (N-ethylcarbamoyl) phenyl] methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (RS) -1 - [(4-carbamoylphenyl) (4-chlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (R) -1 - [(4-carbamo ylphenyl) (4-chlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (S) -1 - [(4-carbamoylphenyl) (4-chlorophenyl) methyl] -3- [ (3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine,

1-[bis(4-chlórfenyl)metyl]-3-[(3,5-dichlórfenyl)(metylsulfonyl) -metylén]azetidin, l-benzhydryl-3-[(3-metylsulfanylfenyl)(metylsulfonyl)metylén]-azetidin, l-benzhydryl-3-[(3-metylsulfanylmetyl)fenyl)] (metylsulfonyl) -metylén)azetidin,1- [bis (4-chlorophenyl) methyl] -3 - [(3,5-dichlorophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-methylsulfanylphenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-methylsulfanylmethyl) phenyl)] (methylsulfonyl) methylene) azetidine,

1-[bis(4-chlórfenyl)metyl]-3-[(3-kyanofenyl)(metylsulfonyl)-metylén]azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - [(3-cyanophenyl) (methylsulfonyl) methylene] azetidine,

1-[bis(4-chlórfenyl)metyl]-3-[(3-karbamoylfenyl)(metylsulfonyl)-metylén]azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - [(3-carbamoyl-phenyl) (methylsulfonyl) methylene] azetidine,

1-[bis(4-chlórfenyl)metyl]-3-[(3-metoxyfenyl)(metylsulfonyl)-metylén]azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - [(3-methoxyphenyl) (methylsulfonyl) methylene] azetidine,

1-[bis(4-chlórfenyl)metyl]-3-[(3-hydroxyfenyl)(metylsulfonyl)-metylén]azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - [(3-hydroxyphenyl) (methylsulphonyl) methylene] azetidine,

1-[bis(4-chlórfenyl)metyl]-3-[(metylsulfonyl)(3-pyrolidinylfenyl)metylén]azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - [(methylsulphonyl) (3-pyrrolidinylphenyl) methylene] azetidine,

1-[bis(4-chlórfenyl)metyl]-3-[(3-hydroxymetylfenyl)(metylsulfonyl )metylén]azetidín,1- [bis (4-chlorophenyl) methyl] -3 - [(3-hydroxymethylphenyl) (methylsulfonyl) methylene] azetidine,

1-[bis(4-chlórfenyl)metyl]-3-{(metylsulfonyl)[3-(N-piperidylkarbamoyl)fenyl]metylén}azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - {(methylsulfonyl) [3- (N-piperidylcarbamoyl) phenyl] methylene} azetidine,

1-[bis(4-chlórfenyl)metyi]-3-[(metylsulfonyl)(3-trifluórmetylsulf anylfenyl)(metylsulfonyl)metylén]azetidín,1- [bis (4-chlorophenyl) methyl] -3 - [(methylsulfonyl) (3-trifluoromethylsulfanylphenyl) (methylsulfonyl) methylene] azetidine,

1-[bis(4-fluórfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)-metylén]azetidín,1- [Bis (4-fluorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine,

1-[bis(2-fluórfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)-metylén]azetidín,1- [Bis (2-fluorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine,

1-[bis (3-fluórfenyl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyl)-metylén]azetidín, (RS)-1-[(4-chlórfenyl)(tiazol-2-yl)metyl]-3-[(metylsulfonyl)-(fenyl)metylén]azetidín, (R)-1-[(4-chlórfenyl)(tiazol-2-yl)metyl]-3-[(metylsulfonyl)-(fenyl)metylén]azetidín, (S) — 1 -[ (4-chlórfenyl) (tiazol-2-yl) metyl]-3- [ (metylsulfonyl) 201- [bis (3-fluorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (RS) -1 - [(4-chlorophenyl) (thiazol-2-yl) methyl ] -3 - [(methylsulfonyl) - (phenyl) methylene] azetidine, (R) -1 - [(4-chlorophenyl) (thiazol-2-yl) methyl] -3 - [(methylsulfonyl) - (phenyl) methylene] Azetidine, (S) -1 - [(4-chlorophenyl) (thiazol-2-yl) methyl] -3 - [(methylsulfonyl) 20]

- (fenyl)metylén]azetidín, [RS)-1-[(4-chlórfenyl) (tlen-2-yl)metyl)-3-[(3,5-difluórfenyl)-(metylsulfonyl)metylén]azetidin, (R) -1-[(4-chlórfenyl) (tien-2-yl)metyl]-3-[(3,5-difluórfenyl)-(metylsulfonyl)metylén]azetidin, (S) -l-[(4-chlórfenyl) (tien-2-yl)metyl]-3-[(3,5-difluórfenyl)-(metylsulfonyl)metylén]azetidín, l-benzhydryl-3-[(etylsulfonyl)(fenyl)metylén]azetidín,- (phenyl) methylene] azetidine, [RS] -1 - [(4-chlorophenyl) (ethylen-2-yl) methyl) -3 - [(3,5-difluorophenyl) - (methylsulfonyl) methylene] azetidine, (R) ) -1 - [(4-chlorophenyl) (thien-2-yl) methyl] -3 - [(3,5-difluorophenyl) - (methylsulfonyl) methylene] azetidine, (S) -1 - [(4-chlorophenyl) (thien-2-yl) methyl] -3 - [(3,5-difluorophenyl) - (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(ethylsulfonyl) (phenyl) methylene] azetidine,

1-[bis(4-chlórfenyl)metyl]-3-{{3-[N-(4-metylpiperazinyl)-karbamoyl]fenyl](metylsulfonyl)metylén}azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - {{3- [N- (4-methylpiperazinyl) carbamoyl] phenyl] (methylsulfonyl) methylene} azetidine,

1-[bis(4-chlórfenyl)metyl]-3-{[3-(2,2-dimetylkarbohydrazido)-fenyl](metylsulfonyl)metylén}azetidin,1- [Bis (4-chlorophenyl) methyl] -3 - {[3- (2,2-dimetylkarbohydrazido) phenyl] (methylsulfonyl) methylene} azetidine,

1-[bis(tien-2-yl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)-metylén]azetidín,1- [bis (thien-2-yl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine,

1-[bis(p-tolyl)metyl]-3-[(metylsulfonyl)(fenyl)metylén]azetidín,1- [bis (p-tolyl) methyl] -3 - [(methylsulfonyl) (phenyl) methylene] azetidine,

1- [ (4-chlórfenyl) (4-hydroxymetylfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1 - [(4-chlorophenyl) (4-hydroxymethylphenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine,

1-[bis(4-chlórfenyl)metyl]-3-[(3-metylaminofenyl)(metylsulfonyl) metylén] azetidín, (RS)-1-[(4-chlórfenyl)(tiazol-2-yl)metyl]-3-[(3,5-difluórfenyl)- (metylsulfonyl)metylén]azetidín, (R) -1-[(4-chlórfenyl)(tiazol-2-yl)metyl]-3-[(3,5-difluórfenyl)- (metylsulfonyl)metylén]azetidín, (S) -1-[(4-chlórfenyl)(tiazol-2-yl)metyl]-3-[(3,5-difluórfenyl)- (metylsulfonyl)metylén]azetidín,1- [bis (4-chlorophenyl) methyl] -3 - [(3-methylaminophenyl) (methylsulfonyl) methylene] azetidine, (RS) -1 - [(4-chlorophenyl) (thiazol-2-yl) methyl] -3 - [(3,5-difluorophenyl) - (methylsulfonyl) methylene] azetidine, (R) -1 - [(4-chlorophenyl) (thiazol-2-yl) methyl] -3 - [(3,5-difluorophenyl) - (methylsulfonyl) methylene] azetidine, (S) -1 - [(4-chlorophenyl) (thiazol-2-yl) methyl] -3 - [(3,5-difluorophenyl) - (methylsulfonyl) methylene] azetidine,

1- [bis(4-chlórfenyl)metyl]-3-[(metylsulfonyl) (2-metoxykarbonyltien-5-yl)metylén]azetidín, (RS)-1-[[bis(4-chlórfenyl)metyl]-3-hydroxy-3-[(metylsulfonyi)1- [bis (4-chlorophenyl) methyl] -3 - [(methylsulfonyl) (2-methoxycarbonylthien-5-yl) methylene] azetidine, (RS) -1 - [[bis (4-chlorophenyl) methyl] -3- hydroxy-3 - [(methylsulfonyl)

-(2-metoxykarbonyltieň-5-y1)metyl]azetidín,- (2-methoxycarbonylthien-5-y1) methyl] azetidine,

1-[bis(4-chlórfenyl) metyl]-3-[(2-izcbutylaminokarbonyltien-5-yl)(metylsulfonyi)metylén]azetidín,1- [bis (4-chlorophenyl) methyl] -3 - [(2-isobutylaminocarbonythien-5-yl) (methylsulfonyl) methylene] azetidine,

1-[bis(4-chlórfenyl) metyl]-3-[(3-metoxykarbonylfenyl)-(metylsulfonyi)metyl- (PS)]azetidin-3-ol,1- [bis (4-chlorophenyl) methyl] -3 - [(3-methoxycarbonylphenyl) - (methylsulfonyl) methyl- (PS)] azetidin-3-ol,

1-[bis(4-chlórfenyl)metyl]-3-[(metylsulfonyi)(pyrid-4-yl)-metyl-(RS)]azetidin-3-ol,1- [Bis (4-chlorophenyl) methyl] -3 - [(methylsulfonyl) (pyrid-4-yl) methyl- (RS)] azetidin-3-ol,

1-[[bis(4-chlórfenyl)metyl]-3-[(metylsulfonyi)(pyrid-3-yl)-metyl-{RS)]azetidin-3-ol,1 - [[Bis (4-chlorophenyl) methyl] -3 - [(methylsulfonyl) (pyrid-3-yl) methyl {RS)] azetidin-3-ol,

3-({1-[bis(4-chlórfenyl) mety l]a zet idin-3-ylidén} metánsulf onylmetyl)-N-(3-morfolin-4-ylpropyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] and zetidin-3-ylidene} methanesulfonylmethyl) -N- (3-morpholin-4-ylpropyl) benzamide,

3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén]metánsulfonyl metyl)-N-(3-dimetylaminopropyi)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene] methanesulfonylmethyl) -N- (3-dimethylaminopropyl) benzamide,

3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfonyl metyl)-N-(2-(pyrolidin-l-yl)etyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -N- (2- (pyrrolidin-1-yl) ethyl) benzamide,

3- ({1- [bis (4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfonylmetyl)-N-(2-dimetylamino-l-metyletyl)benzamid,3- ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -N- (2-dimethylamino-1-methylethyl) benzamide,

3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfonyl metyl)-N-(piperidín-1-yl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -N- (piperidin-1-yl) benzamide,

3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén]metánsulfonyl metyl)-N-izobutylbenzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene] methanesulfonylmethyl) -N-isobutylbenzamide,

3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-y1idén}metánsulfonyl metyl)-N-(3-imidazol-1-ylpropyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -N- (3-imidazol-1-ylpropyl) benzamide,

3-({1-(bis(4-chlórfenyl)metyl]azetidin-3-ylidén]metánsulfonyl metyl)-N-(2-dimetylaminoetyl)benzamid,3 - ({1- (bis (4-chlorophenyl) methyl) azetidin-3-ylidene] methanesulfonylmethyl) -N- (2-dimethylaminoethyl) benzamide,

N'-metylhydrazid kyseliny 3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfonylmetyl)benzoovej,3 '- ({1- [Bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) benzoic acid N'-methylhydrazide,

3-({1-[bis(4-chlórfenyl)metylazetidin-3-ylidén}metánsulfonylmetyl)-N-(2-morfolin-4-yletyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl-azetidin-3-ylidene} methanesulfonylmethyl) -N- (2-morpholin-4-yl-ethyl) -benzamide,

3-({1-bis(4-chlórfenyl)metyl]azetidin-3-ylidén[metánsulfonyimetyl)-N-(l-etylpyrolidin-2-ylmetyl)benzamid,3 - ({1-bis (4-chlorophenyl) methyl] azetidin-3-ylidene [metánsulfonyimetyl) -N- (l-ethyl-pyrrolidin-2-ylmethyl) -benzamide,

3-({1-(bis(4-chlórfenyl)metyl]azetidin-3-ylidén(metánsulfonylmetyl)-N-(2,2-dimetylpropyl)benzamid,3 - ({1- (bis (4-chlorophenyl) methyl] azetidin-3-ylidene (methanesulfonylmethyl) -N- (2,2-dimethylpropyl) benzamide,

3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfony1metyl)-N-(cyklohexylmetyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} metánsulfony1metyl) -N- (cyclohexylmethyl) -benzamide,

3-({1-[bis (4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfonylmetyl)-N-(cyklopropylmetyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -N- (cyclopropylmethyl) benzamide,

3-((1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfonylmetyl) -N-(2-metylbutyl)benzamid,3 - ((1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -N- (2-methylbutyl) benzamide,

3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén)metánsulfony1metyl)-N-(2-fenylpropyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene) metánsulfony1metyl) -N- (2-phenylpropyl) benzamide,

- ({1- [bis (4-chlórfenyl)metyl]azetidin-3-ylidén[metánsulfonylmetyl)-N- (tetrahydrofuran-2-ylmetyl)benzamid,- ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene [methanesulfonylmethyl) -N- (tetrahydrofuran-2-ylmethyl) benzamide,

3-((1-[bis (4-chlórfenyl)metyl]azetidin-3-ylidén[metánsulfonylmetyl)-N-(2,2-difenyletyl)benzamid,3 - ((1- [bis (4-chlorophenyl) methyl) azetidin-3-ylidene [methanesulfonylmethyl) -N- (2,2-diphenylethyl) benzamide,

3-((1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén)metánsulfonylmetyl)-N-(2-etylbutyi)benzamid, metylester kyseliny 4-{[3-((1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén[metánsulfonylmetyl)benzoylamino]metyl}cyklohexánkarboxylovej,3 - ((1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene) methanesulfonylmethyl) -N- (2-ethylbutyl) benzamide, 4 - {[3 - ((1- [bis (4- chlorophenyl) methyl] azetidin-3-ylidene [methanesulfonylmethyl) -benzoylamino] methyl} cyclohexanecarboxylate,

2-amino-l-(4-(3- ({l-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}-metánsulfonylmetyl)fenyl]piperazin-1-y1[etanón, terc-butylester kyseliny (2-{4-[3-({l-[bis(4-chlórfenyl)metyl]-azetidin-3-ylidén)metánsulfonylmetyl)fenyl]piperazin-l-yl)-2-oxoetyl)karbamovej, l-{4-[3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén)-metánsulfonylmetyl)fenyl]piperazin-l-yl}-2-metylaminoetanón, terc-butylester kyseliny (2-{4-[3-({l-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén)metánsulfonylmetyl)fenyl]piperazin-l-yl)-2-oxoetyl)-N-metylkarbamovej,2-Amino-1- (4- (3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} -methanesulfonylmethyl) phenyl] piperazin-1-yl) ethanone, tert-butyl ester (2) - {4- [3 - ({1- [bis (4-chloro-phenyl) -methyl] -azetidin-3-ylidene) -methanesulfonylmethyl) -phenyl] -piperazin-1-yl) -2-oxo-ethyl) -carbamic acid, 1- {4- [ 3 - ({1- [Bis (4-Chloro-phenyl) -methyl] -azetidin-3-ylidene) -methanesulfonylmethyl) -phenyl] -piperazin-1-yl} -2-methylamino-ethanone, tert-butyl ester (2- {4- [3- ({l- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene) methanesulfonylmethyl) phenyl] piperazin-l-yl) -2-oxo-ethyl) -N-butyl ester,

N-metylamid kyseliny 4-[3-({[1-bis(4-chlórfenyl)metyl]-azetidin-3-ylidén)metánsulfonylmetylfenyl]piperazin-1-karbotioovej,4- [3 - ({[1-Bis (4-chlorophenyl) methyl] azetidin-3-ylidene) methanesulfonylmethylphenyl] piperazine-1-carbothioic acid N-methylamide,

N-metylamid kyseliny 4-[3-({1-[bis(4-chlórfenyl)metyl]-azetidin-3-ylidén}metánsulfonylmetylfenyl]piperazín-1-karboxylovej, metylester kyseliny 4-[3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén)metánsulfonylmetyl)fenyl]piperazín-1-karboxylovej,4- [3 - ({1- [Bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethylphenyl] piperazine-1-carboxylic acid N-methylamide, methyl 4- [3 - ({1- [bis] (4-chlorophenyl) methyl] azetidin-3-ylidene) methanesulfonylmethyl) phenyl] piperazine-1-carboxylic acid,

1-[3-({1-[bi s(4-chlórfenyl)metyl]azetidin-3-ylidénImetánsulf onylmetyl) fenyl]-4-izobutylpiperazín, l-[3-({l-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén)metánsulfonylmetyl)fenyl]-4-etylpiperazín,1- [3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene-methanesulfonylmethyl) phenyl] -4-isobutylpiperazine, 1- [3 - ({1- [bis (4-chlorophenyl) methyl] ] azetidin-3-ylidene) methanesulfonylmethyl) phenyl] -4-ethylpiperazine,

4-acetyl-1-[3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}-metánsulfonylmetyl)fenyl]piperazin, l-{4-[3-({l-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfonylmetyl)fenyl]piperazin-l-yl}-2-dimetylaminoetanón, i4-acetyl-1- [3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} -methanesulfonylmethyl) phenyl] piperazine, 1- {4- [3 - ({1- [bis ( 4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) phenyl] piperazin-1-yl} -2-dimethylaminoethanone; i

1—[3—({1—[bis(4-chlórfenyl)metyl]azetidin-3-ylidén)metánI sulfonylmetyl)fenyl]piperazin, terc-butylester kyseliny 4-[3-({1-[bis(4-chlórfenyl)metyl]244- [3 - ({1- [Bis (4-chlorophenyl) -1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene) methanesulfonylmethyl) phenyl] piperazine, tert -butyl ester ) -methyl] 24

-azetidin-3-ylidén}metánsulfonylmetyl)fenyl]piperazín-l-karboxylovéj,azetidin-3-ylidene} methanesulfonylmethyl) phenyl] piperazine-l-carboxylic acid,

1-[bis(4-metoxykarbonylfenyl)metyl]-3-[(3,5-difluórfenyl)-(metylsulfonyl)metylén]azetidín,1- [Bis (4-methoxycarbonylphenyl) methyl] -3 - [(3,5-difluorophenyl) - (methylsulphonyl) methylene] azetidine,

3- acetoxy-l-[bis (4 -metoxy karbonyl fenyl·) metyl] -3 - [ (3, 5-dif luórfenyl)(metylsulfonyl)metyl-(RS)]azetidín, (RS)-4-[4-((4-chlórfenyl){3-[(3,5-difluórfenyl)metánsulfony1metylén]azetidin-l-yl}metyl)benzyl]morfolín,3-Acetoxy-1- [bis (4-methoxycarbonylphenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methyl (RS)] azetidine, (RS) -4- [4- ((4-chlorophenyl) {3 - [(3,5-difluorophenyl) metánsulfony1metylén] azetidin-l-yl} methyl) benzyl] morpholine,

4- (4-{3-[(l-benzhydrylazetidin-3-ylidén)metánsulfonylmetyl]-fenoxy}butyl)morfolín,4- (4- {3 - [(1-benzhydrylazetidin-3-ylidene) methanesulfonylmethyl] -phenoxy} butyl) morpholine,

- (4-{3-[(l-benzhydrylazetidin-3-ylidén)metánsulfonylmetyl]-fenoxy}propyl)morfolín,- (4- {3 - [(1-benzhydrylazetidin-3-ylidene) methanesulfonylmethyl] -phenoxy} propyl) morpholine,

N-(1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}tíen-2-ylsulfónamid,N- (1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} thien-2-ylsulfonamide,

N-(1- [bis(4-chlórfenyl)metyl]azetidin-3-yl}-4-metoxyfeny1sulfónamid,N- (1- [bis (4-chlorophenyl) methyl] azetidin-3-yl) -4-methoxyphenylsulfonamide,

N-[4-(N-{l-[bis(4-chlórfenyl)metyl]azetidin-3-yl}sulfamoyi)-fenyl]acetamid,N- [4- (N- {l- [bis (4-chlorophenyl) methyl] azetidin-3-yl} sulfamoyl) phenyl] acetamide,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-4-metylfenylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -4-methylphenylsulfonamido,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-3,4-dimetoxyfenylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3,4-dimetoxyfenylsulfónamid,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-3-fluórfenylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3-fluorophenylsulfonamido,

N-{1- [bis(4-chlórfenyl)metyl]azetidin-3-yl}-3,4-dichlórfenyisulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3,4-dichlorophenyisulfonamide,

N-(1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-3-kyanofenylsulfónamid,N- (1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3-kyanofenylsulfónamid,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-2,5-dimetoxyfenylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -2,5-dimetoxyfenylsulfónamid,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-3-trifluórmetylfenylsulfdnamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3-trifluórmetylfenylsulfdnamid,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl} naft-2-ylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} naphth-2-ylsulfonamide,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}naft-l-ylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} naphth-l-ylsulfonamide,

N-[1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-3,4-difluórfenylsulfónamid,N- [1- [Bis (4-chlorophenyl) methyl] azetidin-3-yl} -3,4-difluórfenylsulfónamid,

N- {1- [bis (4-chlór f enyl) metyl] azetidin-3-yl }-1-metyl-lH-imidazol-4-ylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -1-methyl-1H-imidazol-4-ylsulfonamide,

N-[4-(N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-ylJsulfamoyl)-2-chlórfenyl]acetamid,N- [4- (N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-ylJsulfamoyl) -2-chlorophenyl] acetamide,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}pyrid-3-ylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} pyrid-3-ylsulfonamide,

N-{1-[bis (4-chlórfenylmetyl]azetidin-3-yl}-4-fluórfenylsulfónamid,N- {1- [bis (4-chlorophenylmethyl) azetidin-3-yl} -4-fluorophenylsulfonamide,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}chinol-8-ylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} quinolin-8-ylsulfonamide,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}fenylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} phenylsulfonamide,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}(fenylmetyl)sulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} (phenylmethyl) sulfonamide,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-3,5-difluórfenylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3,5-difluórfenylsulfónamid,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}pyrid-2-y1sulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} pyridin-2-y1sulfónamid,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-(3-fluór-5-pyrolidin-l-ylfenyl)sulfónamid, íN- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} - (3-fluoro-5-pyrrolidin-1-ylphenyl) sulfonamide;

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-metyl-4-fluór26 fenylsulfónamid,N- {1- [bis (4-chloro-phenyl) -methyl] -azetidin-3-yl} -N-methyl-4-fluoro-26-phenylsulfonamide,

N-{1-[bis[4-chlórfenyl)metyl]azetidin-3-yl}-N-metylchinol-8-ylsulfónamid,N- {1- [bis [4-chlorophenyl) methyl] azetidin-3-yl} -N-methyl-quinolin-8-ylsulfonamide,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-metylfenylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N-methylphenylsulfonamido,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-metyl(fenylmetyl) -sulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N-methyl (phenylmethyl) sulfonamide,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-3-sulfamoylfenylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3-sulfamoylfenylsulfónamid,

2-benzénsulfonyl-N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-acetamid,2-benzenesulfonyl-N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -acetamide,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-2-(4-toluén-4-sulfonyl)acetamid, (3-chlór-4-metylsulfonyltiofén-2-karboxy)-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl]amid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -2- (4-toluene-4-sulfonyl) acetamide, (3-chloro-4-methylsulfonylthiophene-2-carboxy) - {1 - [bis (4-chlorophenyl) methyl] azetidin-3-yl] -amide,

N-{1- [bis (4-chlórfenyl)metyl]azetidin-3-yl}-3-(2-fenyletylénsulfonyl)propiónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3- (2-phenylethylenesulfonyl) propionamide,

