HUE031366T2 - Katechol-O-metiltranszferáz aktivitást gátló vegyületek - Google Patents

Katechol-O-metiltranszferáz aktivitást gátló vegyületek Download PDF

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Publication number
HUE031366T2
HUE031366T2 HUE13730284A HUE13730284A HUE031366T2 HU E031366 T2 HUE031366 T2 HU E031366T2 HU E13730284 A HUE13730284 A HU E13730284A HU E13730284 A HUE13730284 A HU E13730284A HU E031366 T2 HUE031366 T2 HU E031366T2
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HU
Hungary
Prior art keywords
alkyl
dihydroxy
aryl
hydroxy
alkoxy
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HUE13730284A
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English (en)
Inventor
Marko Ahlmark
Belle David Din
Mika Kauppala
Anne Luiro
Taina Pajunen
Jarmo Pystynen
Eija Tiainen
Matti Vaismaa
Josef Messinger
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Orion Corp
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Publication of HUE031366T2 publication Critical patent/HUE031366T2/hu

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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/275—Nitriles; Isonitriles
    • A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid, pantothenic acid
    • A61K31/198—Alpha-aminoacids, e.g. alanine, edetic acids [EDTA]
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
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    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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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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    • C07C255/59—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
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    • C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
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    • C07D333/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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Claims (27)

  1. Kateeh«f«0»w«tiltransxferáx aktivitást gátló vogyCIf tfk ZRéBADééZT X:@llM¥l?Qgf:ÖK: 1- ig?
    képleté vegyülök amelyben R; jelentése 1-6 szénaiomos alkik 2-6 szénaiomos alkenií-; 2-6 szénatomon aikinik 3^7 izénátöfttos cíkloaíki'h 4-10 szérlaténtoa éikioaikeoih aríl-, {RzkC-C-· oéépört, ihaioginatorn, hidroxl-, 1-6 szénatomos aíkoxi-, ÍR? szénatomos aikií-S-, 4-10 szénatomos cikloeíkenií-oxk 4-10 szén atomos oiktoaíkenií-S-, arlí-oxi, anj-S-, hetemahi-oxé, hetemanl-S-, (R^N-, (Rí)íCk~R-, heierooiktik heteroaPk ani-{1-6' szári a torzos alkil V, (1 -aotkio-1 -ka!t>oxi-motk)“(l-6 szénatomos alkil)-, haiogén-{1-6 szénatomos alkil}-: hklroxla'1-6 szénatomos alkil)-, (1-6 szénatomos aíkoxl}-(1-6 szénaténlös alkil}-, {1-6 szénatoméi alkii)-S~(1-6 szénatomos alkil)-, (R-.6sN-(1-6 szénatomos alkil)-, hoterocskRá 1-6 szénatomos alkil)-, karboxi-(2-6 szénaiomos alkenií)-, (3-7 szénatomos eikloaíkiíH2-6 szénatomos alkenií)-. ariM2-6 szénatomos alkenií)-, f i-6 szénatomos aikoxiH2-6 szóaafomos alkenií)-, heiorocíklll-{2-6 szénatomos alkenií)-, hefaroanl-{2~6 szénatomos alkenií}-, karboxi-(2-6 szénatomos allé ni I)-, (3-7 szénatomos cíkioalkil)-(2-8 szénatomos alklnsi)-, anl-{2~8 szén-atomos alkinií)-, (1 -6 szénatomos aikoxi)-{2-6 szénatomos alkinil)I heleroolklil-(2-6 szénatomos alkinil)··, heLeroanl-(2-6 szénatomos alkinil)-, halogén^ 1-6 szénatomos alkoxi)-, hidroxK'l-Ö szénatomos alkoxi}, (1-6 szénatomos alkoxi)-(1-6 szén-atomos alkoxi)-, (1-6 szénatomos