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    Carbazolyl-(4)-oxypropanolamine compounds and therapeutic compositions
    4.
    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
    8.
    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。

    Quinoxalinyloxy-amino-propanol compounds with blood pressure lowering and .beta.-blocking properties, their use and pharmaceutical compositions containing them
    9.
    发明授权
    Quinoxalinyloxy-amino-propanol compounds with blood pressure lowering and .beta.-blocking properties, their use and pharmaceutical compositions containing them 失效
    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

    公开(公告)号：US4438116A

    公开(公告)日：1984-03-20

    申请号：US302894

    申请日：1981-09-16

    申请人： Carl H. Ross ,  Wolfgang Kampe ,  Wolfgang Bartsch ,  Gisbert Sponer ,  Egon Roesch

    发明人： Carl H. Ross ,  Wolfgang Kampe ,  Wolfgang Bartsch ,  Gisbert Sponer ,  Egon Roesch

    IPC分类号： A61K31/505 ,  A61P9/00 ,  C07D241/38 ,  C07D241/44 ,  C07D401/12 ,  C07D401/14 ,  A61K31/495 ,  C07D241/42

    CPC分类号： C07D241/38 ,  C07D241/44 ,  Y10S514/929

    摘要： 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.

    摘要翻译： 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。