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    • 5. 发明授权
    • Pyrozala-pyridyl aminoabkoxyphenol compounds
    • 吡罗扎 - 吡啶基氨基氨基苯酚化合物
    • US5182291A
    • 1993-01-26
    • US716252
    • 1991-06-17
    • Jean GubinPierre ChatelainMarcel DescampsDino NisatoHenri InionJean LucchettiJean-Marie MahauxJean-Noel Vallat
    • Jean GubinPierre ChatelainMarcel DescampsDino NisatoHenri InionJean LucchettiJean-Marie MahauxJean-Noel Vallat
    • C07D209/30C07D213/70C07D213/71C07D215/36C07D235/22C07D261/10C07D277/36C07D307/64C07D471/04C07D495/04
    • C07D213/70C07C309/00C07C317/00C07D209/30C07D213/71C07D215/36C07D235/22C07D261/10C07D277/36C07D307/64C07D471/04C07D495/04
    • Aminoalkoxyphenyl derivatives useful in the treatment of certain pathological syndromes of the cardiovascular system of formula: ##STR1## in which: B represents a --S--, --SO-- or --SO.sub.2 -- group,R.sub.1 and R.sub.2, which are identical or different, each denote hydrogen, a methyl or ethyl radical or a halogen,A denotes a straight- or branched-alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxypropylene radical, in which the hydroxy is optionally substituted by a lower alkyl radical,R.sub.3 denotes an alkyl radical or a radical of formula:--Alk--R.sub.5in which Alk denotes a single bond or a linear- or branched-alkylene radical having from 1 to 5 carbon atoms and R.sub.5 denotes a pyridyl, phenyl, 2,3-methylenedioxyphenyl or 3,4-methylenedioxyphenyl radical or a phenyl group substituted with one or more substituents, which may be identical or different, selected from halogen atoms, lower alkyl groups or lower alkoxy groups,R.sub.4 denotes hydrogen or an alkyl radical orR.sub.3 and R.sub.4 when taken together, denote an alkylene or alkenylene radical having from 3 to 6 carbon atoms and optionally substituted with a phenyl radical or optionally interrupted by --O--, ##STR2## R.sub.6 denoting hydrogen or a lower alkyl or pheny radical, Cy represents a cyclic group with the proviso that when Cy represents a benzo[b]furyl or benzo[b]thienyl group and B represents a --SO.sub.2 -- group, R.sub.3 represents a radical --Alk--R.sub.5, as well as the N-oxide derivative thereof and a pharmaceutically acceptable salt thereof.
    • 用于治疗下列心血管系统的某些病理学综合征的氨基烷氧基苯基衍生物:其中:B表示-S-,-SO-或-SO 2 - 基团,R 1和R 2各自相同或不同, 表示氢,甲基或乙基或卤素,A表示具有2至5个碳原子的直链或支链亚烷基或2-羟基亚丙基,其中羟基任选被低级烷基取代,R 3 表示烷基或式Al-R 5的基团,其中Alk表示单键或具有1至5个碳原子的直链或支链亚烷基,R5表示吡啶基,苯基,2,3-亚甲二氧基苯基 或3,4-亚甲二氧基苯基或被一个或多个选自卤素原子,低级烷基或低级烷氧基的取代基取代的苯基,R4表示氢或烷基或R3和R4,当 一起表示 具有3至6个碳原子并且任选被苯基取代或任选地被-O - , - 表示氢或低级烷基或苯基的-C 1-6的亚烷基或亚烯基,Cy表示环状基团,条件是 当Cy表示苯并[b]呋喃基或苯并[b]噻吩基,B表示-SO 2 - 基时,R 3表示基团-Alk-R 5,以及其N-氧化物衍生物及其药学上可接受的盐。
    • 8. 发明授权
    • Aminoalkoxyphenyl derivatives, process of preparation and compositions
containing the same
    • 氨基烷氧基苯基衍生物,制备方法和含有它们的组合物
    • US5215988A
    • 1993-06-01
    • US745268
    • 1991-08-14
    • Jean GubinPierre ChatelainMarcel DescampsDino NisatoHenri InionJean LucchettiJean-Marie MahauxJean-Noel Vallat
    • Jean GubinPierre ChatelainMarcel DescampsDino NisatoHenri InionJean LucchettiJean-Marie MahauxJean-Noel Vallat
    • C07D209/30C07D213/70C07D213/71C07D215/36C07D235/22C07D261/10C07D277/36C07D307/64C07D471/04C07D495/04
    • C07D213/70C07C309/00C07C317/00C07D209/30C07D213/71C07D215/36C07D235/22C07D261/10C07D277/36C07D307/64C07D471/04C07D495/04
    • The present invention relates to aminoalkoxyphenyl compounds of formula: ##STR1## in which: B is selected from --S--, --SO-- and --SO.sub.2 --,R.sub.1 and R.sub.2, which are identical or different, are selected from hydrogen, methyl, ethyl and halogen,A is selected from a straight- or branched-alkylene radical having from 2 to 5 carbon atoms, a 2-hydroxypropylene radical, and a 2-(lower alkoxy) propylene radical,R.sub.3 is selected from C.sub.1 -C.sub.8 alkyl and a radical of formula:--Alk--Ar in which Alk is selected from a single bond and a linear- or branched-alkylene radical having from 1 to 5 carbon atoms; and Ar is selected from pyridyl, phenyl, 2-3-methyleneoxyphenyl, 3,4-methylenedioxyphenyl and phenyl substituted with one or more substituents, which may be identical or different, selected from halogen atoms, C.sub.1 -C.sub.8 alkyl groups and C.sub.1 -C.sub.8 alkoxy groups,R.sub.4 is selected from hydrogen and C.sub.1 -C.sub.8 alkyl, orR.sub.3 and R.sub.4, when taken together, denote a 1,4-tetra-methylene, 1,5-pentamethylene, 3-oxa-1,5-pentamethylene, 3-aza-1,5-pentamethylene, 3-methylaza-1,5-pentamethylene, 3-phenylaza-1,5-pentamethylene or --CH.dbd.CH--N.dbd.CH-- radical,R is selected from hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.6, cycloalkyl, benzyl, phenyl optionally substituted with one or more substituents, which may be identical or different, selected from halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy as well as a pharmaceutically acceptable salt thereof.
    • 本发明涉及下式的氨基烷氧基苯基化合物:其中:B选自-S-,-SO-和-SO 2 - ,R 1和R 2相同或不同,选自氢,甲基,乙基 和卤素,A选自具有2至5个碳原子的直链或支链亚烷基,2-羟基亚丙基和2-(低级烷氧基)丙烯基,R 3选自C 1 -C 8烷基和 其中Alk选自单键和具有1至5个碳原子的直链或支链亚烷基的式:-Alk-Ar的基团; 并且Ar选自吡啶基,苯基,2-3亚甲基氧基苯基,3,4-亚甲二氧基苯基和被一个或多个可以相同或不同的取代基取代的苯基,其可以选自卤素原子,C 1 -C 8烷基和C 1 -C 8 烷氧基,R 4选自氢和C 1 -C 8烷基,或者R 3和R 4一起表示1,4-四亚甲基,1,5-亚戊基,3-氧杂-1,5-五亚甲基,3 1-氮杂-1,5-五亚甲基,3-甲基-1,5-五亚甲基,3-苯基氮杂-1,5-五亚甲基或-CH = CH-N = CH-基,R选自氢,C 1 -C 8烷基 C 3 -C 6,环烷基,苄基,任选被一个或多个选自卤素,C 1 -C 4烷基和C 1 -C 4烷氧基的取代基取代的苯基以及其药学上可接受的盐。