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1. 发明申请

WO2007006732A8 SYNERGISTIC COMBINATION FOR THE TREATMENT OF PAIN (CANNABIOID RECEPTOR AGONIST AND OPIOD RECEPTOR AGONIST) 审中-公开
标题翻译：用于治疗疼痛（CANNABIOID RECPTOR AGONIST AND OPIOD RECEPTOR AGONIST）的协同组合
公开(公告)号：WO2007006732A8
公开(公告)日：2008-01-24
申请号：PCT/EP2006063985
申请日：2006-07-06
申请人： ORGANON NV , ADAM-WORRALL JULIA , HILL DAVID ROBERT , COTTNEY JEAN
发明人： ADAM-WORRALL JULIA , HILL DAVID ROBERT , COTTNEY JEAN
IPC分类号： A61K31/517 , A61K31/135 , A61K31/4468 , A61K31/485 , A61P25/04
CPC分类号： A61K31/135 , A61K31/137 , A61K31/4468 , A61K31/485 , A61K31/517 , A61K45/06 , A61K2300/00
摘要： The invention relates to a pharmaceutical dosage form comprising an analgesic combination for simultaneous or sequential use which comprises a peripherally restricted cannabinoid CB1 receptor agonist having a brain Cmax to plasma Cmax ratio of less than 0.1 and an opioid receptor agonist, as well as to a method for treating pain using said pharmaceutical dosage form.
摘要翻译：本发明涉及一种药物剂型，其包含用于同时或顺序使用的止痛组合物，其包含具有脑C max至血浆C max比小于0.1的外周限制性大麻素CB1受体激动剂和阿片受体激动剂，以及方法用于使用所述药物剂型治疗疼痛。

2. 发明申请

WO2002102808A2 (PYRIDO/THIENO)-[f]-OXAZEPIN-5-ONE DERIVATIVES 审中-公开
标题翻译：（吡啶/噻吩） - [f] -OXAZEPIN-5-ONE衍生物
公开(公告)号：WO2002102808A2
公开(公告)日：2002-12-27
申请号：PCT/EP2002/006364
申请日：2002-06-10
申请人： AKZO NOBEL N.V. , GROVE, Simon, James, Anthony , ADAM-WORRALL, Julia , ZHANG, Mingqiang , GILFILLAN, Robert
发明人： GROVE, Simon, James, Anthony , ADAM-WORRALL, Julia , ZHANG, Mingqiang , GILFILLAN, Robert
IPC分类号： C07D498/14
CPC分类号： C07D498/14
摘要： The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R 1 , R 2 and R 3 are independently H or (C 1-4 )alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C 1-4 )alkyl, (C 1-4 )alkyloxy, (C 1-4 )alkyloxy(C 1-4 )alkyl, CF 3 , halogen, nitro, cyano, NR 4 R 5 , NR 4 COR 6 , and CONR 4 R 5 ; R 4 and R 5 are independently H or (C 1-4 )-alkyl; or R 4 and R 5 form together with the nitrogen atom to which they are bound a 5-or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR 6 ; R 6 is (C 1-4 )alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C 1-4 )alkyl, (C 1-4 )-alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.
摘要翻译：本发明涉及具有通式I的（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物，其中R 1，R 2和R 3独立地为H或（C 1-4）烷基; Ar表示任选被一个或多个选自（C 1-4）烷基，（C 1-4）烷氧基，（C 1-4）烷氧基（C 1-4）烷基，CF 3，卤素，硝基，氰基，NR 4 R 5，NR 4 COR 6和CONR 4 R 5; R 4和R 5独立地为H或（C 1-4） - 烷基; 或R 4和R 5与它们所连接的氮原子一起形成5-或6-元饱和杂环，任选地含有另外选自O，S或NR 6的杂原子; R 6是（C 1-4）烷基; A表示任选含有氧原子的4-7元饱和杂环的残基，该环任选被1-3个选自（C 1-4）烷基，（C 1-4） - 烷氧基，羟基，卤素和氧代; 或其药学上可接受的盐。本发明还涉及包含所述衍生物的药物组合物，以及这些（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物在治疗对增强突触反应有反应的神经疾病和精神疾病的用途中的用途）由AMPA受体介导的中枢神经系统。

