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    • 5. 发明申请
      WO2004074290A1 SUBSTITUTED AMINO HETEROCYCLES AS VR-1 ANTAGONISTS FOR TREATING PAIN 审中-公开
    • 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 LIMITED , BROWN, Rebecca, Elizabeth , BURKAMP, Frank , DOUGHTY, Victoria, Alexandra , FLETCHER, Stephen, Robert , HOLLINGWORTH, Gregory, John , JONES, Brian, A. , SPAREY, Timothy, Jason
    • BROWN, Rebecca, Elizabeth , BURKAMP, Frank , DOUGHTY, Victoria, Alexandra , FLETCHER, Stephen, Robert , HOLLINGWORTH, Gregory, John , JONES, Brian, A. , SPAREY, Timothy, Jason
    • C07D487/04
    • C07D471/04 , C07D487/04
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 9. 发明申请
      WO2005051390A1 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 审中-公开
    • 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 LIMITED , BAYLISS, Tracy , BROWN, Rebecca, Elizabeth , BURKAMP, Frank , JONES, A., Brian , NEDUVELIL, Joseph, George
    • BAYLISS, Tracy , BROWN, Rebecca, Elizabeth , BURKAMP, Frank , JONES, A., Brian , NEDUVELIL, Joseph, George
    • A61K31/4545
    • C07D451/04 , C07D401/04
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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