N-{1- [bis (4-chlórfenyl)metyl]azetidin-3-yl}-4-metylsulfonylbenzamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -4-methylsulfonylbenzamide,

N-{1- [bis (4-chlórfenyl)metyl]azetidin-3-yl}-4-metánsulfonylbenzamid, (5-metylsulfonyltiofén-2-karboxy)-{1-[bis(4-chlórfenyl)-metyl]azetidin-3-yl}amid, (5-metylsulfonyl-3-metyl-4-vinyltiofén-2-karboxy){1-[bis-(4-chlórfenyl)metyl]azetidin-3-yl}amid, (RS)-N-{1-[(4-chlórfenyl)pyridin-3-ylmetyl]azetidin-3-yl}-3,5-difluórbenzénsulfónamid, (RS)-N-{1-[(4-chlórfenyl)pyrimidin-5-ylmetyl]azetidin-3-yl}-3,5'-difluórbenzénsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -4-methanesulfonylbenzamide, (5-methylsulfonylthiophene-2-carboxy) - {1- [bis (4-chlorophenyl) methyl] azetidine- 3-yl} amide, (5-Methylsulfonyl-3-methyl-4-vinylthiophene-2-carboxy) {1- [bis- (4-chlorophenyl) methyl] azetidin-3-yl} amide, (RS) -N- {1 - [(4-chlorophenyl) pyridin-3-ylmethyl] azetidin-3-yl} -3,5-difluorobenzenesulfonamide, (RS) -N- {1 - [(4-chlorophenyl) pyrimidin-5-ylmethyl] azetidine 3-yl} -3,5'-difluoro-benzenesulfonamide,

N-{l-[bis(4-chlórfenyl)metyl]azetidin-3-yl)-N-(6-chlórpyrid-2-yl)metylsulfónamid,N- {l- [bis (4-chlorophenyl) methyl] azetidin-3-yl) -N- (6-chloropyrid-2-yl) methylsulfonamide,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(6-etylpyrid-2-yl)metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (6-ethyl-pyridin-2-yl) methylsulfonamide,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-chinol-6-ylmetylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N-quinol-6-ylmetylsulfónamid,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-y1}-N-chinol-5-y1metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-y1} -N-quinolin-5-y1metylsulfónamid,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-izochinol-5-ylmetylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N-isoquinolin-5-ylmetylsulfónamid,

N-(1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-pyrid-3-ylmetylsulfónamid,N- (1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N-pyrid-3-ylmetylsulfónamid,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(pyrid-l-oxid-3-yl)metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (pyrid-l-oxide-3-yl) methylsulfonamide,

N-(ÍR,2 S,4 S)-bicyklo[2,2,1]hept-2-yl-N-{l-[bis-(4-chlórfenyl·)-metylazetidin-3-yljmetylsulfónamid,N- (1R, 2S, 4S) -bicyclo [2.2.1] hept-2-yl-N- {1- [bis- (4-chloro-phenyl) -methyl-azetidin-3-yl] -methylsulfonamide,

N-(ÍR, 2R, 4S) -(bicyklo[2,2,1] hept-2-yl) -N-{1—(bis-(4-chlórfenyl) -metyl]azetidin-3-y1]metylsulfónamid,N- (1R, 2R, 4S) - (Bicyclo [2.2.1] hept-2-yl) -N- {1- (bis- (4-chloro-phenyl) -methyl] -azetidin-3-yl) -methylsulfonamide,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-y1}-N-(3,5-difluórfenyl)metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-y1} -N- (3,5-difluorophenyl) methylsulfonamide,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-y1}-N-(tiazol-2-yl)-metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-y1} -N- (thiazol-2-yl) methylsulphonamide,

N-{ 1- [bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(3-metoxyfenyl)-metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (3-methoxyphenyl) methylsulfonamide,

N-{1-[bis(4-chlórfenyl)metyl] azetidin-3-y1}-N-(3-hydroxyfenyl)28N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (3-hydroxyphenyl) 28

-metylsulfónamid,methylsulphonamide.

N-{1-[bis(4-chlorfenyl)metyl]azetidin-3-yl}-N-(3-hydroxymetyl fenyl)metylsulfónamid, etyl-N-{1-[bis (4-chlórfenyl)metyl]azetidin-3-yl}-N-(metylsulfonyl) -3-aminobenzoát,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (3-hydroxymethylphenyl) methylsulfonamide, ethyl N- {1- [bis (4-chlorophenyl) methyl] azetidin-3 -yl} -N- (methylsulfonyl) -3-aminobenzoate,

N-{l-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(izobutylpiperid-4-yl)metylsulfónamid,N- {l- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (izobutylpiperid-4-yl) methylsulfonamide,

N-benzyl-N- {1- [bis (4-chlór f enyl) metyl]azetidin-3-yl }amín,N-benzyl-N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} amine,

N-{1-[bis(4-chlórfenyl)metyl]azetidín-3-yl}-N-(3,5-difluórbenzyl)amín,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (3,5-difluorobenzyl) amine,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(3,5-difluórbenzyl)metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (3,5-difluorobenzyl) methylsulfonamide,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(pyrid-3-ylmetyl)metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (pyrid-3-ylmethyl) methylsulfonamide,

N-{1-[bis(4-fluórfenyl)metyl]azetidin-3-yl}—N—(3,5-difluórfenyl) metylsulfónamid, (RS)-N-{1-[(4-chlórfenyl)pyrid-3-ylmetyl]azetidin-3-yl}-N-(3,5-difluórfenyl)metylsulfónamid, (P)-N-{1-[(4-chlórfenyl)pyrid-3-ylmetyl]azetidin-3-yl}-N-(3,5-difluórfenyl)metylsulfónamid, (S)-N-{1-[(4-chlórfenyl)pyrid-3-ylmetyl]azetidín-3-yl}-N-(3,5-difluórfenyl)metylsulfónamid, (RS)-N-(1-[(4-chlórfenyl)pyrid-4-ylmetyl]azetidin-3-yl}-N-(3,5-difluórfenyl)metylsulfónamid, (R)-N-{1-[(4-chlórfenyl)pyrid-4-ylmetyl]azetidin-3-yl}-N-(3,5-difluórfenyl)metylsulfónamid, (S)-N-{1-[(4-chlórfenyl)pyrid-4-ylmetyl]azetidin-3-yl}-N-(3,'5-dif luórfenyl)metylsulfónamid, {RS) —N—{1—[(4-chlórfenyl)pyrimidín-5-ylmetyl]azetidin-3-yl}-N-(3,5-difluórfenyl)metylsulfónamid, (R) -N-{1-[(4-chlórfenyl)pyrimidín-5-ylmetyl]azetidin-3-yl}-N-(3,5-difluórfenyl)metylsulfónamid, (S) -N-{1-[(4-chlórfenyl)pyrimidin-5-ylmetyl]azetidin-3-yl}-N-(3,5-difluórfenyl)metylsulfónamid,N- {1- [bis (4-fluorophenyl) methyl] azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide, (RS) -N- {1 - [(4-chlorophenyl) pyrid-3 -ylmethyl] azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide, (P) -N- {1 - [(4-chlorophenyl) pyrid-3-ylmethyl] azetidin-3-yl} -N - (3,5-difluorophenyl) methylsulfonamide, (S) -N- {1 - [(4-chlorophenyl) pyrid-3-ylmethyl] azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide, ( RS) -N- (1 - [(4-chlorophenyl) pyrid-4-ylmethyl] azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide, (R) -N- {1 - [(4) (chlorophenyl) pyrid-4-ylmethyl] azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide, (S) -N- {1 - [(4-chlorophenyl) pyrid-4-ylmethyl] azetidine- 3-yl} -N- (3,5-difluorophenyl) methylsulfonamide, (RS) -N- {1 - [(4-chlorophenyl) pyrimidin-5-ylmethyl] azetidin-3-yl} -N- (3 (R) -N- {1 - [(4-chlorophenyl) pyrimidin-5-ylmethyl] azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide, (S) -, 5-difluorophenyl) methylsulfonamide, (S) - N {1 - [(4-chlorophenyl) pyrimidin-5-ylmethyl] azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide,

N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(3,5-difluórfenyl) benzylsulfónamid, ich optické izoméry a ich farmaceutický prijateľné soli s anorganickou alebo organickou kyselinou.N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (3,5-difluorophenyl) benzylsulfonamide, their optical isomers, and their pharmaceutically acceptable salts with an inorganic or organic acid.

A ešte najmä výhodné sú nasledovné azetidínové deriváty:And yet particularly preferred are the following azetidine derivatives:

1-[bis(4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)-metyl-(RS)]azetidin-3-ol,1- [Bis (4-chlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methyl- (RS)] azetidin-3-ol,

3-acetoxy-l-[bis(4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl)-(metylsulfonyl)metyl)metylsulfonylmetyl-(RS)]azetidín,3-acetoxy-l- [bis (4-chlorophenyl) methyl] -3 - [(3,5-difluorophenyl) - (methylsulfonyl) methyl) methylsulfonylmethyl (RS)] azetidine,

1-[bis(4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyl)-metylén]azetidín, ich optické izoméry a ich farmaceutický prijateľné soli s anorganickou alebo organickou kyselinou.1- [bis (4-chlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, their optical isomers, and their pharmaceutically acceptable salts with an inorganic or organic acid.

Ako príklady farmaceutický prijateľných solí azetidínových derivátov sa uvádzajú nasledovné soli: benzensulfonát, bromid, chlorid, citrát, etánsulfonát, fumarát, glukonát, jodát, izetionát, maleát, metánsulfonát, metylén-bis-3-oxynaftoát, nitrát, oxalat, pamoát, fosfát, salicylát, sukcinát, sulfát, vínan, teofylínacetát a p-toluénsulfonát.Examples of pharmaceutically acceptable salts of azetidine derivatives include: benzenesulfonate, bromide, chloride, citrate, ethanesulfonate, fumarate, gluconate, iodate, isethionate, maleate, methanesulfonate, methylene-bis-3-oxynaphthate, nitrate, oxalate, pamoate, oxalate, pamoate, oxalate, pamoate salicylate, succinate, sulfate, tartrate, theophylline acetate and p-toluenesulfonate.

Ďalšie antagonisty CB1 na použitie v kombináciách podľa predkladaného vynálezu sú napríklad pyrazolové deriváty opísané v EP 576 357, EP 658 546, EP 656 354, WO 97/19063 a WO 00/46209, benzotiofénové a benzofuránové deriváty opísané vo WO 96/02248 alebo sulfónamidy opísané vo WO 98/37061. Uvádzajú sa najmä produkty známe pod kódom SR141716 a LY320135.Other CB1 antagonists for use in the combinations of the present invention are, for example, the pyrazole derivatives described in EP 576 357, EP 658 546, EP 656 354, WO 97/19063 and WO 00/46209, the benzothiophene and benzofuran derivatives described in WO 96/02248 or sulfonamides described in WO 98/37061. Particular mention is made of the products known under the codes SR141716 and LY320135.

Príklady uskutočnenia vynálezuDETAILED DESCRIPTION OF THE INVENTION

Synergický účinok kombinácie sibutramínu a antagonistu CB1 na príjem potravy sa stanovil podlá nasledovného protokolu.The synergistic effect of the combination of sibutramine and CB1 antagonist on food intake was determined according to the following protocol.

Na štúdiu sa použili obézne potkany Fa/fa Zucker vo veku 7 týždňov a pochádzajúce od Iffa-Credo, Francúzsko. Tieto potkany sa umiestnili do jednotlivých klietok a vážili sa každý deň medzi 8 a 10 hodinou odpoludnia. V rovnakom čase sa vážilo aj množstvo potravy. Táto potrava (M20, Pietrement, Francúzsko) sa menila každý deň a potkany mali volný prístup k potrave počas 24 hodín. Potkany sa ošetrovali počas 1 týždňa vehikulom (miglyol 812N a 0,5 % metylcelulóza/0,2 % polysorbát 80) v dvoch po sebe idúcich podaniach. Potkany sa od 8 dňa ošetrovali orálnou cestou antagonistom CB1 (l-[bis(4-dichlórfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)metylénjazetidín alebo sibutramínom (pozri nasledovnú tabuľku).The obese Fa / fa Zucker rats at 7 weeks of age from Iffa-Credo, France were used for the study. These rats were placed in individual cages and weighed every day between 8 and 10 pm. At the same time, the amount of food was weighed. This food (M20, Pietrement, France) was changed every day and the rats had free access to food for 24 hours. Rats were treated with vehicle (miglyol 812N and 0.5% methylcellulose / 0.2% polysorbate 80) for 1 week in two consecutive administrations. Rats were treated orally from day 8 with CB1 antagonist (1- [bis (4-dichlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene-ketidine or sibutramine (see table below).

Sibutramín sa rozpustil v roztoku zmesi 0,5 % metylcelulóza/0, 2% polysorbát 80 a podal sa v dávke 3 mg/kg; antaaonista CB1 sa rozpustil v miglyole 812N (Huls, Allemagne, Nemecko) v množstve 0,6 mg/kg, a tieto dva produkty sa podali v objeme 1 ml/kg. Každá skupina sa skladala z 12 až 14 zvierat, vytvorili sa nasledovné skupiny a zvieratá sa ošetrovali každý deň počas 5 dní v dvoch po sebe idúcich podaniach.Sibutramine was dissolved in a solution of 0.5% methylcellulose / 0.2% polysorbate 80 and administered at a dose of 3 mg / kg; the CB1 antagonist was dissolved in miglyole 812N (Huls, Allemagne, Germany) at 0.6 mg / kg, and the two products were administered in a volume of 1 ml / kg. Each group consisted of 12-14 animals, the following groups were formed, and the animals were treated every day for 5 days in two consecutive administrations.

Skupina Group Prvé podanie First submission Druhé podanie Second administration 1 „skupina s vehikulom 1 "Vehicle group miglyol Miglyol 0,5 % metylceluióza/0,2 % polysorbát 0,5% methylcellulose / 0,2% polysorbate 2 „sibutramínová skupina 2 "sibutramínová group miglyol Miglyol sibutramín 3 mg/kg sibutramine 3 mg / kg 3 3 antagonista antagonist 0,5 % metylcelulóza/0,2 % 0,5% methylcellulose / 0,2% „skupina antagonistu CB1 "Antagonist group CB1 CB1, 0,6 mg/kg CB1, 0.6 mg / kg polysorbát polysorbate 4 „kombinačná skupina 4 'Combination group antagonista CB1, 0,6 mg/kg antagonist CB1, 0.6 mg / kg sibutramín 3 mg/kg sibutramine 3 mg / kg

Spotreba potravín každého zvieraťa sa merala každý deň. Výsledky sú uvedené ako množstvo potravín spotrebovaných v priebehu ošetrovania uskutočňovaného počas 5 dní. Získané výsledky sú uvedené v nasledovnej tabulke.Food consumption of each animal was measured daily. The results are shown as the amount of food consumed during the treatment for 5 days. The results obtained are shown in the following table.

Liečba treatment Spotreba potravy v priebehu 5 dňovej liečby (g) Food consumption within 5 days treatment (g) Vehikulum vehicle 25,52 ± 0,30 25.52 ± 0.30 Sibutramín 3 mg/kg Sibutramine 3 mg / kg 24,60 ± 0,32* 24.60 ± 0.32 * Antagonista CB1 0,6 mg/kg CB1 antagonist 0.6 mg / kg 24,00 ± 0,24** 24.00 ± 0.24 ** Sibutramín (3 mg/kg) + antagonista CB1 (0,6 mg/kg) Sibutramine (3 mg / kg) + CB1 antagonist (0.6 mg / kg) 22,76 ± 0,02*** 22.76 ± 0.02 ***

*p <,0,05 **p < 0,01 ***p< 0,001* p <, 0.05 ** p <0.01 *** p <0.001

Výsledky ukazujú, že v prípade zvierat, ktoré dostávali kom32 bináciu sibutramínu a antagonistu CB1 je zníženie v spotrebe potravy oveľa väčšie než v prípade zvierat, ktoré dostávali samotný sibutramín alebo samotný antagonista CB1.The results show that in animals receiving sibutramine and CB1 antagonist combinations, the reduction in food consumption is much greater than in animals receiving sibutramine alone or CB1 antagonist alone.

Zlúčeniny sa v kombinácii môžu podávať orálne, parenterálne, transdermálne alebo rektálne, buď súčasne, oddelene alebo postupne.The compounds may be administered orally, parenterally, transdermally, or rectally, either simultaneously, separately or sequentially.

Predkladaný vynález sa týka aj farmaceutických kompozícií obsahujúcich kombináciu sibutramínu, jeho hydrátu alebo jeho farmaceutický prijateľnej soli a antagonistu receptora CB1 v čistom stave s jedným alebo viacerými kompatibilnými riedidlami a/alebo pomocnými látkami a/alebo v kombinácii s iným farmaceutický prijateľným aktívnym produktom na súčasné, oddelené alebo postupné použitie.The present invention also relates to pharmaceutical compositions comprising a combination of sibutramine, a hydrate thereof, or a pharmaceutically acceptable salt thereof, and a CB1 receptor antagonist in pure form with one or more compatible diluents and / or excipients and / or in combination with another pharmaceutically acceptable active product. separate or sequential use.

Ako tuhé kompozície na orálne podanie sa môžu použiť tablety, pilulky, prášky (tvrdé želatínové kapsule, vrecká) alebo granule. V týchto prostriedkoch sa aktívna zložka podľa vynálezu zmieša pod prúdom argónu s jedným alebo viacerými inertnými zrieďovadlami, ako je škrob, celulóza, sacharóza, laktóza alebo oxid kremičitý. Tieto kompozície môžu obsahovať aj iné látky než sú zrieďovadlá, napríklad mazadlá, ako jes stearát horečnatý alebo mastenec, farbivá, povlaky (tablety potiahnuté cukrom) alebo glazúru.As solid compositions for oral administration, tablets, pills, powders (hard gelatin capsules, sachets) or granules may be used. In these compositions, the active ingredient of the invention is mixed under one stream of argon with one or more inert diluents such as starch, cellulose, sucrose, lactose or silica. These compositions can comprise substances other than diluents, e.g. a lubricant such as a magnesium stearate or talc, a coloring, a coating (sugar-coated tablets) or a glaze.

Ako kvapalné kompozície na orálne podanie sa môžu použiť farmaceutický prijateľné roztoky, suspenzie, emulzie, sirupy a elixíry obsahujúce inertné zrieďovadlá, ako je voda, etanol, glycerol, rastlinné oleje alebo parafínový olej. Kompozície môžu obsahovať aj iné látky než sú· zrieďovadlá, napríklad zmáčadlá, sladidlá, zahusťovadlá, aromáty alebo stabilizátory.As liquid compositions for oral administration, pharmaceutically acceptable solutions, suspensions, emulsions, syrups and elixirs containing inert diluents such as water, ethanol, glycerol, vegetable oils or paraffin oil may be used. The compositions may also contain substances other than diluents, for example wetting, sweetening, thickening, flavoring or stabilizing agents.

Sterilnými kompozíciami na parenterálne podanie môžu byť výhodne roztoky, ktoré sú vodné alebo nevodné, suspenzie alebo emulzie. Ako rozpúšťadlo alebo vehikulum sa môže použiť voda, propyléngiykol, polyetylénglykol, rastlinné oleje, najmä olivovýThe sterile compositions for parenteral administration may preferably be solutions which are aqueous or non-aqueous, suspensions or emulsions. Water, propylene glycol, polyethylene glycol, vegetable oils, especially olive oil, can be used as a solvent or vehicle.

I olej', in j ikovatelné organické estery, napríklad etyloleát, alebo iné organické rozpúšťadlá. Tieto kompozície môžu obsahovať pomocné látky, najmä zmáčadlá, izotonizačné látky, emulgátory, dispergátory a stabilizátory. Sterilizácia sa môže uskutočniť niekoľkými spôsobmi, napríklad sterilnou filtráciou, včlenením sterilizačných činidiel do prostriedku, ožiarením alebo zohriatím. Môžu sa pripraviť aj vo forme sterilných tuhých prostriedkov, ktoré sa môžu rozpustiť v čase použitia v sterilnej vode alebo inom injikovatelnom prostredí.Oil, injectable organic esters, for example ethyl oleate, or other organic solvents. These compositions may contain excipients, in particular wetting, isotonic, emulsifying, dispersing and stabilizing agents. Sterilization can be accomplished in several ways, for example by sterile filtration, incorporation of sterilizing agents into the composition, irradiation or heating. They can also be prepared in the form of sterile solid compositions which can be dissolved at the time of use in sterile water or other injectable medium.

Kompozíciami na rektálne podanie sú čapíky alebo rektálne kapsule, ktoré obsahujú okrem aktívnej zložky pomocné látky, ako je kakaové maslo, polosyntetické glyceridy alebo polyetylénglykoly.Compositions for rectal administration are suppositories or rectal capsules which contain, in addition to the active ingredient, excipients such as cocoa butter, semisynthetic glycerides or polyethylene glycols.

Farmaceutické kompozície zvyčajne obsahujú 0,5 až 10 mg sibutramínu a 0,1 až 200 mg antagonistu CB1.The pharmaceutical compositions usually contain 0.5 to 10 mg sibutramine and 0.1 to 200 mg CB1 antagonist.

Predkladaný vynález sa týka aj spôsobu liečenia obezity, ktorý spočíva v podaní pacientovi kombinácie podľa vynálezu buď súčasne alebo oddelene alebo po čiastkových dávkach.The present invention also relates to a method of treating obesity comprising administering to a patient a combination of the invention either simultaneously or separately or in divided doses.

Dávka závisí od požadovaného účinku, od trvania liečby a od cesty podania; vo všeobecnosti sa podáva dospelému pacientovi 1 až 15 mg sibutramínu denne pri orálnom podaní a 0,10 až 500 mg antagonistu CB1 denne pri orálnom podaní.The dose depends on the effect desired, the duration of treatment and the route of administration; in general, 1 to 15 mg sibutramine per day for oral administration and 0.10 to 500 mg CB1 antagonist per day for oral administration are administered to an adult patient.

Vo všeobecnosti ošetrujúci lekár stanoví vhodnú dávku podľa veku, hmotnosti a akéhokolvek ďalšieho faktora špecifického pre subjekt, ktorý sa má liečiť.Generally, the attending physician will determine the appropriate dose according to the age, weight and any other factor specific to the subject to be treated.