aikil)-(C--0)-ö-, R5-(S~Ö)-( Re-(0-3--0)-, hidroxi-(1-6 szénatomos alkoxiHI-6 szénatomos alkil)-, (1-6 szénatomos alkoxi)-(0-0)-(2-6 szénatomos alkenií)- vagy (1-6 szénatomos alkil)-(00)-0-( 1-6 szénatomos aikiiV-csoporL ahol a 4-10 szénatomos dkioaikeníl·, aril··, hetetoelkíik heteroahí- vagy a 3-7 szénatomos dkioaíkiéeégport mint olyan, vagy egy másik csoport részeként szubszfsíuálatlan, vagy pedig 1, 2 vagy 3 számú R$ szubszti-tuenssei szubsztituált; R;> jelentése, függetlenül minden előforduláskor, karboxf- vagy célcsoport ahol az srilcsoport, függetlenül minden előforduláskor, szubsEituáíitlan, vagy pedig t, 2 vagy 3 szemű R§ szubszktuenssei szubsztituált; Rí jelentése, függetlenül minden előforduláskor, H, 1-8 szénatomos aikik 3-7 szénatomos eikloalkik ahk (3-? szénatomos cikloa!kii}-l-6 szénatomos alkii)-, hidroxK1~6 szénatomos alkil}- vagy (1-8 szénatomos aikoxi H'kb szénatomos alkilVcsoport, ahol a 3-7 szénatomos cíkloalkii- vagy árucsoport mint olyan, vagy egy másik csoport részeként, függetlenül minden előforduláskor, szubsztituáialian vagy szubsztituált egy szubsztituenssel, amely 1-8 szénatomos alkilcsoport, hab-génatom, hidroxi-, 1*8 szénatomos aikoxi- vagy hidroxi-(1-8 szénatomos a I ki facsoport; :¾ jelentése, függetiénöl minden eíöfordüliekőr, H vagy anteopori, abőt ál árilésoport, függetlenül' mindeb előforduláskor, szuházfituitátfán vágy szubszfifyált egy szubsztituenssel, amely 1 -8 szénátomös álkiiosoport, hafögédatom vágy 1*8 szénatomos aikoxi-csoport; R·', jelentése 1*8 szénatomos alkil", aril-, hidroxi- vagy 1 -6 szénatomos alkoxl-osoport, ahol az arllosoport szoteszltuájáflon vagy szubsztityili 1,2 vagy 3 számú R$ szubsztityenssé!; Rí, jelentése, függeflénOl minden előforduláskor, 1-8 szénatomos aikik 2-8 szén-atomos síkenii-, karhoxR dano-, arllcsoport, halogénatom, hidroxi», 1-6 szénatomos aikoxi', 1-8 szénatomos alkii-S-. 4-10 szénatomos dkioalkenil-axk 4-10 szénaioniőá olMoaikenil-S-, arii-exR arlkl-, hiteroati-oxí-, heterpartbS-, fÍ%}zNh hetemen!-, karboxi-(1*8 szénatomos alkil), arif-(1~6 szénatomos alkii)-, halogéné i-6 szénatomos alkii}-, hidroxi~{1~8 szénatomos alkii}-, (1-6 szénatomos alkoxi}-(1-8 szénatomos alkii}-, betemcikllí-{1-8 szénatomos alkil)-, (1-6 szénatomos alkii)--(O0)~, (1-6 szénatomos aikoxiMC-'ö}-, heierodkliHCkök ÍR?};;N-(CkO)-, halo-gén-(1"8 szénatomos aikoxi)-, Re-iS-O}-, Ra-fO-S'-O)-, (1-8 szénatomos alkoxi)-í (><)}-( 1 -8 szénatomos aíkil)», {R?)2N-{C~ÖH1-8 szénatomos alkii)- vagy (1-6 szénatomos aIkoxí)-(i -6 szénatomos aikoxi)-(0-0)- csoport, ahol az aril-, heteroadl- vagy heterociklsi-csoport mint olyan, vagy egy másik csoport részeként, függetlenül minden előforduláskor, szubsztitoálatlan vagy szubsztltüáft egy ozuhsztiiuensoef, amely 1-6 szén aló mos aikiicsoport; vagy R$ és R§, amelyek közül mindkettő ugyanahhoz a szén gyürüalomhoz kapcsolódik, azzal a szén gyumafppimaiegyütt, amelyhez kapcsolódnak, egy -(00)-csoportot: képeznek; Rt jelentése, függetlenül minden előforduláskor, H, 1-8 szénatomos alkil-, 3-7 szénatomos cikloalkíl- vagy karboxMI-8 szénatomos alkiD-csoport, ahol a 3-7 szén atomos ciklon skil-osopork függetlenül minden előforduláskor, szuhsziltuálatlan vagy szubsztifuált egy szubszilfuenssel, amely 1-6 szénatomos afkiicsoporf; R« jelentése, függetlenül mindén .előforduláskor, 1-6 szénainmos alfél-, hidrokK 1-6 szénatomos aikoxi- vagy (R«);:N-csoport: R'3 jelentése, függetlenül minden előforduláskor, 1-8 szénafomos aikliesopod, vagy ennek gyogyszerészeilleg elfogadható sója vagy észtere.
