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    Nitroxy amino propanols for treating heart and circulatory diseases
    3.
    发明授权
    Nitroxy amino propanols for treating heart and circulatory diseases 失效
    用于治疗心脏和循环系统疾病的硝基氨基丙醇

    公开(公告)号：US4801596A

    公开(公告)日：1989-01-31

    申请号：US803497

    申请日：1985-12-02

    申请人： Herbert Simon ,  Helmut Michel ,  Walter-Gunar Friebe ,  Wolfgang Bartsch

    发明人： Herbert Simon ,  Helmut Michel ,  Walter-Gunar Friebe ,  Wolfgang Bartsch

    IPC分类号： A61K31/135 ,  A61K31/165 ,  A61K31/21 ,  A61K31/275 ,  A61K31/443 ,  A61K31/445 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P25/02 ,  C07C67/00 ,  C07C231/00 ,  C07C231/02 ,  C07C231/12 ,  C07C233/12 ,  C07C233/16 ,  C07C235/08 ,  C07C235/34 ,  C07C239/00 ,  C07C253/00 ,  C07C255/54 ,  C07C255/59 ,  C07C269/00 ,  C07C275/50 ,  C07C301/00 ,  C07C311/30 ,  C07C311/37 ,  C07C313/00 ,  C07C317/18 ,  C07C317/46 ,  C07D211/22 ,  C07D211/46 ,  C07D295/04 ,  C07D303/22 ,  C07D405/12

    CPC分类号： C07D303/22 ,  C07C255/00 ,  C07D211/22 ,  C07D211/46 ,  C07D405/12

    摘要： The present invention provides new aminopropanol derivatives of the general formula: ##STR1## wherein A is a direct bond, a straight-chained or branched alkylene chain containing up to 3 carbon atoms or a --CO--CH.sub.2 -- group; X is a direct bond or a carbonyl group; B is a straight-chained or branched, saturated or unsaturated alkylene chain containing up to 12 carbon atoms, in which one or two --CH.sub.2 -- groups can also be replaced by a saturated or unsaturated alkylene ring containing 3 to 7 carbon atoms and/or by an oxygen or sulphur atom or an --S(.dbd.O)-- or --S(.dbd.O).sub.2 -- group, n is 1, 2 or 3; R.sub.1 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated alkyl radical containing up to 6 carbon atoms or a --B--(ONO.sub.2).sub.n group, in which B and n have the same meanings as above, or when A is a --CO--CH.sub.2 -- group and X is a direct bond, R.sub.1 together with the nitrogen atom and a carbon atom of chain B can represent a heteroaliphatic ring containing 2 to 7 carbon atoms; R.sub.2 is a hydrogen or halogen atom or a cyano, hydroxyl, amino, nitro, carboxyl, carbamoyl, ureido or sulphamoyl group or an alkyl, alkoxy, alkylamino, alkylthio, hydroxyalkyl, aminoalkyl, alkoxycarbonyl, alkylcarbonyl, alkylaminocarbonyl, alkylcarbonylamino, alkoxycarbonylamino or alkylaminocarbonylamino radical; and R.sub.3 is an alkyl or nitroxyalkyl radical containing 3 to 8 carbon atoms; and the physiologically acceptable salts thereof.The present invention also provides processes for the preparation of these aminopropanol derivatives and pharmaceutical compositions containing them, as well as intermediates for the preparation of the new aminopropanol derivatives.

    摘要翻译： 本发明提供了以下通式的新的氨基丙醇衍生物：其中A是直接键，含有至多3个碳原子的直链或支链亚烷基链或-CO-CH 2 - 基团; X是直接键或羰基; B是含有至多12个碳原子的直链或支链，饱和或不饱和的亚烷基链，其中一个或两个-CH 2 - 基团也可以被含有3至7个碳原子的饱和或不饱和亚烷基环和/或 通过氧或硫原子或-S（= O） - 或-S（= O）2 - 基团，n是1,2或3; R1是氢原子或含有至多6个碳原子的直链或支链，饱和或不饱和的烷基或-B-（ONO 2）n基团，其中B和n具有与上述相同的含义，或当A 是-CO-CH 2 - 基团，X是直接键，R 1与氮原子一起形成，链B的碳原子可以表示含有2至7个碳原子的杂脂肪族环; R2是氢或卤原子或氰基，羟基，氨基，硝基，羧基，氨基甲酰基，脲基或氨磺酰基或烷基，烷氧基，烷基氨基，烷硫基，羟基烷基，氨基烷基，烷氧基羰基，烷基羰基，烷基氨基羰基，烷基羰基氨基，烷氧基羰基氨基或烷基氨基羰基氨基 激进; R3为含有3-8个碳原子的烷基或硝基烷基; 及其生理上可接受的盐。 本发明还提供制备这些氨基丙醇衍生物和含有它们的药物组合物的方法，以及制备新的氨基丙醇衍生物的中间体。