3. 发明申请

WO2007023143A1 (INDOL-3-YL)-HETEROCYCLE DERIVATIVES AS AGONISTS OF THE CANNABINOID CB1 RECEPTOR 审中-公开
标题翻译：（INDOL-3-YL）-HETEROCYCLE DERIVATIVES作为CANNABINOID CB1受体的激动剂
公开(公告)号：WO2007023143A1
公开(公告)日：2007-03-01
申请号：PCT/EP2006/065496
申请日：2006-08-21
申请人： AKZO NOBEL N.V. , RATCLIFFE, Paul David , ADAM-WORRALL, Julia , MORRISON, Angus John , FRANCIS, Stuart John , KIYOI, Takao
发明人： RATCLIFFE, Paul David , ADAM-WORRALL, Julia , MORRISON, Angus John , FRANCIS, Stuart John , KIYOI, Takao
IPC分类号： A61K31/4245 , C07D413/14 , A61P29/00 , A61K31/433 , C07D417/14
CPC分类号： C07D413/14 , C07D417/14
摘要： The invention relates to indole derivative having the general Formula (I) Wherein A, X 1 , X 2 , X 3 , Y, R 1 , R 2 , R 3 and R 4 are as defined in the claims, or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same and to the use of said indol derivatives in the treatment of pain.
摘要翻译：本发明涉及具有通式（I）的吲哚衍生物，其中A，X 1，X 2，X 3，Y，R 3， R 1，R 2，R 3和R 4如权利要求中所定义，或其药学上可接受的盐，包含其的药物组合物和所述吲哚衍生物在治疗疼痛中的用途。

4. 发明申请

WO2007006732A1 SYNERGISTIC COMBINATION FOR THE TREATMENT OF PAIN (CANNABIOID RECEPTOR AGONIST AND OPIOD RECEPTOR AGONIST) 审中-公开
标题翻译：用于治疗疼痛（CANNABIOID RECPTOR AGONIST AND OPIOD RECEPTOR AGONIST）的协同组合
公开(公告)号：WO2007006732A1
公开(公告)日：2007-01-18
申请号：PCT/EP2006/063985
申请日：2006-07-06
申请人： N.V. ORGANON , ADAM-WORRALL, Julia , HILL, David, Robert , COTTNEY, Jean
发明人： ADAM-WORRALL, Julia , HILL, David, Robert , COTTNEY, Jean
IPC分类号： A61K31/517 , A61K31/485 , A61K31/4468 , A61K31/135 , A61P25/04
CPC分类号： A61K31/135 , A61K31/137 , A61K31/4468 , A61K31/485 , A61K31/517 , A61K45/06 , A61K2300/00
摘要： The invention relates to a pharmaceutical dosage form comprising an analgesic combination for simultaneous or sequential use which comprises a peripherally restricted cannabinoid CB1 receptor agonist having a brain Cmax to plasma Cmax ratio of less than 0.1 and an opioid receptor agonist, as well as to a method for treating pain using said pharmaceutical dosage form.
摘要翻译：本发明涉及一种药物剂型，其包含用于同时或顺序使用的止痛组合物，其包含具有脑C max至血浆C max比小于0.1的外周限制性大麻素CB1受体激动剂和阿片受体激动剂，以及方法用于使用所述药物剂型治疗疼痛。

