首页> 外国专利> NOVEL 1,3-BENZODIOXOLE AND 1,2-DIALKOXYBENZENE DERIVATIVES AS OCULAR HYPOTENSIVE AGENTS

NOVEL 1,3-BENZODIOXOLE AND 1,2-DIALKOXYBENZENE DERIVATIVES AS OCULAR HYPOTENSIVE AGENTS

机译:新型1,3-苯并二恶唑和1,2-二氧苯甲醛衍生物作为眼压降压药

摘要

Compounds of the formula IMAGE where W is (CH2)n where n is 1 or 2, or n is O and W represents lower alkyl groups attached to each oxygen; m is an integer between 1 and 8; R1 is COOH or a pharmaceutically acceptable salt thereof, COOR4, CONR5R6, CONR5SO2R7, CH2OH, CH2OR7, CH2O-COR7, CH2O-CONR5, R7, CH2OCOOR7, CH2NH2, CH2NR5R6, CH2NR5COR7, CHO, CH(OR8)2, CHOR9O, -COR10, CR10(OR8)2, or CR10OR9O, where R4 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R4 is phenyl or lower alkylphenyl, R5 and R6 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or phenyl or lower alkylphenyl, R7 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R8 is lower alkyl, and R9 is divalent alkyl radical of 2-5 carbons, R10 is an alkyl OR cycloalkyl containing 1 to 5 carbons; R2 is H, COR7, R7, CO-OR7, CO-NR5, R7, PO(OH)OR7, PO(OR7)2, POR7OH, or POR7(OR7); R3 is lower alkyl, phenyl, lower alkyl or halogen substituted phenyl, phenyl substituted lower alkyl, or heteroaryl substituted lower alkyl, are capable of lowering introaocular pressure in the eye of a mammal.
机译:的化合物,其中W为(CH 2)n,其中n为1或2,或n为O,W表示与每个氧相连的低级烷基; m是1至8之间的整数; R1是COOH或其药学上可接受的盐,COOR4,CONR5R6,CONR5SO2R7,CH2OH,CH2OR7,CH2O-COR7,CH2O-CONR5,R7,CH2OCOOR7,CH2NH2,CH2NR5R6,CH2NR5COR7,CHO,CH(OR8)2,CHOR9 ,CR10(OR8)2或CR10OR9O,其中R4是1至10个碳原子的烷基,或5至10个碳原子的环烷基,或R4是苯基或低级烷基苯基,R5和R6独立地是氢,烷基碳原子数为1至10的碳原子,或碳原子数为5至10的环烷基,或苯基或低级烷基苯基,R 7为碳原子数为1至10的烷基,苯基或低级烷基苯基,R 8为低级烷基,R 9为2-的二价烷基R10为5个碳原子,R10为含1至5个碳原子的烷基OR环烷基; R2为H,COR7,R7,CO-OR7,CO-NR5,R7,PO(OH)OR7,PO(OR7)2,POR7OH或POR7(OR7); R 3是低级烷基,苯基,低级烷基或卤素取代的苯基,苯基取代的低级烷基或杂芳基取代的低级烷基,它们能够降低哺乳动物眼睛的眼内压。

著录项

  • 公开/公告号EP0695300B1

    专利类型

  • 公开/公告日2001-05-16

    原文格式PDF

  • 申请/专利权人 ALLERGAN INC.;

    申请/专利号EP19940915817

  • 发明设计人 BURK ROBERT M.;WOODWARD DAVID F.;

    申请日1994-04-18

  • 分类号C07D319/08;C07D317/50;A61K31/335;

  • 国家 EP

  • 入库时间 2022-08-22 01:17:18

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