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85 条记录 (耗时 0.06 秒)

    3-(1-Substituted-4-piperazinyl)-1H-indazoles
    51.
    发明授权
    3-(1-Substituted-4-piperazinyl)-1H-indazoles 失效
    3-（1-取代的-4-哌嗪基）-1H-吲唑

    公开(公告)号：US5077405A

    公开(公告)日：1991-12-31

    申请号：US526154

    申请日：1990-05-21

    申请人： Joseph T. Strupczewski ,  Kenneth J. Bordeau

    发明人： Joseph T. Strupczewski ,  Kenneth J. Bordeau

    IPC分类号： C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07F9/6558

    CPC分类号： C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07F9/65583

    摘要： This invention relates to 3-(1-substituted-4-piperazinyl)-1H-indazoles having the following formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, arylloweralkyl, acyl, cycloalkylloweralkylene, and phenylsulfonyl; and R.sub.2 is hydrogen, lower alkyl, hydroxyloweralkyl of the formula -(loweralkylene)-OH, arylloweralkyl, acyl, cycloalkylloweralkylene, ##STR2## where Z is selected from hydrogen, halogen, loweralkoxy, CF.sub.3, NO.sub.2, and NH.sub.2 ; ##STR3## where Z is as defined above; ##STR4## where Z is as defined above; ##STR5## where R.sub.3 and R.sub.4 are each independently hydrogen and loweralkyl; ##STR6## where Z is as defined above; ##STR7## where R' and R" are each independently hydrogen and loweralkyl; X is hydrogen, loweralkyl, hydroxyl, halogen, loweralkoxy, CF.sub.3, NO.sub.2 and amino; n is an integer of 1 to 4, with the further proviso that R.sub.2 is not loweralkyl when R.sub.1 is hydrogen or acyl and X is chloro; the pharmaceutically acceptable acid addition salts thereof and where appropriate the geometric isomers, the stereoisomers and racemic mixtures thereof. The compounds of this invention display utility as analgesic and antipsychotic agents.

    摘要翻译： 本发明涉及具有下式的3-（1-取代-4-哌嗪基）-1H-吲唑，其中R1是氢，低级烷基，芳基低级烷基，酰基，环烷基亚烷基和苯基磺酰基; 其中Z选自氢，卤素，低级烷氧基，CF 3，NO 2和NH 2; R 2是氢，式 - （低级亚烷基）-OH的低级烷基，羟基低级烷基，芳基低级烷基，酰基，环烷基亚烷基， 其中Z如上所定义; 其中Z如上所定义; 其中R 3和R 4各自独立地为氢和低级烷基; 其中Z如上所定义; 其中R'和R“各自独立地为氢和低级烷基; X是氢，低级烷基，羟基，卤素，低级烷氧基，CF 3，NO 2和氨基; n为1至4的整数，另外条件是当R 1为氢或酰基且X为氯时，R 2不为低级烷基; 其药学上可接受的酸加成盐，以及适当的几何异构体，其立体异构体和外消旋混合物。 本发明化合物显示出作为止痛剂和抗精神病药物的用途。

    Antihypertensive 1,2-benzisothiazole piperidines
    56.
    发明授权
    Antihypertensive 1,2-benzisothiazole piperidines 失效
    抗高血压1,2-苯并异噻唑哌啶

    公开(公告)号：US4528292A

    公开(公告)日：1985-07-09

    申请号：US603264

    申请日：1984-04-23

    申请人： Joseph T. Strupczewski

    发明人： Joseph T. Strupczewski

    IPC分类号： A61K31/445 ,  A61P9/12 ,  C07D417/04 ,  A61K31/425

    CPC分类号： C07D417/04

    摘要： There are described novel antihypertensive 1,2-benzisothiazole piperidines of the formula ##STR1## where X is hydrogen, halogen, loweralkoxy, loweralkyl, nitro, amino or trifluoromethyl; and R is ##STR2## R.sub.1 being loweralkyl, aryl, aralkyl, cycloalkylloweralkyl or a loweralkyl substituted with an amino, loweralkylamino or diloweralkylamino, and R.sub.2 being hydrogen, loweralkyl or aryl; antihypertensive compositions comprising said compounds or pharmaceutically acceptable acid addition salts thereof; and methods for synthesizing the same.

    摘要翻译： 描述了新颖的抗低血压1,2-苯并异噻唑哌啶类，其中X是氢，卤素，低级烷氧基，低级烷基，硝基，氨基或三氟甲基; R 1为低级烷基，芳基，芳烷基，环烷基低级烷基或被氨基，低级烷基氨基或二低级烷基氨基取代的低级烷基，R 2为氢，低级烷基或芳基; 包含所述化合物或其药学上可接受的酸加成盐的抗高血压组合物; 及其合成方法。