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    • 1. 发明授权
    • Heterocyclic oxypropanolamine compounds and pharmaceutical compositions
    • US4346093A
    • 1982-08-24
    • US117190
    • 1980-01-31
    • Walter-Gunar FriebeHelmut MichelCarl H. RossFritz WiedemannWolfgang BartschKarl Dietmann
    • Walter-Gunar FriebeHelmut MichelCarl H. RossFritz WiedemannWolfgang BartschKarl Dietmann
    • C07D251/72A61K31/40A61K31/403A61K31/404A61K31/415A61K31/4184A61K31/44A61K31/4427A61K31/443A61P9/00A61P9/08A61P9/12A61P25/02C07D209/04C07D209/08C07D209/42C07D209/43C07D231/56C07D233/00C07D235/02C07D235/06C07D235/26C07D235/28C07D249/08C07D249/18C07D401/12C07D405/12A61K31/41
    • C07D209/08C07D209/42C07D235/26C07D249/18Y10S514/929
    • 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.
    • 6. 发明授权
    • Nitroxy amino propanols for treating heart and circulatory diseases
    • 用于治疗心脏和循环系统疾病的硝基氨基丙醇
    • US4801596A
    • 1989-01-31
    • US803497
    • 1985-12-02
    • Herbert SimonHelmut MichelWalter-Gunar FriebeWolfgang Bartsch
    • Herbert SimonHelmut MichelWalter-Gunar FriebeWolfgang Bartsch
    • A61K31/135A61K31/165A61K31/21A61K31/275A61K31/443A61K31/445A61P9/08A61P9/10A61P9/12A61P25/02C07C67/00C07C231/00C07C231/02C07C231/12C07C233/12C07C233/16C07C235/08C07C235/34C07C239/00C07C253/00C07C255/54C07C255/59C07C269/00C07C275/50C07C301/00C07C311/30C07C311/37C07C313/00C07C317/18C07C317/46C07D211/22C07D211/46C07D295/04C07D303/22C07D405/12
    • C07D303/22C07C255/00C07D211/22C07D211/46C07D405/12
    • 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.
    • 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。