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    • 5. 发明申请
    • SUBSTITUTED AMINO HETEROCYCLES AS VR-1 ANTAGONISTS FOR TREATING PAIN
    • 作为VR-1拮抗剂治疗疼痛的替代氨基酸异种
    • WO2004074290A1
    • 2004-09-02
    • PCT/GB2004/000702
    • 2004-02-20
    • MERCK SHARP & DOHME LIMITEDBROWN, Rebecca, ElizabethBURKAMP, FrankDOUGHTY, Victoria, AlexandraFLETCHER, Stephen, RobertHOLLINGWORTH, Gregory, JohnJONES, Brian, A.SPAREY, Timothy, Jason
    • BROWN, Rebecca, ElizabethBURKAMP, FrankDOUGHTY, Victoria, AlexandraFLETCHER, Stephen, RobertHOLLINGWORTH, Gregory, JohnJONES, Brian, A.SPAREY, Timothy, Jason
    • C07D487/04
    • C07D471/04C07D487/04
    • The present invention provides compounds of formula I: in which: one of T 1 and T 4 is N and the other is C; T 2 and T 3 are independently N or C(CH 2 ) n R 2 ; X, Y and Z are independently N or C(CH 2 ) n R 3 ; R 1 is Ar 1 or R 1 is C 1-6 alkyl optionally substituted with one or two groups Ar1; Ar1 is an optionally substituted cyclohexyl, piperidinyl, piperazinyl, morpholinyl, adamantyl, phenyl, naphthyl, a six - membered heteroaromatic ring containing one, two or three nitrogen atoms, a five-membered heteroaromatic ring containing one, two, three or four heteroatoms chosen from O, N and S, at most one O or S atom being present, or a nine - or ten - membered bicyclic heteroaromatic ring in which phenyl or a six - membered heteroaromatic ring as defined above is fused to a six - or five - membered heteroaromatic ring as defined above; Ar is an optionally substituted phenyl, a six - membered heteroaromatic ring containing one, two or three nitrogen atoms or a five - membered heteroaromatic ring containing one, two, three or four heteroatoms chosen from O, N and S, at most one heteroatom being O or S, Ar being optionally substituted by one, two or three groups chosen from halogen, CF 3 , OCF 3 , C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, nitro, cyano, isonitrile, hydroxy, C 1-6 alkoxy, C 1-6 alkylthio, -NR 6 R 7 , -CONR 6 R 7 , -COH, CO 2 H, C 1-6 alkoxycarbonyl, haloC 1-6 alkyl, hydroxyC 1-6 alkyl, aminoC 1-6 alkyl, C 1-6 alkylcarbonyl and a five - membered heteroaromatic ring containing one, two, three or four heteroatoms chosen from O, N and S, at most one heteroatom being O or S, optionally substituted by C 1-6 alkyl, halogen, amino, hydroxy or cyano; or a pharmaceutically acceptable salt thereof as a VR-1 ligand; pharmaceutical compositions comprising it; its use in therapy; use of it in the manufacture of a medicament to treat pain; and methods of treating subjects suffering from pain.
