首页> 外国专利> Compounds derived from indole; Pharmaceutical composition comprising these Compounds, and their use to treat Pain as Perioperative Pain, Chronic Pain, neuropathic pain,Cancer pain and pain and Spasticity associated with sclerosis

Compounds derived from indole; Pharmaceutical composition comprising these Compounds, and their use to treat Pain as Perioperative Pain, Chronic Pain, neuropathic pain,Cancer pain and pain and Spasticity associated with sclerosis

机译：吲哚化合物;包含这些化合物的药物组合物，及其在治疗围手术期疼痛，慢性疼痛，神经性疼痛，癌性疼痛以及与硬化相关的疼痛和痉挛中的用途

页面导航

摘要
著录项
相似文献

摘要

The invention relates to indole derivative having the general Formula I wherein A represents a 5-membered aromatic heterocyclic ring, wherein X1, X2 and X3 are independently selected from N, O, S and CH; Y represents CH2, O, S or SO2; R1 is H, (C1-4)-alkyl, (C1-4)alkyloxy, CN or halogen; R2, R2', R3, R3', R4, R4', R5 and R5' are independently hydrogen, (C1-4)alkyl (optionally substituted with OH) or CO-OR8; or one pair of geminal substituents R3 and R3' or R5 and R5' together represent a keto group, and the others are all hydrogen or (C1-4)alkyl; or R2 and R5 together represent a methylene or an ethylene bridge, and R2', R3, R3', R4, R4' and R5' are hydrogen; n is 1 or 2; R6 is H, (C1-4)alkyl (optionally substituted with OH, (C1-4)alkyloxy, CO-NR9R10, CO-OR11 or 1,2,4-oxadiazol-3-yl), SO2NR12R13 or COOR14; R7 is H or halogen; R8 is (C1-4)alkyl; R9 and R10 are independently hydrogen, (C1-4)alkyl or (C3-7)cycloalkyl, the alkyl groups being optionally substituted with OH or (C1-4)alkyloxy; R11 is H or (C1-4)alkyl; R12 and R13 are independently H or (C1-4)alkyl; R14 is (C1-6)alkyl; 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.

机译：本发明涉及具有通式I的吲哚衍生物，其中A代表5元芳族杂环，其中X 1，X 2和X 3独立地选自N，O，S和CH。 Y代表CH 2，O，S或SO 2; R1是H，（C1-4）-烷基，（C1-4）烷氧基，CN或卤素; R2，R2'，R3，R3'，R4，R4'，R5和R5'独立地是氢，（C1-4）烷基（任选被OH取代）或CO-OR8;或一对双取代基R3和R3′或R5和R5′一起代表酮基，其余全部为氢或（C1-4）烷基。 R2和R5一起代表亚甲基或亚乙基桥，R2′，R3，R3′，R4，R4′和R5′是氢;或n为1或2; R6为H，（C1-4）烷基（任选地被OH，（C1-4）烷氧基，CO-NR9R10，CO-OR11或1,2,4-恶二唑-3-基取代），SO2NR12R13或COOR14; R7是H或卤素; R8是（C1-4）烷基; R9和R10独立地是氢，（C1-4）烷基或（C3-7）环烷基，烷基任选地被OH或（C1-4）烷氧基取代; R11是H或（C1-4）烷基; R12和R13独立地是H或（C1-4）烷基; R14为（C1-6）烷基;或其药学上可接受的盐，作为大麻素CB1受体的激动剂，可用于治疗疼痛，例如围手术期疼痛，慢性疼痛，神经性疼痛，癌症疼痛以及与多发性硬化症相关的疼痛和痉挛。

著录项

公开/公告号CL2008000514A1

专利类型
公开/公告日2008-06-20

原文格式PDF
申请/专利权人 N.V. ORGANON;
展开▼

申请/专利号CL20080000514
发明设计人 ADAM JULIA;
展开▼

申请日2008-02-20
分类号A61K31/496;A61P29/00;C07D209/14;C07D277/28;C07D285/08;C07D309/06;C07D335/02;C07D413/04;C07D417/04;
国家 CL
入库时间 2022-08-21 20:08:33

相似文献

专利
外文文献
中文文献