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1. 发明授权

US4367235A 2-Benzimidazolinone compounds and therapeutic compositions 失效
标题翻译： 2-苯并咪唑啉酮化合物和治疗组合物
公开(公告)号：US4367235A
公开(公告)日：1983-01-04
申请号：US171940
申请日：1980-07-18
申请人： Carl H. Ross , Walter-Gunar Friebe , Wolfgang Kampe , Wolfgang Bartsch , Egon Roesch
发明人： Carl H. Ross , Walter-Gunar Friebe , Wolfgang Kampe , Wolfgang Bartsch , Egon Roesch
IPC分类号： A61K31/415 , A61K31/4184 , A61P9/00 , A61P25/02 , C07D235/02 , C07D235/26
CPC分类号： A61K31/415 , C07D235/02 , C07D235/26
摘要： 2-benzimidazolinone compounds of the formula ##STR1## wherein R is lower alkyl,R.sub.1 and R.sub.2, which can be the same or different, are lower straight-chained or branched alkyl and one of R.sub.1 and R.sub.2 can also be hydrogen orR.sub.1 and R.sub.2 together represent an alkylene radical and R.sub.3 is hydrogen or acyl, i.e., alkanoyl or aromatic carboxylic acid moieties;and the pharmacologically acceptable salts thereof; have marked .beta.-receptor blocking action and are outstandingly useful in the treatment or prophylaxis of cardiac and circulatory diseases.
摘要翻译：其中R是低级烷基，可以相同或不同的R 1和R 2的低级直链或支链烷基，R 1和R 2之一也可以是氢或R 1和R 2 一起代表亚烷基，R3是氢或酰基，即烷酰基或芳族羧酸部分; 及其药理学上可接受的盐; 具有明显的β-受体阻断作用，并且在治疗或预防心脏和循环系统疾病方面非常有用。

2. 发明授权

US4215134A 4-Hydroxy-2-benzimidazoline-thione compounds and pharmaceutical compositions containing them 失效
标题翻译： 4-羟基-2-苯并咪唑啉 - 硫酮化合物和含有它们的药物组合物
公开(公告)号：US4215134A
公开(公告)日：1980-07-29
申请号：US2129
申请日：1979-01-09
申请人： Carl H. Ross , Walter-Gunar Friebe , Wolfgang Kampe , Wolfgang Bartsch , Egon Roesch
发明人： Carl H. Ross , Walter-Gunar Friebe , Wolfgang Kampe , Wolfgang Bartsch , Egon Roesch
IPC分类号： A61K31/415 , A61K31/4184 , A61P9/00 , C07D235/02 , C07D235/28 , C07D303/22
CPC分类号： C07D235/02 , C07D235/28 , C07D303/22
摘要： Novel 4-hydroxy-2-benzimidazoline-thione compound of the formula: ##STR1## wherein R is lower alkyl;R.sub.1 and R.sub.2, which can be the same or different, are hydrogen or lower straight-chained or branched alkyl orR.sub.1 and R.sub.2 together represent alkylene; andR.sub.3 is a hydrogen atom or an acyl radical;and the pharmacologically acceptable salts thereof; have marked .beta.-receptor blocking action and are outstandingly useful in the treatment or prophylaxis of cardiac and circulatory diseases.
摘要翻译：下式的新型4-羟基-2-苯并咪唑啉 - 硫酮化合物：其中R是低级烷基; R 1和R 2可以相同或不同，为氢或低级直链或支链烷基或R 1和R 2一起表示亚烷基; 并且R 3是氢原子或酰基; 及其药理学上可接受的盐; 具有明显的β-受体阻断作用，并且在治疗或预防心脏和循环系统疾病方面非常有用。

3. 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
标题翻译：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。

4. 发明授权

US4428955A Benzopyran compounds, pharmaceutical compositions containing them and methods of use 失效
标题翻译：苯并吡喃化合物，含有它们的药物组合物和使用方法
公开(公告)号：US4428955A
公开(公告)日：1984-01-31
申请号：US372415
申请日：1982-04-27
申请人： Walter-Gunar Friebe , Wolfgang Kampe , Egon Roesch , Otto-Henning Wilhelms
发明人： Walter-Gunar Friebe , Wolfgang Kampe , Egon Roesch , Otto-Henning Wilhelms
IPC分类号： C07D409/14 , A61K31/35 , A61K31/443 , A61K31/4433 , A61K31/445 , A61P37/08 , A61P43/00 , C07D311/22 , C07D405/06 , C07D405/12 , C07D405/14
CPC分类号： C07D405/12 , Y10S514/87
摘要： The present invention provides benzopyranyl ethers of the general formula: ##STR1## wherein A is an alkylene radical containing 2 to 4 carbon atoms and R is a hydrogen atom or an acyl radical; as well as the salts thereof with pharmacologically acceptable acids.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 treating allergic diseases.
摘要翻译：本发明提供以下通式的苯并吡喃基醚：其中A是含有2至4个碳原子的烷基，R是氢原子或酰基; 以及其与药理学上可接受的酸的盐。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。此外，本发明涉及这些化合物用于治疗过敏性疾病的用途。