    Pharmaceutical compositions containing nitroxyalkylamines, novel nitroxyalkylamines and processes for the preparation thereof
    5.
    发明授权
    Pharmaceutical compositions containing nitroxyalkylamines, novel nitroxyalkylamines and processes for the preparation thereof 失效
    含有硝基烷基胺，新型硝基烷基胺的药物组合物及其制备方法

    公开(公告)号：US5037849A

    公开(公告)日：1991-08-06

    申请号：US424452

    申请日：1989-10-20

    申请人： Herbert Simon ,  Helmut Michel ,  Michael Schultz ,  Wolfgang Bartsch

    发明人： Herbert Simon ,  Helmut Michel ,  Michael Schultz ,  Wolfgang Bartsch

    IPC分类号： A61K31/21 ,  A61K31/395 ,  A61K31/40 ,  A61K31/445 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  C07C235/10 ,  C07C235/26 ,  C07C235/40 ,  C07C237/08 ,  C07C237/18 ,  C07C275/10 ,  C07C275/14 ,  C07C275/16 ,  C07C275/26 ,  C07D211/06 ,  C07D295/13 ,  C07D295/14 ,  C07D295/215

    CPC分类号： C07D295/215 ,  A61K31/21 ,  C07C235/10 ,  C07C235/26 ,  C07C235/40 ,  C07C237/08 ,  C07C275/10 ,  C07C275/14 ,  C07C275/16 ,  C07C275/26 ,  C07D295/13 ,  C07C2101/14

    摘要： The present invention provides pharmaceutical compositions effective against angina-like heart and circulatory diseases containing at least one nitroxyalkylamine derivative of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom, a lower-alkyl radical, a C.sub.3 -C.sub.8 -cycloalkyl or C.sub.3 -C.sub.8 -cycloalkenyl radical, an aminocarbonyl, C.sub.1 -C.sub.6 -mono- or di-alkylaminocarbonyl radical, R.sup.2 is a hydrogen atom, a lower-alkyl radical or a C.sub.3 -C.sub.8 -cycloalkyl or cycloalkenyl radical or R.sup.2, together with R.sup.1 and the nitrogen atom to which they are attached, form a heteroaliphatic ring containing up to 6 carbon atoms, A is a valency bond or a straight-chained or branched lower-alkylene radical, in which a --CH.sub.2 -- group can be replaced by a cycloalkylene radical, B is a lower-alkylene radical, in which a --CH.sub.2 -- group can be replaced by a cycloalkylene radical and X is an --NR.sup.3 --CO-- or --CO--NR.sup.3 -- radical, in which R.sup.3 is a hydrogen atom or a lower-alkyl radical, when X is an --NR.sup.3 --CO-- radical, R.sup.3, together with the nitrogen atom and a carbon atom of the group A, bridge a heterocyclic ring containing 4 to 6 carbon atoms or R.sup.3, together with R.sup.2, A and the two nitrogen atoms, bridge a heterocyclic ring containing 3 to 5 carbon atoms; and the optically-active forms and physiologically acceptable salts thereof.