5. 发明申请

WO2005089754A1 (INDOL-3-YL)-HETEROCYCLE DERIVATIVES AS AGONISTS OF THE CANNABINOID CB1 RECEPTOR 审中-公开
标题翻译：（INDOL-3-YL）-HETEROCYCLE DERIVATIVES作为CANNABINOID CB1受体的激动剂
公开(公告)号：WO2005089754A1
公开(公告)日：2005-09-29
申请号：PCT/EP2005/050833
申请日：2005-02-28
申请人： AKZO NOBEL N.V. , ADAM-WORRALL, Julia , MORRISON, Angus John , WISHART, Grant , KIYOI, Takao , MCARTHUR, Duncan, Robert
发明人： ADAM-WORRALL, Julia , MORRISON, Angus John , WISHART, Grant , KIYOI, Takao , MCARTHUR, Duncan, Robert
IPC分类号： A61K31/4245
CPC分类号： C07D403/04 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D513/04
摘要： The invention relates to (indol-3-yl)-heterocycle derivatives having general Formula (I) wherein A represents a 5-membered aromatic heterocyclic ring, wherein X 1 , X 2 and X 3 are independently selected from N, O, S and CR; R is H or (C 1-4 )alkyl; or R, when present in X 2 or X 3 , may form together with R 3 a 5-8 membered ring; R 1 is a 5-8 membered saturated carbocyclic ring, optionally containing a heteroatom selected from O and S; R 2 is H, CH 3 or CH 2 -CH 3; or R 2 is joined together with R 7 to form a 6-membered ring, optionally containing a heteroatom selected from O and S, and which heteroatom is bonded to the 7-position of the indole ring; R 3 and R 4 are independently H, (C 1-6 )alkyl or (C 3-7 )cycloalkyl, the alkyl groups being optionally substituted with OH, (C 1-4 )alkyloxy, (C 1-4 )alkylthio, (C 1-4 )alkylsulfonyl, CN or halogen; or R 3 together with R 4 and the N to which they are bonded form a 4-8 membered ring optionally containing a further heteroatom selected from O and S, and which is optionally substituted with OH, (C 1-4 )alkyl, (C 1-4 )alkyloxy, (C 1-4 )alkyloxy- (C 1-4 )alkyl, or halogen; or R 3 together with R 5 forms a 4-8 membered ring optionally containing a further heteroatom selected from O and S, and which is optionally substituted with OH, (C 1- 4)alkyl, (C 1-4 )alkyloxy, (C 1-4 )alkyloxy- (C 1-4 )alkyl, or halogen; or R 3 together with R, when present in X 2 or X 3 , forms a 5-8 membered ring; R 5 is H or (C 1-4 )alkyl; or R 5 together with R 3 forms a 4-8 membered ring optionally containing a further heteroatom selected from O and S, and which is optionally substituted with OH, (C 1-4 )alkyl, (C 1-4 )alkyloxy, (C 1-4 ) alkyloxy- (C 1-4 )alkyl, or halogen; R 5 ' is H or (C 1-4 )alkyl; R 6 represents 1-3 substituents independently selected from H, (C 1-4 alkyl, (C 1-4 ) alkyloxy, CN and halogen; R 7 is H, (C 1-4 )alkyl, (C 1-4 )alkyloxy, CN or halogen; or R 7 is joined together with R 2 to form a 6-membered ring, optionally containing a further heteroatom selected from O and S, and which heteroatom is bonded to the 7-position of the indole ring; or a pharmaceutically acceptable salt thereof, as agonists of the cannabinoid CB1 receptor, which can be used in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis.
摘要翻译：本发明涉及具有通式（I）的（吲哚-3-基） - 杂环衍生物，其中A表示5元芳族杂环，其中X1，X2和X3独立地选自N，O，S和CR; R是H或（C 1-4）烷基; 或R 2当存在于X 2或X 3中时，可以与R 3一起形成5-8元环; R1是5-8元饱和碳环，任选地含有选自O和S的杂原子; R2是H，CH3或CH2-CH3; 或R 2与R 7一起形成6元环，任选地含有选自O和S的杂原子，哪个杂原子与吲哚环的7-位键合; R 3和R 4独立地为H，（C 1-6）烷基或（C 3-7）环烷基，该烷基任选被OH，（C 1-4）烷氧基，（C 1-4）烷硫基，（C 1-4），CN或卤素; 或R 3与R 4和它们所键合的N形成4-8元环，任选地含有选自O和S的另外的杂原子，并且其任选被OH，（C 1-4）烷基，（C 1-4））烷氧基，（C 1-4）烷氧基 - （C 1-4）烷基或卤素; 或R 3与R 5一起形成任选含有另外选自O和S的杂原子的4-8元环，其任选被OH，（C 1-4）烷基，（C 1-4）烷氧基，（C 1-4）烷氧基，烷氧基 - （C 1-4）烷基或卤素; 或R 3与R一起形成5-8元环，当存在于X 2或X 3中时， R5是H或（C1-4）烷基; 或R 5与R 3一起形成任选地含有选自O和S的另外的杂原子的4-8元环，其任选被OH，（C 1-4）烷基，（C 1-4）烷氧基，（C 1-4）烷氧基，烷氧基 - （C 1-4）烷基或卤素; R5'是H或（C1-4）烷基; R6代表独立地选自H，（C 1-4烷基，（C 1-4）烷氧基，CN和卤素）的1-3个取代基; R 7是H，（C 1-4）烷基，（C 1-4）烷氧基，CN或卤素; 或R 7与R 2一起形成6元环，任选地含有选自O和S的另外的杂原子，并且该杂原子与吲哚环的7-位键合;或其药学上可接受的盐作为激动剂的大麻素CB1受体，其可用于治疗疼痛，例如围手术期疼痛，慢性疼痛，神经性疼痛，癌症疼痛和与多发性硬化相关的痉挛状态。

