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27 条记录 (耗时 0.048 秒)

    4-piperazinyl benzenesulfonyl indoles and uses thereof
    25.
    发明授权
    4-piperazinyl benzenesulfonyl indoles and uses thereof 失效
    4-哌嗪基苯磺酰基吲哚及其用途

    公开(公告)号：US07022708B2

    公开(公告)日：2006-04-04

    申请号：US10687091

    申请日：2003-10-16

    申请人： Robin Douglas Clark ,  Ralph New Harris, III ,  David Bruce Repke

    发明人： Robin Douglas Clark ,  Ralph New Harris, III ,  David Bruce Repke

    IPC分类号： C07D403/04 ,  A61K31/496

    CPC分类号： C07D209/08 ,  C07D209/30

    摘要： This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula I: wherein R1, R2, R3, R4, and R5 are as defined herein; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

    摘要翻译： 本发明涉及通常具有5-HT 6受体亲和性并由式I表示的化合物：其中R 1，R 2，R 3， >，R 4，R 5和R 5如本文所定义; 或各异构体，异构体的外消旋或非外消旋混合物，或其药学上可接受的盐或溶剂合物。 本发明还涉及含有这些化合物的药物组合物，其用作治疗剂的方法及其制备方法。

    4-piperazinylindole derivatives with 5-HT6 receptor affinity
    26.
    发明授权
    4-piperazinylindole derivatives with 5-HT6 receptor affinity 失效
    具有5-HT 6受体亲和力的4-哌嗪基吲哚衍生物

    公开(公告)号：US06790848B2

    公开(公告)日：2004-09-14

    申请号：US10172360

    申请日：2002-06-14

    申请人： Andrew John Briggs ,  Robin Douglas Clark ,  Ralph New Harris, III ,  David Bruce Repke ,  Douglas Leslie Wren

    发明人： Andrew John Briggs ,  Robin Douglas Clark ,  Ralph New Harris, III ,  David Bruce Repke ,  Douglas Leslie Wren

    IPC分类号： C07D40304

    CPC分类号： C07D209/40

    摘要： This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula I: wherein R3 is SO2—Ar, Ar is aryl or heteroaryl; and R1, R2, R4 and R5 are as defined herein; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

    摘要翻译： 本发明涉及通常具有5-HT 6受体亲和性并由式I表示的化合物：其中R 3是SO 2 -Ar，Ar是芳基或杂芳基; 且R 1，R 2，R 4和R 5如本文所定义; 或各异构体，异构体的外消旋或非外消旋混合物，或其药学上可接受的盐或溶剂合物。 本发明还涉及含有这些化合物的药物组合物，其用作治疗剂的方法及其制备方法。

    �3-(4-phenylpiperazin-1-yl)propyl-amino, thio and oxy!-pyridine, pyrimidine and benzene derivatives as .alpha..sub.1 -adrenoceptor antagonists
    27.
    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。