    摘要翻译： 本发明提供了有效抗心绞痛的心脏和循环系统疾病的药物组合物，其含有至少一种以下通式的硝基烷基胺衍生物：其中R 1是氢原子，低级烷基，C 3 -C 8 - 环烷基或C 3 -C 8 - 环烯基，氨基羰基，C 1 -C 6 - 单 - 或二 - 烷基氨基羰基，R 2是氢原子，低级烷基或C 3 -C 8 - 环烷基或环烯基或R 2，连同 R1和它们所连接的氮原子形成含有至多6个碳原子的杂脂族环，A是价键或直链或支链的低级亚烷基，其中-CH 2 - 基团可以被 亚环烷基，B是低级亚烷基，其中-CH 2 - 基团可被亚环烷基代替，X是-NR 3 -CO-或-CO-NR 3 - 基，其中R 3是氢原子 或低级烷基，当X是-NR 3 -CO-基时，R 3与硝基一起形成 原子和A基团的碳原子，桥接含有4至6个碳原子的杂环或R3与R2，A和两个氮原子一起桥接含有3至5个碳原子的杂环; 和其光学活性形式和生理上可接受的盐。

    Pharmaceutical phenylacetonitrile derivatives
    7.
    发明授权
    Pharmaceutical phenylacetonitrile derivatives 失效
    药用苯乙腈衍生物

    公开(公告)号：US4612313A

    公开(公告)日：1986-09-16

    申请号：US774354

    申请日：1985-09-10

    申请人： Herbert Leinert ,  Wolfgang Kampe ,  Klaus Strein ,  Bernd Muller-Beckmann ,  Wolfgang Bartsch

    发明人： Herbert Leinert ,  Wolfgang Kampe ,  Klaus Strein ,  Bernd Muller-Beckmann ,  Wolfgang Bartsch

    IPC分类号： A61K31/21 ,  A61K31/275 ,  A61K31/445 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07C67/00 ,  C07C253/00 ,  C07C255/24 ,  C07C255/32 ,  C07C255/42 ,  C07C255/43 ,  C07C255/53 ,  C07C255/58 ,  C07C255/59 ,  C07D207/08 ,  C07D211/22 ,  C07D241/04 ,  C07D295/16 ,  C07D295/18 ,  A61K31/495 ,  C07C121/80

    CPC分类号： C07C255/00 ,  C07D211/22

    摘要： The present invention provides phenylacetonitrile derivatives of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5, which can be the same or different, are hydrogen or haolgen atoms or alkyl, alkoxy, nitro, amino or acylamino radicals and two adjacent substituents can together also form a methylenedioxy or ethylenedioxy radical, A is a radical of the general formula: ##STR2## in which R.sub.6 is a straight-chained, cyclic or branched, saturated or unsaturated alkyl radical containing 2 to 12 carbon atoms, R.sub.7 is a hydrogen atom or a straight-chained or branched, saturated alkyl radical containing up to 6 carbon atoms, m and n, which can be the same or different, are 2 or 3, p is 1 or 2 and X is a straight-chained, cyclic or branched alkyl radical containing 2 to 10 carbon atoms which is optionally substituted by an amino group or is a grouping of the general formula: ##STR3## wherein Y and Z, which can be the same or different, are straight-chained or branched alkyl radicals containing up to 8 carbon atoms or cycloalkyl, alkylcycloalkyl or cycloalkylalkyl radicals, in which these radicals are optionally interrupted by an oxygen or sulphur atom, and one of the groups Z in general formula II can also be a hydrogen atom or both Z groups are joined to form a ring containing 4 to 6 carbon atoms which is optionally interrupted by a further nitrogen atom which can be substituted by alkyl or alkanoyl, the --O--NO.sub.2 groups being substituents of Y as well as of Z; as well as the salts thereof with physiologically acceptable acids.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.

    摘要翻译： 本发明提供以下通式的苯乙腈衍生物：其中R 1，R 2，R 3，R 4和R 5可以相同或不同，为氢或卤素原子或烷基，烷氧基，硝基，氨基或 酰基氨基和两个相邻的取代基可以一起形成亚甲二氧基或亚乙二氧基，A是下列通式的基团：其中R 6是含有2至12个直链的直链，环状或支链的饱和或不饱和烷基 碳原子，R7是氢原子或含有至多6个碳原子的直链或支链饱和烷基，m和n可相同或不同，为2或3，p为1或2，X为 是含有2至10个碳原子的直链，环状或支链烷基，其任选被氨基取代，或者是通式如下的基团：其中Y和Z可以相同或不同， 是直链或支链烷基基团 引入多达8个碳原子或环烷基，烷基环烷基或环烷基烷基，其中这些基团任选地被氧或硫原子中断，通式II中的基团Z之一也可以是氢原子或两个Z基团连接 形成含有4至6个碳原子的环，其任选被可被烷基或烷酰基取代的另外的氮原子中断，-O-NO 2基团是Y和Z的取代基; 以及其与生理上可接受的酸的盐。 本发明还提供了制备这些化合物的方法和含有它们的药物组合物。

