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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

WO2005047280A1 SUBSTITUTED NITROGEN-CONTAINING SIX-MEMBERED AMINO-HETEROCYCLES AS VANILLOID-1 RECEPTOR ANTAGONISTS FOR TREATING PAIN 审中-公开
标题翻译：用作治疗疼痛的VANILLOID-1受体拮抗剂的含有NITRUTED的含六聚氨基甲酰胺的氨基酸
公开(公告)号：WO2005047280A1
公开(公告)日：2005-05-26
申请号：PCT/GB2004/004730
申请日：2004-11-09
申请人： MERCK SHARP & DOHME LIMITED , MERCK & CO. INC. , CAI, Dongwei , HOLLINGWORTH, Gregory, John , JONES, A., Brian , MCIVER, Edward, Giles , MOYES, Christopher, Richard , ROGERS, Lauren
发明人： CAI, Dongwei , HOLLINGWORTH, Gregory, John , JONES, A., Brian , MCIVER, Edward, Giles , MOYES, Christopher, Richard , ROGERS, Lauren
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D471/04
摘要： The present invention provides a compound of formula(I): Y-J-NH-Z (I) wherein: Y is a quinoline or isoquinoline optionally substituted with one or two substituents independently chosen from halogen, haloC 1-4 alkyl, C 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, nitro and amino; J is pyridine, pyridazine, pyrazine, pyrimidine or triazine optionally substituted with one or two substituents independently chosen from halogen, haloC 1-4 alkyl, C 1-4 alkyl, C 3-5 cycloalkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, nitro and amino; wherein J is substituted at positions meta to each other by NH and Y; and Z is phenyl or pyridyl optionally substituted with one or two substituents independently elected from halogen, haloC 1-4 alkyl, C 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, nitro and amino; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions containing the same; the compound for use in therapy; and use of the compound for the manufacture of a medicament for treating or preventing diseases requiring administration of an antagonist of the vanilloid-1 (VR1) receptor.
摘要翻译：本发明提供式（I）化合物：YJ-NH-Z（I）其中：Y是喹啉或异喹啉，其任选地被一个或两个独立地选自卤素，卤代C 1-4烷基，C 1-4烷基，C 1 -4-烷氧基，卤代C 1-4烷氧基，硝基和氨基; J是吡啶，哒嗪，吡嗪，嘧啶或三嗪，任选地被一个或两个独立地选自卤素，卤代C 1-4烷基，C 1-4烷基，C 3-5环烷基，C 1-4烷氧基，卤代C 1-4烷氧基，硝基和氨基 ; 其中J在NH和Y彼此间位置取代; Z是任选被一个或两个独立地选自卤素，卤代C 1-4烷基，C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，硝基和氨基的取代基取代的苯基或吡啶基; 或其药学上可接受的盐; 含有该组合物的药物组合物; 用于治疗的化合物; 以及该化合物在制备用于治疗或预防需要施用香草素-1（VR1）受体拮抗剂的疾病的药物中的用途。