    • 本发明提供了式I化合物:其中:T 1和T 4中的一个是N,另一个是C; T 2和T 3独立地是N或C(CH 2)n R 2; X,Y和Z独立地为N或C(CH 2)n R 3; R 1是Ar 1或R 1是任选被一个或两个Ar 1基团取代的C 1-6烷基; Ar1是任选取代的环己基,哌啶基,哌嗪基,吗啉基,金刚烷基,苯基,萘基,含有一个,两个或三个氮原子的六元杂芳环,含有一个,两个,三个或四个的五元杂芳环 选自O,N和S,至多存在一个O或S原子的杂原子,或其中如上所定义的苯基或六元杂芳环的九个或十元二环杂芳环是 与如上定义的六个或五元杂芳族杂环稠合; Ar是任选取代的苯基,含有一个,两个或三个氮原子的六元杂芳族环或含有一个,两个,三个或四个选自O,N和S的杂原子的五元杂芳环,在 大多数一个杂原子是O或S,Ar任选被一个,两个或三个选自卤素,CF 3,OCF 3,C 1-6烷基,C 2-6烯基,C 2-6炔基,硝基,氰基,异氰酸酯,羟基,C 1-6烷氧基 ,C 1-6烷硫基,-NR 6 R 7,-CONR 6 R 7,-COH,CO 2 H,C 1-6烷氧基羰基,卤代C 1-6烷基,羟基C 1-6烷基,氨基C 1-6烷基,C 1-6烷基羰基和 含有一个,两个,三个或四个选自O,N和S的杂原子的五元杂芳环,最多一个杂原子是O或S,任选被C 1-6烷基,卤素,氨基,羟基或氰基取代; 或其药学上可接受的盐作为VR-1配体; 包含它的药物组合物; 其用于治疗; 在制造治疗疼痛的药物中的用途; 以及治疗痛苦患者的方法。
    • 9. 发明申请
    • E-FLUORO-4-(PYRIDIN-2-YL)-PIPERIDINE-1-CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1) FOR THE TREATMENT OF PAIN
    • E-FLOROR-4-(PYRIDIN-2-YL) - 哌啶-1-羧酰胺衍生物及其相关化合物,其调节VANILLOID-1受体(VR1)用于治疗疼痛的功能
    • WO2005051390A1
    • 2005-06-09
    • PCT/GB2004/004538
    • 2004-10-27
    • MERCK SHARP & DOHME LIMITEDBAYLISS, TracyBROWN, Rebecca, ElizabethBURKAMP, FrankJONES, A., BrianNEDUVELIL, Joseph, George
    • BAYLISS, TracyBROWN, Rebecca, ElizabethBURKAMP, FrankJONES, A., BrianNEDUVELIL, Joseph, George
    • A61K31/4545
    • C07D451/04C07D401/04
    • Compounds of formula (I): wherein: A 1 is phenyl, a six-membered aromatic heterocycle containing one, two or three nitrogen atoms, or a five-membered aromatic heterocycle containing up to four heteroatoms chosen from O, N and S, at most one heteroatom being O or S; A 2 is phenyl, a six-membered aromatic heterocycle containing one, two or three nitrogen atoms, or a five-membered aromatic heterocycle containing up to four heteroatoms chosen from 0, N and S, at most one heteroatom being O or S; L is a bond or C 1-6 alkylene; R 1 and R 2 independently chosen from hydrogen and C 1-6 alkyl or R l and R 2 may, together, form a methylene or ethylene bridge; W is halogen, C 1-6 alkyl, haloC 1-6 alkyl, C 1-6 alkoxy or haloC 1-6 alkoxy; X is O, S or NR 3 or X, together with the atom to which it is attached, and Y, form an unsaturated five-membered ring together with A 2 ; Y is a bond, C 1-4 alkylene, NH or NH(CH 2 ) 1-3 ; or a pharmaceutically acceptable salt thereof; other substituents are defined in claim 1; which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).
    • 式(I)的化合物:其中:A 1是苯基,含有一个,两个或三个氮原子的六元芳族杂环,或含有至多四个选自O,N和S的杂原子的五元芳族杂环 至多一个杂原子是O或S; A 2是苯基,含有一个,两个或三个氮原子的六元芳族杂环,或含有至多四个选自0,N和S的杂原子的五元芳族杂环,最多一个杂原子是O或S ; L是键或C1-6亚烷基; R 1和R 2独立地选自氢和C 1-6烷基或R 1和R 2可以一起形成亚甲基或亚乙基桥; W是卤素,C 1-6烷基,卤代C 1-6烷基,C 1-6烷氧基或卤代C 1-6烷氧基; X是O,S或NR 3或X,连同其所连接的原子,Y与A 2一起形成不饱和五元环; Y是键,C1-4亚烷基,NH或NH(CH2)1-3; 或其药学上可接受的盐; 其它取代基如权利要求1中所定义; 其可用作治疗化合物,特别是用于治疗通过调节香草素-1受体(VR1)的功能而改善的疼痛和其它病症。