  2. 2, Egy 1. igénypont szerinti vegyülő! amelyben Rí jelentése 1 ~8 szénafomos alkil-, £-8 szénatomos alkenll-, 2-6 szénafomos Bikinik 4"10 szénafomos cikfoalkenik aril-, halogénafom, hidroxh 4-1Ö szénatomos cikloai-kenil-oxl-, aril-ox! anl-S-, heteroadl-S-, (Ro.kN'-, (ΕφΟ-'ΤΚ heierocikiik heferoani-, arií-{1-6 szénatomos alkil}··, h;droxl-(1-8 szénafomos alkil}-·, (IkdsN-CI-o szénatomos alkllih he!eroclklik(1-6 szénafomos alkil)", karboxi-{2-6 szénafomos alkenll)-, (3-7 széilátomöe eikloalkit)-(2-8 szénatomod alkenll)-, aní-(2-6 szénafomos alkenll)-, (1-6 szénetomoB alkoxl)-(2-8 szénafomos alkenii}a HétemanK2-6 szénatomos alkenll)-, arii-(2-8 szénafomos alkinll}-·, (1-6 szénafomos alkoxi)-(2-6 szénatomos alkinilk R5-(S--0)-, Fk-(C)-'S--Oé vagy (1-6 szénafomos 3ÍkoxiHC--0)~(2-6 szénatomos afkeniiVcsoport, ahol a 4-10 szónatomosőikioaikenih ári!-, heterodkill··., heieroarib vagy a 3-7 szénatomős cikioalkll-csoport mint olyan, vagy egy másik csoport részeként szubsztifuáiatfan, vagy pedig 1, 2 vagy 3 számú Re szubszüfuenssel szabsz-fítuált; R5 jelentése, függetlenül minden előforduláskor. H, 1-6 szénafomos alkil-, 3-7 szénatomos cikioalklk anl··, (3-7 szénatomos dkíoalkil)-1-6 szénafomos alkil)-, hk1roxi-(1-6 szénatomos alkil}- vagy (1-6 szénatomos aIkox!)-(1-6 szénatomos alkiil-esoport, ahol a 3-7 szénafomos olkioalkll- vagy árucsoport mini olyan, vagy egy másik csoport részeként szubsztituálafian vagy szubsziituált egy szubsztituenssel, amely 1-6 szénatomos alkilcsopon; R4 jelentése, függetlenül minden előforduláskor, H vagy adlcsoport ahol az árucsoport, függetlenül mmden előforduláskor, szubszfiiuélt egy szubsztltuenssel, amely 1-8 szénatomos alküesopori, nalogénatom vagy 1-8 azénatomos aiköxbcso-post; R;·.: jelentése árucsoport, ahol az anicsoport sxubsxtltuáit egy R* szubsztiteenasel; Re jelentése, függetlenül minders előforduláskor, 1 -8 szénatomos aikil·, 2-6 szénafo-mos elkenik karboxl·, ciano-, árucsoport halogénatom,, hidroxh 1-6 szénaiomos atkoxh 1-8 szénatomos aikil-S-, anl-cxh hateroahk karboxMI-ö szénatomos alki!)-, ant'(1"b szénatomon aikil)-, balogém-H-8 szénatomos aikil}-, hklroxi-(1-6 szénatomos akii)-, (1-6 szénatomos aikoxi>'(1-6 szénatomos aikil)-, heierociklll-(1-6 szénaiomos akii)-, < 1 '0 szénatomos aikií)-(C~Ö}\ (1-8 szénatőitté#'-.atkoxiHC~Oy< heteroclklll· (C-~Ok (Rv^N-ÍC-ö)-, halogénül-6 szénaiomos aikoxiV, R&amp;-(0”S~0k (1-6 szén-atomos alkox!)-(C~0)“(1-6 szénatomos akii)-, (RksNkC-0)-(1-6 szénatomom aikil}-vagy (1-8 szénatomos aíkoxi}-(1~8 szénaiomos akoxi)-(C™0)- csoport, ahol az aril-, heteroarl!