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    • 1. 发明授权
    • Heterocyclic substituted indolinones
    • 杂环取代的二氢吲哚酮
    • US4870077A
    • 1989-09-26
    • US94871
    • 1987-09-10
    • Wolfgang Von Der SaalWalter-Gunar FriebeAlfred MertensBernd Muller-BeckmannLothar Kling
    • Wolfgang Von Der SaalWalter-Gunar FriebeAlfred MertensBernd Muller-BeckmannLothar Kling
    • A61K31/50A61K31/535A61K31/54A61P9/00C07D209/34C07D209/46C07D403/04C07D413/04C07D417/04
    • C07D403/04C07D209/34C07D413/04C07D417/04
    • Heterocyclic substituted indolinones of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl or hydroxyalkyl radical, R.sub.2 is a carboxyl group or an alkoxy-carbonyl, hydroxyalkyl or alkylcarbonyloxyalkyl radical or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a lactone having 4, 5 or 6 ring atoms, A-B is --CH.sub.2 --CH(R.sub.3)--, --CH.dbd.CR.sub.3 --, --CH.sub.2 --NH--, --NH--CH.sub.2 --, --CH.sub.2 --O--, --O--CH.sub.2 --, --CH.sub.2 --S-- or --S--CH.sub.2 -- radical, R.sub.3 being a hydrogen atom or an alkyl or hydroxyalkyl radical, or A is a valency bond and B is a methylene radical ##STR2## or an imino group ##STR3## R.sub.4, R.sub.5, and R.sub.6 independently being hydrogen atoms or alkyl radicals wherein the alkyl groups independently contain 1 to 6 carbon atoms; as well as the tautomers thereof and the physiologically acceptable salt thereof and the physiologically acceptable salts thereof with inorganic and organic acids, are disclosed, such as, for instance, the compound 5-(2,3,4,5-tetrahydro-3-oxopyridazin-6-yl)-3-ethoxycarbonyl-3-methyl-1H-indol n-2-one. The compounds of the invention are useful in the treatment of heart and circulatory diseases, for example, by producing a positive inotropic action in a patient to whom the compounds are administered.
    • 式(I)的杂环取代的二氢吲哚酮:其中R 1是氢原子或烷基或羟烷基,R 2是羧基或烷氧羰基,羟基烷基或烷基羰基氧基烷基或R 1和R 2与碳 它们连接的原子形成具有4,5或6个环原子的内酯,AB是-CH 2 -CH(R 3) - , - CH = CR 3 - , - CH 2 -NH-,-NH-CH 2 - , - CH 2 -O-,-O-CH 2 - , - CH 2 -S-或-S-CH 2 - 基,R 3是氢原子或烷基或羟烷基,或A是价键,B是亚甲基。 或亚氨基基团R4,R5和R6独立地为氢原子或烷基,其中烷基独立地含有1至6个碳原子; 以及其与无机和有机酸的互变异构体及其生理上可接受的盐及其生理上可接受的盐,例如化合物5-(2,3,4,5-四氢-3- 氧基哒嗪-6-基)-3-乙氧基羰基-3-甲基-1H-吲哚-2-酮。 本发明的化合物可用于治疗心脏和循环系统疾病,例如通过在施用化合物的患者中产生正性肌力作用。
    • 2. 发明授权
    • Heterocyclic-substituted indoles and pharmaceutical compositions
containing them
    • 杂环取代的吲哚和含有它们的药物组合物
    • US4851406A
    • 1989-07-25
    • US904092
    • 1986-09-04
    • Alfred MertensWolfgang von der SaalWalter-Gunar FriebeBernd Muller-BeckmannGisbert Sponer
    • Alfred MertensWolfgang von der SaalWalter-Gunar FriebeBernd Muller-BeckmannGisbert Sponer
    • C07D409/14A61K31/44A61K31/4427A61K31/4433A61K31/445A61K31/50A61K31/53A61K31/535A61P9/00C07D237/00C07D333/00C07D401/14C07D403/04C07D403/14C07D413/14C07D417/14
    • C07D401/14
    • The present invention provides indole derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl, cycloalkyl, cycloalkenyl, carboxyl, cyano, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl or aryl radical, R.sub.2 is a hydrogen atom or an alkyl, trihalogenomethyl, hydroxyl, cycloalkyl, cyano, carboxyl, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl radical; R.sub.2 is a heterocyclic five-membered ring containing 1 to 4 heteroatoms or a heterocyclic six-membered ring containing 1 to 5 heteroatoms, the heteroatoms of the five- and six-membered rings being the same or different and being nitrogen, oxygen or sulphur and one or more of the nitrogen atoms optionally carrying an oxygen atom, the said five- and six-membered rings optionally being substituted by one or more alkyl, alkoxy, alkylthio, oxo, hydroxyl, nitro, amino, halogen or cyano groups; or R.sub.2 is ##STR2## the tautomers thereof and the physiologically acceptable salts thereof with inorganic and organic acids.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.Furthermore, the present invention provides intermediates of the general formula: ##STR3## in which R.sub.1, R.sub.2, A and X have the same meanings as above, and processes for the preparation of these intermediates.
