HRP20160421T1 - Derivat azola - Google Patents

Derivat azola Download PDF

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Publication number
HRP20160421T1
HRP20160421T1 HRP20160421TT HRP20160421T HRP20160421T1 HR P20160421 T1 HRP20160421 T1 HR P20160421T1 HR P20160421T T HRP20160421T T HR P20160421TT HR P20160421 T HRP20160421 T HR P20160421T HR P20160421 T1 HRP20160421 T1 HR P20160421T1
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HR
Croatia
Prior art keywords
acetamide
ethyl
phenyl
propan
triazol
Prior art date
Application number
HRP20160421TT
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English (en)
Inventor
Mitsukane Yoshinaga
Takeshi Kuwada
Naoki Miyakoshi
Tomoko Ishizaka
Daisuke Wakasugi
Shin-Ichi Shirokawa
Nobutaka Hattori
Youichi Shimazaki
Original Assignee
Taisho Pharmaceutical Co., Ltd
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Publication date
Application filed by Taisho Pharmaceutical Co., Ltd filed Critical Taisho Pharmaceutical Co., Ltd
Publication of HRP20160421T1 publication Critical patent/HRP20160421T1/hr

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/445—Non condensed piperidines, e.g. piperocaine
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    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/537—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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Claims (12)

1. Derivat azola prikazan s Formulom (I): [image] [u Formuli (I), R1 predstavlja vodikov atom, C1-5 alkil (C1-5 alkil je proizvoljno supstituiran s jednom do tri skupine odabrane iz skupa koji sadrži hidroksi, halogene atome, cijano, C3-7 cikloalkil, i C1-5 alkoksi), C3-7 cikloalkil, ili 4- do 8-člani zasićeni heterocikal; R2 predstavlja vodikov atom ili C1-5 alkil; R3 predstavlja aril ili heteroaril (aril i heteroaril su proizvoljno supstituirani s jednom ili dvije skupine koje su odabrane iz skupa koji sadrži C1-5 alkoksi, C1-5 alkil, halogene atome, trifluorometil, trifluorometoksi, cijano, hidroksi, difluorometoksi, i C1-5 alkilsulfonil); R4 i R5 koji mogu biti isti ili različiti svaki predstavljaju vodikov atom, C1-5 alkil (C1-5 alkil je proizvoljno supstituiran s jednom do tri skupine odabrane iz skupine koja sadrži hidroksi, halogene atome, cijano, C3-7 cikloalkil, i C1-5 alkoksi), C3-7 cikloalkil, ili 4- do 8-člani zasićeni ili nezasićeni heterocikal koji sadrži jedan ili više atoma dušika, kisika ili sumpora u prstenu (4- do 8-člani zasićeni ili nezasićeni heterocikal je proizvoljno supstituiran s jednom ili dvije skupine koje su odabrane iz skupa koji sadrži hidroksi, C1-5 alkil, C1-5 alkoksi, halogene atome, cijano, C2-5 alkanoil, te trifluorometil), ili R4 i R5, zajedno sa susjednim dušikovim atomom, tvore 4- do 8-člani zasićeni ili nezasićeni heterocikal koji proizvoljno sadrži jedan ili više atoma dušika, kisika ili sumpora u prstenu pored susjednog atoma dušika (4- do 8-člani zasićeni ili nezasićeni heterocikal je proizvoljno supstituiran s jednom ili dvije skupine koje su odabrane iz skupa koji sadrži hidroksi, C1-5 alkil (C1-5 alkil je proizvoljno supstituiran s jednom ili dvije hidroksilne skupine), C1-5 alkoksi, halogene atome, cijano, C2-5 alkanoil, okso, aminokarbonil, mono-C1-5 alkilaminokarbonil, di-C1-5 alkilaminokarbonil, trifluorometil, amino, mono-C1-5 alkilamino, di-C1-5 alkilamino i C2-5 alkanoilamino, te 4- do 8-člani zasićeni ili nezasićeni heterocikal proizvoljno ima skupinu C1-5 alkilen koji unakrsno povezuje dva različita ugljikova atoma u prstenu) ili tvori 2-oksa-6-azaspiro[3.3]hept-6-il ili 7-oksa-2-azaspiro[3.5]non-2-il; proizvoljno supstituiran azol prsten koji je predstavljen sa slijedećom formulom (α): [image] ima bilo koju od struktura uz slijedeće skupine formula (II): [image] gdje Ry predstavlja vodikov atom ili C1-5 alkil; X1 i X2 su takvi da i) kada X1 je jednostruka veza ili formula -CO-, X2 predstavlja -C1-5 alkilen- ili -O-C1-5 alkilen-; i ii) kada X1 je formula -CONRx1-, X2 predstavlja jednostruku vezu; Rx1 predstavlja vodikov atom ili C1-5 alkil; i prsten A predstavlja benzenski prsten, 6-člani aromatski heterocikal (benzenski prsten i 6-člani aromatski heterocikal su proizvoljno supstituirani s jednom ili dvije skupine koje su odabrane iz skupa koji sadrži halogene atome i C1-5 alkoksi), 4- do 8-člani zasićeni ili djelomično nezasićeni heterocikal koji sadrži jedan ili dva dušikova atoma (4- do 8-člani zasićeni ili nezasićeni heterocikal je proizvoljno supstituiran s jednim okso) ili C3-7 cikloalkan] ili farmaceutski prihvatljiva sol derivata azola.
