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19 条记录 (耗时 0.023 秒)

    Adenosine-5'-carboxylic acid amides
    8.
    发明授权
    Adenosine-5'-carboxylic acid amides 失效
    腺苷-5'-羧酸酰胺

    公开(公告)号：US4224438A

    公开(公告)日：1980-09-23

    申请号：US161338

    申请日：1971-07-09

    申请人： Erich Fauland ,  Wolfgang Kampe ,  Max Thiel ,  Karl Dietmann ,  Wolfgang Juhran

    发明人： Erich Fauland ,  Wolfgang Kampe ,  Max Thiel ,  Karl Dietmann ,  Wolfgang Juhran

    IPC分类号： C07H19/16 ,  A61K31/70 ,  C07H19/18

    CPC分类号： C07H19/16

    摘要： Adenosine-5'-carboxylic acid derivatives of the general formula: ##STR1## wherein Z is two hydrogen atoms or a divalent lower alkylidene radical, ##STR2## R is an aliphatic or arylaliphatic radical, and R.sub.1 and R.sub.2 are independently a hydrogen, hydroxyl, amino, lower alkyl, lower alkenyl, optionally N-alkylated lower aminoalkyl, cycloalkyl, hydroxyalkyl or piperidinyl radical, orR.sub.1 and R.sub.2 taken together are a divalent ethylene radical containing 4-7 carbon atoms optionally interrupted by an oxygen or sulfur atom or by an imino, alkylimino or arylimino radical or a pharmacologically compatible salt thereof.The esters surprisingly can be prepared by esterifying the acid in the presence of sulfuric acid without hydrolyzing the sugar group. While the esters have some activity, they can be used to make the amides which are characterized by marked coronary activity.

    摘要翻译： 具有以下通式的腺苷-5'-羧酸衍生物：其中Z为两个氢原子或二价低级亚烷基，其中R 1和R 2独立为 氢，羟基，氨基，低级烷基，低级烯基，任选N-烷基化的低级氨基烷基，环烷基，羟基烷基或哌啶基，或者R 1和R 2一起是含有4-7个碳原子的任选被氧或硫中断的二价亚乙基 或亚氨基，亚氨基亚氨基或芳基亚氨基或其药理学上相容的盐。 这些酯令人惊奇地可以通过在硫酸存在下酯化酸而不水解糖基来制备。 虽然酯具有一些活性，但它们可用于制备以标记的冠状动脉为特征的酰胺。

    Carbazolyl-(4)-oxypropanolamine compounds and therapeutic compositions
    9.
    发明授权
    Carbazolyl-(4)-oxypropanolamine compounds and therapeutic compositions 失效
    （4） - 氧丙醇胺化合物和治疗组合物

    公开(公告)号：US4503067A

    公开(公告)日：1985-03-05

    申请号：US479921

    申请日：1983-04-04

    申请人： Fritz Wiedemann ,  Wolfgang Kampe ,  Max Thiel ,  Gisbert Sponer ,  Egon Roesch ,  Karl Dietmann

    发明人： Fritz Wiedemann ,  Wolfgang Kampe ,  Max Thiel ,  Gisbert Sponer ,  Egon Roesch ,  Karl Dietmann

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61P9/08 ,  A61P25/02 ,  C07D209/88 ,  C07D317/64 ,  C07D401/12 ,  C07D405/12 ,  C07D209/82

    CPC分类号： C07D209/88 ,  C07D317/64

    摘要： Carbazolyl-(4)-oxypropanolamine compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkanoyl or aroyl;R.sub.2 is hydrogen, lower alkyl or arylalkyl;R.sub.3 is hydrogen or lower alkyl;R.sub.4 is hydrogen or lower alkyl, or when X is oxygen, R.sub.4 together with R.sub.5 can represent --CH.sub.2 --O--;X is a valency bond, --CH.sub.2 --, oxygen or sulfur;Ar is mono- or bicyclic aryl or pyridyl;R.sub.5 and R.sub.6 are individually selected from hydrogen, halogen, hydroxyl, lower alkyl, aminocarbonyl, lower alkoxy, aralkyloxy, lower alkylthio, lower alkylsulphinyl or lower alkylsulphonyl;R.sub.5 and R.sub.6 together can represent methylenedioxy;and the salts thereof with physiologically acceptable acids are outstandingly effective in the treatment and prophylaxis of circulatory and cardiac diseases, e.g., hypertension and angina pectoris.

