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    1,2-ANNELATED QUINOLINE DERIVATIVES
    6.
    发明申请
    1,2-ANNELATED QUINOLINE DERIVATIVES 审中-公开
    1,2-取代的喹啉衍生物

    公开(公告)号：WO0039082A3

    公开(公告)日：2000-10-26

    申请号：PCT/EP9910214

    申请日：1999-12-17

    Applicant: JANSSEN PHARMACEUTICA NV ,  ANGIBAUD PATRICK RENE ,  VENET MARC GASTON ,  BOURDREZ XAVIER MARC

    Inventor： ANGIBAUD PATRICK RENE ,  VENET MARC GASTON ,  BOURDREZ XAVIER MARC

    IPC: C07D215/06 ,  A61K31/4365 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/498 ,  A61K31/519 ,  A61P35/00 ,  C07D215/18 ,  C07D401/06 ,  C07D403/06 ,  C07D471/04 ,  C07D487/04

    CPC classification number: C07D401/06 ,  A61K31/4745 ,  A61K31/498 ,  A61K31/519 ,  C07D403/06 ,  C07D471/04 ,  C07D487/04

    Abstract: This invention concerns compounds of formula (I), the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein =X -X -X - is a trivalent radical; >Y -Y - is a trivalent radical; r and s are each independently 0, 1, 2, 3, 4 or 5; t is 0, 1, 2 or 3; each R and R are independently hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkylthio, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)amino, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, aryl, arylC1-6alkyl, aryloxy or arylC1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl; or two R or R on adjacent positions form together a bivalent radical; R is hydrogen, halo, C1-6alkyl, cyano, haloC1-6alkyl, hydroxyC1-6alkyl, cyanoC1-6alkyl, aminoC1-6alkyl, C1-6alkyloxyC1-6alkyl, C1-6alkylthio-C1-6alkyl, aminocarbonylC1-6alkyl, hydroxycarbonyl, hydroxycarbonylC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, C1-6alkylcarbonylC1-6alkyl, C1-6alkyloxycarbonyl, aryl, arylC1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, or a radical of formula -O-R , -S-R or -NR R ; R is an optionally substituted imidazolyl; aryl is an optionally substituted phenyl or naphthalenyl; having farnesyl transferase and geranylgeranyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

    Abstract translation: 本发明涉及式（I）化合物，其药学上可接受的酸加成盐及其立体化学异构形式，其中= X 1 -X 2 -X 3 - 为三价基团; Y 1 -Y 2 - 为三价基团; r和s各自独立地为0,1,2,3,4或5; t是0,1,2或3; 每个R 1和R 2独立地为羟基，卤素，氰基，C 1-6烷基，三卤甲基，三卤甲氧基，C 2-6烯基，C 1-6烷氧基，羟基C 1-6烷氧基，C 1-6烷硫基，C 1-6烷氧基C 1-6烷氧基， 单或二（C1-6烷基）氨基，单或二（C1-6烷基）氨基C1-6烷氧基，芳基，芳基C1-6烷基，芳氧基或芳基C1-6烷氧基，羟基羰基，C1-6烷氧基羰基; 或者在相邻位置上的两个R 1或R 2一起形成二价基团; R 3是氢，卤素，C 1-6烷基，氰基，卤代C 1-6烷基，羟基C 1-6烷基，氰基C 1-6烷基，氨基C 1-6烷基，C 1-6烷氧基C 1-6烷基，C 1-6烷硫基-C 1-6烷基，氨基羰基C 1-6烷基， ，羟基羰基C1-6烷基，C1-6烷氧基羰基C1-6烷基，C1-6烷基羰基C1-6烷基，C1-6烷氧基羰基，芳基，芳基C1-6烷氧基C1-6烷基，单或二（C1-6烷基）氨基C1-6烷基， -SR 10或-NR 11 R 12; R 4是任选取代的咪唑基; 芳基是任选取代的苯基或萘基; 具有法尼基转移酶和香叶基香叶基转移酶抑制活性; 它们的制备，含有它们的组合物以及它们作为药物的用途。

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