    Heterocyclic oxypropanolamine compounds and pharmaceutical compositions
    9.
    发明授权
    Heterocyclic oxypropanolamine compounds and pharmaceutical compositions 失效

    公开(公告)号：US4346093A

    公开(公告)日：1982-08-24

    申请号：US117190

    申请日：1980-01-31

    申请人： Walter-Gunar Friebe ,  Helmut Michel ,  Carl H. Ross ,  Fritz Wiedemann ,  Wolfgang Bartsch ,  Karl Dietmann

    发明人： Walter-Gunar Friebe ,  Helmut Michel ,  Carl H. Ross ,  Fritz Wiedemann ,  Wolfgang Bartsch ,  Karl Dietmann

    IPC分类号： C07D251/72 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61P9/00 ,  A61P9/08 ,  A61P9/12 ,  A61P25/02 ,  C07D209/04 ,  C07D209/08 ,  C07D209/42 ,  C07D209/43 ,  C07D231/56 ,  C07D233/00 ,  C07D235/02 ,  C07D235/06 ,  C07D235/26 ,  C07D235/28 ,  C07D249/08 ,  C07D249/18 ,  C07D401/12 ,  C07D405/12 ,  A61K31/41

    CPC分类号： C07D209/08 ,  C07D209/42 ,  C07D235/26 ,  C07D249/18 ,  Y10S514/929

    摘要： The present invention provides heterocyclic oxypropanol derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl, aralkyl or lower alkanoyl radical, R.sub.2 and R.sub.3, which can be the same or different, are hydrogen atoms or lower alkyl, hydroxyalkyl, alkoxycarbonyl or alkanoyloxyalkyl radicals or together represent an alkylene radical, R.sub.4 is a hydrogen atom or a lower alkanoyl radical or an aroyl radical, R.sub.5 is a hydrogen atom or a lower alkyl radical or an aralkyl radical, R.sub.6 is a hydrogen atom or a lower alkyl radical, R.sub.7 is a hydrogen atom, a hydroxyl group or a lower alkyl radical, Z is a valency bond, a methylene radical or an oxygen or sulphur atom, Ar is a carbocyclic aryl radical or a pyridyl radical, R.sub.8, R.sub.9 and R.sub.10, which can be the same or different, are hydrogen or halogen atoms, hydroxyl groups, lower alkanoyl radicals, lower alkyl radicals, lower alkenyl radicals, lower alkoxy radicals, aralkoxy radicals, allyloxy radicals, lower alkylthio radicals, aminocarbonyl radicals, aminosulphonyl radicals or lower alkanoylamino radicals or R.sub.8 and R.sub.9 together represent a lower alkylenedioxy radical or R.sub.7 and R.sub.8 together represent a --CH.sub.2 --O-- radical and A is --X.sub.1 --Y.sub.1, in which X.sub.1 is a methylene or --NR.sub.11 -- radical, R.sub.11 being a hydrogen atom or a lower alkyl radical, and Y.sub.1 is a methylene radical or .dbd.C.dbd.Q, Q being an oxygen or sulphur atom; or A is --X.sub.2 .dbd.Y.sub.2 --, in which X.sub.2 and Y.sub.2, which can be the same or different and signify nitrogen atoms or .dbd.C(R.sub.12)-- groups, R.sub.12 being a hydrogen atom or a lower alkyl or an alkoxycarbonyl radical, and when --X.sub.2 .dbd.Y.sub.2 -- represents a --CH.dbd.N-- group and R.sub.1 is an alkyl or aralkyl radical, because of the ability of indazole to tautomerise, this can also be localized on the nitrogen atom represented by Y.sub.2, with the proviso that Y.sub.1 or Y.sub.2 is joined to .dbd.N--R.sub.1 in general formula (I), and, when Q is an oxygen atom or --X.sub.2 .dbd.Y.sub.2 -- represents --CR.sub.12 .dbd.CR.sub.12 -- and Z is a valency bond or when --X.sub.1 --Y.sub.1 -- represents ##STR2## and Z is an oxygen atom or a valency bond, either the two symbols R.sub.2 and R.sub.3 do not simultaneously represent hydrogen atoms or R.sub.7 and R.sub.8 together must form a --CH.sub.2 --O-- radical; and the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.Furthermore, the present invention is concerned with the use of these compounds for the treatment of cardiac and circulatory diseases.

