发明名称 Alfa1-adrenerjik reseptör antagonistleri olarak, yeni £3-(4-fenilpiperazin-1-il) propilamino|-piridin, pirimidin ve benzen türevleri.
摘要 The present invention relates to novel alpha 1-adrenoceptor antagonists of Formula I: <CHEM> in which: p is 0 or 1; t is 0, 1 or 2; X is O, S or NR<6> (in which R<6> is hydro or (C1-6)alkyl); Y and Z are independently CH or N; R<1> is hydro, hydroxy, halo, nitro, amino, cyano, (C1-4)alkylthio, acetylamino, trifluoroacetylamino, methylsulfonylamino, (C1-6)alkyl, (C3-6)cycloalkyl, (C3-6)cycloalkyl(C1-4)alkyl, oxazol-2-yl, aryl, heteroaryl, aryl(C1-4)alkyl, heteroaryl(C1-4)alkyl, (C1-6)alkyloxy, (C3-6)cycloalkyloxy, (C3-6)cycloalkyl(C1-4)alkyloxy, 2-propynyloxy, aryloxy, heteroaryloxy, aryl(C1-4)alkyloxy or heteroaryl(C1-4)alkyloxy (wherein alkyl is optionally substituted with one to three halo atoms and aryl or heteroaryl is optionally substituted with one to two substituents independently selected from halo and cyano); R<2> is hydro, hydroxy, halo, cyano, (C1-6)alkyl or (C1-6)alkyloxy (wherein alkyl is optionally substituted with one to three halo atoms); R<3> is -C(O)R<7> (wherein R<7> is (C1-6)alkyl, (C3-6)cycloalkyl, di(C1-4)alkylamino, N-(C1-4)alkyl-N-(C1-4)alkyloxyamino, (C1-4)alkyl((C1-4)alkyloxy)amino, pyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl or piperazin-1-yl); R<4> is halo, hydroxy, cyano, (C1-6)alkyl or (C1-6)alkyloxy; and R<5> is (C1-6)alkyl; and the pharmaceutically acceptable salts and N-oxides thereof.
申请公布号 TR9501387(A2) 申请公布日期 1996.07.21
申请号 TR19950001387 申请日期 1995.11.08
申请人 F.HOFFMANN-LA ROCHE & CO. AG. 发明人 DAVID ERNEST CLARKE;TRODD RICHARD ELWORTHY;DAVID JOHN MORGANS;JURG ROLAND PFISTER;DAVID BRUCE REPKE;ERIC BRIAN SJOGREN;HELEN YEN-HUI WU
分类号 C07D295/12;A61K31/44;A61K31/4412;A61K31/4418;A61K31/495;A61K31/505;A61K31/535;A61K31/5375;A61P13/02;A61P15/00;A61P43/00;C07D213/61;C07D213/74;C07D213/80;C07D213/82;C07D213/85;C07D213/89;C07D239/42;C07D241/04;C07D295/13;C07D403/12;C07D413/12;(IPC1-7):A61K 主分类号 C07D295/12
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