Claims (12)

PATENTOVÉ NÁROKYPATENT CLAIMS 1. Kombinácia antagonistú CB1 a sibutramínu, jeho hydrátu alebo jednej z jeho farmaceutický prijateľných solí.A combination of a CB1 antagonist and sibutramine, a hydrate thereof, or one of its pharmaceutically acceptable salts. 2. Kombinácia podlá nároku 1, kde antagonistom CB1 je zlúčenina všeobecného vzorca (I)The combination of claim 1, wherein the CB1 antagonist is a compound of formula (I) R3 kde každá skupina R znamená reťazec A alebo B, /S02Rl ?r’ so2r‘R 3 where each R is A or B, / SO 2 R 1 ? r 'so 2 r' C CH alebo C-CHC CH or C-CH R2 R2 (A) (B)R 2 R 2 (A) (B) R1 znamená metylovú skupinu alebo etylovú skupinu,R 1 is methyl or ethyl, R2 znamená buď aromatickú skupinu vybranú z fenylovej skupiny, naftylovej skupiny alebo indenylovej skupiny, pričom tieto aromatické skupiny môžu byť nesubstituované alebo substituované jedným alebo viacerými atómami halogénu, alkylovými skupinami, alkoxyskupinami, skupinami -CO-alk, hydroxylovými skupinami, skupinami -COOR5, formylovými skupinami, trifluórmetylovými skupinami, trifluórmetylsulfanyiovými skupinami, trifluórmetoxyskupinami, nitroskupinami, skupinamiR 2 represents either an aromatic group selected from phenyl, naphthyl and indenyl, these aromatics being unsubstituted or substituted by one or more halogen, alkyl, alkoxy, -CO-alk, hydroxyl, -COOR 5 , formyl groups, trifluoromethyl groups, trifluoromethylsulfanyl groups, trifluoromethoxy groups, nitro groups, groups -NR6R7, skupinami -CO-NH-NR6R7, skupinami -N (alk) COOR8, kyanoskupinami, skupinami -CONHR9, skupinami -CO-NRi6R17, alkylsulf anylovými skupinami, hydroxyalkylovými skupinami, skupinami -O-alk-NR12R13 alebo alkyltioalkylovými skupinami, alebo ' heteroaromatickú skupinu vybranú z benzofurylovej skupiny, benzotiazolylovej skupiny, benzotienylovej skupiny, benzoxazolylovej skupiny, chromanylovej skupiny, 2,3-dihydroxybenzofurylovej skupiny, 2,3-dihydrobenzotienylovej skupiny, indolinylovej skupiny, indolylovej skupiny, izochromanyiovej skupiny, izochinolylovej skupiny, pyridylovej skupiny, chinolylovej skupiny, 1,2,3,4-tetrahydroizochinolylovej skupiny, 1,2,3,4-tetrahydrochinolylovej skupiny, tiazolylovej skupiny alebo tienylovej skupiny, pričom tieto heteroaromatické skupiny môžu byť nesubstituovaná alebo substituované atómom halogénu, alkylovou skupinou, alkoxyskupinou, skupinou -COOR5, trifluórmetylovou skupinou, trifluórmetylsulfanylovou skupinou, trifluórmetoxyskupinou, nitroskupinou, skupinou -NR6R7, skupinou -CO-NH-NR6R7, kyanoskupinou, skupinou -CONHR9, alkylsulfanylovou skupinou, hydroxyalkylovou skupinou alebo alkyltioalkylovou skupinou,-NR 6 R 7 , -CO-NH-NR 6 R 7 groups, -N (alk) COOR 8 groups, cyano groups, -CONHR 9 groups, -CO-NR 16 R 17 groups, alkylsulfanyl groups, hydroxyalkyl groups, groups -O-alk-NR 12 R 13 or alkylthioalkyl groups, or a heteroaromatic group selected from benzofuryl, benzothiazolyl, benzothienyl, benzoxazolyl, chromanyl, 2,3-dihydroxybenzofuryl, 2,3-dihydrobenzothienyl, indolinyl , indolyl, isochromanyl, isoquinolyl, pyridyl, quinolyl, 1,2,3,4-tetrahydroisoquinolyl, 1,2,3,4-tetrahydroquinolyl, thiazolyl or thienyl groups, which heteroaromatic groups may be unsubstituted or substituted by halogen, alkyl, alkoxy, -COOR 5 , trifluoromethyl, trifluoromethylsulfanyl, trifluoromethoxy, nitro, -NR 6 R 7 , -CO-NH-NR 6 R 7 , cyano, -CONHR 9 , alkylsulfanyl, hydroxyalkyl or alkylthioalkyl, R3 a R4, ktoré sú rovnaké alebo rôzne, predstavujú buď aromatickú skupinu vybranú z fenylovej skupiny, naftylovej skupiny alebo indenylovej skupiny, pričom tieto aromatické skupiny môžu byť nesubstituovaná alebo substituované jedným alebo viacerými atómami halogénu, alkylovými skupinami, alkoxyskupinami, formylovými skupinami, hydroxylovými skupinami, trifluórmetylovými skupinami, trifluórmetoxyskupinami, skupinami -CO-alk, kyanoskupinami, skupinami -COOR5, skupinami -CONR10R11, skupinami -CO-NH-NR6R7, alkylsulfanylovými skupinami, hydroxyalkylovými skupinami, skupinami -alk-NR6R7 alebo alkyltioaikylovými skupinami, alebo heteroaromatickú skupinu vybranú z benzofurylovej skupiny, benzotiazolylovej skupiny, benzotienylovej skupiny, benzoxazolylovej skupiny, chromanylovej skupiny, 2,3-dihydrobenzofurylovej skupiny,R 3 and R 4 , which are the same or different, represent either an aromatic group selected from a phenyl group, a naphthyl group or an indenyl group, which aromatic groups may be unsubstituted or substituted by one or more halogen atoms, alkyl groups, alkoxy groups, formyl groups, hydroxyl groups, trifluoromethyl groups, trifluoromethoxy groups, -CO-alk groups, cyano groups, -COOR 5 groups, -CONR 10 R 11 groups, -CO-NH-NR 6 R 7 groups, alkylsulfanyl groups, hydroxyalkyl groups, -alk-NR groups 6 R 7 or alkylthioalkyl, or a heteroaromatic group selected from benzofuryl, benzothiazolyl, benzothienyl, benzoxazolyl, chromanyl, 2,3-dihydrobenzofuryl, J 2,3-dihydrobenzotienylovej skupiny, furylovej skupiny, izoI chromanylovej skupiny, izochinolylovej skupiny, pyrolylovej skupiny, chinolylovej skupiny, 1,2,3, 4-tetrahydroizochinolylovej skupiny, tiazolylovej skupiny alebo tienylovej sku36 piny, pričom tieto heteroaromatické skupiny môžu byť nesubstituované alebo substituované jedným alebo viacerými atómami halogénu, alkylovými skupinami, alkoxyskupinami, hydroxylovými skupinami, trifluórmetylovými skupinami, trifluórmetoxyskupinami, kyanoskupinami, skupinami -COOR5, skupinami -CO-NH-NRCR7, skupinami -CONR10Rn, skupinami -alk-NR6R7, alkylsulfanylovými skupinami, hydroxyalkylovými skupinami alebo alkyltioalkylovými skupinami,J 2,3-dihydrobenzothienyl, furyl, chromanyl, isoquinolyl, pyrrolyl, quinolyl, 1,2,3,4-tetrahydroisoquinolinyl, thiazolyl or thienyl groups, these heteroaromatic groups may be unsubstituted or substituted by one or more halogen, alkyl, alkoxy, hydroxyl, trifluoromethyl, trifluoromethoxy, cyano, -COOR 5, -CO-NH-NR C R 7, -CONR 10 R n, -alk-NR 6 R 7 , alkylsulfanyl, hydroxyalkyl or alkylthioalkyl groups, R5 je alkylová skupina alebo fenylová skupina prípadne substituovaná jedným alebo viacerými atómami halogénu,R 5 is an alkyl or phenyl group optionally substituted with one or more halogen atoms, R6 a R7, ktoré sú rovnaké alebo rôzne, predstavujú atóm vodíka, alkylovú skupinu, skupinu -COOalk, cykloalkylovú skupinu, alkylcykloalkylovú skupinu, skupinu -alk-O-alk alebo hydroxyalkylovú skupinu, alebo R6 a R7 spoločne s atómom dusíka, na ktorý sa viažu, tvoria nasýtenú alebo nenasýtenú a monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 členov, prípadne obsahujúcu ďalší heteroatóm vybraný z atómu kyslíka, atómu síry alebo atómu dusíka a prípadne substituovanú jednou alebo viacerými alkylovými skupinami, skupinami -CO-alk, skupinami -COOalk, skupinami -CONHalk, skupinami -CSNHalk, skupinami -CO-alk-NR^R, oxoskupinami, hydroxyalkylovými skupinami, skupinami -alk-O-alk alebo skupinami -CO-NH2,R 6 and R 7 , which are the same or different, represent a hydrogen atom, an alkyl group, a -COOalk group, a cycloalkyl group, an alkylcycloalkyl group, an -alk-O-alk group or a hydroxyalkyl group, or R 6 and R 7 together with a nitrogen atom to which they are attached form a saturated or unsaturated and monocyclic or bicyclic heterocyclic group containing from 3 to 10 members, optionally containing another heteroatom selected from oxygen, sulfur or nitrogen and optionally substituted by one or more alkyl groups, -CO-alk groups , -COOalk groups, groups -CONHalk, -CSNHalk radicals, -CO-alk-NR R, oxo, hydroxyalkyl, -alk-O-alk or -CO-NH 2, R8 znamená alkylovú skupinu,R 8 represents an alkyl group, R9 znamená atóm vodíka, alkylovú skupinu alebo alkylovú skupinu substituovanú dialkylaminoalkylovou skupinou, fenylovou skupinou, cykloalkylovou skupinou (prípadne substituovanou skupinou -COOalk) alebo nasýtenou alebo nenasýtenou monocyklickou alebo bicyklickou heterocyklickou skupinou obsahujúcou 3 až 10 členov, prípadne obsahujúcou jeden alebo viacero heteroatómov vybraných z atómu kyslíka, atómu síry a atómu dusíka a prípadne substituovanou jedným alebo viacerými alkylovými skupinami,R 9 represents a hydrogen atom, an alkyl group or an alkyl group substituted with a dialkylaminoalkyl group, a phenyl group, a cycloalkyl group (optionally substituted with -COOalk group) or a saturated or unsaturated monocyclic or bicyclic heterocyclic group containing 3 to 10 members, optionally containing one or more heteroatoms selected from an oxygen atom, a sulfur atom and a nitrogen atom and optionally substituted by one or more alkyl groups, R10 )a R11, ktoré sú rovnaké alebo rôzne, predstavujú atóm vodíka 1 alebo alkylovú skupinu, alebo R10 a R11 tvoria spoločne s atómom dusíka, na ktorý sa viažu, nasýtenú monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 členov, prípadne obsahujúcu ďalší heteroatóm vybraný z atómu kyslíka, atómu síry a atómu dusíka a prípadne substituovanú jedným alebo viacerými alkylovými skupinami,R 10 ) and R 11 , which are the same or different, represent a hydrogen atom 1 or an alkyl group, or R 10 and R 11 together with the nitrogen atom to which they are attached form a saturated monocyclic or bicyclic heterocyclic group containing 3 to 10 members, optionally containing a further heteroatom selected from oxygen, sulfur and nitrogen and optionally substituted with one or more alkyl groups, R12 a R13, ktoré sú rovnaké alebo rôzne, predstavujú atóm vodíka alebo alkylovú skupinu alebo cykloalkylovú skupinu, alebo R12 a R13 tvoria spoločne s atómom dusíka, na ktorý sa viažu, nasýtenú monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 členov, prípadne obsahujúcu ďalší heteroatóm vybraný z atómu kyslíka, atómu síry a atómu dusíka a prípadne substituovanú alkylovou skupinou, skupinou -CO-alk, skupinou -COOalk, skupinou -CONHalk, skupinou CSNHalk, skupinou -CO-alk-NR14R15 alebo nasýtenou monocyklickou alebo bicyklickou heterocyklickou skupinou obsahujúcou 3 až 10 členov a obsahujúcou heteroatóm vybraný z atómu kyslíka, atómu síry a atómu dusíka,R 12 and R 13 , which are the same or different, represent a hydrogen atom or an alkyl or cycloalkyl group, or R 12 and R 13 together with the nitrogen atom to which they are attached form a saturated monocyclic or bicyclic heterocyclic group containing 3 to 10 members optionally containing another heteroatom selected from oxygen, sulfur and nitrogen and optionally substituted with alkyl, -CO-alk, -COOalk, -CONHalk, CSNHalk, -CO-alk-NR 14 R 15 or saturated a 3 to 10 membered monocyclic or bicyclic heterocyclic group containing a heteroatom selected from oxygen, sulfur and nitrogen, R14 a R15, ktoré sú rovnaké alebo rôzne, predstavujú atóm vodíka, alkylovú skupinu alebo skupinu -COOalk,R 14 and R 15 , which are the same or different, represent a hydrogen atom, an alkyl group or a -COOalk group, R16 a R17 tvoria spoločne s atómom dusíka, na ktorý sa viažu, nasýtenú monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 členov, prípadne obsahujúcu ďalšie heteroatómy vybrané z atómu kyslíka, atómu síry a atómu dusíka,R 16 and R 17 together with the nitrogen atom to which they are attached form a saturated monocyclic or bicyclic heterocyclic group containing from 3 to 10 members, optionally containing further heteroatoms selected from oxygen, sulfur and nitrogen, R' znamená atóm vodíka alebo skupinu -CO-alk, alebo R znamená skupinu CHR18, aR 'is H or -CO-alk, or R represents a CHR 18 radical, and R18 - znamená skupinu -NHCOR19 alebo skupinu -N (R20)-Y-R21,R 18 - represents a radical -NHCOR 19 or -N (R 20) -YR 21, Y 1 je skupina CO alebo skupina SO2,Y 1 is CO or SO 2 , R4 a R3, ktoré sú rovnaké alebo rôzne, predstavujú buď aromatickú skupinu vybranú z fenylovej skupiny, naftylovej skupiny alebo índenylovej skupiny, pričom tieto aromatické skupiny môžu byť nesubstituované alebo substituované jedným alebo viacerými atómami halogénu, alkylovými skupinami, alkoxyskupinami, formylovými skupinami, hydroxylovými skupinami, trifluórmetylovými skupinami, trifluórmetoxyskupinami, skupi,nami -CO-alk, kyanoskupinami, skupinami -COOH, skupinami -COOalk, skupinami -CONR22R23, skupinami -CO-NH-NR24R25, alkylsulf anylovými skupinami, alkylsulfinylovými skupinami, alkylsulfonylovými skupinami, alkylsulfanylalkylovými skupinami, alkylsulfinylalkylovými skupinami, alkylsulfonylalkylovými skupinami, hydroxyalkylovými skupinami alebo skupinami -alk-NR22R23, alebo heteroaromatickú skupinu vybranú z benzofurylovej skupiny, benzotiazolylovej skupiny, benzotienylovej skupiny, benzoxazolylovej skupiny, chromanylovej skupiny, 2,3-dihydroxybenzofurylovej skupiny, 2,3-di'nydrobenzotienylovej skupiny, pyrimidinylovej skupiny, furylovej skupiny, imidazolylovej skupiny, izochromanylovej skupiny, izochinolylovej skupiny, pyrolylovej skupiny, pyridylovej skupiny, chinolylovej skupiny, 1,2, 3, 4-tetrahydroizochinolylovej skupiny, tiazolylovej skupiny alebo tienylovej skupiny, pričom tieto heteroaromatické skupiny môžu byť nesubstituované alebo substituované atómom halogénu, alkylovou skupinou, alkoxyskupinou, hydroxylovou skupinou, trifluórmetylovou skupinou, trifluórmetoxyskupinou, kyanoskupinou, skupinou -COOH, skupinou -COOalk, skupinou -CO-NH-NR24R25, skupinou -CONR22R23, skupinou-alk-NR24R25, alkylsulf anylovou skupinou, alkylsulfinyiovou skupinou, alkylsulfonylovou skupinou, alkylsulfanylalkylovou skupinou, alkylsulfinylakylovou skupinou, alkylsulfonylalkylovou skupinou alebo hydroxyalkylovou skupinou,R 4 and R 3 which are the same or different represent either an aromatic group selected from phenyl, naphthyl or indenyl, which aromatic groups may be unsubstituted or substituted by one or more halogen atoms, alkyl groups, alkoxy groups, formyl groups, hydroxyl, trifluoromethyl, trifluoromethoxy, -CO-alk, cyano, -COOH, -COOalk, -CONR 22 R 23 , -CO-NH-NR 24 R 25 , alkylsulfanyl, alkylsulfinyl groups , alkylsulfonyl groups, alkylsulfanylalkyl groups, alkylsulfinylalkyl groups, alkylsulfonylalkyl groups, hydroxyalkyl groups or -alk-NR 22 R 23 groups, or a heteroaromatic group selected from benzofuryl group, benzothiazolyl group, benzothienyl group, benzothiazolyl group, 2-chromanyl group, chromanyl , 3-dihydroxybenzofuryl, 2,3-diynylbenzothienyl, pyrimidinyl, furyl, imidazolyl, isochromanyl, isoquinolyl, pyrrolyl, pyridyl, quinolyl, 1,2,3,4-tetrahydroisoquinolyl thiazolyl or thienyl, wherein the heteroaromatic groups may be unsubstituted or substituted by halogen, alkyl, alkoxy, hydroxyl, trifluoromethyl, trifluoromethoxy, cyano, -COOH, -COOalk, -CO-NH-NR 24 R 25 , -CONR 22 R 23 , -alk-NR 24 R 25 , alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, alkylsulfanylalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl or hydroxyalkyl, R19 znamená skupinu -alk-SO2R26, skupinu -alk-SO2-CH=CH-R26, skupinu Het1 substituovanú skupinou -SO2-R26 alebo fenylovú sku39 , pinu substituovanú skupinou -SO2-R26 alebo skupinou -alk-SO2-R26,R 19 represents an -alk-SO 2 R 26, -alk-SO 2 -CH = CH-R 26, Het 1 is substituted by -SO 2 -R 26 or a phenyl sku39, pin substituted by -SO 2 -R 26 or - alk-SO 2 -R 26 R20 znamená atóm vodíka alebo alkylovú skupinu,R 20 represents a hydrogen atom or an alkyl group, R21 znamená fenylalkylovú skupinu, skupinu Het1 alebo skupinu Ar1,R 21 represents a phenylalkyl group, a Het 1 group or an Ar 1 group, R22 a R23, ktoré sú rovnaké alebo rôzne, predstavujú atóm vodíka alebo alkylovú skupinu, alebo R22 a R23 tvoria spoločne s atómom dusíka, na ktorý sa viažu, nasýtenú monocyklickú alebo bicyklickú skupinu obsahujúcu 3 až 10 členov, prípadne obsahujúcu ďalší heteroatóm vybraný z atómu kyslíka, atómu síry a atómu dusíka a prípadne substituovanú jedným alebo viacerými alkylovými skupinami,R 22 and R 23 , which are the same or different, represent a hydrogen atom or an alkyl group, or R 22 and R 23 together with the nitrogen atom to which they are attached form a saturated monocyclic or bicyclic group containing 3 to 10 members, optionally containing further a heteroatom selected from oxygen, sulfur and nitrogen and optionally substituted with one or more alkyl groups, R24 a R25, ktoré sú rovnaké alebo rôzne, predstavujú atóm vodíka, alkylovú skupinu, skupinu -COOalk, cykloalkylovú skupinu, alkylcykloalkylovú skupinu, skupinu -alk-O-alk alebo hydroxyalkylovú skupinu, alebo R24 a R25 spoločne s atómom uhlíka, na ktorý sa viažu, tvoria nasýtenú alebo nenasýtenú monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 členov, prípadne obsahujúcu ďalší heteroatóm vybraný z atómu kyslíka, atómu síry alebo atómu dusíka a prípadne substituovanú jednou alebo viacerými alkylovými skupinami, skupinami -CO-alk, skupinami -COOalk, skupinami -CONHalk, skupinami -CSNHalk, oxoskupinami, hydroxyalkylovými skupinami, skupinami -alk-O-alk alebo skupinami -CO-NH2,R 24 and R 25 , which are the same or different, represent a hydrogen atom, an alkyl group, a -COOalk group, a cycloalkyl group, an alkylcycloalkyl group, an -alk-O-alk group or a hydroxyalkyl group, or R 24 and R 25 together with a carbon atom to which they are attached form a saturated or unsaturated monocyclic or bicyclic heterocyclic group containing from 3 to 10 members, optionally containing another heteroatom selected from oxygen, sulfur or nitrogen and optionally substituted by one or more alkyl, -CO-alk, -COOalk groups, -CONHalk groups, -CSNHalk groups, oxo groups, hydroxyalkyl groups, -alk-O-alk groups or -CO-NH 2 groups, R26 znamená alkylovú skupinu, skupinu Ar1 alebo skupinu Het1,R 26 represents an alkyl group, an Ar 1 group or a Het 1 group, Ar1 znamená fenylovú skupinu, naftylovú skupinu alebo indenylovú skupinu, pričom tieto skupiny sú prípadne substituované ' jedným alebo viacerými atómami halogénu, alkylovými skupina1 mi, alkoxyskupinami, kyanoskupinami, skupinami -CO-alk, skuI ’ pinami -COOH, skupinami -COOalk, skupinami -CONR27R28, sku1 pinami -CO-NH-NR29R30, alkylsulfanylovými skupinami, alkyl40 sulfinylovými skupinami, alkylsulfonylovými skupinami, skupinami -alk-NR29R30, skupinami -NR29R30, alkyltioalkylovými skupinami, formylovými skupinami, hydroxylovými skupinami, hydroxyalkýlovými skupinami, skupinami Het, skupinami -O-alk-NH-cykloalkyl, trifluórmetoxyskupinami, trifluórmetylovými skupinami, skupinami -NH-CO-alk, skupinami -SO2NH2, skupinami -NH-COCH3, skupinami -NH-COOalk, skupinami Het alebo ešte dve susedné skupiny môžu tvoriť dioxymetylénovú skupinu,Ar 1 is phenyl, naphthyl or indenyl, these groups being optionally substituted by one or more halogen, alkyl, alkoxy, cyano, -CO-alk, -COOH, -COOalk, -COOalk, CONR 27 R 28, Item 1 Pina -CO-NH-NR 29 R 30, alkylsulfanyl, alkyl40 sulfinyl, alkylsulfonyl, -alk-NR 29 R 30, -NR 29 R 30, alkylthioalkyl, formyl , hydroxyl groups, hydroxyalkyl groups, Het groups, -O-alk-NH-cycloalkyl groups, trifluoromethoxy groups, trifluoromethyl groups, -NH-CO-alk groups, -SO2NH2 groups, -NH-COCH3 groups, -NH-COOalk groups, Het or two adjacent groups may form a dioxymethylene group, Het1 znamená nenasýtenú alebo nasýtenú monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 kruhových členov, obsahujúcu jeden alebo viacero heteroatómov vybraných z atómu kyslíka, atómu síry a atómu dusíka, ktorá je prípadne substituovaná jednou alebo viacerými alkylovými skupinami, alkoxyskupinami, vinylovými skupinami, atómami halogénu, alkoxykarbonylovými skupinami, oxoskupinami, hydroxylovými skupinami, trifluórmetoxyskupinami alebo trifluórmetylovými skupinami, pričom atómy dusíka heterocyklov sú prípadne v N-oxidovanej forme,Het 1 means an unsaturated or saturated monocyclic or bicyclic heterocyclic group containing 3 to 10 ring members, containing one or more heteroatoms selected from oxygen, sulfur and nitrogen, optionally substituted by one or more alkyl, alkoxy, vinyl, atoms halogen, alkoxycarbonyl, oxo, hydroxyl, trifluoromethoxy or trifluoromethyl groups, the nitrogen atoms of the heterocycles optionally being in the N-oxidized form, R27 a R28, ktoré sú rovnaké alebo rôzne, predstavujú atóm vodíka alebo alkylovú skupinu, alebo R27 a R28 spoločne s atómom uhlíka, na ktorý sa viažu, tvoria nasýtenú monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 členov, prípadne obsahujúcu ďalší heteroatóm vybraný z atómu kyslíka, atómu síry alebo atómu dusíka a prípadne substituovanú jednou alebo viacerými alkylovými skupinami,R 27 and R 28 , which are the same or different, represent a hydrogen atom or an alkyl group, or R 27 and R 28 together with the carbon atom to which they are attached form a saturated monocyclic or bicyclic heterocyclic group containing from 3 to 10 members, optionally containing another heteroatom selected from oxygen, sulfur or nitrogen and optionally substituted with one or more alkyl groups, R29 a R30, ktoré sú rovnaké alebo rôzne, predstavujú atóm vodíka, alkylovú skupinu, skupinu -COOalk, cykloalkylovú skupinu, alkylcykloalkylovú skupinu, skupinu -alk-O-alk alebo hydroxyalkylovú skupinu, alebo R29 a R30 spoločne s atómom uhlíka, na ktorý sa viažu, tvoria nasýtenú alebo nenasýtenú monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 členov, prípadne obsahujúcu ďalší heteroatóm ' vybraný z atómu kyslíka, atómu síry alebo atómu dusíka a prípadne substituovanú jednou alebo viacerými alkylovými skupinami, skupinami -CO-alk, skupinami -COOalk, skupinami -CONHalk, skupinami -CSNHalk, oxoskupinami, hydroxyalkylovými