- vagy hotemckllbcsoport mint olyan, vagy egy másik csoport részekért, függetlenül minden előforduláskor, szubszíliuálaiían vagy szubszfituált egy szubsz-tltuenssel, amely 1-6 szénaiomos alkilcsoport; vagy Re és Rö: amelyek közül mindkettő ugyanahhoz a szén gyürüatomhoz kapcsolódik, azzal a szén· f|yürőatéfppi#.é§ydft? kapcsolódnak, egy -(0-0)- cso portot képeznek; Fb jelentése, függetlenül minden előforduláskor, H, 1-6 szénaiomos aikil-, 3-7 szénatomos clkloaíkli- vagy karboxi-fl-8 szénaiomos alkilj-osoport, ahol a 3-? szénatomos cikloaikil-csoport szubsztltuálatlan; Rg jelentése, függetlenül minden előforduláskor. 1-8 szénaiomos akii- vagy ÍR^sN-csoport; Rs jelentése, függetlenül minden előforduláskor, 1-8 szénaiomos alkilosoport,
  3. 3. Egy 2. igénypont, szerinti vegyiket amelyben Rí jelentése 1-8 szénatomos aikil-, 2-8 szénaiomos elkenik 2-8 szénatomos alkínik 4-10 szénatomos clkioalkeníb, aril·, halogénatom, 4-1 ö szénatomos cikbalkenil-oxl··. arü-oxi, aril-S-, heteroarií-S-, (Rjphk (R^sC-N-, heterociklik heferoarik aril-{1-8 szénatomos aikil)-, <R.j)>M-( 1 -6 szénaiomos aikil}-, karboxM'2-8 szénatomos alkenll)-, (3-7 szénatomos cikloaíkil}-{2-8 szénatomos alkenll)- vagy aril-(2-8 szénatomos aíkenllVcsopotl, ahol a 4-10 szénatomos elkloalkenik aril-, heterodklil·, heteroaril- vagy a 3-7 szénatomos cikioatkií'csoport mint olyan, vagy agy másik csoport részeként szuhsztiiuálaUan, vagy pedig 1, 2 vagy 3 számú Rs szuhszíiiuensaei szabsz-kiuait; Rs jelentése, függetlenül minden előforduláskor. H 1-6 ezénatomsa alklh vagy (Is# szénafömos slkoxiH 1 -6 szénatoméi; áiklj-esopod, R.i jelentése, függetlenül minden előforduláskor, H vagy alcsoport, ahol az aril·· csoport, függetlenül minden előforduláskor, szubszfifuált egy szubszfituenssel, amely 1-6 szénafomos aiklicsopod, halogénatom vagy 1-6 szénatomos aikoxi-csoport; Rís jelentése, függetlenül minden előforduláskor, 1-6 szénatomos alkil-, cíano-, árucsoport, halogénatom, hidroxl··, 1-6 szénatomos alkoxl··, 1-6 szénafomos alkil-S-·, anl-oxk, karboxi-fl-ő szénafomos alkil)-, arii-f 1 -6 szénatomos alkíl)-, halogéné 1-6 szénafomos alkil}-, hidmza(1-6 szénatomos alkil}-, {1 -6 szénatomos alkoxfH'f-6 szénafomos alkil)-, hetemcikíiMC~OK (Ry^N-CC-Oj-RrtO-S-O}- vagy (1-6 szénafomos aikoz 1)60--0)-(1-6 szénatomos alkil/-csoport, ahol az anl- vagy heferocíklíl-csoport mint olyan, vagy egy másik csoport részeként szubszfituálaflan; R? jelentése, függetlenül minder? előforduláskor, H, 1-6 szénafomos alkil- vagy 3-7 szénatomos dkioalkil-csopmn, ahol