2. Derivat azola ili njegova farmaceutski prihvatljiva sol prema zahtjevu 1, naznačen time da u gornjoj Formuli (I), R4 i R5 koji mogu biti isti ili različiti svaki predstavljaju vodikov atom, C1-5 alkil (C1-5 alkil je proizvoljno supstituiran s jednom do tri skupine koje su odabrane iz skupine koja sadrži hidroksi, halogene atome, cijano, C3-7 cikloalkil, i C1-5 alkoksi), C3-7 cikloalkil, ili 4- do 8-člani zasićeni ili nezasićeni heterocikal koji sadrži jedan ili više atoma dušika, kisika ili sumpora u prstenu (4- do 8-člani zasićeni ili nezasićeni heterocikal je proizvoljno supstituiran s jednom ili dvije skupine koje su odabrane iz skupa koji sadrži hidroksi, C1-5 alkil, C1-5 alkoksi, halogene atome, cijano, C2-5 alkanoil, i trifluorometil), ili R4 i R5, zajedno sa susjednim dušikovim atomom, tvore 4- do 8-člani zasićeni ili nezasićeni heterocikal koji proizvoljno sadrži jedan ili više atoma dušika, kisika ili sumpora u prstenu pored susjednog dušikovog atoma (4- do 8-člani zasićeni ili nezasićeni heterocikal je proizvoljno supstituiran s jednom ili dvije skupine koje su odabrane iz skupa koji sadrži hidroksi, C1-5 alkil (C1-5 alkil je proizvoljno supstituiran s jednom ili dvije hidroksilne skupine), C1-5 alkoksi, halogene atome, cijano, C2-5 alkanoil, okso, aminokarbonil, mono-C1-5 alkilaminokarbonil, di-C1-5 alkilaminokarbonil i trifluorometil, te 4- do 8-člani zasićeni ili nezasićeni heterocikal proizvoljno ima skupinu C1-5 alkilen koji unakrsno povezuje dva različita ugljikova atoma u prstenu) ili tvori 2-oksa-6-azaspiro[3.3]hept-6-il ili 7-oksa-2-azaspiro[3.5]non-2-il.
3. Derivat azola ili njegova farmaceutski prihvatljiva sol prema zahtjevu 1 ili 2, naznačen time da u gornjoj Formuli (I), X1 predstavlja jednostruku vezu; X2 predstavlja -C1-5alkilen- ili -O-C1-5alkilen-; i prsten A predstavlja benzenski prsten, 6-člani aromatski heterocikal (benzenski prsten i 6-člani aromatski heterocikal su proizvoljno supstituirani s jednom ili dvije skupine koje su odabrane iz skupa koji sadrži halogene atome i C1-5 alkoksi) ili 4- do 8-člani zasićeni ili nezasićeni heterocikal koji sadrži jedan ili dva dušikova atoma (4- do 8-člani zasićeni ili nezasićeni heterocikal je proizvoljno supstituiran s jednim okso).
4. Derivat azola ili njegova farmaceutski prihvatljiva sol prema bilo kojem od zahtjeva 1 do 3, naznačen time da u gornjoj Formuli (I), prsten A predstavlja benzenski prsten ili 6-člani aromatski heterocikal (benzenski prsten i 6-člani aromatski heterocikal su proizvoljno supstituirani s jednom ili dvije skupine koje su odabrane iz skupa koji sadrži halogene atome i C1-5 alkoksi).