skupinami, skupinami -alk-O-alk alebo skupinami -CO-NH2, alebo R znamená skupinu CHR31, aR 29 and R 30 , which are the same or different, represent a hydrogen atom, an alkyl group, a -COOalk group, a cycloalkyl group, an alkylcycloalkyl group, an -alk-O-alk group or a hydroxyalkyl group, or R 29 and R 30 together with a carbon atom to which they are attached form a saturated or unsaturated monocyclic or bicyclic heterocyclic group containing from 3 to 10 members, optionally containing another heteroatom selected from oxygen, sulfur or nitrogen and optionally substituted by one or more alkyl groups, -CO-alk groups , -COOalk groups, groups -CONHalk, -CSNHalk radicals, oxo, hydroxyalkyl, -alk-O-alk or -CO-NH 2 radicals, or R represents a CHR 31 radical, and R31 znamená skupinu -NR32R33, skupinu -NR32-CO-R33 alebo skupinu -NR32-SO2R3\R 31 is -NR 32 R 33 , -NR 32 -CO-R 33, or -NR 32 -SO 2 R 3; R4 a R3, ktoré sú rovnaké alebo rôzne, predstavujú buď aromatickú skupinu vybranú z fenylovej skupiny, naftylovej skupiny alebo indenylovej skupiny, pričom tieto aromatické skupiny môžu byť nesubstituované alebo substituované jedným alebo viacerými atómami halogénu, alkylovými skupinami, alkoxyskupinami, formylovými skupinami, hydroxylovými skupinami, trifluórmetylovými skupinami, trifluórmetoxyskupinami, skupinami -CO-alk, kyanoskupinami, skupinami -COOH, skupinami -COOalk, skupinami -CONR22R23, skupinami -CO-NH-NR24R25, alkylsulfanylovými skupinami, alkylsulfinylovými skupinami, alkylsulfonylovými skupinami, alkylsulfanylalkylovými skupinami, alkylsulfinylalkylovými skupinami, alkylsulfonylalkylovými skupinami, hydroxyalkylovými skupinami alebo skupinami -alk-NR7R8, alebo heteroaromatickú skupinu, vybranú z benzofurylovej skupiny, benzotiazolylovej skupiny, benzotienylovej skupiny, benzoxazolylovej skupiny, chromanylovej skupiny, 2,3-dihydroxybenzofurylovej skupiny, 2,3-dihydrobenzotienylovej skupiny, furylovej skupiny, imidazolylovej skupiny, izochromanylovej skupiny, izochinolylovej skupiny, pyrolylovej skupiny, pyridylovej skupiny, pyrimidinylovej 'skupiny, chinolylovej skupiny, 1,2,3,4-tetrahydroizochinolyJlovej skupiny, tiazolylovej skupiny alebo tienylovej skupiny, pričom tieto heteroaromatické skupiny môžu byť nesub'stituované alebo substituované atómom halogénu, alkylovou skupinou, alkoxyskupinou, hydroxylovou skupinou, trifluórmetylovou skupinou, trifluórmetoxyskupinou, kyanoskupinou, skupinou -COOH, skupinou -COOalk, skupinou -CO-NH-NR24R25, skupinou -CONR22R23, skupinou-alk-NR24R25, alkylsulfanylovou skupinou, alkylsulfinylovou skupinou, alkylsulfonylovou skupinou, alkylsulfanylalkylovou skupinou, alkylsulfinylakylovou skupinou, alkylsulfonylalkylovou skupinou alebo hydroxyalkylovou skupinou,R 4 and R 3 , which are the same or different, represent either an aromatic group selected from phenyl, naphthyl or indenyl, which aromatic groups may be unsubstituted or substituted by one or more halogen atoms, alkyl groups, alkoxy groups, formyl groups, hydroxyl groups, trifluoromethyl groups, trifluoromethoxy groups, -CO-alk groups, cyano groups, -COOH groups, -COOalk groups, -CONR 22 R 23 groups, -CO-NH-NR 24 R 25 groups, alkylsulfanyl groups, alkylsulfinyl groups, alkylsulfonyl groups , alkylsulfanylalkyl groups, alkylsulfinylalkyl groups, alkylsulfonylalkyl groups, hydroxyalkyl groups or -alk-NR 7 R 8 groups, or a heteroaromatic group selected from benzofuryl group, benzothiazolyl group, benzothienyl group, benzoxazolyl group, chromanyl group, 2,3-d ihydroxybenzofuryl, 2,3-dihydrobenzothienyl, furyl, imidazolyl, isochromanyl, isoquinolyl, pyrrolyl, pyridyl, pyrimidinyl, quinolyl, 1,2,3,4-tetrahydroisoquinolyl or thiazolyl, wherein the heteroaromatic groups may be unsubstituted or substituted by a halogen atom, an alkyl group, an alkoxy group, a hydroxyl group, a trifluoromethyl group, a trifluoromethoxy group, a cyano group, a -COOH group, a -COOalk group, a -CO-NH-NR 24 R 25 group , -CONR 22 R 23 , -alk-NR 24 R 25 , alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, alkylsulfanylalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl or hydroxyalkyl, R32 znamená skupinu -C (R35) (R36)-Het2, skupinu -Het2, skupinu -C (R35) (R36)-Ar2, skupinu Ar2, cykloalkylovú skupinu alebo norbornylovú skupinu,R 32 is -C (R 35 ) (R 36 ) -Het 2 , -Het 2 , -C (R 35 ) (R 36 ) -Ar 2 , Ar 2 , cycloalkyl or norbornyl, R33 znamená atóm vodíka, hydroxyalkylovú skupinu, skupinu -alk-COOalk, skupinu -alk-CONR22R23, skupinu -alk-NR22R23, alkoxyskupinu, skupinu Ar2, skupinu Het2, skupinu -CH2Ar2, skupinu -CH2Het2 alebo alkylovú skupinu prípadne substituovanú jedným alebo viacerými atómami halogénu,R 33 is hydrogen, hydroxyalkyl, -alk-COOalk, -alk-CONR 22 R 23 , -alk-NR 22 R 23 , alkoxy, Ar 2 , Het 2 , -CH 2 Ar 2 , - CH 2 Het 2 or an alkyl group optionally substituted by one or more halogen atoms, R34 znamená hydroxyalkylovú skupinu, skupinu -alk-COOalk, skupinu -alk-CONR22R23, skupinu -alk-NR22R23, alkoxyskupinu, skupinu Ar2, skupinu Het2, skupinu -CH2Ar2, skupinu -CH2Hetŕ alebo alkylovú skupinu prípadne substituovanú jedným alebo viacerými atómami halogénu,R 34 represents a hydroxyalkyl, -alk-COOalk, -alk-CONR 22 R 23, -alk-NR 22 R 23, alkoxy, Ar 2, Het 2, -CH 2 Ar 2 group, or a group t -CH2Het an alkyl group optionally substituted by one or more halogen atoms, R35 znamená atóm vodíka, hydroxyalkylovú skupinu, skupinu -alk-COOalk, skupinu -alk-CONR22R23, skupinu -alk-NR22R23, alkoxyalkylovú skupinu, skupinu Ar2, skupinu Het2, skupinu -CH2Ar2, skupinu -CH2Het2 alebo alkylovú skupinu prípadne substituovanú jedným alebo viacerými atómami halogénu,R 35 is hydrogen, hydroxyalkyl, -alk-COOalk, -alk-CONR 22 R 23 , -alk-NR 22 R 23 , alkoxyalkyl, Ar 2 , Het 2 , -CH 2 Ar 2 , -CH 2 Het 2 or an alkyl group optionally substituted by one or more halogen atoms, R35 znamená atóm vodíka alebo hydroxyalkylovú skupinu, skupinu -alk-COOalk, skupinu -alk-CONR22R23, skupinu -alk-NR22R23, alkoxyalkylovú skupinu alebo alkylovú skupinu prípadne substituovanú jedným alebo viacerými atómami halogénu, alebo ešte R35 a R36 tvoria spoločne s atómom uhlíka, na kto43 i rý sa viažu, nasýtený monocyklický alebo bicyklický kruh obsahujúci 3 až 10 členov, prípadne obsahujúci ďalší heteroatóm vybraný z atómu kyslíka, atómu síry a atómu dusíka a prípadne substituovaný jedným alebo viacerými alkylovými skupinami,R 35 is hydrogen or hydroxyalkyl, -alk-COOalk, -alk-CONR 22 R 23 , -alk-NR 22 R 23 , alkoxyalkyl or alkyl optionally substituted with one or more halogen atoms, or R 35 and R 36 together with the carbon atom to which they are attached form a saturated monocyclic or bicyclic ring containing from 3 to 10 members, optionally containing a further heteroatom selected from oxygen, sulfur and nitrogen and optionally substituted with one or more alkyl groups, Ar2 znamená fenylovú skupinu, naftylovú skupinu alebo indenylovú skupinu, pričom tieto skupiny sú prípadne substituované jed'ným alebo viacerými atómami halogénu, alkylovými skupinami, alkoxyskupinami, kyanoskupinami, skupinami -CO-alk, skupinami -COOH, skupinami -COOalk, skupinami -CONR37R38, skupinami -CO-NH-NR39R40, alkylsulfanylovými skupinami, alkylsulfinylovými skupinami, alkylsulfonylovými skupinami, skupinami -alk-NR39R<!0, skupinami -NR39R40, alkyltioalkylovými skupinami, formylovými skupinami, trifluórmetylovými skupinami, trifluórmetoxyskupinami, skupinami Het, skupinami -O-alk-NH-cykloalkyl, skupinami -SO2NH2, hydroxylovými skupinami, hydroxyalkýlovými skupinami, skupinami -NHCOalk, skupinami -NH-COOalk alebo na dvoch susedných atómoch uhlíka dioxymetylénovou skupinou,Ar 2 is phenyl, naphthyl or indenyl, these groups being optionally substituted with one or more halogen atoms, alkyl groups, alkoxy groups, cyano groups, -CO-alk groups, -COOH groups, -COOalk groups, -CONR groups 37 R 38 , -CO-NH-NR 39 R 40 groups, alkylsulfanyl groups, alkylsulfinyl groups, alkylsulfonyl groups, -alk-NR 39 R 10 groups, -NR 39 R 40 groups, alkylthioalkyl groups, formyl groups, trifluoromethyl groups , trifluoromethoxy, Het, -O-alk-NH-cycloalkyl, -SO 2 NH 2 , hydroxyl, hydroxyalkyl, -NHCOalk, -NH-COOalk, or two adjacent carbon atoms with a dioxymethylene group, Het2 znamená nenasýtenú alebo nasýtenú monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 kruhových členov, obsahujúcu jeden alebo viacero heteroatómov vybraných z atómu kyslíka, atómu síry a atómu dusíka, ktorá je prípadne substituovaná jednou alebo viacerými alkylovými skupinami, alkoxyskupinami, atómami halogénu, alkoxykarbonylovými skupinami, oxoskupinami alebo hydroxylovými skupinami, pričom atómy dusíka heterocyklov sú prípadne v N-oxidovanej forme,Het 2 means an unsaturated or saturated monocyclic or bicyclic heterocyclic group containing 3 to 10 ring members, containing one or more heteroatoms selected from oxygen, sulfur and nitrogen, optionally substituted by one or more alkyl, alkoxy, halogen, alkoxycarbonyl groups, oxo or hydroxyl groups, the nitrogen atoms of the heterocycles optionally being in the N-oxidized form, R37 a R38, ktoré sú rovnaké alebo rôzne, predstavujú atóm vodíka ' alebo alkylovú skupinu, alebo R37 a R38 spoločne s atómom uhlíka, na ktorý sa viažu, tvoria nasýtenú monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 členov, 'prípadne obsahujúcu ďalší heteroatóm vybraný 2 atómu kyslíka, atómu síry alebo atómu dusíka a prípadne substituovanú jednou alebo viacerými alkylovými skupinami,R 37 and R 38 , which are the same or different, represent a hydrogen atom or an alkyl group, or R 37 and R 38 together with the carbon atom to which they are attached form a saturated monocyclic or bicyclic heterocyclic group containing 3 to 10 members; optionally containing a further heteroatom selected from 2 oxygen, sulfur or nitrogen and optionally substituted with one or more alkyl groups, R39 a R40, ktoré sú rovnaké alebo rôzne, predstavujú atóm vodíka alebo alkylovú skupinu, alebo R39 a R40 spoločne s atómom uhlíka, na ktorý sa viažu, tvoria nasýtenú monocyklickú alebo bicyklickú heterocyklickú skupinu obsahujúcu 3 až 10 členov, prípadne obsahujúcu ďalší heteroatóm vybraný z atómu kyslíka, atómu síry alebo atómu dusíka a prípadne substituovanú jednou alebo viacerými alkylovými skupinami, alk znamená alkylovú skupinu alebo alkylénovú skupinu, pričom alkylové, alkylénové a alkoxylové časti sú s priamym alebo rozvetveným reťazcom obsahujúcim 1 až 6 atómov uhlíka, a cykloalkylové skupiny obsahujú 3 až 10 atómov uhlíka, optické izoméry týchto zlúčenín a ich farmaceutický prijatelné soli s anorganickou alebo organickou kyselinou.R 39 and R 40 , which are the same or different, represent a hydrogen atom or an alkyl group, or R 39 and R 40 together with the carbon atom to which they are attached form a saturated monocyclic or bicyclic heterocyclic group containing from 3 to 10 members, optionally containing another heteroatom selected from oxygen, sulfur or nitrogen and optionally substituted with one or more alkyl groups, alk represents an alkyl group or an alkylene group, the alkyl, alkylene and alkoxy moieties being straight or branched chain containing 1 to 6 carbon atoms, and cycloalkyl groups containing 3 to 10 carbon atoms, optical isomers of these compounds, and pharmaceutically acceptable salts thereof with an inorganic or organic acid. 3. Kombinácia podľa nároku 2, kde zlúčenina všeobecného vzorca je vybraná zo skupiny, ktorú tvoria nasledovné zlúčeniny:The combination of claim 2, wherein the compound of the formula is selected from the group consisting of the following compounds: l-benzhydryl-3-[(metylsulfonyl)(fenyl)metylén]azetidín, l-benzhydryi-3-[(3-metylfenyl)(metylsulfonyl)metylén]azetidín, l-benzhydryl-3-[(3-chlórfenyl)(metylsulfonyl)metylén]azetidín, l-benzhydryl-3-[(3,5-dichlórfenyl)(metylsulfonyl)metylén]-azetidín, l-benzhydryl-3-[(2,5-dichlórfenyl)(metylsulfonyl)metylén]-azetidín, l-benzhydryl-3-[(2,3-dichlórfenyl)(metylsulfonyl)metylén]-azetidín, l-benzhydryl-3-[(3-fluórfenyl)(metylsulfonyl)metylén]azetidín, l-bénzhydryl-3- [ (3,5-difluórfenyl) (metylsulfonyl)metylén]-azetidín, l-benzhydryl-3-[(3-brómfenyl)(metylsulfonyl)metylén]azetidín, l-benzhydryl-3-[(3-jódfenyl)(metylsulfonyl)metylén]azetidín, l-benzhydryl-3-[(metylsulfonyl)(3-trifluórmetoxyfenyl)-metylén]azetidín, l-benzhydryl-3-[(metylsulfonyl)(3-trifluórmetylfenyl)-metylén]azetidín, l-benzhydryl-3-([3,5-bis(trifluórmetyl)fenyl](metylsulfonyl)-metylén}azetidín, l-benzhydryl-3-[(3,5-dibrómfenyl)(metylsulfonyl)metylén]-azetidín, l-benzhydryl-3-[(3-metoxykarbonylfenyl) (metylsulfonyl)metylén]-azetidín, l-benzhydryl-3-[(3-kyanofenyl)(metylsulfonyl)metylén]azetidín, l-benzhydryl-3-[(3-karbamoylfenyl)(metylsulfonyl)metylén]-azetidín, l-benzhydryl-3-[(metylsulfonyl)(naft-l-yl)(metylsulfonyl)-metylén]azetidín,1-benzhydryl-3 - [(methylsulfonyl) (phenyl) methylene] azetidine, 1-benzhydryl-3 - [(3-methylphenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-chlorophenyl) (methylsulfonyl) ) methylene] azetidine, 1-benzhydryl-3 - [(3,5-dichlorophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(2,5-dichlorophenyl) (methylsulfonyl) methylene] azetidine, 1 -benzhydryl-3 - [(2,3-dichlorophenyl) (methylsulfonyl) methylene] -azetidine, 1-benzhydryl-3 - [(3-fluorophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3, 5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-bromophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-iodophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(methylsulfonyl) (3-trifluoromethoxyphenyl) methylene] azetidine, 1-benzhydryl-3 - [(methylsulfonyl) (3-trifluoromethylphenyl) methylene] azetidine, 1-benzhydryl-3 - ([3, 5-bis (trifluoromethyl) phenyl] (methylsulfonyl) methylene} azetidine, 1-benzhydryl-3 - [(3,5-dibromophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-methoxy) carbonylphenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-cyanophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-carbamoylphenyl) (methylsulfonyl) methylene] azetidine, 1 benzhydryl-3 - [(methylsulphonyl) (naphth-l-yl) (methylsulfonyl) methylene] azetidine, 1- [bis(4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyl) -metylén]azetidín,1- [bis (4-chlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-[bis(4-metoxyfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulf onyl ) metylén ] azetidín,1- [bis (4-methoxyphenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-[bis(4-metylfenyl)metyl]-3-[(3, 5-difluórfenyl) (metylsulfonyl) -metylén]azetidín, (RS)-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]-1-[(4-metoxyfenyl)(fenyl)metyl)]azetidín, (R) -3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]-1-[(4-metoxyfenyl)(fenyl)metyl]azetidín, (S) -3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]-1-[(4-metoxyfenyl)(fenyl)metyl]azetidín,1- [bis (4-methylphenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (RS) -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] - 1 - [(4-methoxyphenyl) (phenyl) methyl)] azetidine, (R) -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] -1 - [(4-methoxyphenyl) (phenyl) methyl] azetidine (S) -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] -1 - [(4-methoxyphenyl) (phenyl) methyl] azetidine, 1-[bis(4-trifluórmetoxyfenyl)metyl]-3-[(3,5-difluórfenyl)-(metylsulfonyl)metylén]azetidín,1- [bis (4-trifluoromethoxyphenyl) methyl] -3 - [(3,5-difluorophenyl) - (methylsulphonyl) methylene] azetidine, 1-[bis(4-trifluórmetylfenyl)metyl]-3-[(3,5-difluórfenyl)-(metylsulfonyl)metylén]azetidín,1- [Bis (4-trifluoromethylphenyl) methyl] -3 - [(3,5-difluorophenyl) - (methylsulphonyl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-{[3,5-bis(trifluórmetyl)fenyl]-metylsulfonylmetylén]azetidín, (RS)-1-[(4-chlórfenyl)(2,4-dichlórfenyl)metyl]-3-[(3,5-difluór fenyl)(metylsulfonyl)metylén]azetidín, (R) -1-[(4-chlórfenyl)(2,4-dichlórfenyl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, (S) -1-[(4-chlórfenyl)(2,4-dichlórfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, (RS)-l-{(4-chlórfenyl)[4-(hydroxymetyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, (R) -l-{(4-chlórfenyl)[4-(hydroxymetyl)fenyl]metyl)-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, (S) -l-{(4-chlórfenyl)[4-(hydroxymetyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, (RS)-l-{(4-chlórfenyl)[4-(pyrolidinylmetyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, (R) -1-{(4-chlórfenyl)[4-(pyrolidinylmetyl)fenyl]metyl}-3- [ (3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, (S) -l-{(4-chlórfenyl)[4-(pyrolidinylmetyl)fenyl]metyl}-3471- [bis (4-chlorophenyl) methyl] -3 - {[3,5-bis (trifluoromethyl) phenyl] methylsulfonylmethylene] azetidine, (RS) -1 - [(4-chlorophenyl) (2,4-dichlorophenyl) methyl] -3 - [(3,5-difluoro phenyl) (methylsulfonyl) methylene] azetidine, (R) -1 - [(4-chlorophenyl) (2,4-dichlorophenyl) methyl] -3 - [(3,5 -difluorophenyl) (methylsulfonyl) methylene] azetidine, (S) -1 - [(4-chlorophenyl) (2,4-dichlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, ( RS) -1 - {(4-chlorophenyl) [4- (hydroxymethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (R) -1 - {(4-chlorophenyl) ) [4- (hydroxymethyl) phenyl] methyl) -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (S) -1 - {(4-chlorophenyl) [4- (hydroxymethyl) phenyl] methyl } -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (RS) -1 - {(4-chlorophenyl) [4- (pyrrolidinylmethyl) phenyl] methyl} -3 - [(3,5- difluorophenyl) (methylsulfonyl) methylene] azetidine, (R) -1 - {(4-chlorophenyl) [4- (pyrrolidinylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, ( S) -1 - {(4-chlorophenyl) [ 4- (pyrrolidinylmethyl) phenyl] methyl} -347 -[ (3,[5-difluórfenyl) (metylsulfonyl)metylén]azetidín,- [(3, [5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-(RS}-(4-chlórfenyl)[4-(3,3-dimetylpiperid-l-ylmetyl) fenyl]-metyl}-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, l-( (R)-(4-chlórfenyl) [4-(3,3-dimetylpiperidin-l-ylmetyl)fenyl]-metyl} -3- [(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, l-{(S)-(4-chlórfenyl)[4-(3,3-dimetylpiperidin-l-ylmetyl)fenyl]-metyl}-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén] azetidín,1- (RS) - (4-Chlorophenyl) [4- (3,3-dimethylpiperid-1-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1- ((R) - (4-Chlorophenyl) [4- (3,3-dimethylpiperidin-1-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1- { (S) - (4-Chlorophenyl) [4- (3,3-dimethylpiperidin-1-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 —{(RS)-(4-chlórfenyl)[4-(tiomorfolin-4-ylmetyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(R)-(4-chlórfenyl)[4-(tiomorfolin-4-ylmetyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(S)-(4-chlórfenyl)[4-(tiomorfolin-4-ylmetyl)fenyl]metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(RS)-(4-chlórfenyl)[4-(N-etyl-N-cyklohexylaminometyl)fenyl]-metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1 - {(RS) - (4-chlorophenyl) [4- (thiomorpholin-4-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(R) - (4-chlorophenyl) [4- (thiomorpholin-4-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(S) - (4-chlorophenyl) [4- (thiomorpholin-4-ylmethyl) phenyl] methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(RS) - (4-chlorophenyl) [4- (N- ethyl-N-cyclohexylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-{(R)-(4-chlórfenyl)[4-(N-etyl-N-cyklohexylaminometyl)fenyl]-metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1 - {(R) - (4-chlorophenyl) [4- (N-ethyl-N-cyclohexylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1- {(S)-(4-chlórfenyl)[4-(N-etyl-N-cyklohexylaminometyl)fenyl]-metyl}-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, l-{((RS)-(4-chlórfenyl)(4-[(4-etoxykarbonylpiperazinyl)metyl]-fenyljmetyl]}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]-azetidín, l-({(R)-(4-chlórfenyl)(4-[(4-etoxykarbonylpiperazinyl)metyl]-fenyl}metyl)}}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]-azetidín,1 - {(S) - (4-chlorophenyl) [4- (N-ethyl-N-cyclohexylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - { ((RS) - (4-chlorophenyl) (4 - [(4-ethoxycarbonylpiperazinyl) methyl] phenylphenyl)} - 3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - ({(R ) - (4-chlorophenyl) (4 - [(4-etoxykarbonylpiperazinyl) methyl] phenyl} methyl)}} - 3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, II 1-{{(S)-(4-chlórfenyl)(4-[(4-etoxykarbonylpiperazinyl)metyl]I1 - {{(S) - (4-chlorophenyl) (4 - [(4-etoxykarbonylpiperazinyl) methyl] I -fenylJmetyl}}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]-azetidín,-fenylJmetyl}} - 3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-{(RS)-(4-chlórfenyl)[4-(N-cyklopropyl-N-propylaminometyl)-fenylJmetyl} -3— [(3,5-difluórfenyl) (metylsulfony1)metylénJ -azetidín, l-{(R) (4-chlórfenyl)[4-(N-cyklopropyl-N-propylaminometyl)-fenylJ metyl}-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]-azetidín, l-{(S)-(4-chlórfenyl)[4-(N-cyklopropyl-N-propylaminometyl)-fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]-azetidín,1 - {(RS) - (4-chlorophenyl) [4- (N-cyclopropyl-N-propylaminomethyl) -phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(R) (4-Chlorophenyl) [4- (N-cyclopropyl-N-propylaminomethyl) -phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(S) - (4 