a 3-7 szénatomos clkioalkil-csopor? szubsztltu-álatlan; Rö jelentése, függetlenül minden eiőfdrdylaekpn azánatomos alklh vagy (Rs^N-csoport) Re jelentése, függetlenül mlndan eléfbfduláskof, 1 -8 szénatontös alklteeopoft 4, Egy 3. igénypont szerinti vegyülef, amelyben Rí jelentése 1 -6 szénatomos alkil-, 2-6 szénatomos alkenlh, aril·-, hatogonafom, sárii-oxl, arlI-S-, (RyhN*s (R^OhK hetéroeikiih, hoteroaril··, aril-(1-6 szénatomos alkil)-, (3-7 szénatomos cikloaikll)-(2"6 szénatomos alkenii)- vagy 006(2-6 szénafomos alkenill-osoporf, ahol az aril-, heterociklfl·, beteroanl- vagy a 3-7 szénatomos cikloalkil-osoporf mint olyan, vagy egy másik csoport részeként, szubsztifuálaílan. vagy pedig 1, 2 vagy 3 számú Re szuhsztiiuenssel sx.ubsztltuáii; Rs jelentése, függetlenül minden előforduláskor, H vagy 1-6 szénafomos afkllcsoporf} 1¾ jelentése, függetlenül minden előforduláskor. H vagy arilcsoport, ahol az ári-csoport, függetlenül minden előforduláskor, szubsztltuált egy szubsztifuenssel, amely 1-6 szénafomos aikiiesoporí, halogénatom vagy 1-6 szénatomos alkoxl-osoport; R6 jelentése, függetlenül minden előforduláskor, 1-6 szénatomos alkil·, ciano^ arilcsoport, halogénatom, hidroxl-, 1-6 szénatomos aikoxk 1 -6 szénatomos aikil-S-, karboxi-(1-8 szénatomot; alkil}-, halogénéi m szénatomos óikén, hidroxi-{1-6 szén-atomos alkil)-, (1-6 szénatomos aikoxikl-6 szénatomos alkon·, hoterooiklil-tC-O)-, (R;g?Né(>C3)- vagy EíkO-k-R})-· csoport, ahol az ahl- vagy heferocikliS-osoporl mint olyan, vagy agy másik csoport részeként, szabsz ti tu á I a t la n; Ry jelentése, függetlenül minden előforduláskor, H vagy 1-6 szénatomos aikilcsopdrt; R<* jelentése, függetlenül minden előforduláskor, i ~6 szénatomos aikitosoport,
  4. 5, Egy 4. Igénypont szerinti vegyülát, amelyben Rí jelentése 1-6 szénatomos alkll-, 2-6 szénatomos aíkenll-, árié, halogénatoné ébb óxl, aril-S~, (Rs)sN-, hetemaktil·, heteroaril-, aril-{1-6 szénatomos alkil)- vagy aril~(2-6 szénatomos alkom!^csoport, ahol az anl-, hefarociküí- vagy hoteroahl-csoport mint olyan, vagy egy másik csoport részeként, szubsztltuálatlan, vagy pedig 1, 2 vagy 3 számú Re szubsztiuénssel szubsztituélt' R-j jelentése, függetlenül minden előforduláskor, H vagy 1-6 szénatomos alkllcsoport; Re jelsrrfése, függetlenül minden előforduláskor, 1-6 szénatomos alkll-, halogénaiom, hidroxl-, 1-6 szénatomos alkoxk, karboxh(1-8 szénatomos alkllp. halogénül-6 szénatomos afkii}- vagy (RylyR-iC-O)- csoport; Ry jelentése, függetlenül minden előforduláskor, H vagy 1-6 szénatemos alkllcsoport.
