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1. 发明申请

WO2004046133A1 AMINO-HETEROCYCLES AS VR-1 ANTAGONISTS FOR TREATING PAIN 审中-公开
标题翻译： AMINO-HETEROCYCLES作为VR-1拮抗剂治疗疼痛
公开(公告)号：WO2004046133A1
公开(公告)日：2004-06-03
申请号：PCT/GB2003/004969
申请日：2003-11-14
申请人： MERCK SHARP & DOHME LIMITED , BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen, Robert , HOLLINGWORTH, Gregory, John , JONES, A., Brian , MCIVER, Edward, Giles , MOYES, Christopher, Richard , ROGERS, Lauren
发明人： BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen, Robert , HOLLINGWORTH, Gregory, John , JONES, A., Brian , MCIVER, Edward, Giles , MOYES, Christopher, Richard , ROGERS, Lauren
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D471/04
摘要： the present invention provides a compound of formula (I): wherein V represents NR 5 , O, S, SO or S(O) 2 ; W and X each independently represent CH or N; Y represents N, CH or C-Ar 2 , with the proviso that at least one, but no more than two, of W, X and Y are N; Z represents CH or C-Ar 2 , with the proviso that when Y is N or CH then Z is C-Ar 2 , and with the further proviso that when Y is C-Ar 2 then Z is CH; Ar 1 represents a fused 9 or 10 membered heterobicyclic ring system containing one, two, three or four heteroatoms selected from nitrogen, oxygen and sulfur, wherein at least one of the rings in said ring system is aromatic; Ar 2 represents an aromatic ring selected from phenyl, pyridyl, pyrimidinyl and pyridazinyl which is optionally fused and substituted; R 1 represents halogen, hydroxy, oxo, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, haloC 1-6 alkyl, hydroxyC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, hydroxyC 1-6 alkoxy, C 3-7 cycloalkyl, C 3-7 cycloalkoxy, C 3-5 cycloalkylC 1-4 alkyl, cyano, nitro, SR 6 , SOR 6 , SO 2 R 6 , COR 6 , NR 3 COR 6 , CONR 3 R 4 , NR 3 SO 2 R 6 , SO 2 NR 3 R 4 , -(CH 2 ) m carboxy, esterified -(CH 2 ) m carboxy or -(CH 2 ) m NR 3 R 4 ; R 2 represents hydrogen, halogen, hydroxy, C 1-6 alkyl, haloC 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, unsubstituted phenyl or phenyl substituted with one or two groups selected from halogen, C 1-6 alkyl, haloC 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkoxy or haloC 1-6 alkoxy; R 3 and R 4 are each independently hydrogen, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-7 cycloalkyl or fluoroC 1-6 alkyl; or R 3 and R 4 and the nitrogen atom to which they are attached together form a heteroaliphatic ring of 4 to 7 ring atoms, optionally substituted by one or two groups selected from hydroxy or C 1-4 alkoxy, which ring may optionally contain as one of the said ring atoms an oxygen or a sulfur atom, S(O), S(O) 2 , or NR 5 ; R 5 represents hydrogen, C 1-4 alkyl, hydroxyC 1-4 alkyl or C 1-4 alkoxyC 1-4 alkyl; R 6 represents hydrogen, C 1-6 alkyl, fluoroC 1-6 alkyl, C 3-7 cycloalkyl, unsubstituted phenyl, or phenyl substituted with one or two groups selected from halogen, C 1-6 alkyl, haloC 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkoxy or haloC 1-6 alkoxy; m is either zero or an integer from 1 to 4; n is either zero or an integer from 1 to 3; or a pharmaceutically acceptable salt, N-oxide or a prodrug thereof; a pharmaceutical composition comprising it; its use in methods of treatment; use of it for the manufacture of a medicament for treating VR-1 related conditions such as those in which pain and/or inflammation predominate; and methods of treatment using it.
摘要翻译：本发明提供式（I）化合物：其中V表示NR 5，O，S，SO或S（O）2; W和X各自独立地表示CH或N; Y表示N，CH或C-Ar2，条件是W，X和Y中至少一个，但不超过两个为N; Z表示CH或C-Ar2，条件是当Y为N或CH时，则Z为C-Ar2，进一步条件是当Y为C-Ar 2时，Z为CH; Ar 1表示含有选自氮，氧和硫的一个，两个，三个或四个杂原子的稠合的9或10元杂双环体系，其中所述环系中的至少一个环是芳族的; Ar2表示任选稠合和取代的选自苯基，吡啶基，嘧啶基和哒嗪基的芳环; R 1表示卤素，羟基，氧代，C 1-6烷基，C 2-6烯基，C 2-6炔基，卤代C 1-6烷基，羟基C 1-6烷基，C 1-6烷氧基，卤代C 1-6烷氧基，羟基C 1-6烷氧基，C 3-7环烷基，C 3-7环烷氧基，C 3-8环烷基C 1-4烷基，氰基，硝基，SR 6，SOR 6，SO 2 R 6，COR 6，NR 3 COR 6，CONR 3 R 4，NR SO 2 R 6，SO 2 NR 3 R 4， - （CH 2）m羧基，酯化 - （CH 2）m羧基或 - （CH 2）m NR 3 R 4; R 2表示氢，卤素，羟基，C 1-6烷基，卤代C 1-6烷基，C 3-7环烷基，C 1-6烷氧基，卤代C 1-6烷氧基，未取代的苯基或被一个或两个选自卤素，C 1-6烷基，卤代C C 1-6烷基，C 3-7环烷基，C 1-6烷氧基或卤代C 1-6烷氧基; R 3和R 4各自独立地为氢，C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-7环烷基或氟C 1-6烷基; 或R 3和R 4并且它们所连接的氮原子一起形成4至7个环原子的杂脂肪族环，任选地被一个或两个选自羟基或C 1-4烷氧基的基团取代，该环可任选地被含有所述环原子之一为氧或硫原子，S（O），S（O）2或NR 5; R 5表示氢，C 1-4烷基，羟基C 1-4烷基或C 1-4烷氧基C 1-4烷基; R 6表示氢，C 1-6烷基，氟C 1-6烷基，C 3-7环烷基，未取代的苯基或被一个或两个选自卤素，C 1-6烷基，卤代C 1-6烷基，C 3-7环烷基，C 1-6烷氧基或C 1-6烷基的基团取代的苯基 haloC1-6alkoxy; m为零或1至4的整数; n为0或1至3的整数; 或其药学上可接受的盐，N-氧化物或其前药; 包含它的药物组合物; 其用于治疗方法; 使用它来制造用于治疗VR-1相关病症的药物，例如其中疼痛和/或炎症占优势的病症; 和治疗方法

