Process for the preparation of an optically pure aminoalcohol
    3.
    发明授权
    Process for the preparation of an optically pure aminoalcohol 失效
    制备光学纯氨基醇的方法

    公开(公告)号:US5512680A

    公开(公告)日:1996-04-30

    申请号:US294035

    申请日:1994-08-24

    摘要: A process is described for the preparation of (+)-2-(3,4-dichlorophenyl)-4-hydroxybutylamine (I) by reaction of 3,4-dichlorophenylacetonitrile (II) with an alkali metal halogenoacetate, treatment of the 3-cyano-3-(3,4-dichlorophenyl)propionic acid (III) with D-(-)-N-methylglucamine, with second-order asymmetric conversion, hydrolysis of the D-(-)-N-methylglucamine salt of (-)-3-cyano-3-(3,4-dichlorophenyl)propionic acid and enantioconservative reduction of the resulting levorotatory cyanoacid with a borane.

    摘要翻译: 描述了通过3,4-二氯苯基乙腈(II)与碱金属卤代乙酸酯反应制备(+) - 2-(3,4-二氯苯基)-4-羟基丁胺(I)的方法, 氰基-3-(3,4-二氯苯基)丙酸(III)与D - ( - ) - N-甲基葡糖胺反应,二级不对称转化,( - ) - ( - ) - N-甲基葡糖胺盐 )-3-氰基-3-(3,4-二氯苯基)丙酸,并用硼烷对所得的左旋氰基酸进行保护剂的还原。

    Process for the preparation of an optically pure aminoalcohol
    4.
    发明授权
    Process for the preparation of an optically pure aminoalcohol 失效
    制备光学纯氨基醇的方法

    公开(公告)号:US5780666A

    公开(公告)日:1998-07-14

    申请号:US598001

    申请日:1996-02-07

    摘要: A process is described for the preparation of (+)-2-(3,4-dichlorophenyl)-4-hydroxybutylamine (I) by reaction of 3,4-dichlorophenylacetic acid (II) with an alkali metal halogenoacetate, treatment of the 3-cyano-3-(3,4-dichlorophenyl)propionic acid (III) with D-(-)-N-methylglucamine, with second-order asymmetric conversion, hydrolysis of the D-(-)-N-methylglucamine salt of (-)-3-cyano-3-(3,4-dichlorophenyl,)propionic acid and enantioconservative reduction of the resulting levorotatory cyanoacid with a borane.

    摘要翻译: 描述了通过3,4-二氯苯乙酸(II)与碱金属卤代乙酸酯反应制备(+) - 2-(3,4-二氯苯基)-4-羟丁胺(I)的方法,处理3 ( - ) - ( - ) - N-甲基葡糖胺的氰基-3-(3,4-二氯苯基)丙酸(III),二次不对称转化,( - ) - ( - ) - N-甲基葡糖胺盐水解 - ) - 3-氰基-3-(3,4-二氯苯基)丙酸,并用硼烷对所得的左旋氰基酸进行保护剂的还原。

    Pyrozala-pyridyl aminoabkoxyphenol compounds
    5.
    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。

    Disubstituted glutarimide method for preparing same, and use thereof
    8.
    发明授权
    Disubstituted glutarimide method for preparing same, and use thereof 失效
    用于制备其的二取代戊二酰亚胺方法及其用途

    公开(公告)号:US06242607B1

    公开(公告)日:2001-06-05

    申请号:US09437362

    申请日:1999-11-10

    IPC分类号: C07D2404

    摘要: The invention relates to glutarimides of formula (I): in which Ar represents a phenyl non substituted or substituted one or more times with one of the substituents selected from a halogen atom, a hydroxyl, a (C1-C4)alkoxy, a trifluoromethyl, a (C1-C4)alkyl, said substituents being identical or different; a pyridyl group; a thienyl group and X is methylene or ethylene, their salts and their enantiomers, as well as their method of preparation and their use for the preparation of the corresponding 3,3-disubstituted piperidines.

    摘要翻译: 本发明涉及式(I)的戊二酰亚胺:其中Ar表示未取代或取代一个或多个选自卤原子,羟基,(C 1 -C 4)烷氧基,三氟甲基, (C 1 -C 4)烷基,所述取代基相同或不同; 吡啶基; 噻吩基,X是亚甲基或亚乙基,它们的盐及其对映异构体,以及它们的制备方法及其用于制备相应的3,3-二取代的哌啶的用途。

    Pharmaceutical and veterinary compositions for the treatment of ischemic
cardiac disorders
    9.
    发明授权
    Pharmaceutical and veterinary compositions for the treatment of ischemic cardiac disorders 失效
    用于治疗缺血性心脏病的药物和兽药组合物

    公开(公告)号:US4791137A

    公开(公告)日:1988-12-13

    申请号:US936776

    申请日:1986-12-02

    CPC分类号: C07D307/80 Y10S514/821

    摘要: Pharmaceutical and veterinary compositions having as essential active ingredient at least one benzofuran derivative of the general formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof in which R represents an amino, monoethylamino or diethylamino radical and X.sub.1 and X.sub.2 represent hydrogen or iodine with the proviso that when R represents diethylamino X.sub.1 and X.sub.2 are different.These compositions are useful for the treatment of ischemic cardiac disorders.

    摘要翻译: 作为必需活性成分的具有以下通式的至少一种苯并呋喃衍生物或其药学上可接受的酸加成盐的药物和兽药组合物,其中R表示氨基,单乙氨基或二乙氨基,X 1和X 2表示氢或碘与 条件是当R表示二乙基氨基X1和X2不同时。 这些组合物可用于治疗缺血性心脏病。

    Benzothiophene compounds and the production and use thereof
    10.
    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。