  5. 6. Egy 5. igénypont szerinti vegyidet, amelyben R· jelentése 2-6 szénalornos elkenik anl-, halogénaiom, onl-oxi, aril-S-. (RsV^N-. heteroaril·, aril-(1-6 szénatomos alkil}- vagy an!-{2~ö szénatomos alkenilRcsoport, ahol az aril- vagy hetoroarii-csoport mint olyan, vagy egy másik csoport részeként, szubsziiluálatian, vagy pedig 1 vagy 2 számú R?.; szuhszhluenssei szuhsxfituáii; Rs jélenfése, függetlenül minden előforduláskor, M vagy 1-6 szénafomős áikflősőpörtt Rí;, jelentése, függetlenül minder? előforduláskor, 1 -6 szénalornos alkil-, haiogénatom, 1-6 szénatomos alkoxi-, karboxl-(1-6 szénalornos alkil)- vagy halogéné 1-6 szénatomos alkil)- csoport, T, Egy 6, igényporiszedriti vegyület amelyben Rí jéjehteié 2-6 szénalornos áikőhik érik hafegénatöfk ártl-ip hetéréárih vágy aril· (1-6 szénalornos a!kil)-csoport. ahol az aril- vagy heteroarkcsoport mint olyan, vagy egy másik csoport részeként, szubsztltuálatlan, vagy pedig t vagy 2 számú szubszílíuenssel szubsztituált; Rí: jelentése, függetlenül minden elörordafiskor, 1-6 szénatomom aiklk halogénatom vagy "I -6 szénatomos alkoxl-esoport.
  6. 8, Egy ?. Igénypont szerinti vegyület, amelyben R-; jelentése 2-6 szénatomot afkemi-csopofi, hafogénatom, arii-S- vagy aril~(1~6 szénatomos alkíO-csoport, ahol m ariioiopod mini. olyan, vagy egy másik csoport részeként, szubsztltuálatlan, vagy pedig 1 vagy 2 számú R?, szubsztltuensseí szubsztitüált; Re jelentése, függetlenül minden előforduláskor, 1-6 szénatomos alkil·, halogénatom vagy 1 -6 szénatomos aikoxl-esoport δ. Egy 7. Igénypont szerinti vegyüféh amelyben R-; jelentése 2-8 szénatomos alkenli-csopork aril··, aril-S-, heteroahl- vagy anMt-6 szénatomos alkiij-csoport, ahol az árucsoport mini olyan, vagy egy másik csoport részekén!, 1 vagy 2 számú Rí- szubsztííuenssel szufosziituáit; Rg jelentése, függetlenül minden előforduláskor, 1-6 szénatomba afkif- vágy 1-6 szénatomos alkoxl-csoport.
  7. 10, Egy 9. igénypont szerinti vegyület, amelyben R; jelentése 2-6 szénatomos elkeni!-, arii-S-, vagy aril-(1-6 szénatomos alkilj-csoport, ahol az. árucsoport mint olyan, vagy egy másik csoport részeként, 1 vagy 2 számú Re szgbszfitMénssel szubsztítuáIt; Rg jelentése, függetlenül minden :éfiförd.üiáil<örs· -!MJ: .MéMtörttoi alkil- Vagy i-6 szénatomos alkoxl-csoport.
  8. 11, Egy 7, igénypont szerinti vegyület, amelyben R-j Jelentése 2~6 szénatomos alkenil-csoport.
  9. 12, Egy 7. Igénypont szerinti vegyület, amelyben Rí jelentése alcsoport, ahol az árucsoport 1 vágy 2. számú % szübéMffyenisöl szubsztitüált; Rg jelentése, függetlenül minden előforduláskor, 1-8 szénatomos alkilcsoport halo-génatom vagy 1-6 szénatomos alkoxi-csoporl
  10. 13, Egy 7, Igénypont szerinti vegyület, amelyben Rí jelentése aril-S-< ahol az anlcsopori szubsztituáiaflan vagy 1 vagy 2 szamü R«; szubsztifuenssel szubsztitüált; Re jelentése, függetlenül minden előforduláskor, 1-6 szénatomon alkilcsoport, haló-génatom vagy 1-8 szénatomos alkoxi-osoporf.