3. 发明申请

WO2005047279A1 SUBSTITUTED NITROGEN-CONTAINING SIX-MEMBERED AMINO-HETEROCYCLES AS VANILLOID-1 RECEPTOR ANTAGONISTS FOR TREATING PAIN 审中-公开
标题翻译：用作治疗疼痛的VANILLOID-1受体拮抗剂的含有NITRUTED的含六聚氨基甲酰胺的氨基酸
公开(公告)号：WO2005047279A1
公开(公告)日：2005-05-26
申请号：PCT/GB2004/004719
申请日：2004-11-09
申请人： MERCK SHARP & DOHME LIMITED , HOLLINGWORTH, Gregory, John , JONES, A., Brian , MCIVER, Edward, Giles , MOYES, Christopher, Richard , ROGERS, Lauren
发明人： HOLLINGWORTH, Gregory, John , JONES, A., Brian , MCIVER, Edward, Giles , MOYES, Christopher, Richard , ROGERS, Lauren
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D471/04
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D471/04
摘要： The present invention provides a compound of formula (I): Y-J-NH-Z wherein: Y is a quinoline or isoquinoline optionally substituted with one or two substituents independently chosen from hydroxy, halogen, haloC 1-4 alkyl, C 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, nitro and amino; J is pyridine, pyridazine, pyrazine, pyrimidine or triazine optionally substituted with one or two substituents independently chosen from hydroxy, halogen, haloC 1-4 alkyl, C 1-4 alkyl, C 3-5 cycloalkyl, C 1-4 alkoxy, hydroxyC 1- 4 alkyl, cyano, hydroxy, C 1-4 cycloalkoxy, C 1-4 alkylthio, haloC 1-4 alkoxy, nitro, Q, (CH 2 ) p Q, NR 2 R 3 , -(CH 2 ) p NR 2 R 3 and -O(CH 2 ) p NR 2 R 3 ; wherein J is substituted at positions meta to each other by NH and Y; and Z is phenyl or pyridyl optionally substituted with one or two substituents independently selected from halogen, haloC 1-4 alkyl, C 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, nitro and amino; Q is phenyl, a five-membered heterocyclic ring containing one, two, three or four heteroatoms chosen from O, N and S, at most one heteroatom being O or S, or a six-membered heterocyclic ring containing one, two or three nitrogen atoms, optionally substituted by C 1-4 alkyl; each R 2 and R 3 is chosen from H and C 1-4 alkyl, or R 2 and R 3 , together with the nitrogen atom to which they are attached, may form a six-membered ring optionally containing an oxygen atom or a further nitrogen atom, which ring is optionally substituted by C 1-4 alkyl or Q; p is 1, 2 or 3; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in methods of therapy; use of it for manufacturing medicaments; and methods of using it to treat diseases requiring administration of a VR1 antagonist such as pain, cough, GERD and depression.
摘要翻译：本发明提供式（I）化合物：YJ-NH-Z其中：Y是喹啉或异喹啉，其任选地被一个或两个独立地选自羟基，卤素，卤代C 1-4烷基，C 1-4烷基，C 1-4烷氧基卤代C 1-4烷氧基，硝基和氨基; J是吡啶，哒嗪，吡嗪，嘧啶或三嗪，任选被一个或两个独立地选自羟基，卤素，卤代C 1-4烷基，C 1-4烷基，C 3-5烃基，C 1-4烷氧基，羟基C 1-4烷基，氰基，羟基，C 1 （CH 2）pQ，NR 2 R 3， - （CH 2）p NRR R 3和-O（CH 2）p NRR 2，其中R 1，R 2， > - [R <3>; 其中J在NH和Y彼此间位置取代; Z是任选被一个或两个独立地选自卤素，卤代C 1-4烷基，C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，硝基和氨基的取代基取代的苯基或吡啶基; Q是苯基，含有一个，两个，三个或四个选自O，N和S，至多一个杂原子是O或S的杂原子的五元杂环，或含有一个，两个或三个氮的六元杂环任选被C 1-4烷基取代的原子; 每个R 2和R 3选自H和C 1-4烷基，或R 2和R 3与它们所连接的氮原子一起可以形成任选含有氧原子或另外的氮原子，该环任选被C 1-4烷基或Q取代; p为1,2或3; 或其药学上可接受的盐; 包含它的药物组合物; 其用于治疗方法; 使用它制造药物; 以及使用它来治疗需要施用VR1拮抗剂例如疼痛，咳嗽，GERD和抑郁症的疾病的方法。

4. 发明申请

WO2005028445A2 HETEROAROMATIC UREAS WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1) 审中-公开
标题翻译：调整VANILLOID-1受体（VR1）的功能的异位性尿酸
公开(公告)号：WO2005028445A2
公开(公告)日：2005-03-31
申请号：PCT/GB2004/003968
申请日：2004-09-16
申请人： MERCK SHARP & DOHME LIMITED , FLETCHER, Stephen, Robert , HOLLINGWORTH, Gregory, John , JONES, A., Brian , MOYES, Christopher, Richard , ROGERS, Lauren
发明人： FLETCHER, Stephen, Robert , HOLLINGWORTH, Gregory, John , JONES, A., Brian , MOYES, Christopher, Richard , ROGERS, Lauren
IPC分类号： C07D231/00
CPC分类号： C07D275/04 , C07C275/28 , C07D209/34 , C07D231/56 , C07D235/06 , C07D263/56 , C07D307/79 , C07D471/04
摘要： Compounds of formula (I): 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）化合物可用作治疗化合物，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。