    摘要翻译： 式（I）的羧基 - （4） - 氧丙醇胺化合物，其中R 1是氢，低级烷酰基或芳酰基; R2是氢，低级烷基或芳基烷基; R3是氢或低级烷基; R4是氢或低级烷基，或者当X是氧时，R4与R5一起可以代表-CH2-O-; X是价键，-CH 2 - ，氧或硫; Ar是单环或双环芳基或吡啶基; R5和R6分别选自氢，卤素，羟基，低级烷基，氨基羰基，低级烷氧基，芳烷氧基，低级烷硫基，低级烷基亚磺酰基或低级烷基磺酰基; R5和R6一起可以代表亚甲二氧基; 并且其与生理上可接受的酸的盐在治疗和预防循环和心脏疾病例如高血压和心绞痛方面是显着的。

    3-Cyano-indoles as cardioselective agents
    10.
    发明授权
    3-Cyano-indoles as cardioselective agents 失效
    3-氰基 - 吲哚作为心脏选择剂

    公开(公告)号：US4468520A

    公开(公告)日：1984-08-28

    申请号：US288075

    申请日：1981-07-29

    申请人： Helmut Michel ,  Wolfgang Kampe ,  Roland Ofenloch ,  Karl Dietmann ,  Gisbert Sponer

    发明人： Helmut Michel ,  Wolfgang Kampe ,  Roland Ofenloch ,  Karl Dietmann ,  Gisbert Sponer

    IPC分类号： C07D209/12 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P9/00 ,  C07D209/08 ,  C07D209/42 ,  C07D209/43 ,  C07D209/04

    CPC分类号： C07D209/08

    摘要： The present invention provides aminopropanol derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkanoyl or an aroyl radical, R.sub.2 is a lower alkyl radical or a radical of the general formula: ##STR2## wherein X is a valency bond, a methylene group or an oxygen or sulphur atom, Ar is a monocyclic, carbo- or heterocyclic aryl radical, R.sub.6 and R.sub.7, which can be the same or different, are hydrogen atoms or lower alkyl radicals, R.sub.8 and R.sub.9, which can be the same or different, are hydrogen or halogen atoms, hydroxyl groups, lower alkanoyl radicals, alkenyl radicals, alkynyl radicals, alkyl radicals, lower alkoxy radicals, aralkoxy radicals, alkenyloxy radicals, alkynyloxy radicals, lower alkylthio radicals, aminocarbonyl radicals, aminosulphonyl radicals or acylamino radicals; or R.sub.2 is a 1,4-benzodioxan-2-ylmethyl radical, R'.sub.2 is a hydrogen atom or a benzyl radical, R.sub.3 is a carboxyl group or a lower alkoxycarbonyl, aminocarbonyl, cyano, oximinomethyl, formyl, hydroxymethyl or lower alkoxycarbimidoyl radical, R.sub.4 is a hydrogen atom or a lower alkyl radical or a --CH.sub.2 --O--R.sub.1 radical, R.sub.1 having the same meaning as above, and R.sub.5 is a hydrogen atom or a lower alkyl radical; the optionally-active forms and racemates thereof 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 prophylaxis and treatment of heart and circulatory diseases.

    摘要翻译： 本发明提供以下通式的氨基丙醇衍生物：其中R1是氢原子或低级烷酰基或芳酰基，R2是低级烷基或通式如下的基团：其中 X是价键，亚甲基或氧或硫原子，Ar是单环，碳或杂环芳基，R6和R7可以相同或不同，是氢原子或低级烷基，R8和 R9可相同或不同，为氢或卤原子，羟基，低级烷酰基，烯基，炔基，烷基，低级烷氧基，芳烷氧基，烯氧基，炔氧基，低级烷硫基，氨基羰基 自由基，氨基磺酰基或酰氨基; 或R 2为1,4-苯并二恶烷-2-基甲基，R'2为氢原子或苄基，R 3为羧基或低级烷氧基羰基，氨基羰基，氰基，肟基甲基，甲酰基，羟甲基或低级烷氧基甲脒基 R4是氢原子或低级烷基或-CH2-O-R1基，R1具有与上述相同的含义，R 5是氢原子或低级烷基; 其任选活性形式和外消旋物及其药理学上可接受的盐。 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，本发明涉及这些化合物用于预防和治疗心脏和循环系统疾病的用途。