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(IMIDAZOL-5-YL)METHYL-2-QUINOLINONE DERIVATIVES AS INHIBITORS OF SMOOTH MUSCLE CELL PROLIFERATION

机译:(咪唑-5-基)甲基-2-喹啉酮衍生物作为平滑肌细胞增殖的抑制剂

摘要

The invention comprises the use of compounds of formula (I) wherein the dottedline represents an optional bond; Xis oxygen or sulfur; R1 is hydrogen, C1-12alkyl, Ar1, Ar2C1-6alkyl,quinolinylC1-6alkyl, pyridylC1-6alkyl, hydroxyC1-6alkyl,C1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, aminoC1-6alkyl,or a radical of formula -Alk1-C(=O)-R9, -Alk1-S(O)-R9or -Alk1-S(O)2-R9; R2, R3 and R16 each independently are hydrogen, hydroxy,halo, cyano, C1-6alkyl, C1-6alkyloxy,hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, aminoC1-6alkyloxy, mono- ordi(C1-6alkyl)aminoC1-6alkyloxy, Ar1, Ar2C1-6alkyl, Ar2oxy,Ar2C1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl, trihalomethyl,trihalomethoxy, C2-6alkenyl; R4 and R5 each independentlyare hydrogen, halo, Ar1, C1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl,C1-6alkyoloxy, C1-6alkylthio, amino, hydroxycarbonyl,C1-6alkyloxycarbonyl, C1-6alkylS(O)C1-4alkyl or C1-6alkylS(O)2C1-6alkyl; R6and R7 each independently are hydrogen, halo, cyano,C1-6alkyl, 4,4-dimethyl-oxazolyl, C1-6alkyloxy or Ar2oxy; R8 is hydrogen, C1-6alkyl, cyano, hydroxycarbonyl, C1-6alkyloxycarbonyl,C1-6alkylcarbonylC1-6alkyl, cyanoC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl,carboxyC1-6alkyl, hydroxyC1-6alkyl, aminoC1-6alkyl,mono-- or di(C1-6alkyl)aminoC1-6alkyl, imidazolyl, haloC1-6alkyl, C1-6alkyloxyC1-6alkyl, aminocarbonylC1-6alkyl, or a radical of formula-O-R10, -S-R10, -N-R11O12; R17 is hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxycarbonyl, Ar1; R18 is hydrogen, C1-6alkyl, C1-6alkyloxyor halo; R19 is hydrogen or C1-6alkyl; for the manufacture of a medicament toinhibit smooth muscle cell proliferation.
机译:本发明包括式(I)化合物的用途,其中虚线线表示可选键; X是氧或硫; R1是氢,C1-12烷基,Ar1,Ar2C1-6烷基喹啉基C1-6烷基,吡啶基C1-6烷基,羟基C1-6烷基,C 1-6烷氧基C 1-6烷基,单或二(C 1-6烷基)氨基C 1-6烷基,氨基C 1-6烷基,或式-Alk1-C(= O)-R9,-Alk1-S(O)-R9的基团或-Alk1-S(O)2-R9; R2,R3和R16各自独立地是氢,羟基,卤素,氰基,C1-6烷基,C1-6烷氧基,羟基C1-6烷氧基,C1-6烷氧基C1-6烷氧基,氨基C1-6烷氧基,单或二(C 1-6烷基)氨基C 1-6烷氧基,Ar 1,Ar 2 C 1-6烷基,Ar 2氧基,Ar 2 C 1-6烷氧基,羟基羰基,C 1-6烷氧基羰基,三卤甲基,三卤甲氧基,C 2-6烯基; R4和R5各自独立是氢,卤素,Ar 1,C 1-6烷基,羟基C 1-6烷基,C 1-6烷氧基C 1-6烷基,C 1-6烷氧基,C 1-6烷硫基,氨基,羟羰基,C 1-6烷氧基羰基,C 1-6烷基S(O)C 1-4烷基或C 1-6烷基S(O)2 C 1-6烷基; R6和R7分别独立地是氢,卤素,氰基,C 1-6烷基,4,4-二甲基-恶唑基,C 1-6烷氧基或Ar 2氧基; R8是氢,C1-6烷基,氰基,羟羰基,C1-6烷氧羰基,C 1-6烷基羰基C 1-6烷基,氰基C 1-6烷基,C 1-6烷氧基羰基C 1-6烷基,羧基C1-6烷基,羟基C1-6烷基,氨基C1-6烷基,单或二(C 1-6烷基)氨基C 1-6烷基,咪唑基,卤代C 1-6烷基,C 16烷氧基C1-6烷基,氨基羰基C1-6烷基或下式的基团-O-R10,-S-R10,-N-R11O12; R17是氢,卤素,氰基,C1-6烷基,C1-6烷氧羰基,Ar1; R 18是氢,C 1-6烷基,C 1-6烷氧基或光环R 19为氢或C 1-6烷基;用于制造药物抑制平滑肌细胞增殖。

著录项

  • 公开/公告号CA2290992C

    专利类型

  • 公开/公告日2008-02-12

    原文格式PDF

  • 申请/专利权人 JANSSEN PHARMACEUTICA N.V.;

    申请/专利号CA19982290992

  • 发明设计人 END DAVID WILLIAM;ZELESKO MICHAEL J.;

    申请日1998-05-25

  • 分类号A61K31/4709;A61P9/10;

  • 国家 CA

  • 入库时间 2022-08-21 20:04:02

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