  11. 14, Egy 7, igénypont szerint; vegyuisi amelyben R? jelentése heteroanbcsoporf, ahol az heteroadbesöport sxubszitígáiatiafi vagy f vagy 2 számé R6 szubsztituenssa! szuhsztituálf; Re jelentése, függetlenül minden' elö?ofduláskers;i-6 szértálgmop alkllbiöport, hite-génatom vagy 1-6 szénatomos alkoxbcsopoth
  12. 15, Egy ?, igénypont szennti vegyülef, amelyben Rí jelentése anb(1-8 szénatomos alkiD-csoport, ahol az árucsoport 1 vagy 2 számé Rí, szubsziiiuenssel szubsztiiuált: Re jelénfése, föggjeifpiüí mindén' el#löcáMI#éfcpn. W szénatpmps aRII- vagy 14S szé natomos a I koxi-csoport.
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B enantiomers, 2-[{ciklohexll-metíi}“amínoJ-4.5“di“· hidroxMzofialonitni, 4.5'-dshidroxi'-244d«noxi--k)niL1sD}azoftafonstrsL 4,5niihkiroxidM pisi dindidOdzoftakedinL 4;oajihicfroKi^244'k2.2..24rifiuokatifkbanainnaoffaloaitnf.: 4,5--di·· hldroxi”2-|4-metH-2-{inflaor“nietfi}-b8nzil!4z.oftaionitnl, 4>5-dshidsnnxi“2“{(4*(mosi:ofin-4·· - ka dx> π s I) d e π s Hd kdd xafla 1 ο n i te i, 4.5a3ihidroxi-2-(rnatiHp4oiii)'aniino)4zofiaioniini vagy a 4;5-'dihfdroxi44[i6aiiatoxi'naffayn'-2af)-meffO'-;aoftafonsfriL
    17, Egy 1. igénypont szerinti vegyidet, ahol a vagyaiéi a 4,5'd!Mdroxí-241-matti-1 HgdmahSdl Hzoflalonifnk
    18, Egy 1. igénypont szerinti vegyidet, ahol a vegyidet a d'-ferc-hutíidM-ciihid-ro xik>i fe ni l~2, íkd 1 ka rhon fthl,
    18, Egy 1, igénypont szerinti vegyüiet, ahol a vegyüiet a 3<4”dihidroKi'-2>,5:~dh metií*bífenii"2,8"dikafbonitnl,
  14. 20, Egy 1. igénypont szerinti vegyüiet, ahol a vegyüiet az {£^2-(3^-díroetsl· -but-1 -enii}-4:5~dihidroxi"SZofteionltnL 21 < Egy 1, igénypont szerinti vágyóiét, #tel á vegyidet az (El^jHlJhklroxs'S-· -(prop-1 x-sniO-izofiaionitni.
  15. 22, Egy 1, igénypont szerinti vegyüiet, ahol a vegyüiet a 4veíih3,4~dshídík>xi4:d-fenil-2,6*dikarbonstni.
  16. 23, Egy 1, igéftypötiit sz#f# VegjtfMef, ahol a vagyaiéi a 4J*dihsdföXk2^4-k^eiii45enziirizgftáibhitni.
  17. 24, Egy 1, Igénypont szerinti vegyüiet, ahol a vegyüiet a 4(6“dihidroKÍ-2-(2-me-toxs~benzlí}d2ofíaiorsítnl.
  18. 25, Egy 1. igénypont szerinti vegyüiet, ahol a vegyüiet a 2-{3:S"dimetii-benzli>‘ 4!5'-dihidroxi4zohaioniiril,
  19. 28, Egy 1, Igénypont szerinti vegyüiet, ahol a vegyüiet a 2''{4~etil-benzii)~4,5-db hídroxhizoftaionitrií.