2. 发明申请

WO2004099177A1 SUBSTITUTED-1-PHTHALAZINAMINES AS VR-1 ANTAGONISTS 审中-公开
标题翻译：作为VR-1拮抗剂的替代1-苯二胺
公开(公告)号：WO2004099177A1
公开(公告)日：2004-11-18
申请号：PCT/GB2004/001942
申请日：2004-05-04
申请人： MERCK SHARP & DOHME LIMITED , BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen, Robert , JONES, Brian, A. , MCIVER, Edward, Giles
发明人： BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen, Robert , JONES, Brian, A. , MCIVER, Edward, Giles
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D403/04 , C07D471/04
摘要： The present invention provides a compound of formula (I): in which Ar and R 1 are phenyl or a heteroaromatic group, R 2 is generally hydrogen, R 3 is hydrogen or alkyl and X, Y and Z are generally CH or N as VR-1 antagonists; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; use of it to manufacture medicaments to treat pain or inflammation; and methods of treating pain or inflammation.
摘要翻译：本发明提供式（I）化合物：其中Ar和R 1为苯基或杂芳基，R 2通常为氢，R 3为氢或烷基，X，Y和Z为通常CH或N作为VR-1拮抗剂; 或其药学上可接受的盐; 包含它的药物组合物; 其用于治疗; 使用它来制造治疗疼痛或炎症的药物; 以及治疗疼痛或炎症的方法。