5. 发明授权

US4229464A Aminopropanol substituted indole compounds and compositions for the treatment of cardiac and circulatory diseases 失效
标题翻译：氨基丙醇取代的吲哚化合物和用于治疗心脏和循环系统疾病的组合物
公开(公告)号：US4229464A
公开(公告)日：1980-10-21
申请号：US943512
申请日：1978-09-18
申请人： Wolfgang Kampe , Kurt Stach, deceased , by Werner Plattner, administrator , Max Thiel , Wolfgang Bartsch , Karl Dietmann , Egon Roesch , Wolfgang Schaumann
发明人： Wolfgang Kampe , Kurt Stach, deceased , by Werner Plattner, administrator , Max Thiel , Wolfgang Bartsch , Karl Dietmann , Egon Roesch , Wolfgang Schaumann
IPC分类号： C07D209/43 , A61K31/40 , A61K31/403 , A61K31/404 , A61P25/02 , C07D209/08 , C07D209/12 , C07D209/32 , C07D209/42 , C07D209/18 , C07D209/20
CPC分类号： C07D209/42 , C07D209/08 , C07D209/12 , Y10S514/927
摘要： New aminopropanol compounds of the formula ##STR1## wherein R is lower alkyl, cycloalkyl or alkylthioalkyl,R.sub.1 is hydrogen or lower alkyl, hydroxyalkyl, pivaloyloxyalkyl, alkoxyalkyl, alkoxycarbonyl, carboxyl or --CONR.sub.3 R.sub.4, in which R.sub.3 and R.sub.4 which can be the same or different, represent hydrogen or lower alkyl, andR.sub.2 is lower alkyl, hydroxyalkyl, alkoxyalkyl or pivaloyloxyalkyl or, when R is alkylthioalkyl or R.sub.1 is pivaloyloxyalkyl, R.sub.2 can also be hydrogen and the pharmacologically acceptable salts thereof; are outstandingly effective in the treatment or prophylaxis of cardiac and circulatory diseases.
摘要翻译：新的式（I）的氨基丙醇化合物其中R是低级烷基，环烷基或烷硫基烷基，R1是氢或低级烷基，羟烷基，新戊酰氧基烷基，烷氧基烷基，烷氧基羰基，羧基或-CONR3R4，其中R3和R4可以是 R 2为低级烷基，羟基烷基，烷氧基烷基或新戊酰氧基烷基，或当R为烷硫基烷基或R 1为新戊酰氧基烷基时，R 2也可为氢及其药理学上可接受的盐; 在治疗或预防心脏和循环系统疾病方面非常有效。

6. 发明授权

US4076829A Aminopropanol compounds and compositions for the treatment of cardiac and circulatory diseases 失效
标题翻译：用于治疗心脏和循环系统疾病的氨基丙醇化合物和组合物
公开(公告)号：US4076829A
公开(公告)日：1978-02-28
申请号：US626512
申请日：1975-10-28
申请人： Wolfgang Kampe , Kurt Stach , Max Thiel , Wolfgang Bartsch , Karl Dietmann , Egon Roesch , Wolfgang Schaumann
发明人： Wolfgang Kampe , Kurt Stach , Max Thiel , Wolfgang Bartsch , Karl Dietmann , Egon Roesch , Wolfgang Schaumann
IPC分类号： C07D209/43 , A61K31/40 , A61K31/403 , A61K31/404 , A61P25/02 , C07D209/08 , C07D209/12 , C07D209/32 , C07D209/42 , C07D209/14
CPC分类号： C07D209/42 , C07D209/08 , C07D209/12 , Y10S514/927
摘要： New aminopropanol compounds of the formula ##STR1## wherein R is lower alkyl, cycloalkyl or alkylthioalkyl,R.sub.1 is hydrogen or lower alkyl, hydroxyalkyl, pivaloyloxyalkyl, alkoxyalkyl, alkoxycarbonyl, carboxyl or --CONR.sub.3 R.sub.4, in which R.sub.3 and R.sub.4 which can be the same or different, represent hydrogen or lower alkyl, andR.sub.2 is lower alkyl, hydroxyalkyl, alkoxyalkyl or pivaloyloxyalkyl or, when R is alkylthioalkyl or R.sub.1 is pivaloyloxyalkyl, R.sub.2 can also be hydrogen andThe pharmacologically acceptable salts thereof; are outstandingly effective in the treatment or prophylaxis of cardiac and circulatory diseases.
摘要翻译：式（I）的新的氨基丙醇化合物其中R是低级烷基，环烷基或烷硫基烷基，R1是氢或低级烷基，羟基烷基，新戊酰氧基烷基，烷氧基烷基，烷氧基羰基，羧基或-CONR3R4，其中R3和R4可以是相同或不同，代表氢或低级烷基，R2是低级烷基，羟基烷基，烷氧基烷基或新戊酰氧基烷基，或当R是烷硫基烷基或R1是新戊酰氧基烷基时，R2也可以是氢，并且其药学上可接受的盐; 在治疗或预防心脏病和循环系统疾病方面具有突出优势。