5. Derivat azola ili njegova farmaceutski prihvatljiva sol prema bilo kojem od zahtjeva 1 do 4, naznačen time da u gornjoj Formuli (I), prsten A predstavlja benzenski prsten ili piridinski prsten (benzenski prsten i piridinski prsten su proizvoljno supstituirani s jednom ili dvije skupine koje su odabrane iz skupa koji sadrži halogene atome i C1-5 alkoksi).
6. Derivat azola ili njegova farmaceutski prihvatljiva sol prema bilo kojem od zahtjeva 1 do 5, naznačen time da u gornjoj Formuli (I), R1 je C1-5 alkil; R2 je vodikov atom; i R3 je fenil ili piridil (fenil i piridil su proizvoljno supstituirani s jednom ili dvije skupine koje su odabrane iz skupa koji sadrži C1-5 alkil, C1-5 alkoksi, halogene atome, cijano, trifluorometil, difluorometoksi, trifluorometoksi, i C1-5 alkilsulfonil).
7. Derivat azola ili njegova farmaceutski prihvatljiva sol prema bilo kojem od zahtjeva 1 do 6, naznačen time da u gornjoj Formuli (I), proizvoljno supstituirani azol prsten koji je predstavljen sa slijedećom formulom (α): [image] ima bilo koju od struktura uz slijedeće skupine formula (III): [image] gdje Ry predstavlja vodikov atom ili skupinu metil.
8. Derivat azola ili njegova farmaceutski prihvatljiva sol prema bilo kojem od zahtjeva 1 do 7, naznačen time da u gornjoj Formuli (I), X1 je jednostruka veza; X2 je etilen ili metiletilen; i R4 i R5, zajedno sa susjednim dušikovim atomom, tvore 4- do 8-člani zasićeni ili nezasićeni heterocikal koji proizvoljno sadrži jedan ili više atoma dušika, kisika ili sumpora u prstenu pored susjednog dušikovog atoma (4- do 8-člani zasićeni ili nezasićeni heterocikal je proizvoljno supstituiran s jednom ili dvije skupine koje su odabrane iz skupa koji sadrži hidroksi, C1-5 alkil (C1-5 alkil je proizvoljno supstituiran s jednom ili dvije hidroksilne skupine), C1-5 alkoksi, halogene atome, cijano, C2-5 alkanoil i trifluorometil, i 4- do 8-člani zasićeni ili nezasićeni heterocikal koji proizvoljno ima C1-5 alkilen skupinu koja unakrsno povezuje dva različita ugljikova atoma u prstenu) ili tvore 2-oksa-6-azaspiro[3.3]hept-6-il.
9. Derivat azola ili njegova farmaceutski prihvatljiva sol prema bilo kojem od zahtjeva 1 do 8, naznačen time da u gornjoj Formuli (I), R4 i R5, zajedno sa susjednim dušikovim atomom, tvore 5- ili 6-člani zasićeni heterocikal koji proizvoljno sadrži jedan ili više kisikovih atoma u prstenu pored susjednog dušikovog atoma (6-člani zasićeni heterocikal je proizvoljno supstituiran s jednom ili dvije skupine koje su odabrane iz skupa koji sadrži hidroksil i C1-5 alkil, te 6-člani zasićeni heterocikal proizvoljno ima C1-5 alkilen skupinu koja unakrsno povezuje dva različita ugljikova atoma u prstenu) ili tvore 2-oksa-6-azaspiro[3.3]hept-6-il.