6. 发明申请

WO02102808A3 (PYRIDO/THIENO)-[f]-OXAZEPIN-5-ONE DERIVATIVES AS POSITIVE MODULATORS OF THE AMPA RECEPTOR 审中-公开
标题翻译：（PYRIDO / THIENO） - [f] -OXAZEPIN-5-ONE衍生物作为AMPA受体的阳性调节剂
公开(公告)号：WO02102808A3
公开(公告)日：2003-03-20
申请号：PCT/EP0206364
申请日：2002-06-10
申请人： AKZO NOBEL NV , GROVE SIMON JAMES ANTHONY , ADAM-WORRALL JULIA , ZHANG MINGQIANG , GILFILLAN ROBERT
发明人： GROVE SIMON JAMES ANTHONY , ADAM-WORRALL JULIA , ZHANG MINGQIANG , GILFILLAN ROBERT
IPC分类号： A61K31/553 , A61P9/00 , A61P15/10 , A61P17/02 , A61P25/00 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P43/00 , C07D498/14
CPC分类号： C07D498/14
摘要： The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula (I) wherein R , R and R are independently H or (C1-4)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, CF3, halogen, nitro, cyano, NR R , NR COR , and CONR R ; R and R are independently H or (C1-4)-alkyl; or R and R form together with the nitrogen atom to which they are bound a 5-or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR ; R is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)-alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.
摘要翻译：本发明涉及具有通式（I）的（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物，其中R 1，R 2和R 3独立地为H或（C1- 4）烷基; Ar表示任选被一个或多个选自（C 1-4）烷基，（C 1-4）烷氧基，（C 1-4）烷氧基（C 1-4）烷基，CF 3，卤素，硝基，氰基，NR 4 R 5，NR 4 COR 6和CONR 4 R 5; R 4和R 5独立地为H或（C 1-4） - 烷基; 或R 4和R 5与它们所连接的氮原子一起形成5-或6-元饱和杂环，任选地含有另外选自O，S或NR 6的杂原子; R 6是（C 1-4）烷基; A表示任选含有氧原子的4-7元饱和杂环的残基，该环任选被1-3个选自（C 1-4）烷基，（C 1-4） - 烷氧基，羟基，卤素和氧代; 或其药学上可接受的盐。本发明还涉及包含所述衍生物的药物组合物，以及这些（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物在治疗对增强突触反应有反应的神经疾病和精神疾病的用途中的用途）由AMPA受体介导的中枢神经系统。

7. 发明申请

WO2005058327A1 TRICYCLIC 1-[(3-INDOL-3-YL)CARBONYL] PIPERAZINE DERIVATIVES AS CANNABINOID CB1 RECEPTOR AGONISTS 审中-公开
标题翻译：三茂铁1 - [（3-吲哚-3-基）羰基]哌嗪衍生物作为CANNABINOID CB1受体激动剂
公开(公告)号：WO2005058327A1
公开(公告)日：2005-06-30
申请号：PCT/EP2004/053421
申请日：2004-12-13
申请人： AKZO NOBEL N.V. , ADAM-WORRALL, Julia
发明人： ADAM-WORRALL, Julia
IPC分类号： A61K31/5383
CPC分类号： C07D471/06
摘要： The invention relates to tricyclic 1-[(indol-3-yl)carbonyl]piperazine derivative having the general Formula (I) wherein X is CH 2 , O or S; R represents 1-3 substituents independently selected from H, (C 1-4 )alkyl, (C 1-4 )alkyloxy and halogen; R 1 is (C 5-8 )cycloalkyl; R 2 is H or (C 1-4 )alkyl; R 3 , R 3 ´, R 4 ’ R 4 ’, R 5 , R 5 ’ and R 6 ’ are independently hydrogen or (C 1-4 )-alkyl, optionally substituted with (C 1-4 )alkyloxy, OH or halogen; R 6 is hydrogen or (C 1-4 )alkyl, optionally substituted with (C 1-4 )alkyloxy, OH or halogen; or R 6 forms together with R 7 a 4-7 membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O and S; R 7 forms together with R 6 a 4-7 membered saturated heterocydic ring, optionally containing a further heteroatom selected from O and S; or R 7 is H, (C 1-4 )alkyl or (C 3-5 )cycloalkyl, the alkyl groups being optionally substituted with OH, halogen or (C 1-4 )alkyloxy; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said tricyclic 1-[(indol-3-yl)carbonyl]piperazine derivatives, and to the use of these derivatives in the treatment of pain, such as peri-operative pain, chronic pain neuropathic pain, cancer pain, and pain and spasticity associated with multiple sclerosis.
摘要翻译：本发明涉及具有通式（I）的三环1 - [（吲哚基-3-基）羰基]哌嗪衍生物，其中X是CH 2，O或S; R表示1-3个独立地选自H，（C 1-4）烷基，（C 1-4）烷氧基和卤素的取代基; R1是（C5-8）环烷基; R2是H或（C1-4）烷基; R 3，R 3，R 4'R 4'，R 5，R 5'和R 6'独立地为氢或（C 1-4） - 烷基，任选被（C 1-4）烷氧基，OH或卤素取代; R 6是氢或任选被（C 1-4）烷氧基，OH或卤素取代的（C 1-4）烷基; 或R6与R7一起形成4-7元饱和杂环，任选地含有另外选自O和S的杂原子; R7与R6一起形成4-7元饱和杂环，任选地含有选自O和S的另外的杂原子; 或者R 7为H，（C 1-4）烷基或（C 3-5）环烷基，该烷基任选被OH，卤素或（C 1-4）烷氧基取代; 或其药学上可接受的盐。本发明还涉及包含所述三环1 - [（吲哚-3-基）羰基]哌嗪衍生物的药物组合物，以及这些衍生物在治疗疼痛中的用途，例如手术前疼痛，慢性疼痛神经性疼痛，癌症疼痛以及与多发性硬化相关的疼痛和痉挛状态。

