发明名称 Indole derivatives as 5-HT1 agonists
摘要 Compounds of the formulawhere W isn is 0, 1, or 2; m is 0, 1, 2, or 3: Y and G are each independently oxygen or sulfur; Z is -O-, -S-, -NH, or -CH2; R1 is hydrogen, C1 to C8 alkyl, substituted C1 to C8 alkyl substituted with one hydroxy, C3 to C8 alkenyl, C3 to C8 alkynyl, aryl, C1 to C3 alkylaryl, C1 to C3 alkylheteroaryl, or -Q-R4; R2 and R2 are each independently hydrogen, C1 to C6 alkyl, aryl, C1 to C3 alkylaryl, or C1 to C3 alkylheteroaryl; R4 is cyano, trifluoromethyl, -COR9, -CO2R9, -CONR9R10, -OR9, -SO2NR(R10, or -S(O)4R8; R9 and R10 are each independently hydrogen, C1 to C8 alkyl, C1 to C3 alkylaryl, aryl, or R9 and R10 may together be taken to form a three- to seven-membered alkyl ring or a three- to seven-membered heteroalkyl ring having 1 heteroatom of O; Q is C1 C3 alkyl; R11 is hydrogen, -Or12, or -NHCOR12; R12 is hydrogen, C1 to C6 alkyl, aryl, or C1 to C3 alkyl-aryl; q is ), 1, or 2; a first chiral carbon is designated by an asterisk; a second chiral carbon is designated by #; and the above aryl groups and the aryl moieties of the above alkyl-aryl groups are independently selected from phenyl and substituted phenyl, wherein said substituted phenyl may be substituted with one to three groups selected from C1 to C4 alkyl, halogen, hydroxy, cyano, carboxamido, nitro, and C1 to C4 alkoxy, and the pharmaceutically acceptable salts thereof.These compounds are useful in treating migraine and other disorders 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, and 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.
申请公布号 US6387941(B1) 申请公布日期 2002.05.14
申请号 US20000694809 申请日期 2000.10.23
申请人 PFIZER INC. 发明人 MACOR JOHN EUGENE;WYTHES MARTIN JAMES
分类号 A61K31/40;A61K31/404;A61K31/41;A61P3/04;A61P9/08;A61P9/12;A61P25/04;A61P25/06;A61P25/20;A61P25/24;A61P25/26;A61P43/00;C07D207/08;C07D209/04;C07D263/08;C07D403/06;C07D403/14;C07D413/12;C07D413/14;(IPC1-7):A61K31/40;C07D413/40 主分类号 A61K31/40
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