chlorophenyl) [4- (N-cyclopropyl-N-propylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-{(RS)-(4-chlórfenyl)[4-(diizopropylaminometyl)fenylJmetyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(F)-(4-chlórfenyl)-[4-(diizopropylaminometyl)fenyl]metyl}-3- [(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1 - {(RS) - (4-chlorophenyl) [4- (diisopropylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(F) - (4-chlorophenyl) - [4- (diisopropylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1- {(S)-(4-chlórfenyl)[4-(diizopropylaminometyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén)azetidín,1 - {(S) - (4-chlorophenyl) [4- (diisopropylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene) azetidine, 1-{{(RS)-(4-chlórfenyl)(4-[bis(2-metoxyetyl)aminometyl]fenyl}-metyl} }- 3- [ (3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{í(R)~(4-chlórfenyl){4-[bis(2-metoxyetyl)aminometyl]fenyl}-metyl}}-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín,1 - {{(RS) - (4-chlorophenyl) (4- [bis (2-methoxyethyl) aminomethyl] phenyl} methyl}} - 3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {η (R) - (4-chlorophenyl) {4- [bis (2-methoxyethyl) aminomethyl] phenyl} methyl}} - 3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-{{(S)-(4-chlórfenyl){4-[bis(2-metoxyetyl)aminometyl]fenyl}-metyl}}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1 - {{(S) - (4-chlorophenyl) {4- [bis (2-methoxyethyl) aminomethyl] phenyl} methyl}} - 3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1—{(FS)-(4-chlórfenyl) [4-[di-n-propylaminometyl)fenyl]metyl}-3- [ (3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, l-{(F)-(4-chlórfenyl) [4-(di-n-propylaminometyl)fenyl]metyl}-3-[ (3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín,1 - {(FS) - (4-chlorophenyl) [4- [di-n-propylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(F) - (4-chlorophenyl) [4- (di-n-propylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1—{(S)-(4-chlórfenyl)[4-(di-n-propylaminometyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{ (FS)-(4-chlórfenyl) [4-(piperidin-l-ylmetyl)fenyl]metyl}491 - {(S) - (4-chlorophenyl) [4- (di-n-propylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(FS) - (4-Chlorophenyl) [4- (piperidin-1-ylmethyl) phenyl] methyl} 49 -3—[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(Ŕ)-(4-chlórfenyl)[4-(piperidin-1-ylmety1)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(S)-(4-chlórfenyl)[ 4-(piperidin-l-ylmetyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-((RS)-(4-chlórfenyl)[4-(4-metylpiperazin-l-ylmetyl)fenyl]-metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(R)-(4-chlórfenyl)[4-(4-metylpiperazin-l-ylmetyl)fenyl] -metyl}-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín,3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(R) - (4-chlorophenyl) [4- (piperidin-1-ylmethyl) phenyl] methyl} -3 - [(3 5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(S) - (4-chlorophenyl) [4- (piperidin-1-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) ( methylsulfonyl) methylene] azetidine, 1 - ((RS) - (4-chlorophenyl) [4- (4-methylpiperazin-1-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene ] azetidine, 1 - {(R) - (4-chlorophenyl) [4- (4-methylpiperazin-1-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1- { (S) - (.4-chlórfenyl) [4 - (4-metylpiperazin-l-ylmetyl) fenyl] -metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(RS)-(4-chlórfenyl)[4-(morfolin-4-ylmetyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(R)-(4-chlórfenyl)[4-(morfolin-4-ylmetyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(S)-(4-chlórfenyl)[4-(morfolin-4-ylmetyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(RS)-(4-chlórfenyl)(4-(dietylaminometyl)fenyl]metyl)-3-[ (3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(R)-(4-chlórfenyl)[ 4-(dietylaminometyl)fenyl]metyl)-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1 - {(S) - (4-chlorophenyl) [4- (4-methylpiperazin-1-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1- {(RS) - (4-chlorophenyl) [4- (morpholin-4-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(R) - ( 4-chlorophenyl) [4- (morpholin-4-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(S) - (4-chlorophenyl) [4 - (morpholin-4-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(RS) - (4-chlorophenyl) (4- (diethylaminomethyl) phenyl] methyl) -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(R) - (4-chlorophenyl) [4- (diethylaminomethyl) phenyl] methyl) -3 - [(3,5 difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-((S)-(4-chlórfenyl)[4-(dietylaminometyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{ ((RS) - (4-chlórfenyl) [4- (piperazin-2-on-4-ylmetyl) fenyl] -metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1 - ((S) - (4-chlorophenyl) [4- (diethylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {((RS) - (4 - chlorophenyl) [4- (piperazin-2-one-4-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, I l-((R)-(4-chlórfenyl) [4-(piperazin-2-on-4-ylmetyl)fenyl]-metyl)-3-((3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,11 - ((R) - (4-Chlorophenyl) [4- (piperazin-2-one-4-ylmethyl) phenyl] methyl) -3 - ((3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-( (S) -(4-chlórfenyl)[4-(piperazin-2-on-4-ylmetyl)fenyl]-metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1 - ((S) - (4-chlorophenyl) [4- (piperazin-2-one-4-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1—{ (RS)-(4-chlórfenyl) [4-(imidazol-l-ylmetyl)fenyl]metyl}-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín,1 - {(RS) - (4-chlorophenyl) [4- (imidazol-1-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1—((R)-(4-chlórfenyl)[4-(imidazol-l-ylmetyl)fenyl]metyl}-3-[ (3,-5-difluórfenyl) (metylsulfonyl)metylén] azetidín, l-{(S)-(4-chlórfenyl)[4-(imidazol-l-ylmetyl)fenyl]metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, (RS)-l-{(4-chlórfenyl)[4-(N,N-dimetylkarbamoyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, (R) -l-{(4-chlórfenyl)[4-(N,N-dimetylkarbamoyl)fenyl]metyl}-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, (S) —1—{(4-chlórfenyl)[4-(N,N-dimetylkarbamoyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, (RS)-l-{(4-chlórfenyl)[4-(N-etylkarbamoyl)fenyl]metyl)}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, (R) —1-{(4-chlórfenyl)[4-(N-etylkarbamoyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, (S) -l-{(4-chlórfenyl)[4-(N-etylkarbamoyl)fenyl]mety}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, (RS)-1-[(4-karbamoylfenyl) (4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, (R) -1-[(4-karbamoylfenyl) (4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, (S) -1-[(4-karbamoylfenyl)(4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín,1 - ((R) - (4-chlorophenyl) [4- (imidazol-1-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(S - (4-chlorophenyl) [4- (imidazol-1-ylmethyl) phenyl] methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (RS) -1 - {(4-chlorophenyl) ) [4- (N, N-dimethylcarbamoyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (R) -1 - {(4-chlorophenyl) [4- (N , N-dimethylcarbamoyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (S) -1 - {(4-chlorophenyl) [4- (N, N-dimethylcarbamoyl) phenyl methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (RS) -1 - {(4-chlorophenyl) [4- (N-ethylcarbamoyl) phenyl] methyl)} - 3- [ (3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (R) -1 - {(4-chlorophenyl) [4- (N-ethylcarbamoyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) ( methylsulfonyl) methylene] azetidine, (S) -1 - {(4-chlorophenyl) [4- (N-ethylcarbamoyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (RS) ) -1 - [(4-carbamoylphenyl) (4-chlorophenyl) methyl] -3 - [(3,5-difluoro) (phenyl) (methylsulfonyl) methylene] azetidine, (R) -1 - [(4-carbamoylphenyl) (4-chlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (S) - 1 - [(4-carbamoylphenyl) (4-chlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(3,5-dichlórfenyl)(metylsulfonyl)1- [Bis (4-chlorophenyl) methyl] -3 - [(3,5-dichlorophenyl) (methylsulphonyl) -metylén]azetidín,methylene] azetidine, I l-bénzhydryl-3-[(3-metylsulfanylfenyl)(metylsulfonyl)metylén]-azetidín, l-benzhydryl-3-[(3-metylsulfanylmetyl)fenyl) ] (metylsulfonyl)-metylén)azetidín,11-benzhydryl-3 - [(3-methylsulfanylphenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-methylsulfanylmethyl) phenyl)] (methylsulfonyl) methylene) azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(3-kyanofenyl)(mety1sulfony1)-metylén]azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - [(3-cyanophenyl) (mety1sulfony1) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(3-karbamoylfenyl) (metylsulfonyl)-metylén]azetidín,1- [bis (4-chlorophenyl) methyl] -3 - [(3-carbamoylphenyl) (methylsulfonyl) methylene] azetidine, 1- [bis(4-chlórfenyl)metyl]-3-[(3-metoxyfenyl) (metylsulfonyl)-metylén]azetidín,1- [bis (4-chlorophenyl) methyl] -3 - [(3-methoxyphenyl) (methylsulfonyl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(3-hydroxyfenyl)(metylsulfonyl)-metylén]azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - [(3-hydroxyphenyl) (methylsulphonyl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(metylsulfonyl)(3-pyrolidinylfenyl)metylén]azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - [(methylsulphonyl) (3-pyrrolidinylphenyl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(3-hydroxymetylfenyl)(metylsulfonyl) metylén]azetidín,1- [bis (4-chlorophenyl) methyl] -3 - [(3-hydroxymethylphenyl) (methylsulfonyl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-((metylsulfonyl) [3-(N-piperidylkarbamoyl)fenyl]metylén}azetidín,1- [bis (4-chlorophenyl) methyl] -3 - ((methylsulfonyl) [3- (N-piperidylcarbamoyl) phenyl] methylene} azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(metylsulfonyl) (3-trifluórmetylsulfanylfenyl)(metylsulfonyl)metylén]azetidín,1- [bis (4-chlorophenyl) methyl] -3 - [(methylsulfonyl) (3-trifluoromethylsulfanylphenyl) (methylsulfonyl) methylene] azetidine, 1-[bis(4-fluórfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)-metylén]azetidín,1- [Bis (4-fluorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-[bis(2-fluórfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)-metylén]azetidín,1- [Bis (2-fluorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1- [bis(3-fluórfenyl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyl)-metylén]azetidín, (RS]-1-[(4-chlórfenyl)(tiazol-2-yl)metyl]-3-[(metylsulfonyi)-(fenyl)metylén]azetidín, (R) -1-[(4-chlórfenyl) (tiazol-2-yl)metyl]-3 - [(metylsulfonyi)-(fenyl)metylén]azetidín, (S) —1—[ (4-chlórfenyl) (tiazol-2-yl)metyl]-3- [ (metylsulfonyi) -(fenyl)metylén]azetidín, (RS)-1-[(4-chlórfenyl)(tien-2-yl)metyl]-3- [(3,5-difluórfenyl)-(metylsulfonyi)metylén]azetidín, (R) -1-[(4-chlórfenyl)(tieň-2-yl)metyl]-3-[(3,5-difluórfenyl)-(metylsulfonyi)metylén]azetidín, (S) -1-[(4-chlórfenyl) (tien-2-yl)metyl]-3-[(3,5-difluórfenyl)-(metylsulfonyi)metylén]azetidín, l-benzhydryl-3-[(etylsul·fonyl)(fenyl)metylén]azetidín,1- [bis (3-fluorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (RS) -1 - [(4-chlorophenyl) (thiazol-2-yl) methyl ] -3 - [(methylsulfonyl) - (phenyl) methylene] azetidine, (R) -1 - [(4-chlorophenyl) (thiazol-2-yl) methyl] -3 - [(methylsulfonyl) - (phenyl) methylene] azetidine, (S) -1 - [(4-chlorophenyl) (thiazol-2-yl) methyl] -3 - [(methylsulfonyl) - (phenyl) methylene] azetidine, (RS) -1 - [(4-chlorophenyl) (Thien-2-yl) methyl] -3 - [(3,5-difluorophenyl) - (methylsulfonyl) methylene] azetidine, (R) -1 - [(4-chlorophenyl) (shadow-2-yl) methyl] - 3 - [(3,5-difluorophenyl) - (methylsulfonyl) methylene] azetidine, (S) -1 - [(4-chlorophenyl) (thien-2-yl) methyl] -3 - [(3,5-difluorophenyl) - (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(ethylsulfonyl) (phenyl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-{{3-[N-(4-metylpiperazinyl)-karbamoyl]fenyl](metylsulfonyl)metylén)azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - {{3- [N- (4-methylpiperazinyl) carbamoyl] phenyl] (methylsulfonyl) methylene) azetidine, 1-[bis(4-chlórfenyl)metyl]-3-{[3-(2,2-dimetylkarbohydrazido)-fenyl](metylsulfonyi)metylén}azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - {[3- (2,2-dimetylkarbohydrazido) phenyl] (methylsulfonyl) methylene} azetidine, 1- [bis(tien-2-yl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyi)-metylén]azetidín,1- [bis (thien-2-yl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-[bis(p-tolyl)metyl]-3-[(metylsulfonyi)(fenyl)metylén]azetidín1- [bis (p-tolyl) methyl] -3 - [(methylsulfonyl) (phenyl) methylene] azetidine 1-[(4-chlórfenyl) (4-hydroxymetylfenyl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyi)metylén]azetidín,1 - [(4-chlorophenyl) (4-hydroxymethylphenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1- [bis(4-chlórfenyl)metyl]-3-[(3-metylaminofenyl) (metylsulfonyl)metylén]azetidín, (RS)-1-[(4-chlórfenyl)(tiazol-2-yl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyi)metylén]azetidín, (R) -1-[(4-chlórfenyl) (tiazol-2-yl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, (S) -1-[(4-chlórfenyl)(tiazol-2-yl)metyl]-3-[(3,5-difluórfenyl·) (metylsulfonyl)metylén]azetidín, (RS)-1-[bis(4-chlórfenyi)metyl]-3-[(metylsulfonyl)(2-metoxykarbonyltien-5-yl)metylén]azetidín,1- [bis (4-chlorophenyl) methyl] -3 - [(3-methylaminophenyl) (methylsulfonyl) methylene] azetidine, (RS) -1 - [(4-chlorophenyl) (thiazol-2-yl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (R) -1 - [(4-chlorophenyl) (thiazol-2-yl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) (methylene) azetidine, (S) -1 - [(4-chlorophenyl) (thiazol-2-yl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (RS) -1 - [bis (4-chlorophenyl) methyl] -3 - [(methylsulfonyl) (2-methoxycarbonylthien-5-yl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-hydroxy-3-[(metylsulfonyl)(2-meto xykarbonyltieň-5-y1)metylén]azetidín,1- [bis (4-chlorophenyl) methyl] -3-hydroxy-3 - [(methylsulfonyl) (2-methoxycarbonythien-5-yl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(2-izobutylaminokarbonyltien-5-yl)(metylsulfonyl)metylén]azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - [(2-izobutylaminokarbonyltien-5-yl) (methylsulfonyl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(3-metoxykarbonylfenyl) -(metylsulfonyl)metyl-(RS)]azetidín-3-ol,1- [bis (4-chlorophenyl) methyl] -3 - [(3-methoxycarbonylphenyl) - (methylsulfonyl) methyl- (RS)] azetidin-3-ol, 1-[bis(4-chlórfenyl)metyl]-3-[(metylsulfonyl)(pyrid-4-yl)-metyl-(RS)]azetidin-3-ol,1- [Bis (4-chlorophenyl) methyl] -3 - [(methylsulphonyl) (pyridin-4-yl) methyl- (RS)] azetidin-3-ol, 1-[[bis(4-chlórfenyl)metyl]-3-[(metylsulfonyl)(pyrid-3-yl)-metyl-(RS)]azetidin-3-ol,1 - [[Bis (4-chlorophenyl) methyl] -3 - [(methylsulphonyl) (pyridin-3-yl) methyl- (RS)] azetidin-3-ol, 3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfonylmetyl) -N-(3-morfolin-4-ylpropyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -N- (3-morpholin-4-ylpropyl) benzamide, 3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidénImetánsulfonylmetyl)-N-(3-dimetylaminopropyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidénImetánsulfonylmetyl) -N- (3-dimethylaminopropyl) benzamide. 3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfonylmetyl)-N-(2-(pyrolidin-l-yl)etyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -N- (2- (pyrrolidin-l-yl) ethyl) benzamide, 3-({1-[bis(4-chlórfenyl) mety l]azetidin-3-ylidén[metánsulfony1metyl)-N-(2-dimetylamino-l-metyletyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene [methanesulfonylmethyl) -N- (2-dimethylamino-1-methylethyl) benzamide, 3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfonylmetyl)-N-(piperidin-l-yl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -N- (piperidin-l-yl) benzamide, 3-({Ϊ-[bis(4-chlórfenyl)metyl]azetidín-3-ylidén}metánsulfonyl54 metyl)-N-izobutylbenzamid,3 - ({Ϊ- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonyl-54-methyl) -N-isobutylbenzamide, 3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfonylmetyl)-N-(3-imidazol-l-ylpropyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -N- (3-imidazol-l-yl-propyl) -benzamide, 3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfonylmetyl)-N-(2-dimetylaminoetyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -N- (2-dimethylamino-ethyl) -benzamide, N'-metylhydrazid kyseliny 3-({1-[bis(4-chlórfenyl)metyl]-azetidin-3-ylidén}metánsulfonylmetyl)benzoovej,3 - ({1- [Bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) benzoic acid N'-methylhydrazide, 3-({1-[bis (4-chlórfenyl)metylazetidin-3-ylidén}metánsulfonylmetyl)-N-(2-morfolin-4-yletyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methylazetidin-3-ylidene} methanesulfonylmethyl) -N- (2-morpholin-4-ylethyl) benzamide, 3- ({1-bis(4-chlórfenyl)metyl]azetidin-3-ylidénJmetánsulfonylmetyl)-N-(l-etylpyrolidin-2-ylmetyl)benzamid,3- ({1-bis (4-chlorophenyl) methyl] azetidin-3-ylidene) methanesulfonylmethyl) -N- (1-ethylpyrrolidin-2-ylmethyl) benzamide, 3-((1- (bis(4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfonylmetyl)-N-(2,2-dimetylpropyl)benzamid,3 - ((1- (bis (4-chlorophenyl) methyl) azetidin-3-ylidene} methanesulfonylmethyl) -N- (2,2-dimethylpropyl) benzamide, 3-([1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidénJmetánsulfonylmetyl)-N-(cyklohexylmetyl)benzamid,3 - ([1- [Bis (4-chlorophenyl) methyl] azetidin-3-ylidénJmetánsulfonylmetyl) -N- (cyclohexylmethyl) -benzamide, 3-({1-[bis(4-chlórfenyl)metyl]azetidín-3-ylidénJmetánsulfonylmetyl)-N- (cyklopropylmetyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene) methanesulfonylmethyl) -N- (cyclopropylmethyl) benzamide, 3-((1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén]metánsulfonylmetyl)-N-(2-metylbutyl)benzamid,3 - ((1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene] methanesulfonylmethyl) -N- (2-methylbutyl) benzamide, 3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfonylmetyl)-N-(2-fenylpropyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -N- (2-phenylpropyl) benzamide, 3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfonylmetyl)-N-(tetrahydrofuran-2-ylmetyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -N- (tetrahydrofuran-2-ylmethyl) -benzamide, 3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidénJmetánsulfonylmetyl)-N-(2,2-difenyletyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidénJmetánsulfonylmetyl) -N- (2,2-diphenyl-ethyl) -benzamide, 3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylídén]metánsulfonylmetyl)-N-(2-etylbutyl)benzamid, metylester kyseliny 4-{[3-({1-[bis(4-chlórfenyl)metyl]-azetidin-3-ylidén}metánsulfonylmetyl)benzoylamino]metyl}-cyklohexánkarboxyiovej,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene] methanesulfonylmethyl) -N- (2-ethylbutyl) benzamide, methyl 4 - {[3 - ({1- [bis (4- chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -benzoylamino] -methyl} -cyklohexánkarboxyiovej, 2-amino-l-{ 4 - (3- ({l-[bis (4-chlórfenyl)metyl]aze t idin-3-ylidén}-metánsulfonylmetyl)fenyl]pipeŕazin-l-yl}etanón, terc-butylester kyseliny (2-{4-[3-({1-[bis(4-chlórfenyl)metyl] azetidin-3-ylidén}metánsulfonylmetyl)fenyl]piperazin-l-yl}-2-oxoetyl)karbamovej,2-Amino-1- {4- (3- ({1- [bis (4-chloro-phenyl) -methyl] -azolidin-3-ylidene} -methanesulfonylmethyl) -phenyl] -piperazin-1-yl} -ethanone, tert-butyl ester (2- {4- [3 - ({1- [Bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) phenyl] piperazin-1-yl} -2-oxoethyl) carbamic acid, 1—{4-[3—({1—[bis(4-chlórfenyl)metyl]azetidin-3-ylidén]-metánsulfonylmetyl)fenyl]piperazin-l-yl}-2-metylaminoetanón, terc-butylester kyseliny (2-{4-[3-((1-[bis(4-chlórfenyl)metyl] azetidin-3-ylidén}metánsulfonylmetyl)fenyl]piperazin-l-yl}-2-oxoetyl)-N-metylkarbamovej,1- {4- [3 - ({1- [Bis (4-chloro-phenyl) -methyl] -azetidin-3-ylidene] -methanesulfonylmethyl) -phenyl] -piperazin-1-yl} -2-methylamino-ethanone, 2- (tert-butyl) ester {4- [3 - ((1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) phenyl] piperazin-1-yl} -2-oxoethyl) -N-methylcarbamic acid, N-metylamid kyseliny 4-[3-({[1-bis(4-chlórfenyl)metyl]-azetidin-3-ylidén}metánsulfonylmetyl)fenyl]piperazín-1-karbotioovej,4- [3 - ({[1-Bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) phenyl] piperazine-1-carbothioic acid N-methylamide, N-metylamid kyseliny 4-[3-({1-[bis(4-chlórfenyl)metyl]-azetidin-3-ylidén}metánsulfonyl)metylfenyl]piperazín-1-karboxylovej, metylester kyseliny 4-[3-({1-[bis(4-chlórfenyl)metyl]-azetidin-3-ylidén]metánsulfonylmetyl)fenyl]piperazín-1-karboxylovéj,4- [3 - ({1- [Bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonyl) methylphenyl] piperazine-1-carboxylic acid N-methylamide, methyl 4- [3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene] methanesulfonylmethyl) phenyl] piperazine-1-carboxylic acid, 1-[3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidénJmetánsulfonylmetyl)fenyl]-4-izobutylpiperazín,1- [3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidénJmetánsulfonylmetyl) phenyl] -4-isobutylpiperazine, 1-[3-({1-[bis(4-chlórfenyl) metyl]azetidin-3-ylidén}metánsulfonylmetyl)fenyl]-4-etylpiperazín,1- [3 - ({1- [Bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) phenyl] -4-ethylpiperazine, II 4-acetyl-1-[3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}-metánsulfonylmetyl)fenyl]piperazín,4-Acetyl-1- [3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} -metánsulfonylmetyl) phenyl] piperazine, 