会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 2. 发明申请
    • SUBSTITUTED 1-ISOQUINOLONE DERIVATIVES AS ANGIOTENSIN II ANTAGONISTS
    • 取代的1-异喹啉酮衍生物作为ANGIOTENSIN II拮抗剂
    • WO1993014086A1
    • 1993-07-22
    • PCT/US1993000188
    • 1993-01-15
    • SYNTEX (U.S.A.) INC.FISHER, Lawrence, E.CAROON, Joan, M.STABLER, Stephen, R.CLARK, Robin, D.
    • SYNTEX (U.S.A.) INC.
    • C07D401/10
    • C07D221/20C07D217/24C07D401/10C07D409/10
    • 1-Isoquinolone derivatives and related compounds according to formula (I) wherein, Y is selected from the group consisting of H, OH, lower alkoxy, and halo; X is selected from the group consisting of H, lower alkyl acid, lower alkyl ester, and lower alkyl; and R is selected from the group consisting of H, alkenyl, lower alkyl, lower cycloalkyl, unsubstituted or substituted 3-spiro-1H-indane of structure (II) wherein R is H, OH, lower alkyl, lower alkoxy or halo, and 3-spiro-cycloalkyl of structure (III) wherein n is an integer from zero to six, provided that when R is spiro- X is H, or a pharmaceutically acceptable salt thereof, with the proviso that when R is spiro-, X is H, and when R is H, alkenyl, lower alkyl or lower cycloalkyl substituted at the 3-position of the isoquinolone moiety and X is H or lower alkyl, the (2"-1H--tetrazol-5-yl)biphenyl-4'-ylmethyl group cannot be at the 2(N) position, are useful as angiotensin II receptor antagonists. Also disclosed are methods of synthesis, intermediates, pharmaceutical formulations and methods of treatment.
    • 1-异喹诺酮衍生物和根据式(I)的相关化合物,其中Y选自H,OH,低级烷氧基和卤素; X选自H,低级烷基酸,低级烷基酯和低级烷基; 和R 1选自H,烯基,低级烷基,低级环烷基,结构(II)的未取代或取代的3-螺-1H-二氢化茚,其中R 2是H,OH,低级烷基, 低级烷氧基或卤素,和结构(III)的3-螺环烷基,其中n为0至6的整数,条件是当R 1为螺环X为H时,或其药学上可接受的盐,条件是 当R 1为螺 - ,X为H时,当R 1为H时,在异喹啉酮部分的3位被取代的链烯基,低级烷基或低级环烷基,X为H或低级烷基,( 2“-1H-四唑-5-基)联苯-4'-基甲基不能在2(N)位,可用作血管紧张素II受体拮抗剂。还公开了合成方法,中间体,药物制剂和方法 的治疗。