发明名称 BENZYL(IDENE)-LACTAM DERIVATIVES, THEIR PREPARATION AND THEIR USE AS SELECTIVE (ANT)AGONISTS OF 5-HT1A- AND/OR 5-HT1D RECEPTORS
摘要 A compound of formula (I) wherein R<1> is a group of formula G<1>, G<2>, G<3>, G<4> or G<5>; R<2> is hydrogen, (C1-C4)alkyl, phenyl or naphthyl, wherein said phenyl or naphthyl may optionally be substituted with one or more substituents, preferably from zero to three substituents, independently selected from chloro, fluoro, bromo, iodo, (C1-C6)alkyl, (C1-C6)alkoxy, trifluoromethyl, cyano and SOg(C1-C6)alkyl wherein g is zero, one or two; R<3> is (CH2)mB, wherein m is zero, one, two or three and B is hydrogen, phenyl, naphthyl or a 5- or 6-membered heteroaryl group containing from one to four hetero atoms in the ring (e.g., furyl, thienyl, pyridyl, pyrimidyl, thiazolyl, pyrazolyl, isothiazolyl, oxazolyl, isoxazolyl, pyrrolyl, triazolyl, tetrazolyl, imidazolyl, etc.), and wherein each of the foregoing aryl and heteroaryl groups may optionally be substituted with one or more substituents, preferably from zero to three substituents, independently selected from chloro, fluoro, bromo, iodo, (C1-C6)alkyl, (C1-C6)alkoxy, trifluoromethyl, cyano hydroxy, COOH and SOg(C1-C6)alkyl, wherein g is zero, one or two; Z is CR<4>R<5>, wherein R<4> and R<5> are independently selected from hydrogen, (C1-C6)alkyl and trifluoromethyl; or Z may be one of the aryl or heteroaryl groups referred to in the definition of B above and wherein two adjacent ring members of Z are also members of ring A; X is hydrogen, chloro, fluoro, bromo, iodo, cyano, (C1-C6)alkyl, hydroxy, trifluoromethyl, (C1-C6)alkoxy, -SOg(C1-C6)alkyl, wherein g is zero one or two, CO2R<10> or CONR<11>R<12>; each of R<10>, R<11> and R<12> is selected, independently, from the radicals set forth in the definition of R<2>; or R<11> and R<12>, together with the nitrogen to which they are attached, form a 5- to 7-membered ring that may contain from zero to four heteroatoms selected from nitrogen, sulfur and oxygen; n is one, two, three or four; and the broken line indicates an optional double bond; and R<6>, R<7>, R<8>, R<9>, R<13>, E, p and x are defined as in the specification; with the proviso that n must be one when Z is a heteroaryl group; or a pharmaceutically acceptable salt thereof. These compounds are selective (ant)agonists of 5-HT1A- and/or 5-HT1D receptors and thus are useful as psychotherapeutic agents.
申请公布号 WO9736867(A1) 申请公布日期 1997.10.09
申请号 WO1997IB00076 申请日期 1997.02.03
申请人 PFIZER INC.;HOWARD, HARRY, R. 发明人 HOWARD, HARRY, R.
分类号 C07D215/22;A61K31/395;A61K31/397;A61K31/40;A61K31/4015;A61K31/403;A61K31/404;A61K31/445;A61K31/47;A61K31/472;A61K31/495;A61K31/496;A61K31/497;A61K31/55;A61P1/00;A61P3/04;A61P9/00;A61P9/12;A61P25/00;A61P43/00;C07D205/08;C07D207/26;C07D207/36;C07D207/38;C07D209/34;C07D211/76;C07D211/86;C07D217/24;C07D223/10;C07D401/10;C07D403/00;C07D403/10 主分类号 C07D215/22
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