    • 本发明提供以下通式的吲哚衍生物:其中R 1是氢原子或烷基,烯基,环烷基,环烯基,羧基,氰基,烷基羰基,烷氧基羰基,氨基羰基,烷基氨基羰基,二烷基氨基羰基或芳基, R2是氢原子或烷基,三卤代甲基,羟基,环烷基,氰基,羧基,烷氧基羰基,烷基羰基,氨基羰基,烷基氨基羰基或二烷基氨基羰基; R2是含有1至4个杂原子的杂环五元环或含有1至5个杂原子的杂环六元环,五元和六元环的杂原子相同或不同,为氮,氧或硫, 一个或多个氮原子任选地带有氧原子,所述五元和六元环任选被一个或多个烷基,烷氧基,烷硫基,氧代,羟基,硝基,氨基,卤素或氰基取代; 或者R2是其互变异构体及其与无机和有机酸的生理上可接受的盐。 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。 此外,本发明提供通式如下的中间体:其中R1,R2,A和X具有与上述相同的含义,以及制备这些中间体的方法。
    • 10. 发明授权
    • Pyrrolobenzimidazoles, pharmaceutical compositions containing them, and
use of them to treat certain heart and circulatory diseases
    • 吡咯并苯并咪唑,含有它们的药物组合物,以及它们用于治疗某些心脏和循环系统疾病
    • US4710510A
    • 1987-12-01
    • US807260
    • 1985-12-10
    • Alfred MertensJens-Peter HolckWolfgang KampeBernd Muller-BeckmannKlaus StreinWolfgang Schaumann
    • Alfred MertensJens-Peter HolckWolfgang KampeBernd Muller-BeckmannKlaus StreinWolfgang Schaumann
    • A61K31/415A61K31/4184A61P9/00A61P9/04C07D209/34C07D209/42C07D487/04A61K31/55
    • C07D487/04C07D209/34C07D209/42
    • The present invention provides new pyrrolobenzimidazoles of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical; R.sub.2 is a hydrogen atom, cyano group or alkyl or alkenyl radical or a carbonyl group substituted by hydroxyl, alkyl, alkoxy, amino, alkylamino, dialkylamino or hydrazino or together with R.sub.1 forms a cycloalkylene radical or R.sub.1 and R.sub.2 together form an alkylidene or cycloalkylidene radical; R.sub.3, R.sub.4 and R.sub.5, which can be the same or different, each represent a hydrogen atom or an alkanesulphonyloxy, trifluoromethanesulphonyloxy, alkanesulphonylamino, trifluoromethanesulphonylamino, N-alkyl-alkanesulphonylamino, N-alkyl-trifluoromethanesulphonylamino, alkylsulphenylmethyl, alkylsulphinylmethyl or alkylsulphonylmethyl radical, a carbonyl group substituted by hydroxyl, alkoxy, amino, alkylamino or dialkylamino, a sulphonyl group substituted by amino, alkylamino, dialkylamino or cyclic imino, whereby a methylene group in the 4-position can be replaced by a sulphur or oxygen atom, an alkylcarbonylamino, aminocarbonylamino or alkylaminocarbonylamino radical, an alkylthio, alkylsulphinyl or alkylsulphonyl radical, a nitro, halogen, amino, hydroxyl, alkyl, trifluoromethyl, alkoxy, alkenyloxy, alkynyloxy, cyanoalkoxy, carboxyalkoxy, alkoxycarbonylalkoxy, dialkylamino, 1-imidazolyl or cyano group; X is a valency bond, a C.sub.1 -C.sub.4 alkylene radical or a vinyl radical; and T is an oxygen or sulphur atom; the tautomers thereof and the physiologically acceptable salts thereof with inorganic and organic acids.The present invention also provides processes for the preparation of these compounds and pharmaceuticals containing them for the prophylaxis and treatment of heart and circulatory diseases.
    • 本发明提供了以下通式的新的吡咯并苯并咪唑:其中R 1是氢原子或烷基,烯基或环烷基; R2是氢原子,氰基或烷基或烯基或被羟基,烷基,烷氧基,氨基,烷基氨基,二烷基氨基或肼基取代的羰基或与R1一起形成亚环烷基,或者R 1和R 2一起形成亚烷基或亚环烷基 激进; 可以相同或不同的R 3,R 4和R 5各自表示氢原子或烷磺酰氧基,三氟甲磺酰氧基,烷磺酰氨基,三氟甲磺酰氨基,N-烷基 - 烷磺酰氨基,N-烷基 - 三氟甲磺酰氨基,烷基亚磺酰基甲基,烷基亚磺酰基甲基或烷基磺酰基甲基,羰基 被羟基,烷氧基,氨基,烷基氨基或二烷基氨基取代的基团,被氨基,烷基氨基,二烷基氨基或环状亚氨基取代的磺酰基,其中4-位中的亚甲基可以被硫或氧原子,烷基羰基氨基,氨基羰基氨基 或烷基氨基羰基氨基,烷硫基,烷基亚磺酰基或烷基磺酰基,硝基,卤素,氨基,羟基,烷基,三氟甲基,烷氧基,烯氧基,炔氧基,氰基烷氧基,羧基烷氧基,烷氧基羰基烷氧基,二烷基氨基,1-咪唑基或氰基; X是价键,C1-C4亚烷基或乙烯基; 和T是氧或硫原子; 其互变异构体及其与无机和有机酸的生理上可接受的盐。 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用于预防和治疗心脏和循环系统疾病。