5. 发明申请

WO2003080578A1 HETEROAROMATIC UREA DERIVATIVES AS VR-1 RECEPTOR MODULATORS FOR TREATING PAIN 审中-公开
标题翻译：作为用于治疗疼痛的VR-1受体调节剂的异位尿素衍生物
公开(公告)号：WO2003080578A1
公开(公告)日：2003-10-02
申请号：PCT/GB2003/001302
申请日：2003-03-21
申请人： MERCK SHARP & DOHME LIMITED , BROWN, Rebecca, Elizabeth , DOUGHTY, Victoria, Alexandra , HOLLINGWORTH, Gregory, John , JONES, A., Brian , LINDON, Matthew, John , MOYES, Christopher, Richard , ROGERS, Lauren
发明人： BROWN, Rebecca, Elizabeth , DOUGHTY, Victoria, Alexandra , HOLLINGWORTH, Gregory, John , JONES, A., Brian , LINDON, Matthew, John , MOYES, Christopher, Richard , ROGERS, Lauren
IPC分类号： C07D215/38
CPC分类号： C07D401/12 , C07D215/38 , C07D217/02 , C07D217/08 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The present invention provides compounds of formula (I); pharmaceutically acceptable salts and N-oxides thereof in which A, B, D and E are C or N with the proviso that one or more are N, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are simple substituents, n is 0-3 and y is an aryl, heteroaryl, carbocyclyl or fused-carbocyclyl group; as VR-1 antagonists for treating conditions or diseases in which pain and/or inflammation predominates; the use of the same for manufacturing medicaments, pharmaceutical compositions comprising them and methods of treatment utilising them.
摘要翻译：本发明提供式（I）化合物; 其中A，B，D和E为C或N，其条件是一个或多个为N，R 1，R 2，R 3，R 4， R 5和R 6是简单取代基，n是0-3，y是芳基，杂芳基，碳环基或稠合碳环基; 作为用于治疗其中疼痛和/或炎症占优势的病症或疾病的VR-1拮抗剂; 使用它们制造药物，包含它们的药物组合物和使用它们的治疗方法。

6. 发明申请

WO2006122200A1 2,3-SUBSTITUTED FUSED BICYCLIC PYRIMIDIN-4(3H)-ONES MODULATING THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1) 审中-公开
标题翻译： 2,3-取代的双酚二吡啶-4（3H） - 调节VANILLOID-1受体（VR1）的功能
公开(公告)号：WO2006122200A1
公开(公告)日：2006-11-16
申请号：PCT/US2006/018119
申请日：2006-05-10
申请人： MERCK SHARP & DOHME LIMITED , NEUROGEN CORPORATION , BROWN, Rebecca Elizabeth , HUMPRIES, Alexander Charles , ROGERS, Lauren , BAYLISS, Tracey , JONES, A., Brian , MOYES, Christopher Richard , HOLLINGWORTH, Gregory John , BLUM, Charles, A. , ZHENG, Xiaozhang , BAKTHALVATCHALAM, Rajagopal , CAPITOSTI, Scott
发明人： BROWN, Rebecca Elizabeth , HUMPRIES, Alexander Charles , ROGERS, Lauren , BAYLISS, Tracey , JONES, A., Brian , MOYES, Christopher Richard , HOLLINGWORTH, Gregory John , BLUM, Charles, A. , ZHENG, Xiaozhang , BAKTHALVATCHALAM, Rajagopal , CAPITOSTI, Scott
IPC分类号： C07D495/04 , C07D513/04 , C07D473/00 , A61K31/495 , A61P11/00 , A61P29/00
CPC分类号： C07D495/04 , C07D473/00 , C07D513/04
摘要： The use of a compound of formula (I): for the manufacture of a medicament for the treatment of conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1, also known as TRPV1).
摘要翻译：使用式（I）化合物：用于制备用于治疗通过调节香草素-1受体（VR1，也称为TRPV1）的功能而改善的病症的药物。

