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    �3-(4-phenylpiperazin-1-yl)propyl-amino, thio and oxy!-pyridine, pyrimidine and benzene derivatives as .alpha..sub.1 -adrenoceptor antagonists
    1.
    发明授权
    �3-(4-phenylpiperazin-1-yl)propyl-amino, thio and oxy!-pyridine, pyrimidine and benzene derivatives as .alpha..sub.1 -adrenoceptor antagonists 失效
    [3-（4-苯基哌嗪-1-基）丙基 - 氨基，硫代和氧基] - 吡啶，嘧啶和苯衍生物作为α1-肾上腺素受体拮抗剂

    公开(公告)号：US5688795A

    公开(公告)日：1997-11-18

    申请号：US336368

    申请日：1994-11-08

    申请人： Jurg Roland Pfister ,  David Ernest Clarke ,  Todd Richard Elworthy ,  David John Morgans, Jr. ,  David Bruce Repke ,  Eric Brian Sjorgren ,  Helen Yen-hui Wu

    发明人： Jurg Roland Pfister ,  David Ernest Clarke ,  Todd Richard Elworthy ,  David John Morgans, Jr. ,  David Bruce Repke ,  Eric Brian Sjorgren ,  Helen Yen-hui Wu

    IPC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 ,  C07D401/12 ,  C07D413/14

    CPC分类号： C07D213/74 ,  C07D213/82 ,  C07D213/85 ,  C07D213/89 ,  C07D239/42 ,  C07D295/13 ,  C07D403/12

    摘要： The present invention relates to novel .alpha..sub.1 -adrenoceptor antagonists of Formula I: ##STR1## in which: p is 0 or 1; t is 0, 1 or 2; X is O, S or NR.sup.6 (in which R.sup.6 is hydro or (C.sub.1-6)alkyl); Y and Z are independently CH or N; R.sup.1 is hydro, hydroxy, halo, nitro, amino, cyano, (C.sub.1-4)alkylthio, acetylamino, trifluoroacetylamino, methylsulfonylamino, (C.sub.1-6)alkyl, (C.sub.3-6)cycloalkyl, (C.sub.3-6)cycloalkyl (C.sub.1-4)alkyl, oxazol-2-yl, aryl, heteroaryl, aryl (C.sub.1-4)alkyl, heteroaryl (C.sub.1-4)alkyl, (C.sub.1-6)alkyloxy, (C.sub.3-6)cycloalkyloxy, (C.sub.3-6)cycloalkyl (C.sub.1-4)alkyloxy, 2-propynyloxy, aryloxy, heteroaryloxy, aryl (C.sub.1-4)alkyloxy or heteroaryl (C.sub.1-4)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.sup.2 is hydro, hydroxy, halo, cyano, (C.sub.1-6)alkyl or (C.sub.1-6)alkyloxy (wherein alkyl is optionally substituted with one to three halo atoms); R.sup.3 is -C (O)R.sup.7 (wherein R.sup.7 is (C.sub.1-6)alkyl, (C.sub.3-6)cycloalkyl, di(C.sub.1-4)alkylamino, N-(C.sub.1-4)alkyl-N-(C.sub.1-4)alkyloxyamino, (C.sub.1-4)alkyl((C.sub.1-4)alkyloxy)amino, pyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl or piperazin-1-yl); R.sup.4 is halo, hydroxy, cyano, (C.sub.1-6)alkyl or (C.sub.1-6)alkyloxy; and R.sup.5 is (C.sub.1-6)alkyl; and the pharmaceutically acceptable salts and N-oxides thereof.

    摘要翻译： 本发明涉及式I的新型α1-肾上腺素受体拮抗剂：其中：p为0或1; t为0,1或2; X是O，S或NR6（其中R6是氢或（C1-6）烷基）; Y和Z独立地为CH或N; R1为氢，羟基，卤素，硝基，氨基，氰基，（C1-4）烷硫基，乙酰氨基，三氟乙酰氨基，甲基磺酰氨基，（C1-6）烷基，（C3-6）环烷基，（C3-6）环烷基 4）烷基，恶唑-2-基，芳基，杂芳基，芳基（C 1-4）烷基，杂芳基（C 1-4）烷基，（C 1-6）烷氧基，（C 3-6）环烷氧基，（C 3-6）环烷基 （C 1-4）烷氧基，2-丙炔氧基，芳氧基，杂芳氧基，芳基（C 1-4）烷氧基或杂芳基（C 1-4）烷氧基（其中烷基任选被一至三个卤素原子取代，芳基或杂芳基任选被 一至两个独立地选自卤素和氰基的取代基）; R 2是氢，羟基，卤素，氰基，（C 1-6）烷基或（C 1-6）烷氧基（其中烷基任选被一至三个卤素原子取代）; R3是-C（O）R7（其中R7是（C1-6）烷基，（C3-6）环烷基，二（C1-4）烷基氨基，N-（C1-4）烷基-N-（C1-4） 烷氧基氨基，（C 1-4）烷基（（C 1-4）烷氧基）氨基，吡咯烷-1-基，哌啶-1-基，吗啉-4-基或哌嗪-1-基）; R4是卤素，羟基，氰基，（C1-6）烷基或（C1-6）烷氧基; 并且R 5是（C 1-6）烷基; 及其药学上可接受的盐和N-氧化物。