    27, Egy 1, igénypont szerinti vegyidet, ahol a vegyidet a 4,5xühkiroxs-242-me-tlhprop-t -ensh-izoftaionitsii.
    28, Egy 1, igénypont szerinti vegyüíet ahol a vegyüíet a 4s5'dihidroxi'2'-vinii-nzoftaionitni,
  20. 29, Egy 1. igénypont szénné vegyüíet ahol a vegyidet a 4,Soiibidroxi"2~(p?x5p~ Ί - 8 rs- 2 η i i n zo fia ίο n it rí i,
  21. 38, Egy 1. igénypont szerinti vágyóiét, ahol a vagyaiét a: 242-atpxt~tiáZél“S->-ít^ -4,5-d i h i d roxMzotta í on itrli, 31 < Egy 1, igénypont szerinti vegyüíet, ahol a vegyüíet a 2~a0iM:5néhkiroxl·· 'izoftalonitril.
    32, Egy 1, igénypont szerinti vegyilei, ahéi a vegyulet a 3,4<iiMd?ó)&amp;4M2b*· propil'blfenil-S^-ciikarbonitni,
    33, Egy 1, igénypont szerinti vagyaiéi ahoi a vegyüíet a 3,4<1 i h i d nxx i ~ 4' ~ p ro p i b 'bifenil«2.8~dikarbonitnl.
    34, Egy 1. igénypont szedné vagy diai, ahol a vagyaiéi a 3:4--díhidroxi*3,.4'~dl~ metihbifenih2;6~dlkarbonÍtnl,
    33, Egy 1, igénypont szerinti yegyüiéi ahol: a vegyCM a 4ih4t5-dihidroxi~izoftaioditrlf.
    38, Egy 1. igénypont szerinti vegyüíet, ahol a vegyüíet a 4,6-dihidroxi -2-(t-izo·· bytiMH«pirazol-4-tl)-izoftalonitní.
    37, Egy 1, igénypont szerinti vpgyütei, ahol a Vegyült! a.ll^diHidtOMNaniéílb' 'bifenil'-S^S-'dikarbonitni,
    38, Egy 1, igénypont szerinti vegyüíet, ahol a vegyüíet a 244llhfinii4ioMJr -dihidroxí-izofiaíonitrsl,
  22. 39, Egy 1, Igénypont szerinti vegyüíet, ahoi a vegyüíet a 4,5<JihidroxidMo4oíia 4idiazpfta!onJtnÍ, 40, * Egy 1, igénypont szeré# wgyüiet ahol tox afaníl-ti o}- ízofta Ιο n ítrí 1,
  23. 41, Egy 1. Igénypont szerinti vegyüíet, ahoi a vegyüíet a 3,4-dihid?Oxi-4'~me-toxi>bífenii-2.6-dikarbonitrii,
  24. 42, Egy 1. igénypont szerinti vegyilét, ahol a vegyüíet a 2~C2-e!iR>enzli}'4,5~dl· hidroxblzoftaloníinh
  25. 43, Egy 1-42. igénypontok bármelyike szerinti vegyüíet gyógyszerként való alkalmazásra.
  26. 44. Egy 1-42. igénypontok bármelyike szerinti vegyület egy olyan betegség vagy körülmény kezelésében való alkalmazásra, amely esel eben egy CÖMT gátló szer használhatóként van indikálva. 4S<. Egy 44. Igényperé szerinti vágyóiét, ahol a betegség a Parkinsomker. 4!L Gyógyszerkészítmény, amely hatóanyagként tartalmaz legalább egy, az 1-42. igénypontok bármelyike szeriná vegyületet valamiéi egy gégyszerészefiíeg elfogadható hordozót, hígítói., kötőanyagot vagy ezek keverékét 4?. Egy 46, Igénypont szerinti gyógyszerkészítmény, -ahol a készítmény továbbá tartalmaz legalább egy további hatóanyagét,
  27. 48. Egy 47. igénypont szerinti gyógyszerkészítmény, ahol a készimény ievodopaá és carbidopa-t tartalmaz.
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