    Indolin-2-one derivatives preparation thereof and intermediates for the preparation thereof
    10.
    发明授权
    Indolin-2-one derivatives preparation thereof and intermediates for the preparation thereof 失效

    公开(公告)号：US4642309A

    公开(公告)日：1987-02-10

    申请号：US780704

    申请日：1985-09-26

    申请人： Helmut Michel ,  Klaus Marzenell ,  Wolfgang Kampe ,  Wolfgang Bartsch ,  Wolfgang Schaumann

    发明人： Helmut Michel ,  Klaus Marzenell ,  Wolfgang Kampe ,  Wolfgang Bartsch ,  Wolfgang Schaumann

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P9/00 ,  A61P9/08 ,  A61P25/02 ,  C07D209/34 ,  C07D401/06 ,  C07D403/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06

    CPC分类号： C07D401/06 ,  C07D209/34 ,  C07D403/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06

    摘要： The present invention provides indolin-2-one derivatives of the general formula: ##STR1## wherein R.sub.1 is a C.sub.1 -C.sub.6 alkyl radical or a radical of the general formula: ##STR2## in which A is a straight-chained or branched C.sub.2 -C.sub.4 alkylene radical and Z is an oxygen or sulphur atom, R.sub.2 and R.sub.3, which can be the same or different, are hydrogen or halogen atoms, hydroxyl groups, C.sub.2 -C.sub.6 alkanoyl radicals, C.sub.2 -C.sub.4 alkenyl radicals, C.sub.2 -C.sub.4 alkynyl radicals, C.sub.1 -C.sub.6 alkyl radicals, C.sub.1 -C.sub.6 alkoxy radicals, C.sub.2 -C.sub.4 alkenyloxy radicals, C.sub.2 -C.sub.4 alkynyloxy radicals, C.sub.1 -C.sub.6 alkylthio radicals, C.sub.2 -C.sub.6 alkanoylamido radicals or radicals of the general formula: ##STR3## in which R.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms, C.sub.1 -C.sub.6 alkyl radicals or C.sub.3 -C.sub.10 cycloalkyl radicals or R.sub.4 and R.sub.5 together represent a C.sub.2 -C.sub.8 alkylene radical optionally interrupted by an oxygen or sulphur atom or by an >N-R.sub.6 group, in which R.sub.6 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl radical, X is a hydrogen atom, Y is a hydrogen atom or a group of the general formula ##STR4## in which Q is a hydrogen atom or, together with X, can also represent a bond and R.sub.7 is a heterocyclic radical which is optionally substituted one or more times by hydroxyl or C.sub.1 -C.sub.6 alkyl or is a phenyl radical which is optionally substituted one or more times by halogen, hydroxyl, mercapto, carboxyl, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulphinyl, C.sub.1 14 C.sub.6 alkylsulphonyl, C.sub.2 -C.sub.6 alkanoylamido, C.sub.1 -C.sub.6 alkylsulphonylamido, methylenedioxy, nitro, cyano or amino, with the proviso that R.sub.1 cannot be a C.sub.1 -C.sub.6 alkyl radical when X and Y are both hydrogen atoms; as well as the pharmacologically acceptable salts thereof.The present invention also provides intermediates of the general formula: ##STR5## in which R.sub.7 is a heterocyclic radical which is optionally substituted one or more times by hydroxy or C.sub.1 -C.sub.6 alkyl or is a phenyl radical which is optionally substituted one or more times by hydroxyl, halogen, mercapto, carboxyl, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 14 C.sub.6 alkylsulphinyl, cyano C.sub.1 -C.sub.6 alkylsulphonyl, C.sub.2 -C.sub.6 alkanoylamido, C.sub.1 -C.sub.6 alkylsulphonylamido, nitro amino or methylenedioxy.Furthermore, the invention provides processes for the preparation of the above indolin-2-one derivatives and the above intermediates, as well as pharmaceutical compositions containing the above indolin-2-one derivatives.