8. 发明申请

WO2004000832A1 1-[(INDOL-3-YL)CARBONYL] PIPERAZINE DERIVATIVES 审中-公开
标题翻译： 1 - [（吲哚-3-基）羰基]哌嗪衍生物
公开(公告)号：WO2004000832A1
公开(公告)日：2003-12-31
申请号：PCT/EP2003/050226
申请日：2003-06-13
申请人： AKZO NOBEL N.V. , COWLEY, Phillip, Martin , CAULFIELD, Wilson , TIERNEY, Jason , CAIRNS, James , ADAM-WORRALL, Julia , YORK, Mark
发明人： COWLEY, Phillip, Martin , CAULFIELD, Wilson , TIERNEY, Jason , CAIRNS, James , ADAM-WORRALL, Julia , YORK, Mark
IPC分类号： C07D403/06
CPC分类号： C07D471/04 , C07D209/42 , C07D487/04
摘要： The present invention relates to 1-[(indol-3-yl)carbonyl]piperazine derivative according to the general formula (I), wherein R represents 1-4 substituents independently selected from H, (C 1-4 )alkyl (optionally substituted with halogen), (C 1-4 )alkyloxy (optionally substituted with halogen), halogen, OH, NH 2 , CN and NO 2 ; R 1 is (C 5-8 )cycloalkyl or (C 5-8 )cycloalkenyl; R2 is H, methyl or ethyl; R 3 , R 3 ', R 4 ' R 4 ', R 5 , R 5 ' and R 6 ' are independently hydrogen or (C 1-4 )alkyl, optionally substituted with (C 1-4 )alkyloxy, halogen or OH; R 6 is hydrogen or (C 1-4 )alkyl, optionally substituted with (C 1-4 )alkyloxy, halogen or OH; or R 6 forms together with R 7 a 4-7 membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O and S; R 7 forms together with R 6 a 4-7 membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O and S; or R 7 is H, (C 1-4 )alkyl or (C 3-5 )cycloalkyl, the alkyl groups being optionally substituted with OH, halogen or (C 1-4 )alkyloxy; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said 1-[(indol-3-yl)carbonyl]piperazine derivatives, and to the use of these derivatives in the treatment of pain, such as peri-operative pain, chronic pain neuropathic pain, cancer pain, and pain and spasticity associated with multiple sclerosis.
摘要翻译：本发明涉及根据通式（I）的1 - [（吲哚基-3-基）羰基]哌嗪衍生物，其中R表示1-4个独立地选自H，（C 1-4）烷基的取代基（任选被卤素），（C 1-4）烷氧基（任选被卤素取代），卤素，OH，NH 2，CN和NO 2; R1是（C5-8）环烷基或（C5-8）环烯基; R2是H，甲基或乙基; R 3，R 3'，R 4'R 4'，R 5，R 5'和R 6'独立地为氢或（C 1-4）烷基，任选被（C 1-4）烷氧基，卤素或OH取代; R 6为氢或任选被（C 1-4）烷氧基，卤素或OH取代的（C 1-4）烷基; 或R6与R7一起形成4-7元饱和杂环，任选地含有另外选自O和S的杂原子; R7与R6一起形成4-7元饱和杂环，任选地含有另外选自O和S的杂原子; 或者R 7为H，（C 1-4）烷基或（C 3-5）环烷基，该烷基任选被OH，卤素或（C 1-4）烷氧基取代; 或其药学上可接受的盐。本发明还涉及包含所述1 - [（吲哚-3-基）羰基]哌嗪衍生物的药物组合物，以及这些衍生物在治疗疼痛中的用途，例如手术前疼痛，慢性疼痛神经性疼痛，癌症疼痛，与多发性硬化相关的疼痛和痉挛状态。

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