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2. 发明申请

WO2004074290A1 SUBSTITUTED AMINO HETEROCYCLES AS VR-1 ANTAGONISTS FOR TREATING PAIN 审中-公开
标题翻译：作为VR-1拮抗剂治疗疼痛的替代氨基酸异种
公开(公告)号：WO2004074290A1
公开(公告)日：2004-09-02
申请号：PCT/GB2004/000702
申请日：2004-02-20
申请人： MERCK SHARP & DOHME LIMITED , BROWN, Rebecca, Elizabeth , BURKAMP, Frank , DOUGHTY, Victoria, Alexandra , FLETCHER, Stephen, Robert , HOLLINGWORTH, Gregory, John , JONES, Brian, A. , SPAREY, Timothy, Jason
发明人： BROWN, Rebecca, Elizabeth , BURKAMP, Frank , DOUGHTY, Victoria, Alexandra , FLETCHER, Stephen, Robert , HOLLINGWORTH, Gregory, John , JONES, Brian, A. , SPAREY, Timothy, Jason
IPC分类号： C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： 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.
摘要翻译：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。

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