1-{4-[3-({1- [bis(4-chlórfenyl)metyl]azetidin-3-ylidén[metánsulf onylmetyl)fenyl]piperazin-l-yl}-2-dimetylaminoetanón,1- {4- [3 - ({1- [Bis (4-chlorophenyl) methyl] azetidin-3-ylidene [methanesulfonylmethyl) phenyl] piperazin-1-yl} -2-dimethylaminoethanone, 1-[3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-y1idén]metánsulf onylmetyl ) fenyl]piperazín, terc-butylester kyseliny 4-[3-({l-[bis(4-chlórfenyl)metyl]azetidín-3-ylidén}metánsulfonylmetyl)fenyl]piperazín-l-karboxylovej,4- [3 - ({1- [Bis (4-Chloro-phenyl) -methyl] -phenyl] -piperazine-1- [3 - ({1- [bis (4-chloro-phenyl) -methyl] -azetidin-3-ylidene] -methanesulfonylmethyl) -phenyl] -piperazine ) methyl] azetidin-3-ylidene} methanesulfonylmethyl) phenyl] piperazine-l-carboxylic acid, 1-[bis(4-metoxykarbonylfenyl)metyl]-3-[(3,5-difluórfenyl)-(metylsulfonyl)metylén]azetidin,1- [Bis (4-methoxycarbonylphenyl) methyl] -3 - [(3,5-difluorophenyl) - (methylsulphonyl) methylene] azetidine, 3- acetoxy-l-[bis(4-metoxykarbonylfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)metyl-(RS)]azetidín, (RS)-4-[4-((4-chlórfenyl){3-[(3,5-difluórfenyl)metánsulfonylmetylén]azetidín-l-yl}metyl)benzyl]morfolín,3-Acetoxy-1- [bis (4-methoxycarbonylphenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methyl- (RS)] azetidine, (RS) -4- [4 - ((4- chlorophenyl) {3 - [(3,5-difluorophenyl) metánsulfonylmetylén] azetidin-l-yl} methyl) benzyl] morpholine, 4- (4-{3-[(1-benzhydrylazetidin-3-y1idén)metánsulfonylmetyl]-fenoxy]butyl)morfolín,4- (4- {3 - [(1-benzhydrylazetidin-3-ylidene) methanesulfonylmethyl] phenoxy] butyl) morpholine, 4-(4-{3-[(1-benzhydrylazetidin-3-ylidén)metánsulfonylmetyl]-fenoxy]propyl)morfolín,4- (4- {3 - [(1-benzhydryl-azetidin-3-ylidene) methanesulfonylmethyl] phenoxy] propyl) morpholine, N-{1-[bis(4-chlórfenyl)metyl]azetidín-3-y1}tien-2-ylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-y1} thien-2-ylsulfonamide, N-(1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-4-metoxyfenylsulf ónamid,N- (1- [bis (4-chlorophenyl) methyl] azetidin-3-yl) -4-methoxyphenylsulfonamide, N- [4-(N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-y1}sulfamoyl)-fenyl]acetamid,N- [4- (N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} sulfamoyl) phenyl] acetamide, N-(1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-4-metylfeny1sulfónamid,N- (1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -4-metylfeny1sulfónamid, N-{1-[bis(4-chlórfenyl)metyl]azetidín-3-yl}-3,4-dimetoxyfenylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3,4-dimetoxyfenylsulfónamid, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-3-fluórfenyl57 sulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3-fluorophenyl57 sulfonamide, II II N- { ί-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-3, 4-dichlórfenylsulfónamid,N- {N - [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3,4-dichlorophenylsulfonamide, N - {1-[bis(4-chlórfenyl)metyl]azetidin-3-yl)-3-kyanofény1sulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl) -3-cyanophenylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-2,5-dimetoxyfenylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -2,5-dimetoxyfenylsulfónamid, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-3-trifluórmetylfenylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3-trifluórmetylfenylsulfónamid, N- {1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}naft-2-ylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} naphth-2-ylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}naft-1-ylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} naphth-1-ylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yi}-3,4-difluórfenylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3,4-difluórfenylsulfónamid, N- {1- [bis (4-chlórfenyl)metyl] azetidin-3-yl} -1-metyl-1H-imidazol-4-ylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -1-methyl-1H-imidazol-4-ylsulphonamide, N-[4-(N-[l-[bis(4-chlórfenyl)metyl]azetidin-3-yl}sulfamoyl)-2-chlórfenyl]acetamid,N- [4- (N- [l- [bis (4-chlorophenyl) methyl] azetidin-3-yl} sulfamoyl) -2- chlorophenyl] acetamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}pyrid-3-ylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} pyrid-3-ylsulfonamide, N-{1-[bis(4-chlórfenylmetyl]azetidin-3-yl}-4-fluórfenylsulfónamid,N- {1- [bis (4-chlorophenyl methyl] azetidin-3-yl} -4-fluorophenylsulfonamido, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}chinol-8-ylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} quinolin-8-ylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}fenylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} phenylsulfonamide, II N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}(fenylmetyl)IN- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} (phenylmethyl) I -sulfónamid,sulfonamide, II N-[i-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-3,5-difluórfenyl58 sulfónamid,N- [1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3,5-difluorophenyl58 sulfonamide, N-{1- [bis (4-chlórfenyl)metyl]azetidin-3-yl}pyrid-2-ylsulfónamid,N- {1- [bis (4-chloro-phenyl) -methyl] -azetidin-3-yl} -pyrid-2-ylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-(3-fluór-5-pyrolidin-l-ylfenyl)sulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} - (3-fluoro-5-pyrrolidin-l-yl-phenyl) sulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-metyl-4-fluórfenyl· sulf ónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N-methyl-4-fluorophenylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl)-N-metylchinol-8-ylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl) -N-methyl-quinolin-8-ylsulfonamide, N-(1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-metylfenylsulfónamid,N- (1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N-methylphenylsulfonamido, N-(1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-metyl(fenyimety1)-sulfónamid,N- (1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N-methyl (fenyimety1) sulfonamide, N-{1- [bis(4-chlórfenyl)metyl]azetidin-3-yl}-3-sulfamoylfenylsulf ónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3-sulfamoylphenylsulfonamide, 2-benzénsulfonyl-N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-acetamid,2-benzenesulfonyl-N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -acetamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-2-(4-toluén-4-sulfonyl)acetamid, (3-chlór-4-metylsulfonyltiofén-2-karboxy)-{1-[bis(4-chlórfenyl)-metyl]azetidin-3-yl]amid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -2- (4-toluene-4-sulfonyl) acetamide, (3-chloro-4-methylsulfonylthiophene-2-carboxy) - {1 - [bis (4-chlorophenyl) methyl] azetidin-3-yl] -amide, N-(1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-3-(2-fenyletylénsulfonyl)propiónamid,N- (1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3- (2-fenyletylénsulfonyl) propionamide, N-(l-[bis(4-chlórfenyl)metyl]azetidin-3-yl)-4-metylsulfonyl·benzamid,N- (l- [bis (4-chlorophenyl) methyl] azetidin-3-yl) -4-methylsulfonyl benzamide ·, N - {1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-4-metánsulfonylbenzamid, (5-metylsulfonyltiofén-2-karboxy)-(1-[bis(4-chlórfenyl)metyl]59N - {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -4-methanesulfonylbenzamide, (5-methylsulfonylthiophene-2-carboxy) - (1- [bis (4-chlorophenyl) methyl] 59 II -azetidín-3-yl}amid,azetidin-3-yl} amide, I (5-metylsulfonyl-3-mety1-4-vinyltiofén-2-karboxy)- {1-, [bis (4 -chlórfenyl) metyl ] azetidín-3-yl} amid, (RS)-N-{1-[(4-chlórfenyl)pyridin-3-ylmetyl]azetidin-3-yl}-3,5-difluórbenzénsulfónamid, (RS)-N-{1-[(4-chlórfenyl)pyrimidin-5-ylmetyl] azetidin-3-yl}-3,5-difluórbenzénsulfónamid,(RS) -N- {1- [1- (5-Methylsulfonyl-3-methyl-4-vinyl-thiophene-2-carboxy) - {1-, [bis (4-chloro-phenyl) -methyl] -azetidin-3-yl} -amide] (4-Chlorophenyl) pyridin-3-ylmethyl] azetidin-3-yl} -3,5-difluorobenzenesulfonamide, (RS) -N- {1 - [(4-chlorophenyl) pyrimidin-5-ylmethyl] azetidin-3-yl } -3,5-difluoro-benzenesulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl)-N-(6-chlórpyrid-2-yl)metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl) -N- (6-chloropyrid-2-yl) methylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(6-etylpyrid-2-yl)metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (6-ethyl-pyridin-2-yl) methylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl)-N-chinol-6-ylmetylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl) -N-quinolin-6-ylmetylsulfónamid, N-(1-[bis(4-chlórfenyl)metyl]azetidín-3-y1}-N-chinol-5-ylmetylsulfónamid,N- (1- [bis (4-chlorophenyl) methyl] azetidin-3-y1} -N-quinolin-5-ylmetylsulfónamid, N-{1-[bis(4-chlórfenyl)metyl]azetidín-3-y1}-N-izochinol-5-ylmetylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-y1} -N-isoquinolin-5-ylmetylsulfónamid, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-pyrid-3-ylmetylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N-pyrid-3-ylmetylsulfónamid, N-{1- [bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(pyrid-l-oxid-3-yl)metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (pyrid-1-oxide-3-yl) methylsulfonamide, N-(1F, 2 S,4S)-bicyklo[2,2,1]hept-2-yl-N-{1-[bis-(4-chlórfenyl)-metyl]azetidin-3-yl}metylsulfónamidN- (1F, 2S, 4S) -bicyclo [2.2.1] hept-2-yl-N- {1- [bis- (4-chloro-phenyl) -methyl] -azetidin-3-yl} -methylsulfonamide N- (1/?, 2R, 4 5) - (bicyklo [2,2,1] hept-2-yl) -N-{ 1- (bis - (4-chlórfenyl) -metyl]azetidin-3-y1[metylsulfónamid,N- (1H, 2R, 4,5) - (bicyclo [2.2.1] hept-2-yl) -N- {1- (bis- (4-chlorophenyl) methyl) azetidin-3-yl [methyl sulfonamide. II II N- {1-- [bis (4-chlórfenyl) metyl] azetidin-3-yl} -N- (3, 5-difluórfenyí)metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide, N-[1-[bis(4-chlórfenyl)metyl]azetidin-3-yl)-N-(tiazol-2-yl)-metylsulfónamid,N- [1- [Bis (4-chlorophenyl) methyl] azetidin-3-yl) -N- (thiazol-2-yl) methylsulphonamide, N-{1-(bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(3-metoxyfenyl)-metylsulfónamid,N- {1- (bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (3-methoxyphenyl) methylsulphonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl]-N-(3-hydroxyfenyl) -metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl] -N- (3-hydroxyphenyl) methylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(3-hydroxymetylfenyl)metylsulfónamid, etyl-N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(metylsulfonyl) -3-aminobenzoát,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (3-hydroxymethylphenyl) methylsulfonamide, ethyl N- {1- [bis (4-chlorophenyl) methyl] azetidin-3- yl} -N- (methylsulfonyl) -3-aminobenzoate, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(izobutylpiperid-4-yi)metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (izobutylpiperid-4-yl) methylsulfonamide, N-benzyl-N-(1-[bis(4-chlórfenyl) met yl]azetidin-3-yl}amín,N-benzyl-N- (1- [bis (4-chlorophenyl) methyl] azetidin-3-yl) amine, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(3,5-difluórbenzyl)amín,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (3,5-difluorobenzyl) amine, N-(1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(3,5-difluórbenzyl)metylsulfónamid,N- (1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (3,5-difluorobenzyl) methylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl]-N-(pyrid-3-ylmetyl)metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl] -N- (pyridin-3-ylmethyl) methylsulfonamide, N-{1-[bis(4-fluórfenyl)metyl]azetidin-3-yl}-N-(3,5-difluórfenyl) metyl sulf ónamid, (RS)-N-{1-[(4-chlórfenyl)pyrid-3-ylmetyl]azetidin-3-yl)-N- (3,5-difluórfény1)metylsulfónamid, (R) -N-{1-[(4-chlórfenyl)pyrid-3-ylmetyl]azetidin-3-yl}-N- (3,5-difluórfenyl)metylsulfónamid, (S) -N-{1-[(4-chlórfenyl)pyrid-3-ylmetyl]azetidin-3-yl}-N- (3,5-difluórfenyl)metylsulfónamid, (RS^-N-{1-[(4-chlórfenyl)pyrid-4-ylmetyl]azetidín-3-y1}-N- (3,' 5-difluórfenyl)metylsulfónamid, (R) -N-{1—[(4-chlórfenyl)pyrid-4-ylmetyl]azetidin-3-yi)-N-(3,5-difluórfenyl)metylsulfónamid, (S) -N-{1-[(4-chlórfenyl)pyrid-4-ylmetyl]azetidin-3-yl}-N-(3,5-difluórfenyl)metylsulfónamid, (RS)-N-{1- [(4-chlórfenyl)pyrimidin-5-ylmetyl]azetidin-3-yl}-N-(3,5-difluórfenyl)metylsulfónamid, (R) —N-{1—[(4-chlórfenyl)pyrimidín-5-ylmetyl]azetidin-3-yl}-N-(3,5-difluórfenyl)metylsulfónamid, (S) -N-(1-[(4-chlórfenyl)pyrimidín-5-ylmetyl]azetidin-3-yl}-N(3,5-difluórfenyl)metylsulfónamid,N- {1- [bis (4-fluorophenyl) methyl] azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide, (RS) -N- {1 - [(4-chlorophenyl) pyridine -3-ylmethyl] azetidin-3-yl) -N- (3,5-difluorophenyl) methylsulfonamide, (R) -N- {1 - [(4-chlorophenyl) pyrid-3-ylmethyl] azetidin-3-yl} N- (3,5-difluorophenyl) methylsulfonamide, (S) -N- {1 - [(4-chlorophenyl) pyrid-3-ylmethyl] azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide (RS) -N- {1 - [(4-chlorophenyl) pyrid-4-ylmethyl] azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide, (R) -N- {1- [(4-chlorophenyl) pyrid-4-ylmethyl] azetidin-3-yl) -N- (3,5-difluorophenyl) methylsulfonamide, (S) -N- {1 - [(4-chlorophenyl) pyrid-4-ylmethyl] Azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide, (RS) -N- {1 - [(4-chlorophenyl) pyrimidin-5-ylmethyl] azetidin-3-yl} -N- ( 3,5-Difluorophenyl) methylsulfonamide, (R) -N- {1 - [(4-chlorophenyl) pyrimidin-5-ylmethyl] azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide, (S) N- (1 - [(4-chlorophenyl) pyrimidin-5-ylmethyl] azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(3,5-difluórfenyl) benzylsulfónamid, ich optické izoméry a ich farmaceutický prijateľné soli.N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (3,5-difluorophenyl) benzylsulfonamide, their optical isomers, and their pharmaceutically acceptable salts. 4. Kombinácia podľa nároku 2, kde zlúčenina všeobecného vzorca I je vybraná z nasledovných zlúčenín:The combination of claim 2, wherein the compound of Formula I is selected from the following compounds: 1-[bis(4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)metyl-(RS)]azetidin-3-ol,1- [Bis (4-chlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methyl- (RS)] azetidin-3-ol, 3-acetoxy-l-[bis(4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl)-(metylsulfonyl)metyl)metylsulfonylmetyl-(RS)]azetidín,3-acetoxy-l- [bis (4-chlorophenyl) methyl] -3 - [(3,5-difluorophenyl) - (methylsulfonyl) methyl) methylsulfonylmethyl (RS)] azetidine, 1- [bis (4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyl)-metylén]azetidín, a ich optické izoméry a ich farmaceutický prijateľné soli.1- [bis (4-chlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) -methylene] azetidine, and their optical isomers and pharmaceutically acceptable salts thereof. 5. ίKombinácia podľa nároku 1, kde antagonista CBl je SR141716, jeho hydráty a farmaceutický prijateľné soli alebo LY320135 a jeho farmaceutický prijateíné soli.The combination of claim 1, wherein the CB1 antagonist is SR141716, hydrates thereof, and pharmaceutically acceptable salts thereof, or LY320135, and pharmaceutically acceptable salts thereof. 6. Farmaceutická kompozícia, vyznačujúca sa tým, že obsahuje antagonistu CB1 a sibutramín, jeho hydrát alebo jednu z jeho farmaceutický prijateľných solí v čistom stave alebo s jedným alebo viacerými kompatibilnými a farmaceutický prijatelnými zrieďovadlami a/alebo pomocnými látkami a/alebo prípadne v kombinácii s ďalším farmaceutický kompatibilným a fyziologicky aktívnym produktom.A pharmaceutical composition comprising a CB1 antagonist and sibutramine, a hydrate thereof, or one of its pharmaceutically acceptable salts, in pure form or with one or more compatible and pharmaceutically acceptable diluents and / or excipients and / or optionally in combination with another pharmaceutically compatible and physiologically active product. 7. Farmaceutická kompozícia podlá nároku 6, vyznačujúca sa tým, že antagonista CB1 je zlúčenina všeobecného vzorca I, ako je definované v nároku 2.Pharmaceutical composition according to claim 6, characterized in that the CB1 antagonist is a compound of formula I as defined in claim 2. 8. Farmaceutická kompozícia podľa nároku 7, vyznačujúca sa t ý m, že sa pre ňu zlúčenina všeobecného vzorca I vyberie zo skupiny, ktorú tvoria nasledovné zlúčeniny:Pharmaceutical composition according to claim 7, characterized in that the compound of the formula I is selected from the group consisting of the following compounds: l-benzhydryl-3-[(metylsulfonyl)(fenyl)metylén]azetidín, l-benzhydryl-3-[(3-metylfenyl)(metylsulfonyl)metylén]azetidín, l-benzhydryl-3-[(3-chlórfenyl)(metylsulfonyl)metylén]azetidín, l-benzhydryl-3-[(3,5-dichlórfenyl)(metylsulfonyl)metylén]-azetidín, l-benzhydryl-3- [ (2,5-dichló.rfenyl) (metylsulf onyl) metylén] -azetidín, l-benzhydryl-3-[(2,3-dichlórfenyl)(metylsulfonyl)metylén]-azetidín, l-benzhydryl-3-[(3-fluórfenyl)(metylsulfonyl)metylén]azetidín, l-benzhydryl-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]-azetidín, l-benzhydryl-3-[(3-brómfenyl) (metylsulfonyl)metylén]azetidín, l-benzhydryl-3-[(3-jódfenyl)(metylsulfonyl)metylén]azetidín, l-benzhydryl-3-[(metylsulfonyl) (3-trifluórmetoxyfenyl)metylén]-azetidín, l-benzhydryl-3-[(metylsulfonyl) (3-trifluórmetylfenyl)metylén]-azetidín, l1-benzhydryl-3 - [(methylsulfonyl) (phenyl) methylene] azetidine, 1-benzhydryl-3 - [(3-methylphenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-chlorophenyl) (methylsulfonyl) ) methylene] azetidine, 1-benzhydryl-3 - [(3,5-dichlorophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(2,5-dichlorophenyl) (methylsulfonyl) methylene] - azetidine, 1-benzhydryl-3 - [(2,3-dichlorophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-fluorophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3- [ (3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-bromophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-iodophenyl) (methylsulfonyl) methylene ] azetidine, 1-benzhydryl-3 - [(methylsulfonyl) (3-trifluoromethoxyphenyl) methylene] azetidine, 1-benzhydryl-3 - [(methylsulfonyl) (3-trifluoromethylphenyl) methylene] azetidine, 1 l-benzhydryl-3-{[3,5-bis(trifIuórmetyl)fenyl](metylsulfonyl)-metylén}azetidín, l-benzhydryl-3-[(3,5-dibrómfenyl)(metylsulfonyl)metylén]-azetidín, l-benzhydryl-3-[(3-metoxykarbony1fenyl)(metylsulfonyl)metylén]-azetidín, l-benzhydryl-3-[(3-kyanofenyl)(metylsulfonyl)metylén]azetidín, l-benzhydryl-3-[(3-karbamoylfenyl)(metylsulfonyl)metylén]-azetidín, l-benzhydryl-3-[(metylsulfonyl) (naft-l-yl) (metylsulfonyl)-metylén]azetidín,1-benzhydryl-3 - {[3,5-bis (trifluoromethyl) phenyl] (methylsulfonyl) methylene} azetidine, 1-benzhydryl-3 - [(3,5-dibromophenyl) (methylsulfonyl) methylene] azetidine, 1- benzhydryl-3 - [(3-methoxycarbonylphenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-cyanophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-carbamoylphenyl) ( methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(methylsulfonyl) (naphth-1-yl) (methylsulfonyl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl) -metylén]azetidín,1- [bis (4-chlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-[bis(4-metoxyfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1- [Bis (4-methoxyphenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-[bis(4-metylfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl) -metylén]azetidín, {RS)-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]-1-[(4-metoxyfenyl) (fenyl)metyl)]azetidín, (P)-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]-1-[(4-metoxyfenyl) (fenyl)metyl]azetidín, (S)-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]-1-[(4-metoxyfenyl)(fenyl)metyl]azetidín,1- [bis (4-methylphenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (RS) -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] - 1 - [(4-methoxyphenyl) (phenyl) methyl)] azetidine, (P) -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] -1 - [(4-methoxyphenyl) (phenyl) methyl] azetidine (S) -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] -1 - [(4-methoxyphenyl) (phenyl) methyl] azetidine, 1-[bis(4-trifluórmetoxyfenyl)metyl]-3-[(3,5-difluórfenyl)-(metylsulfonyl)metylén]azetidín,1- [bis (4-trifluoromethoxyphenyl) methyl] -3 - [(3,5-difluorophenyl) - (methylsulphonyl) methylene] azetidine, 1-[bis(4-trifluórmetylfenyl)metyl]-3-[(3,5-difluórfenyl)-(metylsulfonyl)metylén]azetidín, l-[bis(4-chlórfenyl)metyl]-3-{[3,5-bis(trifluórmetyl)-feny1]mety1sulfonylmetylén}azetidín, (FS)-1-[(4-chlórfenyl)(2,4-dichlórfenyl)metyl]-3-[(3,5-difluór fenyl)(metylsulfonyl)metylén]azetidín, (F)-1-[(4-chlórfenyl) (2,4-dichlórfenyl)metyl] -3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, (S)-1-[(4-chlórfenyl) (2,4-dichlórfenyl)metyl] - 3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, (FS)-1—{(4-chlórfenyl)[4-(hydroxymetyl)fenyl]metyl)-3- [ (3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, (F)-l-{(4-chlórfenyl)[4-(hydroxymetyl)fenyl]metyl)-3- [ (3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, (S)— 1—{(4-chlórfenyl)[4-(hydroxymetyl)fenyl]metyl}-3- [ (3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, (FS)-1-{(4-chlórfenyl)[4-(pyrolidinylmetyl)fenyl]metyl}-3- [ (3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, (F)-l-{(4-chlórfenyl) [4-(pyrolidinylmetyl)fenyl]metyl}-3- [ (3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, (S)-1{(4-chlórfenyl) [4-(pyrolidinylmetyl)fenyl]metyl}-3- [ (3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín,1- [bis (4-trifluoromethylphenyl) methyl] -3 - [(3,5-difluorophenyl) - (methylsulfonyl) methylene] azetidine, 1- [bis (4-chlorophenyl) methyl] -3 - {[3,5- bis (trifluoromethyl) phenyl] methylsulfonylmethylene} azetidine, (FS) -1 - [(4-chlorophenyl) (2,4-dichlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine (F) -1 - [(4-chlorophenyl) (2,4-dichlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (S) -1 - [(4- chlorophenyl) (2,4-dichlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (FS) -1 - {(4-chlorophenyl) [4- (hydroxymethyl) phenyl] methyl ) -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (F) -1 - {(4-chlorophenyl) [4- (hydroxymethyl) phenyl] methyl) -3 - [(3,5- (S) -1 - {(4-chlorophenyl) [4- (hydroxymethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, ( FS) -1 - {(4-chlorophenyl) [4- (pyrrolidinylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (F) -1 - {(4-chlorophenyl) ) [4- (pyrrolidinylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (S) -1 {(4-chlorophenyl) [4- (pyrrolidinylmethyl) phenyl] methyl} -3- [ (3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-(FS)-(4-chlórfenyl) [4-(3, 3-dimetylpiperidin-l-ylmetyl)65 fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]-azetidín,1- (FS) - (4-Chlorophenyl) [4- (3,3-dimethylpiperidin-1-ylmethyl) 65-phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1—{ (R)-(4-chlórfenyl) [4-(3,3-dimetylpiperid-l-ylmetyl)fenyl]-metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1 - {(R) - (4-chlorophenyl) [4- (3,3-dimethylpiperid-1-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1—{ (S)-(4-chlórfenyl) [4-(3,3-dimetylpiperid-l-ylmetyl)fenyl]-3-metyl}-3-[ (3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, l-{(RS)-(4-chlórfenyl)[4-(tiomorfolin-4-ylmetyl)fenyl]metyl}-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(R)-(4-chlórfenyl)[4-(tiomorfolin-4-ylmetyl)fenyl]metyl}-3-[(3, 5-difluórfenyl) (metylsulfonyl)metylén]azetidín,1 - {(S) - (4-chlorophenyl) [4- (3,3-dimethylpiperid-1-ylmethyl) phenyl] -3-methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine 1,1 - {(RS) - (4-chlorophenyl) [4- (thiomorpholin-4-ylmethyl) phenyl] methyl} - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(R) - (4-chlorophenyl) [4- (thiomorpholin-4-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1- {(S) - (4-chlórfenyl) [4 - (tiomorfolin-4-ylmetyl) fenyl]metyl} -3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(RS)-(4-chlórfenyl)[4-(N-etyl-N-cyklohexylaminometyl)fenyl]-metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(R)_(4-chlórfenyl)[4-(N-etyl-N-cyklohexylaminometyl)fenyl]-metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(S)-(4-chlórfenyl)[4-(N-etyl-N-cyklohexylaminometyl)fenyl]-metyl}-3-[(3, 5-difluórfenyl) (metylsulfonyl)metylén]azetidín, l-{{(RS)-(4-chlórfenyl)(4-[(4-etoxykarbonylpiperazinyl)metyl]-fenylJmetylJ J-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]-azetidín,1 - {(RS) - 1 - {(S) - (4-chlorophenyl) [4- (thiomorpholin-4-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] - (4-chlorophenyl) [4- (N-ethyl-N-cyclohexylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(R) _ (4 -chlorophenyl) [4- (N-ethyl-N-cyclohexylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(S) - (4-chlorophenyl) [4- (N-ethyl-N-cyclohexylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {{(RS) - (4-chlorophenyl) (4 - [(4-ethoxycarbonylpiperazinyl) methyl] -phenyl] methyl] -3- [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-{((R)-(4-chlórfenyl)(4-[(4-etoxykarbonylpiperazinyl)metyl]-fenylJmetyl) J J-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]-azetidín,1 - {((R) - (4-chlorophenyl) (4 - [(4-ethoxycarbonylpiperazinyl) methyl] phenyl) methyl) -N-3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1- { {[(S) - (4-chlórfenyl) {4- [ (4-etoxykarbonylpiperazinyl) metyl ] -fenylJmetylJ J-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]-azetidín, l-{(RS)-(4-chlórfenyl)[4-(N-cyklopropyl-N-propylaminometyl)661 - {{[(S) - (4-Chlorophenyl) {4 - [(4-ethoxycarbonylpiperazinyl) methyl] phenyl] methyl} -3- [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - { (RS) - (4-chlorophenyl) [4- (N-cyclopropyl-N-propylaminomethyl) 66 -fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]-azetidín,phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 —{(R)-(4-chlórfenyl)[4-(N-cyklopropyl-N-propylaminometyl)-fenyl]metyl}-3—[(3,5-difluórfenyl)(metylsulfonyl)metylén]-azetidín, l-{(S)-(4-chlórfenyl)[4-(N-cyklopropyl-N-propylaminometyl)-fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]-azetidín,1 - {(R) - (4-Chlorophenyl) [4- (N-cyclopropyl-N-propylaminomethyl) -phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1- {(S) - (4-chlorophenyl) [4- (N-cyclopropyl-N-propylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1—{(RS)-(4-chlórfenyl)[4-(diizopropylaminometyl)fenyl]metyl}-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, l-{(R)-(4-chlórfenyl)-[4-(diizopropylaminometyl)fenyl]metyl}-3-[(3, 5-difluórfenyl) (metylsulfonyl)metylén]azetidín,1 - {(RS) - (4-chlorophenyl) [4- (diisopropylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(R) - (4- chlorophenyl) - [4- (diisopropylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1- {(S)-(4-chlórfenyl)(4-(diizopropylaminometyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén)azetidín,1 - {(S) - (4-chlorophenyl) (4- (diisopropylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene) azetidine, 1-{((RS)-(4-chlórfenyl){4-[bis(2-metoxyetyl)aminometyl]fenyl}-metyl}}-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín,1 - {((RS) - (4-chlorophenyl) {4- [bis (2-methoxyethyl) aminomethyl] phenyl} methyl}} - 3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-{((R)-(4-chlórfenyl){4-[bis(2-metoxyetyl)aminometyl]fenyl}-metyl}}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1 - {((R) - (4-chlorophenyl) {4- [bis (2-methoxyethyl) aminomethyl] phenyl} methyl}} - 3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-{{(S)-(4-chlórfenyl){4-[bis(2-metoxyetyl)aminometyl]fenyl}-metyl}}-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín,1 - {{(S) - (4-chlorophenyl) {4- [bis (2-methoxyethyl) aminomethyl] phenyl} methyl}} - 3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-{(RS)-(4-chlórfenyl) [4-[di-n-propylaminometyl)fenyl]metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1 - {(RS) - (4-chlorophenyl) [4- [di-n-propylaminomethyl) phenyl] methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-{(R)-(4-chlórfenyl) [4-(di-n-propylaminometyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{ (S) - (4-chlórfenyl)[4-(di-n-propylaminometyl)fenyl] inetyl}-3 - [ (3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, l-{(RS)-(4-chlórfenyl) [4-(piperidin-l-ylmetyl)fenyl]metyl} -3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1 - {(R) - (4-chlorophenyl) [4- (di-n-propylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(S) - (4-chlorophenyl) [4- (di-n-propylaminomethyl) phenyl] ethyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(RS) - (4-chlorophenyl) [4- (piperidin-1-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-((R)-(4-chlórfenyl)[4-(piperidin-l-ylmetyl)fenyl]metyl)-3-[(3, 5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(S)-(4-chlórfenyl)[4-(piperidin-l-ylmetyl)fenyl]metyl}-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén] azetidín, l-{(RS)-(4-chlórfenyl)[4-(4-metylpiperazin-l-ylmetyl)fenyl]-metyl)-3- [(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(R)-(4-chlórfenyl)[4-(4-metylpiperazin-l-ylmetyl)fenyl]-metyl}-3-[ (3, 5-difluórfenyl) (metylsulfonyl)metylén]azetidín,1 - ((R) - (4-chlorophenyl) [4- (piperidin-1-ylmethyl) phenyl] methyl) -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(S) - (4-chlorophenyl) [4- (piperidin-1-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(RS) - (4-chlorophenyl) [4- (4-methylpiperazin-1-ylmethyl) phenyl] methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(R) - (4-chlorophenyl) [4- (4-Methylpiperazin-1-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 —{(S)-(4-chlórfenyl)[4-(4-metylpiperazin-l-ylmetyl)fenyl]-metyl)-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1 - {(S) - (4-chlorophenyl) [4- (4-methylpiperazin-1-ylmethyl) phenyl] methyl) -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-{(RS)-(4-chlórfenyl)[4-(morfolin-4-ylmetyl)fenyl]metyl·}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1 - {(RS) - (4-chlorophenyl) [4- (morpholin-4-ylmethyl) phenyl] methyl} · 3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-{(R)-(4-chlórfenyl)[4-(morfolin-4-ylmetyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(S)-(4-chlórfenyl)[4-(morfolin-4-ylmetyl)fenyl]metyl)-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1 - {(R) - (4-chlorophenyl) [4- (morpholin-4-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(S) - (4-chlorophenyl) [4- (morpholin-4-ylmethyl) phenyl] methyl) -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-{(RS)-(4-chlórfenyl)(4-(dietylaminometyl)fenyl]metyl}-3-[ (3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, l-{(R)-(4-chlórfenyl)[4-(dietylaminometyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín, l-{(S)-(4-chlórfenyl)[4-(dietylaminometyl)fenyl]metyl)-3-[ (3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín, l-{((RS)-(4-chlórfenyi)[4-(piperazin-2-on-4-ylmetyl)fenyl]metyl)-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidín,1 - {(RS) - (4-chlorophenyl) (4- (diethylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(R) - (4- chlorophenyl) [4- (diethylaminomethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(S) - (4-chlorophenyl) [4- (diethylaminomethyl) phenyl] methyl) -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {((RS) - (4-chlorophenyl) [4- (piperazin-2-on-4-ylmethyl) phenyl] methyl ) -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-{(R)-(4-chlórfenyl)[4-(piperazin-2-on-4-ylmetyl)fenyl]menyl} -3 - [, ( 3, 5-difluórfenyl) (metylsulfonyl) metylén] azetidín, l-{ (S)-(4-chlórfenyl) [4-(piperazin-2-on-4-ylmetyl)fenyl]metyl}1 - {(R) - (4-chlorophenyl) [4- (piperazin-2-one-4-ylmethyl) phenyl] phenyl} -3 - [, (3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(S) - (4-Chlorophenyl) [4- (piperazin-2-one-4-ylmethyl) phenyl] methyl} -3-[(3, 5-difluórfenyl) (metylsulfonyl)metylén]azetidin, l-{(RS)-(4-chlórfenyl) [4-(imidazol-l-ylmetyl)fenyl]metyl}-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidin, l-{(R)-(4-chlórfenyl)[4-(imidazol-l-ylmetyl)fenyl]metyl}-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidin, l-{(S)-(4-chlórfenyl)[4-(imidazol-l-ylmetyl)fenyl]metyl}-3-[(3, 5-difluórfenyl) (metylsulfonyl)metylén]azetidin, (RS)-l-{(4-chlórfenyl)[4-(N,N-dimetylkarbamoyl)fenyl]metyl}-3-[(3, 5-difluórfenyl) (metylsulfonyl)metylén]azetidin, (R) -l-{(4-chlórfenyl)[4-(N,N-dimetylkarbamoyl) fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén] azetidin, (S) —1—{(4-chlórfenyl)[4-(N,N-dimetylkarbamoyl)fenyl]metyl}-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidin, (RS)-l-((4-chlórfenyl)[4-(N-etylkarbamoyl)fenyl]metyl)}-3-[(3, 5-difluórfenyl) (metylsulfonyl)metylén]azetidin, (R) -l-{(4-chlórfenyl)[4-(N-etylkarbamoyl)fenyl]metyl}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidin, (S) -l-{(4-chlórfenyl)[4-(N-etylkarbamoyl)fenyl]mety}-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidin, (RS) -1-[(4-karbamoylfenyl) (4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)metylén]azetidin, (R) -1-[(4-karbamoylfenyl)(4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidin, (S) -1-[(4-karbamoylfenyl)(4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl )(metylsulfonyl)metylén]azetidin,-3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(RS) - (4-chlorophenyl) [4- (imidazol-1-ylmethyl) phenyl] methyl} -3 - [(3 5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1 - {(R) - (4-chlorophenyl) [4- (imidazol-1-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) ( methylsulfonyl) methylene] azetidine, 1 - {(S) - (4-chlorophenyl) [4- (imidazol-1-ylmethyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (RS) -1 - {(4-chlorophenyl) [4- (N, N-dimethylcarbamoyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (R) -1- {(4-chlorophenyl) [4- (N, N-dimethylcarbamoyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (S) -1 - {(4-chlorophenyl) [4- (N, N-dimethylcarbamoyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (RS) -1 - ((4-chlorophenyl) [4- (N- ethylcarbamoyl) phenyl] methyl)} - 3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (R) -1 - {(4-chlorophenyl) [4- (N-ethylcarbamoyl) phenyl] methyl} - 3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (S) -1 - {(4-chlorophenyl) [4- (N-ethylcarbamoyl) phenyl] methyl} -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (RS) -1 - [(4-carbamoylphenyl) ( 4-chlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (R) -1 - [(4-carbamoylphenyl) (4-chlorophenyl) methyl] -3 - [(3, 5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (S) -1 - [(4-carbamoylphenyl) (4-chlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-((3,5-dichlórfenyl)(metylsulfonyl) -metylén]azetidin, l-benzhydryl-3-[(3-metylsulfanylfenyl)(metylsulfonyi)metylén]-azetidín, l-benzhydryl-3-[(3-metylsulfanylmetyl) fenyl) ] (metylsulfonyi)-metylén)azetidín,1- [bis (4-chlorophenyl) methyl] -3 - ((3,5-dichlorophenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-methylsulfanylphenyl) (methylsulfonyl) methylene] azetidine, 1-benzhydryl-3 - [(3-methylsulfanylmethyl) phenyl)] (methylsulfonyl) methylene) azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(3-kyanofenyl)(metylsulfonyi)-metylén]azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - [(3-cyanophenyl) (methylsulfonyl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(3-karbamoylfenyl)(metylsulfonyi)-metylén]azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - [(3-carbamoyl-phenyl) (methylsulfonyl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(3-metoxyfenyl)(metylsulfonyi)-metylén]azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - [(3-methoxyphenyl) (methylsulfonyl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(3-hydroxyfenyl)(metylsulfonyi)-metylén]azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - [(3-hydroxyphenyl) (methylsulfonyl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(metylsulfonyi)(3-pyrolidinylfenyl)metylén]azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - [(methylsulfonyl) (3-pyrrolidinylphenyl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(3-hydroxymetylfenyl)(metylsulf onyl) metylén]azetidín,1- [bis (4-chlorophenyl) methyl] -3 - [(3-hydroxymethylphenyl) (methylsulfonyl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-{(metylsulfonyi)[3-(N-piperidylkarbamoyl)fenyl]metylén]azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - {(methylsulfonyl) [3- (N-piperidylcarbamoyl) phenyl] methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(metylsulfonyi)(3-trifluórmetylsulfanylfenyl)(metylsulfonyi)metylén]azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - [(methylsulfonyl) (3-trifluoromethylsulfanylphenyl) (methylsulfonyl) methylene] azetidine, 1-[bis(4-fluórfenyl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyi)-metylén]azetidín,1- [bis (4-fluorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1- [bis (2-fluórfenyl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyi)-metylén]azetidín,1- [bis (2-fluorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-[bis(3-fluórfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyi)-metylén]azetidín, (RS)!-1- [ (4-chlórfenyl) (tiazol-2-yl) metyl] -3- [ (metylsulfonyi) 701- [bis (3-fluorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, (RS) ! -1 - [(4-chlorophenyl) (thiazol-2-yl) methyl] -3 - [(methylsulfonyl) 70] -(fenyl)metylén]azetidín, (F)-1-[(4-chlórfenyl)(tiazol-2-yl)metyl]-3-[(metylsulfonyl)-(fenyl)metylén]azetidín, (S) -l-[(4-chlórfenyl) (tiazol-2-yl)metyl]-3- [ (metylsulfonyl) -(fenyl)metylén]azetidín, (FS)-1-[(4-chlórfenyl)(tien-2-yl)metyl]-3-[(3,5-difluórfenyl)-(metylsulfonyl)metylén]azetidín, (F)-1-[(4-chlórfenyl)(tieň-2-yl)metyl]-3-[(3,5-dífluórfenyl)-(metylsulfonyl)metylén]azetidín, (S)-1-[(4-chlórfenyl)(tíen-2-yl)metyl]-3-[(3,5-difluórfenyl)-(metylsulfonyl)metylén]azetidín, l-benzhydryl-3-[(etylsulfonyl)(fenyl)metylén]azetidín,- (phenyl) methylene] azetidine, (F) -1 - [(4-chlorophenyl) (thiazol-2-yl) methyl] -3 - [(methylsulfonyl) - (phenyl) methylene] azetidine, (S) -1- [(4-chlorophenyl) (thiazol-2-yl) methyl] -3 - [(methylsulfonyl) - (phenyl) methylene] azetidine, (FS) -1 - [(4-chlorophenyl) (thien-2-yl) methyl 3 - [(3,5-difluorophenyl) - (methylsulfonyl) methylene] azetidine, (F) -1 - [(4-chlorophenyl) (shadow-2-yl) methyl] -3 - [(3,5- difluorophenyl) - (methylsulfonyl) methylene] azetidine, (S) -1 - [(4-chlorophenyl) (thien-2-yl) methyl] -3 - [(3,5-difluorophenyl) - (methylsulfonyl) methylene] azetidine, l-benzhydryl-3 - [(ethylsulfonyl) (phenyl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]—3—{{3—[N—(4-metylpiperazinyl)-karbamoyl]fenyl](metylsulfonyl)metylén}azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - {{3- [N- (4-methylpiperazinyl) carbamoyl] phenyl] (methylsulfonyl) methylene} azetidine, 1- [bis (4-chlórfenyl)metyl]-3-{[3-(2,2-dimetylkarbohydrazido)-fenyl](metylsulfonyl)metylén}azetidín,1- [bis (4-chlorophenyl) methyl] -3 - {[3- (2,2-dimethylcarbohydrazido) phenyl] (methylsulfonyl) methylene} azetidine, 1- [bis(tieň-2-yl)metyl]-3-[(3, 5-difluórfenyl) (metylsulfonyl)-metylén]azetidín,1- [bis (shadow-2-yl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1-[bis(p-tolyl)metyl]-3-[(metylsulfonyl)(fenyl)metylén]azetidín,1- [bis (p-tolyl) methyl] -3 - [(methylsulfonyl) (phenyl) methylene] azetidine, 1- [ (4-chlórfenyl) (4-hydroxymetylfenyl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyl)metylén]azetidín,1 - [(4-chlorophenyl) (4-hydroxymethylphenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, 1- [bis (4-chlórfenyl)metyl]-3-[(3-metylaminofenyl) (metylsulf onyl) metylén] azetidín, (FS)-1-[(4-chlórfenyl) (tiazol-2-yl)metyl]-3-[(3,5-difluórfenyl)-(metylsulfonyl)metylén]azetidín, (F) -1- [ (4-chlórfenyl) (tiazol-2-y1)metyl]-3-[(3,5-difluórfenyl)71 (S)-1-[(4-chlórfenyl)(tiazol-2-y1)metyl]-3-[(3,5-difluórfenyl)1- [bis (4-chlorophenyl) methyl] -3 - [(3-methylaminophenyl) (methylsulfonyl) methylene] azetidine, (FS) -1 - [(4-chlorophenyl) (thiazol-2-yl) methyl] - 3 - [(3,5-difluorophenyl) - (methylsulfonyl) methylene] azetidine, (F) -1 - [(4-chlorophenyl) (thiazol-2-yl) methyl] -3 - [(3,5-difluorophenyl) 71 (S) -1 - [(4-chlorophenyl) (thiazol-2-yl) methyl] -3 - [(3,5-difluorophenyl) -(metylsulfonyl)metylén]azetidín,- (methylsulfonyl) methylene] azetidine, -(metylsulfonyl)metylén]azetidín,- (methylsulfonyl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(metylsulfonyl)(2-metoxykarbonyl tieň-5-yl)metylén]azetidín, (RS)-1-[[bis(4-chlórfenyl)metyl]-3-hydroxy-3-[(metylsulfonyl)-(2-metoxykarbonyltien-5-yl)metyl]azetidín,1- [bis (4-chlorophenyl) methyl] -3 - [(methylsulfonyl) (2-methoxycarbonyl shadow-5-yl) methylene] azetidine, (RS) -1 - [[bis (4-chlorophenyl) methyl] -3 hydroxy-3 - [(methylsulfonyl) - (2-methoxycarbonylthien-5-yl) methyl] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(2-izobutylaminokarbonyltien-5-yl)(metylsulfonyl)metylén]azetidín,1- [Bis (4-chlorophenyl) methyl] -3 - [(2-izobutylaminokarbonyltien-5-yl) (methylsulfonyl) methylene] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(3-metoxykarbonylfenyl)(metylsulfonyl) metyl- (RS)]azetidin-3-ol,1- [bis (4-chlorophenyl) methyl] -3 - [(3-methoxycarbonylphenyl) (methylsulfonyl) methyl- (RS)] azetidin-3-ol, 1-[bis(4-chlórfenyl) metyl]-3-[(metylsulfonyl) (pyrid-4-yl)-metyl-(RS)]azetidin-3-ol,1- [bis (4-chlorophenyl) methyl] -3 - [(methylsulfonyl) (pyrid-4-yl) methyl (RS)] azetidin-3-ol, 1-[(bis(4-chlórfenyl)metyl]-3-[(metylsulfonyl)(pyrid-3-yl)-metyl-(RS)]azetidin-3-ol,1 - [(bis (4-chlorophenyl) methyl] -3 - [(methylsulphonyl) (pyridin-3-yl) methyl- (RS)] azetidin-3-ol, 3 - ({1- [bis (4-chlórfenyl) mety l]azet idin-3-ylidén} metánsul f onylmetyl) -N-(3-morfolin-4-ylpropyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -N- (3-morpholin-4-ylpropyl) benzamide, 3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-y1idén}metánsulfonylmetyl) -N-(3-dimetylaminopropyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -N- (3-dimethylaminopropyl) benzamide, 3 - ((1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén[metánsulfonylmetyl) -N-(2-(pyrolidin-l-yl)etyl)benzamid,3 - ((1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene [methanesulfonylmethyl) -N- (2- (pyrrolidin-1-yl) ethyl) benzamide), 3-((1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfonylmetyl)-N-(2-dimetylamino-1-metylety1)benzamid,3 - ((1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -N- (2-dimethylamino-1-1methylethyl) benzamide, 3- ({,1- [bis (4-chlórfenyl)metyl] azetidin-3-ylidén)metánsulfonylmetyl)-N-(piperidin-l-yl)benzamid,3- ({, 1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene) methanesulfonylmethyl) -N- (piperidin-1-yl) benzamide, II 3 - ((Ť-[bis(4-chlórfenyl)metyl]azetidin-3-y1idén}metánsulfonylmetyl) -N-izobutylbenzamid,3 - ((N - [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -N-isobutylbenzamide, 3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfonyl metyl) -N-(3-imidazol-l-ylpropyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -N- (3-imidazol-1-ylpropyl) benzamide, 3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén Jmetánsulfonyl metyl) -N-(2-dimetylaminoetyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene) methanesulfonylmethyl) -N- (2-dimethylaminoethyl) benzamide, N'-metylhydrazid kyseliny 3-({l-[bis(4-chlórfenyl)metyl]-azetidin-3-ylidénJmetánsulfonylmetyl)benzoovej,3 - ({1- [Bis (4-Chloro-phenyl) -methyl] -azetidin-3-ylidene] -methanesulfonylmethyl) -benzoic acid N'-methylhydrazide, 3-({1-[bis(4-chlórfenyl)metylazetidin-3-ylidénJmetánsulfonylmetyl)-N-(2-morfolin-4-yletyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl-azetidin-3-ylidénJmetánsulfonylmetyl) -N- (2-morpholin-4-yl-ethyl) -benzamide, 3-({1-bis(4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfonylmetyl)-N-(1-etylpyrolidin-2-ylmetyl)benzamid,3 - ({1-bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -N- (1-ethyl-pyrrolidin-2-ylmethyl) -benzamide, 3-({1-(bis(4-chlórfenyl)metyl]azetidin-3-ylidén Jmetánsulfonyl metyl)-N-(2,2-dimetylpropyl)benzamid,3 - ({1- (bis (4-chlorophenyl) methyl) azetidin-3-ylidene) methanesulfonylmethyl) -N- (2,2-dimethylpropyl) benzamide, 3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfonyl metyl)-N-(cyklohexylmetyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) -N- (cyclohexylmethyl) benzamide, 3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidénJmetánsulfonyl metyl) -N-(cyklopropylmetyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene) methanesulfonylmethyl) -N- (cyclopropylmethyl) benzamide, 3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén Jmetánsulfonyl metyl)-N-(2-metylbutyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene) methanesulfonylmethyl) -N- (2-methylbutyl) benzamide, 3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidénJmetánsulfonyl metyl)-N-(2-fenylpropyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene) methanesulfonylmethyl) -N- (2-phenylpropyl) benzamide, 3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén Jmetánsulfonyl metylJ-N-(tetrahydrofurán-2-ylmetylJ benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene) methanesulfonylmethyl] -N- (tetrahydrofuran-2-ylmethyl) benzamide, 3-({1-[bis(4-chlórfenyl) metyl]azetidin-3-ylidén Jmetánsulfonyl metyl)-N-(2,2-difenyletyl)benzamid,3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene) methanesulfonylmethyl) -N- (2,2-diphenylethyl) benzamide, 3-({1-[bis(4-chlórfenyl·)metyl]azetidin-3-ylidénJmetánsulfonyl metyl)-N-(2-etylbutyl)benzamid, metylester kyseliny 4-{[3-({1-[bis(4-chlórfenyl)metyl]133 - ({1- [bis (4-chlorophenyl)) methyl] azetidin-3-ylidene] methanesulfonylmethyl) -N- (2-ethylbutyl) benzamide, 4 - {[3 - ({1- [bis (4- chlorophenyl) methyl] 13 I iI i azetidin-3-ylidén}metánsulfonylmetyl)benzoylamino]metyl}iazetidin-3-ylidene} methanesulfonylmethyl) -benzoylamino] -methyl} i -cyklohexánkarboxylovej,-cyclohexanecarboxylic 2-amino-1- {4-(3-({l-[bis(4-chlórfenyl·) metyI]a zetidin-3-y1idén}-metánsulfonylmetyl)fenyl]piperazin-l-yl[etanón, terc-butylester kyseliny (2-{4-[3-({1-[bis(4-chlórfenyl)metyl] azetidin-3-ylidén}metánsulfonylmetyl)fenyl]piperazin-l-yl}-2-oxoetyl)karbamovej,2-Amino-1- {4- (3 - ({1- [bis (4-chlorophenyl)) methyl] and zetidin-3-ylidene} -methanesulfonylmethyl) phenyl] piperazin-1-yl [ethanone, tert-butyl ester (2- {4- [3 - ({1- [Bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) phenyl] piperazin-1-yl} -2-oxoethyl) carbamic acid, 1-{4-[3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-y1idén}metánsulf ony lmetyl )fenyl]piperazin-l-yl}-2-metylaminoetanón, terc-butylester kyseliny (2-{4-[3-({1-[bis(4-chlórfenyl)mezyl] -azetidin-3-ylidén}metánsulfonylmetyl)fenyl]piperazin-l-yl} -2-oxoetyl)-N-metylkarbamovej,1- {4- [3 - ({1- [Bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) phenyl] piperazin-1-yl} -2-methylaminoethanone, tert-butyl ester (2) - {4- [3 - ({1- [Bis (4-chlorophenyl) mesyl] -azetidin-3-ylidene} methanesulfonylmethyl) phenyl] piperazin-1-yl} -2-oxoethyl) -N-methylcarbamic acid, N-metylamid kyseliny 4-[3-({[l-bis(4-chlórfenyl)metyl]-azetidin-3-y1idén[metánsulfonylmetyl)fenyl]piperazín-l-karbotioovej,4- [3 - ({[1-Bis (4-chlorophenyl) methyl] azetidin-3-ylidene [methanesulfonylmethyl) phenyl] piperazine-1-carbothioic acid N-methylamide, N-metylamid kyseliny 4-[3-({1-[bis(4-chlórfenyl)metyl]-azetidin-3-y1idén[metánsulfonyl)metylfenyl]piperazín-1-karboxylovej, metylester kyseliny 4-[3-({l-[bis(4-chlórfenyl)metyl]-azetidin-3-ylidén[metánsulfonylmetyl)fenyl]piperazín-1-karboxylovej, l-[3-({l-[bis(4-chlórfenyl) metyl] azetidin-3-y1idénJmetánsulfonylmetyl)fenyl]-4-izobutylpiperazín, l-[3-({l-[bis(4-chlórfenyl)metyl] azetidin-3-y1idén[metánsulfonylmetyl)fenyl]-4-etylpiperazín,4- [3 - ({1- [Bis (4-chlorophenyl) methyl] azetidin-3-ylidene [methanesulfonyl) methylphenyl] piperazine-1-carboxylic acid N-methylamide, methyl 4- [3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene [methanesulfonylmethyl) phenyl] piperazine-1-carboxylic acid, 1- [3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene] methanesulfonylmethyl) phenyl] -4-isobutylpiperazine, 1- [3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene [methanesulfonylmethyl) phenyl] -4-ethylpiperazine, II 4-acetyl-1-[3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}I4-Acetyl-1- [3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} I -metánsulfonylmetyl)fenyl] piperazín,-methanesulfonylmethyl) phenyl] piperazine II I l-{ 4,- [3- ({1- [bis (4-chlórfenyl) metyl ] a ze t idin-3-y 1 idén [metán74 sulfonylmetyl)fenyl]piperazin-l-yl]-2-dímetylaminoetanón,11- {4, - [3 - ({1- [bis (4-chlorophenyl) methyl] and zolidin-3-ylidene [methan74 sulfonylmethyl) phenyl] piperazin-1-yl] -2-dimethylaminoethanone, 1-[3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-ylidén}metánsulfonylmetyl) fenyl]piperazin, terc-butylester kyseliny 4-[3-({1-[bis(4-chlórfenyl)metyl]azetidin-3-y1idén}metánsulfonylmetyl)fenyl]piperazín-1-karboxylovej,4- [3 - ({1- [bis (4-chlorophenyl)] - tert -butyl ester 1- [3 - ({1- [bis (4-chlorophenyl) methyl] azetidin-3-ylidene} methanesulfonylmethyl) phenyl] piperazine methyl] azetidin-3-methanesulfonylmethyl y1idén}) phenyl] piperazine-1-carboxylic acid, 1-[bis(4-metoxykarbonylfenyl)metyl]-3-[(3,5-difluórfenyl)-(metylsulfonyl)metylén]azetidín,1- [Bis (4-methoxycarbonylphenyl) methyl] -3 - [(3,5-difluorophenyl) - (methylsulphonyl) methylene] azetidine, 3- acetoxy-l-[bis(4-metoxykarbonylfenyl)metyl]-3-[(3,5-difluórfenyl)(metylsulfonyl)metyl-(RS)]azetidín, (RS)-4-[4-((4-chlórfenyl){3-[(3,5-difluórfenyl)metánsulfonylmetylén]azetidin-1-yl)metyl)benzyl]morfolín,3-Acetoxy-1- [bis (4-methoxycarbonylphenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methyl- (RS)] azetidine, (RS) -4- [4 - ((4- chlorophenyl) {3 - [(3,5-difluorophenyl) metánsulfonylmetylén] azetidin-1-yl) methyl) benzyl] morpholine, 4- (4-{3-[(l-benzhydrylazetidin-3-ylidén)metánsulfonylmetyl]-fenoxy)butyl)morfolín,4- (4- {3 - [(1-benzhydrylazetidin-3-ylidene) methanesulfonylmethyl] -phenoxy) butyl) morpholine, 4-(4-{3-[(l-benzhydrylazetidin-3-ylidén)metánsulfonylmetyl]-fenoxy}propyl)morfolín,4- (4- {3 - [(l-benzhydryl-azetidin-3-ylidene) methanesulfonylmethyl] phenoxy} propyl) morpholine, N-(1-[bis(4-chlórfenyl)metyl]azetidin-3-y1}tien-2-ylsulfónamid,N- (1- [bis (4-chlorophenyl) methyl] azetidin-3-y1} thien-2-ylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-4-metoxyfenylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -4-Methoxyphenylsulfonyl-, N-[4-(N-[l-[bis(4-chlórfenyl)metyl]azetidin-3-yl}sulfamoyl)-fenyl]acetamid,N- [4- (N- [l- [bis (4-chlorophenyl) methyl] azetidin-3-yl} sulfamoyl) phenyl] acetamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl)-4-metylfenylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl) -4-methylphenylsulfonamido, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-y1}-3,4-dimetoxyfenyl sulf ónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3,4-dimethoxyphenyl sulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidín-3-yl}-3-fluórfenylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3-fluorophenylsulfonamido, N-{1η[bis(4-chlórfenyl)metyl]azetidin-3-yl}-3,4-dichlórfenylI sulfónamid,N- {1η [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3,4-dichlorophenyl sulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-3-kyanofenylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3-kyanofenylsulfónamid, N-{1- [bis(4-chlórfenyl)metyl]azetidin-3-yl}-2,5-dimetoxyfenylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -2,5-dimethoxyphenylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-3-trifiuórmetylfenylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3-trifiuórmetylfenylsulfónamid, N-(1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}naft-2-ylsulfónamid,N- (1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} naphth-2-ylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}naft-1-ylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} naphth-1-ylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-3, 4-difluórfenylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3,4-difluorophenylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-1-metyl-1H-imidazol-4-yisulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -1-methyl-1H-imidazol-4-yisulfónamid, N-[4-(N-{l-[bis(4-chlórfenyl)metyl]azetidin-3-yl}sulfamoyl)-2-chlórfenyl]acetamid,N- [4- (N- {l- [bis (4-chlorophenyl) methyl] azetidin-3-yl} sulfamoyl) -2- chlorophenyl] acetamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}pyrid-3-ylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} pyrid-3-ylsulfonamide, N-{1-[bis(4-chlórfenyimetyl]azetidin-3-yl}-4-fluórfenylsulfónamid,N- {1- [bis (4-chlórfenyimetyl] azetidin-3-yl} -4-fluorophenylsulfonamido, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}chino1-8-ylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} chino1-8-ylsulfonamide, N-(1- [bis(4-chlórfenyl)metyl]azetidin-3-yl}fenylsulfónamid,N- (1- [bis (4-chlorophenyl) methyl] azetidin-3-yl) phenylsulfonamide, N-(1-[bis(4-chlórfenyl)metyl]azetidin-3-yl)(fenylmetyl)-sulfónamid,N- (1- [bis (4-chlorophenyl) methyl] azetidin-3-yl) (phenylmethyl) sulfonamide, II N-{ly[bis(4-chlórfenyl)metyl]azetidin-3-yl}-3,5-difluórfenyli sulfónamid,N- {γ [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3,5-difluorophenyl sulfonamide, N-{1- [bis(4-chlórfenyl)metyl]azetidin-3-yl}pyrid-2-ylsulfónamid,N- {1- [bis (4-chloro-phenyl) -methyl] -azetidin-3-yl} -pyrid-2-ylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-(3-fluór-5-pyrolidin-1-ylfenyl)sulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} - (3-fluoro-5-pyrrolidin-1-yl-phenyl) sulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-metyl-4-fluórfenyl sulf ónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N-methyl-4-fluorophenyl sulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-mety1chinol-8-y1sulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N-mety1chinol-8-y1sulfónamid, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl]-N-metylfeny1sulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl] -N-metylfeny1sulfónamid, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl)-N-metyl(fenylmetyl)-sulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl) -N-methyl (phenylmethyl) sulfonamide, N-{1- [bis(4-chlórfenyl)metyl]azetidin-3-yl}-3-sulfamoylfenyisulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3-sulfamoylphenyisulfonamide, 2-benzénsulfonyl-N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-acetamid,2-benzenesulfonyl-N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -acetamide, N-{1- [bis(4-chlórfenyl)metyl]azetidin-3-yl}-2-[4-toluén-4-sulfonyl)acetamid, (3-chlór-4-metylsuifonyltiofén-2-karboxy)-{1-[bis(4-chlórfenyl)-metyl]azetidin-3-yl]amid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -2- [4-toluene-4-sulfonyl) acetamide, (3-chloro-4-methylsulfonylthiophene-2-carboxy) - {1 - [bis (4-chlorophenyl) methyl] azetidin-3-yl] -amide, N-{1- [bis (4-chlórfenyl)metyl]azetidin-3-yl}-3-(2-fenyletylénsulfonyl)propiónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -3- (2-phenylethylenesulfonyl) propionamide, N-{1- [bis(4-chlórfenyl)metyl]azetidin-3-yl}-4-metylsulfonylbenzamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -4-methylsulfonylbenzamide, N-{1- [bis(4-chlórfenyl)metyl]azetidin-3-yl}-4-metánsulfonylbenzamid, (5-metylsulfonyltiofén-2-karboxy) -{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl]amid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -4-methanesulfonylbenzamide, (5-methylsulfonylthiophene-2-carboxy) - {1- [bis (4-chlorophenyl) methyl] azetidin-3 yl] -amide, II I , ηΊ ιI η Ί ι (5-metylsul·fony1-3-metyl-4-vinyitiofén-2-karboxy) -{l-[ [bis(4-chlórfenylJmetyl]azetidin-3-yl}amid, (RS)-N-{1-[(4-chlórfenyl)pyridín-3-ylmetyl]azetidín-3-yl}-3,5-difluórbenzénsulfónamid, (RS)-N-{1- [ (4-chlórfenyl)pyrimidin-5-ylmetyl]azetidin-3-yl}-3,5-difluórbenzensulfónamid,(RS) -N- {1 - [(5-Methylsulfonyl-3-methyl-4-vinylthiophene-2-carboxy) - {1 - [[bis (4-chlorophenyl) methyl] azetidin-3-yl} amide] 4-Chlorophenyl) pyridin-3-ylmethyl] azetidin-3-yl} -3,5-difluorobenzenesulfonamide, (RS) -N- {1 - [(4-chlorophenyl) pyrimidin-5-ylmethyl] azetidin-3-yl} -3,5-difluoro-benzenesulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidín-3-yl}-N-(6-chlórpyrid-2-y1)metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (6-chloropyrid-2-y1) methylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(6-etylpyrid-2-yl)metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (6-ethyl-pyridin-2-yl) methylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-chinol-6-ylmetylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N-quinol-6-ylmetylsulfónamid, N-[1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-chinol-5-ylmetylsulfónamid,N- [1- [Bis (4-chlorophenyl) methyl] azetidin-3-yl} -N-quinol-5-ylmetylsulfónamid, N-{1-[bis(4-chlórfenyl)metyl]azetídin-3-yl}-N-izochinol-5-ylmetylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N-isoquinolin-5-ylmetylsulfónamid, N-{1-[bis(4-chlórfenyl)metyl]azetidín-3-y1}-N-pyrid-3-ylmetylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-y1} -N-pyrid-3-ylmetylsulfónamid, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(pyrid-l-oxid-3-y1)metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (pyrid-l-oxide-3-y1) methyl sulfonamide, N- (ÍR, 2S,4 S)-bicyklo[2,2,1]hept-2-yl-N-{1-[bis-(4-chlórfenyl)-metyl]azetidin-3-yl}metylsulfónamid,N- (1R, 2S, 4S) -bicyclo [2.2.1] hept-2-yl-N- {1- [bis- (4-chloro-phenyl) -methyl] -azetidin-3-yl} -methylsulfonamide, N- (ÍR, 2R,4S)-(bicyklo[2,2,1]hept-2-yl)-N-{1-(bis-(4-chlórfenyl)-metyl]azetidín-3-y1}metylsulfónamid, N- (1R, 2R, 4S) - (Bicyclo [2.2.1] hept-2-yl) -N- {1- (bis- (4-chloro-phenyl) -methyl] -azetidin-3-yl} -methylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(3,5-difluórfenyl·) metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide, N- {l1— [bis (4-chlórfenyl) metyl] azetidín-3-y 1) - N- (tiazol-2-yl) 78N- {l 1 - [bis (4-chlorophenyl) methyl] azetidin-3-y1) - N- (thiazol-2-yl) 78 -metylsulfónamid,methylsulphonamide. N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(3-metoxyfenyl)-metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (3-methoxyphenyl) methylsulphonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidín-3-yl}-N-(3-hydroxyfenyl)-metylsulfónamid, .N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (3-hydroxyphenyl) methylsulfonamide,. N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(3-hydroxymetylfenyl)metylsulfónamid, etyl-N-(1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(metylsulfonyl) -3-aminobenzoát,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (3-hydroxymethylphenyl) methylsulfonamide, ethyl N- (1- [bis (4-chlorophenyl) methyl] azetidin-3- yl} -N- (methylsulfonyl) -3-aminobenzoate, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl]-N-(izobutylpiperid-4-yl)metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl] -N- (izobutylpiperid-4-yl) methylsulfonamide, N-benzyl-N-{ 1- [bis (4-chlórfenyl) metyl]azetidin-3-yl [amín,N-benzyl-N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl [amine, N-{1-[bis (4-chlórfenyl)metyl]azetidín-3-yl}-N-(3,5-difluórbenzyl)amín,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (3,5-difluorobenzyl) amine, N-{1-[bis(4-chlórfenyl)metyl]azetidín-3-yl}-N-(3,5-difluórbenzyl)metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (3,5-difluorobenzyl) methylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidín-3-yl}-N-(pyrid-3-ylmetyl) -metylsulfónamid,N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (pyrid-3-ylmethyl) methylsulfonamide, N-{1-[bis(4-fluórfenyl)metyl]azetidín-3-yl}-N-(3,5-difluórfenyl) metylsulfónamid, (RS)-N-{1-[(4-chlórfenyl) pyrid-3-ylmety1]azetidin-3-yl}-N-(3,5-difluórfenyl)metylsulfónamid, (R) -N-{1-[(4-chlórfenyl)pyrid-3-ylmetyl]azetidín-3-yl}-N-(3,5-difluórfenyl)metylsulfónamid, (S) -N-{1-[(4-chlórfenyl)pyrid-3-ylmetyl]azetidin-3-yl}-N- (3,5-difluórfenyl)metylsulfónamid, (RS)i-N-{ 1- [ (4-chlórfenyl) pyrid-4-ylmetyl] a zet idin-3-yl} -NIN- {1- [bis (4-fluorophenyl) methyl] azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide, (RS) -N- {1 - [(4-chlorophenyl) pyrid-3 -ylmethyl] azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide, (R) -N- {1 - [(4-chlorophenyl) pyrid-3-ylmethyl] azetidin-3-yl} -N - (3,5-difluorophenyl) methylsulfonamide, (S) -N- {1 - [(4-chlorophenyl) pyrid-3-ylmethyl] azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide, ( RS) N - {1 - [(4-chlorophenyl) pyrid-4-ylmethyl] and zetidin-3-yl} -NI - (3,'5-dif luórfenyl) met ylsul f ónamid,- (3,5-difluorophenyl) methylsulfonamide, I (R) -N-(1-[(4-chlórfenyl)pyrid-4-ylmetyl]azetidin-3-yl)-N-(3,5-difluórfenyl)metylsulfónamid, (S) -N - {1- [(4-chlórfenyl)pyrid-4-ylmetyl]azetidin-3-yl}-N-(3, 5-difluórfenyl)metylsulfónamid, (RS)-N-{1-[(4-chlórfenyl)pyrimidin-5-ylmetyl]azetidin-3-yl}-N-(3,5-difluórfenyl)metylsulfónamid, (R) -N-{1-[(4-chlórfenyl)pyrimidin-5-ylmetyl]azetidin-3-yl}-N-(3,5-difluórfenyl)metylsulfónamid, (S) -N-{1-[(4-chlórfenyl)pyrimidin-5-ylmetyl]azetidin-3-yl} -N-(3, 5-difluórfenyl)metylsulfónamid,(R) -N- (1 - [(4-chlorophenyl) pyrid-4-ylmethyl] azetidin-3-yl) -N- (3,5-difluorophenyl) methylsulfonamide, (S) -N - {1- [ (4-chlorophenyl) pyrid-4-ylmethyl] azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide, (RS) -N- {1 - [(4-chlorophenyl) pyrimidin-5-ylmethyl] (R) -N- {1 - [(4-chlorophenyl) pyrimidin-5-ylmethyl] azetidin-3-yl} -N- (3) azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide (S) -N- {1 - [(4-chlorophenyl) pyrimidin-5-ylmethyl] azetidin-3-yl} -N- (3,5-difluorophenyl) methylsulfonamide, 5-difluorophenyl) methylsulfonamide, N-{1-[bis(4-chlórfenyl)metyl]azetidin-3-yl}-N-(3,5-difluórfenyl ) benzy lsulf ónamid, ich optické izoméry a ich farmaceutický prijatelné soli.N- {1- [bis (4-chlorophenyl) methyl] azetidin-3-yl} -N- (3,5-difluorophenyl) benzylsulfonamide, their optical isomers and their pharmaceutically acceptable salts. 9. Farmaceutická kompozícia podlá nároku 7, vyznačujúca sa t ý m, že sa pre ňu zlúčenina všeobecného vzorca I vyberie zo skupiny, ktorú tvoria nasledovné zlúčeniny:Pharmaceutical composition according to claim 7, characterized in that the compound of the formula I is selected from the group consisting of the following compounds: 1-[bis(4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyl)metyl-(RS)]azetidin-3-ol,1- [bis (4-chlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methyl- (RS)] azetidin-3-ol, 3-acetoxy-l-[bis(4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl)-(metylsulfonyl)metyl)metylsulfonylmetyl-(RS)]azetidín,3-acetoxy-l- [bis (4-chlorophenyl) methyl] -3 - [(3,5-difluorophenyl) - (methylsulfonyl) methyl) methylsulfonylmethyl (RS)] azetidine, 1-[bis(4-chlórfenyl)metyl]-3-[(3,5-difluórfenyl) (metylsulfonyl)-metylén]azetidín,1- [bis (4-chlorophenyl) methyl] -3 - [(3,5-difluorophenyl) (methylsulfonyl) methylene] azetidine, I ichjoptické izoméry a ich farmaceutický prijatelné soli.Ijoptical isomers and pharmaceutically acceptable salts thereof. II 10. Farmaceutická kompozícia podľa nároku 6, vyznaču80 júca sa tým, že antagonista CB1 je SR141716, jeho hydráty a farmaceutický prijateľné soli alebo LY320135 a jeho farmaceutický prijateľné solí.The pharmaceutical composition of claim 6, wherein the CB1 antagonist is SR141716, hydrates thereof, and pharmaceutically acceptable salts thereof, or LY320135, and pharmaceutically acceptable salts thereof. 11. Farmaceutická kompozícia podlá jedného z nárokov 6 až 10 na súčasné, oddelené alebo postupné použitie.Pharmaceutical composition according to one of claims 6 to 10 for simultaneous, separate or sequential use. 12. Farmaceutická kompozícia podľa jedného z nárokov 6 až 11, vyznačujúca sa tým, že obsahuje 0,5 mg sibutramínu a 0,1 až 200 mg antagonistu CB1.Pharmaceutical composition according to one of Claims 6 to 11, characterized in that it contains 0.5 mg of sibutramine and 0.1 to 200 mg of the CB1 antagonist.
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