3. 发明申请

WO2007054739A1 TETRAHYDROINDOLE DERIVATIVES FOR TREATMENT OF ALZHEIMER'S DISEASE 审中-公开
标题翻译：用于治疗阿尔茨海默病的四氢吡啶衍生物
公开(公告)号：WO2007054739A1
公开(公告)日：2007-05-18
申请号：PCT/GB2006/050368
申请日：2006-11-03
申请人： MERCK SHARP & DOHME LIMITED , BURKAMP, Frank , CHECKSFIELD, Graham, David , FLETCHER, Stephen, Robert , LEWIS, Stephen, John , MCIVER, Edward, Giles , OAKLEY, Paul, Joseph , TEALL, Martin, Richard
发明人： BURKAMP, Frank , CHECKSFIELD, Graham, David , FLETCHER, Stephen, Robert , LEWIS, Stephen, John , MCIVER, Edward, Giles , OAKLEY, Paul, Joseph , TEALL, Martin, Richard
IPC分类号： C07D209/30 , C07D209/42 , C07D209/08 , C07D405/04 , C07D231/56 , C07D209/86 , C07D401/04 , A61K31/403 , A61K31/404 , A61K31/416 , A61P25/28
CPC分类号： C07D209/30 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/42 , C07D209/86 , C07D231/56 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.
摘要翻译：公开了式（I）的四氢吲哚衍生物：这些化合物调节γ-分泌酶的活性，因此可用于治疗或预防阿尔茨海默病。

4. 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。

5. 发明申请

WO2004014865A1 PHENYLPYRIDAZINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS 审中-公开
标题翻译：作为GABA受体配体的苯基吡啶衍生物
公开(公告)号：WO2004014865A1
公开(公告)日：2004-02-19
申请号：PCT/GB2003/003376
申请日：2003-08-04
申请人： MERCK SHARP & DOHME LIMITED , BLACKABY, Wesley, Peter , BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen, Robert , JENNINGS, Andrew , LEWIS, Richard, Thomas , MACLEOD, Angus, Murray , STREET, Leslie, Joseph , THOMAS, Steve , VAN NIEL, Monique, Bodil , WILSON, Kevin
发明人： BLACKABY, Wesley, Peter , BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen, Robert , JENNINGS, Andrew , LEWIS, Richard, Thomas , MACLEOD, Angus, Murray , STREET, Leslie, Joseph , THOMAS, Steve , VAN NIEL, Monique, Bodil , WILSON, Kevin
IPC分类号： C07D237/24
CPC分类号： C07D231/12 , C07D233/56 , C07D237/08 , C07D237/14 , C07D237/20 , C07D237/24 , C07D249/08 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D409/04 , C07D417/14
摘要： A class of 4-phenylpyridazine derivatives of Formula (I), being selective ligands for GABA A receptors, in particular having high affinity for the α2 and/or α3 and or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译：一类式（I）的4-苯基哒嗪衍生物，作为GABA A受体的选择性配体，特别是对α2和/或其α3和α5亚基具有高亲和力，因此在治疗和/或预防中枢神经系统的不利条件，包括焦虑，抽搐和认知障碍。

6. 发明申请

WO2002081474A1 TRIAZOLOPHTHALAZINE / QUINOLINE / ISOQUINOLINE DERIVATIVES WHICH ARE LIGANDS FOR GABA-A RECEPTORS CONTAINING THE ALPHA 5 SUBTYPE 审中-公开
标题翻译：用于含有ALPHA 5亚型的GABA-A受体的配体的三唑盐/喹啉/异喹啉衍生物
公开(公告)号：WO2002081474A1
公开(公告)日：2002-10-17
申请号：PCT/GB2002/001502
申请日：2002-03-28
申请人： MERCK SHARP & DOHME LIMITED , BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen, Robert
发明人： BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen, Robert
IPC分类号： C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention provides a compound of formula (I): in which R 1 is an aromatic or heteroaromatic ring, M is a bond, -CH 2 -, -O- or -S-, R 2 , R 3 and R 4 are as defined herein, and X, Y and Z generally define a 1,2,4-triazolo[3,4-a]phthalazine, 1,2,3-triazolo[1,5-a]quinoline or 1,2,4-triazolo[3,4-a]isoquinoline core, as a ligand for GABA-A receptors containing the alpha 5 subtype and which is preferably an inverse agonist thereat and is thus useful for enhancing cognition in conditions such as Alzheimer's disease, compositions containing it, its use in therapy, use of it for making medicaments and methods of treatment using it.
摘要翻译：本发明提供式（I）化合物：其中R 1是芳族或杂芳族环，M是一个键，-CH 2 - ， - O-或-S-，R 2，R 3 和R 4如本文所定义，X，Y和Z通常定义1,2,4-三唑并[3,4-a]酞嗪，1,2,3-三唑并[1,5-a] 喹啉或1,2,4-三唑并[3,4-a]异喹啉核，作为含有α5亚型的GABA-A受体的配体，优选为其反向激动剂，因此可用于增强作为阿尔茨海默病，含有它的组合物，其在治疗中的用途，其用于制备药物的用途和使用它的治疗方法。

