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    • 11. 发明授权
      US4346093A Heterocyclic oxypropanolamine compounds and pharmaceutical compositions 失效
    • Heterocyclic oxypropanolamine compounds and pharmaceutical compositions
    • US4346093A
    • 1982-08-24
    • US117190
    • 1980-01-31
    • Walter-Gunar Friebe , Helmut Michel , Carl H. Ross , Fritz Wiedemann , Wolfgang Bartsch , Karl Dietmann
    • Walter-Gunar Friebe , Helmut Michel , Carl H. Ross , Fritz Wiedemann , Wolfgang Bartsch , Karl Dietmann
    • 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
    • C07D209/08 , C07D209/42 , C07D235/26 , C07D249/18 , Y10S514/929
    • 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 12. 发明授权
      US4438116A Quinoxalinyloxy-amino-propanol compounds with blood pressure lowering and .beta.-blocking properties, their use and pharmaceutical compositions containing them 失效
    • Quinoxalinyloxy-amino-propanol compounds with blood pressure lowering and .beta.-blocking properties, their use and pharmaceutical compositions containing them
    • 具有降血压和β-阻断性能的喹喔啉氧基 - 氨基 - 丙醇化合物，它们的用途和含有它们的药物组合物
    • US4438116A
    • 1984-03-20
    • US302894
    • 1981-09-16
    • Carl H. Ross , Wolfgang Kampe , Wolfgang Bartsch , Gisbert Sponer , Egon Roesch
    • Carl H. Ross , Wolfgang Kampe , Wolfgang Bartsch , Gisbert Sponer , Egon Roesch
    • A61K31/505 , A61P9/00 , C07D241/38 , C07D241/44 , C07D401/12 , C07D401/14 , A61K31/495 , C07D241/42
    • C07D241/38 , C07D241/44 , Y10S514/929
    • An aminopropanol compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from hydrogen and lower alkyl; orR.sub.1 and R.sub.2 together represent an alkylene radical;R.sub.3 is hydrogen or acyl;A is one of the following structures ##STR2## wherein R.sub.4 is hydrogen or lower alkyl optionally substituted by hydroxyl halogen and lower alkylthio; andR.sub.5 and R.sub.6 are individually selected from lower alkyl;B is alkylamino which optionally carries a phenyl and a phenoxy radical optionally substituted by at at least one of halogen, hydroxyl or lower alkyl, lower acyl, lower alkylthio, acylamino, aminocarbonyl, lower alkoxy, lower alkenyloxy, phenoxy, lower alkenyl, lower alkylsulphonyl, lower alkylsulphinyl or haloalkyl; orB is an aryl- or heteroaryloxymethylpiperidine radical optionally substituted by at least one of halogen hydroxyl or lower alkyl, hydroxyl alkyl or carboxamido alkyl, or by lower alkoxy, lower acyl, amino, carboxamido, lower alkylcarbonylamido or lower alkylsulphonylamino;and the pharmacologically acceptable salts thereof, are outstandingly effective beta blockers and blood-pressure depressants.
    • 式IMAMA的氨基丙醇化合物，其中R 1和R 2分别选自氢和低级烷基; 或者R 1和R 2一起表示亚烷基; R3是氢或酰基; A是下列结构之一，其中R4是氢或任选被羟基卤素和低级烷硫基取代的低级烷基; 并且R 5和R 6分别选自低级烷基; B是烷基氨基，其任选地带有苯基和苯氧基，其任选被至少一个卤素，羟基或低级烷基，低级酰基，低级烷硫基，酰氨基，氨基羰基，低级烷氧基，低级烯氧基，苯氧基，低级烯基，低级烷基磺酰基 ，低级烷基亚磺酰基或卤代烷基; 或B是任选被卤素羟基或低级烷基，羟基烷基或甲酰胺基烷基中的至少一个取代的芳基或杂芳氧基甲基哌啶基，或由低级烷氧基，低级酰基，氨基，甲酰氨基，低级烷基羰基酰氨基或低级烷基磺酰基氨基取代; 和其药理学上可接受的盐是显着有效的β受体阻滞剂和降压药。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 14. 发明授权
      US4642309A Indolin-2-one derivatives preparation thereof and intermediates for the preparation thereof 失效
    • Indolin-2-one derivatives preparation thereof and intermediates for the preparation thereof
    • US4642309A
    • 1987-02-10
    • US780704
    • 1985-09-26
    • Helmut Michel , Klaus Marzenell , Wolfgang Kampe , Wolfgang Bartsch , Wolfgang Schaumann
    • Helmut Michel , Klaus Marzenell , Wolfgang Kampe , Wolfgang Bartsch , Wolfgang Schaumann
    • A61K31/40 , A61K31/403 , A61K31/404 , A61P9/00 , A61P9/08 , A61P25/02 , C07D209/34 , C07D401/06 , C07D403/06 , C07D405/12 , C07D405/14 , C07D409/06
    • C07D401/06 , C07D209/34 , C07D403/06 , C07D405/12 , C07D405/14 , C07D409/06
    • 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 15. 发明授权
      US4612313A Pharmaceutical phenylacetonitrile derivatives 失效
    • Pharmaceutical phenylacetonitrile derivatives
    • 药用苯乙腈衍生物
    • US4612313A
    • 1986-09-16
    • US774354
    • 1985-09-10
    • Herbert Leinert , Wolfgang Kampe , Klaus Strein , Bernd Muller-Beckmann , Wolfgang Bartsch
    • Herbert Leinert , Wolfgang Kampe , Klaus Strein , Bernd Muller-Beckmann , Wolfgang Bartsch
    • 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
    • C07C255/00 , C07D211/22
    • 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.
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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