10. Derivat azola ili njegova farmaceutski prihvatljiva sol prema zahtjevu 1, naznačen time da derivat azola ili koji je predstavljen s Formulom (I) je odabran iz skupine koja sadrži: 2-[2-(3-klorofenil)-4-{4-[2-(piperidin-1-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[2-(3-klorofenil)-4-{4-[2-(morfolin-4-il)etil]phernil}-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[2-(3-klorofenil)-4-(4-{2-[3-(hidroksimetil)pirolidin-1-il]etil}fenil)-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[2-(3-klorofenil)-4-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[2-(4-fluoro-3-metoksifenil)-4-{4-[2-(piperidin-1-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[2-(4-fluoro-3-metoksifenil)-4-{4-[2-(morfolin-4-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[2-(4-fluoro-3-metoksifenil)-4-{4-(2-(pirolidin-1-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[2-(4-fluoro-3-metoksifenil)-4-(4-{2-[(2R)-2-metilpirolidin-1-il]etil}fenil)-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[2-(4-fluoro-3-metoksifenil)-4-{4-[2-(3-hidroksi-8-azabiciklo[3.2.1]okt-8-il)etil]fenil} -1 H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[2-(4-fluoro-3-metoksifenil)-4-{4-[2-(3-metoksipiperidin-1-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[4-{4-[2-(2,6-dimetilmorfolin-4-il)etil]fenil}-2-(4-fluoro-3-metoksifenil)-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[2-(4-fluoro-3-metoksifenil)-4-{4-[2-(3-metilpirolidin-1-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[2-(4-fluoro-3-metoksifenil)-4-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-1 H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[2-(4-fluoro-3-metoksifenil)-4-{4-[2-(1,4-oksazepan-4-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[4-{4-[2-(3,5-dimetilmorfolin-4-il)etil]fenil}-2-(4-fluoro-3-metoksifenil)-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[2-(3-klorofenil)-4- {5-[2-(morfolin-4-il)etil]piridin-2-il}-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[2-(3-klorofenil)-4-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[2-(3-klorofenil)-4-{6-[2-(morfolin-4-il)etil]piridin-3-il}-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[2-(3-metoksifenil)-5-metil-4-{4-[2-(morfolin-4-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[2-(3-metoksifenil)-4-{4-[2-(morfolin-4-il)etil)fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-(2-(3-kloro-4-fluorofenil)-4-{4-[2-(morfolin-4-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[2-(3-metoksifenil)-4-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[2-(3-klorofenil)-4-{2-fluoro-4-[2-(morfolin-4-il)etil)fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[2-(3-klorofenil)-4-{4-[2-(morfolin-4-il)propil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[5-(3-klorofenil)-3-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamid; 2-[5-(3-klorofenil)-3-{4-[2-(morfolin-4-il)etil]fenil}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamid; 2-[5-(3-klorofenil)-3-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamid; 2-[5-(3-metoksifenil)-3-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamid; 2-[5-(4-fluoro-3-metoksifenil)-3-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamid; N-tert-butil-2-[5-(3-metoksifenil)-3-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]acetamid; 2-[5-(3-kloro-4-fluorofenil)-3-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il} -1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamid; N-tert-butil-2-[5-(3-klorofenil)-3-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]acetamid; 2-[5-(3-klorofenil)-3-{5-[2-(morfolin-4-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamid; N-tert-butil-2-[5-(3-klorofenil)-3-{5-[2-(morfolin-4-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]acetamid; 2-[5-(3-kloro-4-fluorofenil)-3-{5-[2-(morfolin-4-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamid; 2-[5-(4-fluoro-3-metoksifenil)-3-{5-[2-(morfolin-4-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamid; N-tert-butil-2-[5-(3-metoksifenil)-3-{5-[2-(morfolin-4-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]acetamid; 2-[5-(3-metoksifenil)-3-{4-[2-(morfolin-4-il)etil]fenil}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamid; 2-[5-(3-metoksifenil)-3-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamid; 2-[3-(2-fluoro-4-[2-(morfolin-4-il)etil]fenil}-5-(3-metoksifenil)-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamid; 2-[3-{3-fluoro-4-[2-(morfolin-4-il)etil]fenil}-5-(3-metoksifenil)-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamid; 2-[5-(3-metoksifenil)-3-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)propil]fenil}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamid; 2-[5-(3-metoksifenil)-3-{4-[2-(7-oksa-2-azaspiro[3.5]non-2-il)etil]fenil}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamid; 2-[5-(3-metoksifenil)-3-{4-[2-(2-oksa-6-azaspiro[3.3]hept-6-il)etil]fenil}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamid; 2-[1-(3-klorofenil)-3-{4-[2-(morfolin-4-il)etil]fenil}-1H-1,2,4-triazol-5-il]-N-(propan-2-il)acetamid; 