7. 发明申请

WO2006100520A1 2,3-SUBSTITUTED FUSED PYRIMIDIN-4(3H)-ONES AS VR1 ANTAGONISTS 审中-公开
标题翻译：作为VR1拮抗剂的2,3-取代的氟吡啶-4（3H） - 酮
公开(公告)号：WO2006100520A1
公开(公告)日：2006-09-28
申请号：PCT/GB2006/050060
申请日：2006-03-21
申请人： MERCK SHARP & DOHME LIMITED , BAYLISS, Tracy , BROWN, Rebecca Elizabeth , HOLLINGWORTH, Gregory John , JONES, A. Brian , MOYES, Christopher Richard , ROGERS, Lauren
发明人： BAYLISS, Tracy , BROWN, Rebecca Elizabeth , HOLLINGWORTH, Gregory John , JONES, A. Brian , MOYES, Christopher Richard , ROGERS, Lauren
IPC分类号： C07D473/32 , C07D471/04 , C07D495/04 , C07D513/04 , A61K31/522 , A61P29/00
CPC分类号： C07D473/18 , C07D471/04 , C07D495/04
摘要： A compound of formula (I), wherein W is formula (1); A is a benzene ring, a fÊve-membered heteroaromatic ring containing 1, 2 or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S atom is present, or a six- membered heteroaromatic ring containing 1, 2 or 3 N atoms; n is zero, one, two or three; when n is zero or one, V is CH 2 ; when n is two or three, V is CH 2 , O or NR 5 ; when V is CH2, the bond formed by V and an adjacent carbon ring atom is optionally fused to a phenyl ring, a five-membered heteroaromatic ring containing 1, 2 or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S is present, or a six-membered heteroaromatic ring containing 1, 2 or 3 N atoms; the ring being optionally substituted by one or more R 1 groups; and R 7 and R 8 are independently hydrogen, hydroxy, halogen or C 1-4 alkyl; Z is a phenyl ring, a five-membered heteroaromatic ring containing one, two, three or four heteroatoms independently chosen from O, N or S, at most one heteroatom being O or S, or a six- membered heteroaromatic ring containing one, two or three N atoms, optionally substituted by one or more groups chosen from halogen, hydroxy, cyano, nitro, NR 2 R 3 or S(O) r NR 2 R 3 where NR 2 R 3 is as defined above, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, haloC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 1-6 alkylthio, haloC 1-6 alkylthio,C 3-7 cycloalkyl, hydroxyC 1-6 alkyl, a five-membered heteroaromatic ring containing 1, 2or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S atom is present, or a six-membered heteroaromatic ring containing 1, 2 or 3 N atoms; or a pharmaceutically acceptable salt or N-oxide thereof; pharmaceutical compositions comprising them; the compounds for use in methods of treatment; and use of the compounds for manufacturing medicaments for treating pain as VRl antagonists, including conditions such as depression, GERD, itch and urinary incontinence.
摘要翻译：式（I）的化合物，其中W为式（1）; A是苯环，含有1,2或3个独立地选自O，N和S的杂原子的f元环杂芳环，条件是不存在不超过一个O或S原子，或含有1个或6个杂芳环 2或3个N原子; n为零，一，二或三; 当n为0或1时，V为CH 2 2; 当n为2或3时，V为CH 2，O或NR 5; 当V为CH 2时，由V形成的键和相邻碳环原子任选地与苯环稠合，含有1,2或3个独立地选自O，N和S的杂原子的五元杂芳环，条件是不再有存在一个O或S，或含有1,2或3个N原子的六元杂芳环; 该环任选地被一个或多个R 1基团取代; R 7和R 8独立地是氢，羟基，卤素或C 1-4烷基; Z是苯环，含有一个，两个，三个或四个独立地选自O，N或S，至多一个杂原子是O或S的杂原子的五元杂芳环或含有一个，二个或三个N原子，任选地被一个或多个选自卤素，羟基，氰基，硝基，NR 2 R 3或S（O）其中NR 2 R 3如上所定义，C 1和R 2如上定义，其中R 1，R 2，R 3， C 1-6烷基，C 2-6链烯基，C 2-6亚炔基，卤代C 1-6烷基，C <亚 > 1-6个烷氧基，卤代C 1-6烷氧基，C 1-6烷硫基，卤代C 1-6烷硫基，C 3-7环烷基，羟基C 1-6烷基，含有独立选自O，N和S的1,2或3个杂原子的五元杂芳环，条件是不再有存在一个O或S原子，或含有1,2或3个N原子的6元杂芳环; 或其药学上可接受的盐或N-氧化物; 包含它们的药物组合物; 用于治疗方法的化合物; 以及用于制备用于治疗作为VR1拮抗剂的疼痛的药物的化合物的使用，包括诸如抑郁症，GERD，瘙痒和尿失禁的病症。

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