7. 发明申请

WO2005080391A1 PRODRUGS OF SUBSTITUTED AMINO HETEROBICYCLES WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1) 审中-公开
标题翻译：调节VANILLOID-1受体（VR1）功能的替代氨基杂环化合物的产物
公开(公告)号：WO2005080391A1
公开(公告)日：2005-09-01
申请号：PCT/GB2005/000548
申请日：2005-02-16
申请人： MERCK SHARP & DOHME LIMITED , BURKAMP, Frank , CASTRO PINEIRO, Jose Luis , HOLLINGWORTH, Gregory John
发明人： BURKAMP, Frank , CASTRO PINEIRO, Jose Luis , HOLLINGWORTH, Gregory John
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds of formula (I) 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).
摘要翻译：可用作治疗化合物的式（I）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。

8. 发明申请

WO2005049601A1 INDAZOL-3-ONES AND ANALOGUES AND DERIVATIVES THEREOF WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1) 审中-公开
标题翻译：调节VANILLOID-1受体（VR1）功能的INDAZOL-3-ONES及其衍生物及其衍生物
公开(公告)号：WO2005049601A1
公开(公告)日：2005-06-02
申请号：PCT/GB2004/004809
申请日：2004-11-12
申请人： MERCK SHARP & DOHME LIMITED , BURKAMP, Frank , FLETCHER, Stephen, Robert
发明人： BURKAMP, Frank , FLETCHER, Stephen, Robert
IPC分类号： C07D401/04
CPC分类号： C07D231/56 , C07D401/04 , C07D471/04
摘要： Compounds of formula (I), 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).
摘要翻译：可用作治疗化合物的式（I）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。

9. 发明申请

WO2006008558A1 ARYLACETIC ACIDS AND RELATED COMPOUNDS FOR TREATMENT OF ALZHEIMER’S DISEASE 审中-公开
标题翻译：用于治疗阿尔茨海默病的ARYLACETIC酸和相关化合物
公开(公告)号：WO2006008558A1
公开(公告)日：2006-01-26
申请号：PCT/GB2005/050114
申请日：2005-07-19
申请人： MERCK SHARP & DOHME LIMITED , BLURTON, Peter , BURKAMP, Frank , CHURCHER, Ian , HARRISON, Timothy , NEDUVELIL, Joseph
发明人： BLURTON, Peter , BURKAMP, Frank , CHURCHER, Ian , HARRISON, Timothy , NEDUVELIL, Joseph
IPC分类号： A61K31/215
CPC分类号： A61K31/215
摘要： Compounds of formula I are useful in treatment of diseases associated with the deposition of β-amyloid in the brain.
摘要翻译：式I化合物可用于治疗与脑中β-淀粉样蛋白沉积相关的疾病。

10. 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
标题翻译： 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
公开(公告)号：WO2005051390A1
公开(公告)日：2005-06-09
申请号：PCT/GB2004/004538
申请日：2004-10-27
申请人： MERCK SHARP & DOHME LIMITED , BAYLISS, Tracy , BROWN, Rebecca, Elizabeth , BURKAMP, Frank , JONES, A., Brian , NEDUVELIL, Joseph, George
发明人： BAYLISS, Tracy , BROWN, Rebecca, Elizabeth , BURKAMP, Frank , JONES, A., Brian , NEDUVELIL, Joseph, George
IPC分类号： A61K31/4545
CPC分类号： C07D451/04 , C07D401/04
摘要： 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).
摘要翻译：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。

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