7. 发明授权

US4152446A Aminopropanol compounds and compositions for the treatment of cardiac and circulatory diseases 失效
标题翻译：用于治疗心脏和循环系统疾病的氨基丙醇化合物和组合物
公开(公告)号：US4152446A
公开(公告)日：1979-05-01
申请号：US805558
申请日：1977-06-10
申请人： Wolfgang Kampe , Kurt Stach , Max Thiel , Wolfgang Bartsch , Karl Dietmann , Egon Roesch , Wolfgang Schaumann
发明人： Wolfgang Kampe , Kurt Stach , Max Thiel , Wolfgang Bartsch , Karl Dietmann , Egon Roesch , Wolfgang Schaumann
IPC分类号： C07D209/08 , C07D209/12 , C07D209/42 , A61K31/40 , C07D209/04
CPC分类号： C07D209/42 , C07D209/08 , C07D209/12
摘要： New aminopropanol compounds of the formula ##STR1## wherein R is lower alkyl, cycloalkyl or alkylthioalkyl,R.sub.1 is hydrogen or lower alkyl, hydroxyalkyl, pivaloyloxyalkyl, alkoxyalkyl, alkoxycarbonyl, carboxyl or --CONR.sub.3 R.sub.4, in which R.sub.3 and R.sub.4 which can be the same or different, represent hydrogen or lower alkyl, andR.sub.2 is lower alkyl, hydroxyalkyl, alkoxyalkyl or pivaloyloxyalkyl or, when R is alkylthioalkyl or R.sub.1 is pivaloyloxyalkyl, R.sub.2 can also be hydrogen and the pharmacologically acceptable salts thereof;Are outstandingly effective in the treatment or prophylaxis of cardiac and circulatory diseases.
摘要翻译：新的式（I）的氨基丙醇化合物其中R是低级烷基，环烷基或烷硫基烷基，R1是氢或低级烷基，羟烷基，新戊酰氧基烷基，烷氧基烷基，烷氧基羰基，羧基或-CONR3R4，其中R3和R4可以是 R 2为低级烷基，羟基烷基，烷氧基烷基或新戊酰氧基烷基，或当R为烷硫基烷基或R 1为新戊酰氧基烷基时，R 2也可为氢及其药理学上可接受的盐; 在治疗或预防心脏病和循环系统疾病方面具有突出优势。

8. 发明授权

US4143149A Indazolyl-(4)-oxypropanolamine compounds and therapeutic compositions 失效
标题翻译：（4） - 异丙醇胺化合物和治疗组合物
公开(公告)号：US4143149A
公开(公告)日：1979-03-06
申请号：US790648
申请日：1977-04-25
申请人： Fritz Wiedemann , Wolfgang Kampe , Max Thiel , Wolfgang Bartsch , Egon Roesch
发明人： Fritz Wiedemann , Wolfgang Kampe , Max Thiel , Wolfgang Bartsch , Egon Roesch
IPC分类号： A61K31/415 , A61P9/00 , A61P25/02 , C07D231/56
CPC分类号： C07D231/56
摘要： New indazolyl-(4)-oxypropanolamine compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or lower alkyl; andR.sub.2 is straight-chain or branched lower alkyl which can be substituted by lower alkylthio;And the pharmacologically compatible salts thereof; are outstandingly effective adrenergic .beta.-receptor inhibitors and useful in the treatment or prevention of a recurrence of cardiac and circulatory diseases.

9. 发明授权

US4436742A 4-Hydroxy-2,1,3-benzthiadiazole compounds and .beta.-adrenergic method of use therefor 失效
标题翻译： 4-羟基-2,1,3-苯并噻二唑化合物和β-肾上腺素能方法
公开(公告)号：US4436742A
公开(公告)日：1984-03-13
申请号：US208741
申请日：1980-11-20
申请人： Erich Fauland , Wolfgang Kampe , Kurt Stach , Wolfgang Bartsch , Egon Roesch
发明人： Erich Fauland , Wolfgang Kampe , Kurt Stach , Wolfgang Bartsch , Egon Roesch
IPC分类号： C07D285/10 , C07D285/14 , C07D285/06
CPC分类号： C07D285/14
摘要： New amine derivatives of 4-hydroxy-2,1,3-benzthiadiazoles of the formula: ##STR1## wherein R is straight-chained or branched alkyl and the pharmacologically compatible salts thereof, that are markedly effected as inhibitors of adrenogenic .beta.-receptors and thus useful for the treatment and prophylaxis of cardiac and circulatory diseases.
摘要翻译：具有下式的4-羟基-2,1,3-苯并噻二唑的新胺衍生物：其中R是直链或支链烷基及其药理学上相容的盐，其显着作为肾上腺素β的抑制剂受体，因此可用于治疗和预防心脏和循环系统疾病。

10. 发明授权

US4503067A Carbazolyl-(4)-oxypropanolamine compounds and therapeutic compositions 失效
标题翻译：（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。

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