Pyrozala-pyridyl aminoabkoxyphenol compounds
    1.
    发明授权
    Pyrozala-pyridyl aminoabkoxyphenol compounds 失效
    吡罗扎 - 吡啶基氨基氨基苯酚化合物

    公开(公告)号:US5182291A

    公开(公告)日:1993-01-26

    申请号:US716252

    申请日:1991-06-17

    摘要: 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.

    摘要翻译: 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。

    Benzothiophene compounds and the production and use thereof
    3.
    发明授权
    Benzothiophene compounds and the production and use thereof 失效
    苯并噻吩化合物及其生产和应用

    公开(公告)号:US4007204A

    公开(公告)日:1977-02-08

    申请号:US569819

    申请日:1975-04-21

    CPC分类号: C07D333/68 C07D333/56

    摘要: Novel benzo[b]thiophene derivatives corresponding to the general formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein R represents a branched- or straight-chain alkyl group containing from 1 to 4 carbon atoms, or a cyclohexyl group, n is an integer in the range of from 3 to 6 inclusive, and Am represents a dimethylamino, diethylamino, di-n-propylamino or di-n-butylamino group.These derivatives are useful for the treatment of pathological conditions of the heart and in particular angina pectoris.

    摘要翻译: 对应于以下通式的新型苯并[b]噻吩衍生物及其药学上可接受的酸加成盐,其中R表示含有1至4个碳原子的支链或直链烷基或环己基 n为3〜6的整数,m表示二甲基氨基,二乙基氨基,二正丙基氨基或二 - 正丁基氨基。

    Aminoalkoxyphenyl derivatives, process of preparation and compositions
containing the same
    6.
    发明授权
    Aminoalkoxyphenyl derivatives, process of preparation and compositions containing the same 失效
    氨基烷氧基苯基衍生物,制备方法和含有它们的组合物

    公开(公告)号:US5215988A

    公开(公告)日:1993-06-01

    申请号:US745268

    申请日:1991-08-14

    摘要: 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.

    摘要翻译: 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。

    Process for the preparation of derivatives of sulfonyl indolizine and
their use as synthetic intermediates
    7.
    发明授权
    Process for the preparation of derivatives of sulfonyl indolizine and their use as synthetic intermediates 失效
    制备磺酰基中氮茚衍生物的方法及其作为合成中间体的用途

    公开(公告)号:US5028710A

    公开(公告)日:1991-07-02

    申请号:US534499

    申请日:1990-06-08

    IPC分类号: C07D471/04

    CPC分类号: C07D471/04 Y02P20/55

    摘要: The object of the invention is a process for the preparation of derivatives of 3-sulfonyl indolizine of general formula: ##STR1## in which: R is selected from hydrogen, alkyl, cycloalkyl, substituted or unsubstituted phenyl,R.sub.1 is a protecting group for hydroxyl,R.sub.2 and R.sub.3, identical or different, is each selected from hydrogen, methyl or ethyl or halogen.These compounds are intermediates which can be used for the preparation of 3-aminoalkoxyphenylsulfonyl-indolizines, which are useful in the treatment of certain diseases of the cardiovascular system.

    摘要翻译: 本发明的目的是制备以下通式的3-磺酰基中氮茚衍生物的方法:其中:R选自氢,烷基,环烷基,取代或未取代的苯基,R 1是羟基的保护基 ,R 2和R 3相同或不同,各自选自氢,甲基或乙基或卤素。 这些化合物是可用于制备3-氨基烷氧基苯基磺酰基 - 中氮茚的中间体,其可用于治疗某些心血管系统疾病。

    4-hydroxyphenylthio derivatives, their preparation and their use for the
preparation of aminoalkoxyphenylsulphonyl derivatives
    8.
    发明授权
    4-hydroxyphenylthio derivatives, their preparation and their use for the preparation of aminoalkoxyphenylsulphonyl derivatives 失效
    4-羟基苯硫基衍生物,它们的制备及其在制备氨基烷氧基苯磺酰基衍生物中的应用

    公开(公告)号:US5401855A

    公开(公告)日:1995-03-28

    申请号:US80171

    申请日:1993-06-23

    CPC分类号: C07D209/30

    摘要: The subject of the invention is 4-hydroxyphenylthio derivatives of general formula: ##STR1## in which: R.sub.1 and R.sub.2, which are identical or different, each represent hydrogen, a methyl or ethyl radical or a halogen atom,R represents a (C.sub.1 -C.sub.6) alkyl, (C.sub.3 -C.sub.6) cycloalkyl or phenyl radical,R.sub.3 represents hydrogen or a halogen atom, X represents --O--, --S-- or --NR.sub.4 -- in which R.sub.4 represents hydrogen or a (C.sub.1 -C.sub.4) alkyl group, useful as synthetic intermediates, especially for the preparation of aminoalkoxyphenylsulphonyl derivatives which are pharmaceutically active compounds.

    摘要翻译: 本发明的主题是以下通式的4-羟基苯硫基衍生物:其中:R 1和R 2相同或不同,各自表示氢,甲基或乙基或卤素原子,R表示(C1 -C 6)烷基,(C 3 -C 6)环烷基或苯基,R 3表示氢或卤素原子,X表示-O - , - S-或-NR 4 - ,其中R 4表示氢或(C 1 -C 4)烷基 可用作合成中间体,特别是用于制备作为药物活性化合物的氨基烷氧基苯基磺酰基衍生物。

    Indolizine derivatives, with pharmaceutical activity
    10.
    发明授权
    Indolizine derivatives, with pharmaceutical activity 失效
    具有药物活性的中氮衍生物

    公开(公告)号:US5403933A

    公开(公告)日:1995-04-04

    申请号:US80173

    申请日:1993-06-23

    CPC分类号: C07D471/04

    摘要: The invention relates to indolizine derivatives of general formula: ##STR1## in which: X denotes an --S or --SO.sub.2 -- group, each of R.sub.1 and R.sub.2, which are identical or different, denotes hydrogen, the methyl or ethyl radical or a halogen atom,R.sub.3 denotes hydrogen or a C.sub.1 -C.sub.4 alkyl radical,R.sub.4 denotes a precursor radical of a carboxyl group,R denotes a C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or phenyl radical, and their use as intermediates for the preparation of pharmaceutically active aminoalkoxybenzenesulphonylindolizine derivatives.

    摘要翻译: 本发明涉及以下通式的中氮茚衍生物:其中:X表示-S或-SO 2 - 基,R 1和R 2各自相同或不同,表示氢,甲基或乙基或 卤素原子,R3表示氢或C1-C4烷基,R4表示羧基的前体基团,R表示C1-C6烷基,C3-C6环烷基或苯基,它们用作制备药物的中间体 活性氨基烷氧基苯磺酰基吲嗪衍生物。