Quinoline derivatives useful for inhibiting farnesyl protein transferase
    2.
    发明授权
    Quinoline derivatives useful for inhibiting farnesyl protein transferase 失效
    用于抑制法呢基蛋白转移酶的喹啉衍生物

    公开(公告)号:US06596735B1

    公开(公告)日:2003-07-22

    申请号:US09724464

    申请日:2000-11-28

    申请人: Bingwei V. Yang

    发明人: Bingwei V. Yang

    IPC分类号: A61K314709

    CPC分类号: C07D401/06

    摘要: The invention relates to compounds of the formula: and to pharmaceutically acceptable salts and solvates thereof wherein Y, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 have the meanings defined in the specification. The invention also relates to pharmaceutical compositions comprising said compounds and to the use of said compounds for inhibiting abnormal cell growth in mammals. The compounds of the above formula have activity as farnesyl protein transferase inhibitors.

    摘要翻译: 本发明涉及下式的化合物及其药学上可接受的盐和溶剂化物,其中Y,R 1,R 2,R 3,R 4,R 5,R 6,R 7,R 8,R 9和R 10具有本说明书中定义的含义。 本发明还涉及包含所述化合物的药物组合物和所述化合物用于抑制哺乳动物异常细胞生长的用途。 上述化合物具有法呢基蛋白转移酶抑制剂的活性。

    Crystal modification B of 8-cyano-1-cyclopropyl-7-(1S,6S-2, 8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
    7.
    发明授权
    Crystal modification B of 8-cyano-1-cyclopropyl-7-(1S,6S-2, 8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid 有权
    8-氰基-1-环丙基-7-(1S,6S-2,8-二氮杂双环[4.3.0]壬烷-8-基)-6-氟-1,4-二氢-4-氧代 - 3-喹啉羧酸

    公开(公告)号:US06664268B1

    公开(公告)日:2003-12-16

    申请号:US09856670

    申请日:2001-05-23

    IPC分类号: A61K314709

    CPC分类号: C07D471/04

    摘要: The present invention relates to a defined crystal modification of 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid of the formula (I), to processes for its preparation and to its use in pharmaceutical preparations. The crystal modification can be distinguished from other crystal modifications of 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid of the formula (I) by its characteristic X-ray powder diffractogram and its differential thermodiagram (see description).

    摘要翻译: 本发明涉及8-氰基-1-环丙基-7-(1S,6S-2,8-二氮杂双环[4.3.0]壬烷-8-基)-6-氟-1,4- 式(I)的二氢-4-氧代-3-喹啉羧酸,其制备方法及其在药物制剂中的应用。晶体修饰可以区别于8-氰基-1-环丙基-7 - (1S,6S-2,8-二氮杂双环[4.3.0]壬烷-8-基)-6-氟-1,4-二氢-4-氧代-3-喹啉羧酸其特征 X射线粉末衍射图及其差示热图(见说明)。

    2-aminoalkylaminoquinolines as dopamine D4 ligands
    10.
    发明授权
    2-aminoalkylaminoquinolines as dopamine D4 ligands 失效
    2-氨基烷基氨基喹啉作为多巴胺D4配体

    公开(公告)号:US06313141B1

    公开(公告)日:2001-11-06

    申请号:US09445661

    申请日:2000-03-08

    申请人: Xiao-Shu He

    发明人: Xiao-Shu He

    IPC分类号: A61K314709

    摘要: Disclosed are compounds of the formula or the pharmaceutically acceptable salts thereof wherein: A represents an optionally substituted alkylene group of from 2-5 carbon atoms; W is COH or CH; Y and Z are nitrogen or CH; and R1, R2, R3, R4, R5, R6 are defined herein. Pharmaceutical compositions and preparations containing such compounds are also provided. The invention further relates to the use of such compounds in the treatment of neuropsychological diseases such as schizophrenia and other central nervous system diseases.

    摘要翻译: 公开了下式的化合物或其药学上可接受的盐,其中:A表示任选取代的2-5个碳原子的亚烷基; W是COH或CH; Y和Z是氮或CH; 并且R1,R2,R3,R4,R5,R6定义为本文。还提供了含有这些化合物的药物组合物和制剂。 本发明还涉及这些化合物在治疗神经心理疾病如精神分裂症和其它中枢神经系统疾病中的应用。