发明名称 Tricyclic compounds acting at serotonin receptor subtypes
摘要 Compounds of Formula I: <IMAGE> I in which Z is CH2 or C=O; X and Y are independently selected from hydrogen, halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, aminocarbonyl, (lower alkyl)amino, di(lower alkyl)amino and (lower alkanoyl)amino; and R1 is a group selected from Formulae (a), (b), (c) (d) and (e): <IMAGE> (a) <IMAGE> (b) <IMAGE> (c) <IMAGE> (d) <IMAGE> (e) in which p is 0 or 1; n is 1, 2 or 3; R2 is hydrogen, lower alkyl, C3-8 cycloalkyl, C3-8 cycloalkyl-C12 alkyl, or a group R6-C1-2 alkyl in which R6 is thienyl, pyrrolyl or furyl optionally substituted by one or two substituents selected from lower alkyl, lower alkoxy, trifluoromethyl or halogen, or is phenyl optionally substituted by one or two substituents selected from C1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy, and C1-4 alkyl optionally further substituted by hydroxy, C1-4 alkoxy, carboxy, esterified carboxy or in vivo hydrolyzable acyloxy; each R3 is independently selected from hydrogen, hydroxy, alkyl and alkoxy; each R4 is independently hydrogen or alkyl; and R5 is hydrogen, lower alkyl, C3-8 cycloalkyl, C3-8 cycloalkyl-C1-2 alkyl, alkenyl, alkynyl or a group R7 -C1-3 alkyl in which R7 is phenyl or phenoxy optionally substituted by one or two substituents selected from C1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy, and C1-4 alkyl optionally further substituted by hydroxy, C1-4 alkoxy, carboxy, esterified carboxy or in vivo hydrolyzable acyloxy; and the pharmaceutically acceptable salts, individual isomers, mixtures of isomers, processes for preparation, compositions, and methods of use thereof.
申请公布号 US5202318(A) 申请公布日期 1993.04.13
申请号 US19910708260 申请日期 1991.05.28
申请人 SYNTEX (U.S.A.) INC. 发明人 BERGER, JACOB;CLARK, ROBIN D.;EGLEN, RICHARD M.;SMITH, WILLIAM L.;WEINHARDT, KLAUS K.
分类号 C07D401/04;C07D451/04;C07D451/14;C07D453/02;C07D471/08 主分类号 C07D401/04
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