发明名称 INDOLE DERIVATIVES
摘要 Compounds of the formula I wherein n is 0, 1, or 2; X is chlorine, bromine, or iodine; R1 is hydrogen; R2 is selected from hydrogen, halogen, cyano, -OR4 -(CH2)m-(C=O)NR5R6, -(CH2)m-SO2NR5R6, -(CH2)m-NR7(C=O)R8 --(CH2)m-NR7SO2R8, -(CH2) m-S(O)xR8, -(CH2)m-NR,(C=O)NR5R6, -(CH2)m-NR,(C=O)OR9, and -CH=CH(CH2)yR10; R3 is C1 to C6 linear or branched alkyl, and the pharmaceutically acceptable salts thereof are new. These compounds are useful psychotherapeutics and are potent serotonin (5-HT1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of a dihalogenated intermediate.
申请公布号 CA2178161(A1) 申请公布日期 1996.12.07
申请号 CA19962178161 申请日期 1996.06.04
申请人 PFIZER INC. 发明人 MACOR, JOHN EUGENE;WYTHES, MARTIN JAMES
分类号 A61K31/00;A61K31/40;A61K31/403;A61K31/404;A61K31/4045;A61K31/4427;A61K31/445;A61K31/4465;A61K31/4523;A61K31/454;A61P1/00;A61P1/08;A61P3/00;A61P3/04;A61P9/00;A61P9/08;A61P9/12;A61P11/00;A61P17/00;A61P19/00;A61P25/04;A61P25/06;A61P25/18;A61P25/20;A61P25/24;A61P25/26;A61P25/30;A61P27/00;A61P29/00;A61P35/00;A61P43/00;C07D401/06;C07D403/06;(IPC1-7):C07D403/06 主分类号 A61K31/00
代理机构 代理人
主权项
地址