2-[1-(3-klorofenil)-3-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-1H-1,2,4-triazol-5-il]-N-(propan-2-il)acetamid; 2-[5-(3-klorofenil)-3-{4-[2-(morfolin-4-il)etil]fenil}-2-okso-2,3-dihidro-1H-imidazol-1-il]-N-(propan-2-il)acetamid; 2-[4-(3-klorofenil)-2-{4-[2-(piperidin-1-il)etil]fenil}-1,3-oksazol-5-il]-N-(propan-2-il)acetamid; 2-[4-(3-klorofenil)-2- {4-[2-(morfolin-4-il)etil]fenil}-1,3-oksazol-5-il]-N-(propan-2-il)acetamid; 2-[4-(3-klorofenil)-2-{4-[2-(2-oksa-6-azaspiro[3.3]hept-6-il)etil]fenil}-1,3-oksazol-5-il]-N-(propan-2-il)acetamid; 2-[5-(3-klorofenil)-2-{4-[2-(piperidin-1-il)etil]fenil}-1,3-tiazol-4-il]-N-(propan-2-il)acetamid; 2-[5-(3-klorofenil)-2-{4-[2-(morfolin-4-il)etil]fenil}-1,3-tiazol-4-il]-N-(propan-2-il)acetamid; 2-[3-(3-klorofenil)-1-{4-[2-(piperidin-1-il)etil]fenil}-1H-pirazol-4-il]-N-(propan-2-il)acetamid; 2-[3-(3-klorofenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-1H-pirazol-4-il]-N-(propan-2-il)acetamid; 2-[5-(3-klorofenil)-3-{4-[2-(morfolin-4-il)etil]fenil}-1H-pirazol-1-il]-N-(propan-2-il)acetamid; 2-[4-(3-klorofenil])-1-{4-[2-(morfolin-4-il)etil]fenil}-2,5-diokso-2,5-dihidro-1H-pirol-3-il]-N-(propan-2-il)acetamid; 2-[4-(3-klorofenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamid; 2-[4-(3-klorofenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamid; N-tert-butil-2-[4-(4-fluoro-3-metoksifenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamid; N-tert-butil-2-[4-(3-metoksifenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamid; N-tert-butil-2-[4-(3-metoksifenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamid; N-tert-butil-2-[4-(4-fluoro-3-metoksifenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamid; N-tert-butil-2-[4-(4-fluoro-3-metoksifenil)-1-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamid; N-tert-butil-2-[4-(3-klorofenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamid; N-tert-butil-2-[4-(3-klorofenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamid; 2-[4-(3-klorofenil)-1-{4-[2-(morfolin-4-il)propil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamid; 2-[4-(3-klorofenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)propil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamid; 2-[4-(3-klorofenil)-1-{3-fluoro-4-[2-(morfolin-4-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamid; 2-[4-(3-klorofenil)-1-{3-fluoro-4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamid; 2-[4-(3-klorofenil)-1-{3-metoksi-4-[2-(morfolin-4-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamid; 2-[4-(3-klorofenil)-1-{3-metoksi-4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamid; 2-[4-(3-kloro-4-fluorofenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamid; 2-[4-(3-kloro-4-fluorofenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamid; N-tert-butil-2-[4-(3-kloro-4-fluorofenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamid; N-tert-butil-2-[4-(3-kloro-4-fluorofenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamid; N-tert-butil-2-[4-(3-kloro-4-fluorofenil)-1-{5-[2-(morfolin-4-il)etil]piridin-2-il}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamid; N-tert-butil-2-[4-(3-kloro-4-fluorofenil)-1-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamid; 2-[4-(3-klorofenil)-1-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)propil]piridin-2-il}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamid; 2-(1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-4-[3-(trifluorometil)fenil]-4,5-dihidro-1H-1,2,4-triazol-3-il)-N-(propan-2-il)acetamid; 2-[4-(3-kloro-4-fluorofenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)propil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamid; 2-[4-(4-fluoro-3-metoksifenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil)-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamid; 2-[4-(4-fluoro-3-metoksifenil)-1-{3-metoksi-4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamid; 2-[1-{3-metoksi-4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-4-(3-metoksifenil)-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamid; 2-[4-(3-kloro-4-fluorofenil)-5-okso-1-{4-[2-(pirolidin-1-il)etil]fenil}-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamid; 2-[4-(3-kloro-4-fluorofenil)-5-okso-1-{4-[2-(piperidin-1-il)etil]fenil}-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamid; i 2-[2-(3-klorofenil)-4-{4-[2-(2-oksa-6-azaspiro[3.3]hept-6-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamid.
11. Farmaceutski pripravak naznačen time da kao aktivni sastojak sadrži derivat azola ili njegovu farmaceutski prihvatljivu sol prema bilo kojem od zahtjeva 1 do 10.
12. Sredstvo za uporabu za tretman ili sprječavanje poremećaja raspoloženja, anksioznosti, shizofrenije, Alzheimerove bolesti, Parkinsonove bolesti, Huntingtonove koree, poremećaja u prehrani, hipertenzije, gastrointestinalne bolesti, ovisnosti o drogama, epilepsije, cerebralnog infarkta, cerebralne ishemije, cerebralnog edema, ozljede glave, upale, imunološki povezanih bolesti, ili alopecije, naznačeno time da kao aktivni sastojak sadrži derivat azola ili njegovu farmaceutski prihvatljivu sol prema bilo kojem od zahtjeva 1 do 10.
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