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1. 发明授权

US4608383A Cardioactive pyrazole and imidazole aryloxypropanolamines 失效
公开(公告)号：US4608383A
公开(公告)日：1986-08-26
申请号：US538693
申请日：1983-10-03
申请人： Fritz Wiedemann, deceased , Wolfgang Kampe , Karl Dietmann, deceased , Gisbert Sponer
发明人： Fritz Wiedemann, deceased , Wolfgang Kampe , Karl Dietmann, deceased , Gisbert Sponer
IPC分类号： A61K31/38 , A61K31/045 , A61K31/135 , A61K31/138 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/435 , A61K31/47 , A61K31/472 , A61K31/473 , A61K31/495 , A61K31/498 , A61K31/50 , A61K31/505 , A61K31/52 , A61K31/522 , A61P9/00 , A61P9/04 , C07C217/32 , C07C217/72 , C07C217/78 , C07C219/06 , C07C219/08 , C07C219/14 , C07D209/48 , C07D213/74 , C07D215/46 , C07D217/22 , C07D219/12 , C07D231/06 , C07D231/20 , C07D231/32 , C07D231/38 , C07D231/46 , C07D231/52 , C07D231/56 , C07D237/20 , C07D239/42 , C07D239/54 , C07D239/545 , C07D239/557 , C07D239/56 , C07D239/84 , C07D239/95 , C07D241/44 , C07D249/18 , C07D333/36 , C07D473/16 , C07D473/32 , C07D473/34 , C07D487/00 , C07D487/04 , C07D231/54 , C07D233/48 , C07D233/88
CPC分类号： C07D473/16 , C07D209/48 , C07D213/74 , C07D215/46 , C07D217/22 , C07D219/12 , C07D231/06 , C07D231/20 , C07D231/32 , C07D231/38 , C07D231/52 , C07D231/56 , C07D237/20 , C07D239/42 , C07D239/545 , C07D239/557 , C07D239/56 , C07D239/84 , C07D239/95 , C07D333/36 , C07D473/34 , C07D487/04
摘要： The present invention provides aryloxypropanolamines of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, are hydrogen or halogen atoms or lower alkyl, cyano, carboxamide, hydroxyl, lower acyloxy, lower alkoxy, lower alkenyloxy or aryl lower alkoxy radicals, R.sub.5 and R.sub.6, which may be the same or different, are hydrogen atoms or lower alkyl radicals, X is a straight or branched alkylene chain containing 2 to 6 carbon atoms, A is a mono-, bi- or tricyclic heteroaromatic or hydroheteroaromatic radical or, when at least one of the symbols R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is other than a hydrogen atom, may also be a phenyl radical, with the proviso that when A is a uracil-6-yl radical, the 5-position of the uracil moiety does not contain a hydrogen atom, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11, which may be the same or different, are mono- or divalent substituents selected from hydrogen, halogen, notro, hydraxylamino, amino, lower acylamino, lower alkylamino, di-(lower alkyl)-amino, hydroxyethylamino, di-(hydroxyethyl)-amino, hydroxyl, lower alkoxy, allyloxy, methoxy lower alkoxy, cyano, carboxamido, carboxy, lower alkoxycarbonyl, hydroxymethyl, lower alkoxymethyl, halomethyl, aminomethyl, lower acylaminomethyl, halomethyl, aminomethyl, lower acylaminomethyl, di(lower alkyl)-aminomethyl, pyrrolidinomethyl, piperidinomethyl, di-(hydroxyethyl)-amino, hydroxyl, lower alkoxy, allyloxy, methoxy lower alkoxy, cyano, carboxamido, carboxy, lower alkoxycarbonyl, hydroxymethyl, lower alkoxymethyl, halomethyl, aminomethyl, lower acyaminomethyl, di-(lower alkyl)-aminomethyl, pyrrolidinomethyl, piperidinomethyl, di-(hydroxyethyl)-aminomethyl, morpholinomethyl, piperazinomethyl, 4-lower acylpiperazinomethyl, 4-lower alkylpiperazinomethyl, lower alkyl, lower alkenyl, 2-cyanoethyl, 2-hydroxyethyl, phenyl lower alkyl and phenyl, the phenyl radicals being optionally substituted with 1 or 2 hydroxyl or methoxy radicals, or from oxygen or sulphur; the optically-active forms and the racemic mixtures thereof, and the pharmacologically compatible salts thereof.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them. These compounds are useful for the prophylaxis and combatting of cardiac and circulatory diseases.

2. 发明授权

US4666923A Pyrrolobenzimidazoles for treating heart or circulatory diseases 失效
标题翻译：用于治疗心脏或循环系统疾病的吡咯并苯并咪唑
公开(公告)号：US4666923A
公开(公告)日：1987-05-19
申请号：US731500
申请日：1985-05-07
申请人： Jens-Peter Holck , Alfred Mertens , Wolfgang Kampe , Bernd Muller-Beckmann , Gisbert Sponer , Klaus Strein
发明人： Jens-Peter Holck , Alfred Mertens , Wolfgang Kampe , Bernd Muller-Beckmann , Gisbert Sponer , Klaus Strein
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/44 , A61P9/00 , A61P9/04 , A61P9/12 , C07D209/34 , C07D209/42 , C07D209/96 , C07D401/12 , C07D403/14 , C07D487/04 , C07D487/10 , C07D487/14
CPC分类号： C07D487/04 , C07D209/34 , C07D209/42 , C07D209/96 , C07D401/12 , C07D487/10
摘要： Pyrrolobenzimidazoles, processes for the preparation thereof and pharmaceutical compositions thereof for the treatment of coronary insufficiencies, cardiac failure, blood circulatory disturbances and occlusive diseases. The new pyrrolobenzimidazoles are of the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl, alkenyl or cycloalkyl, R.sub.2 is hydrogen, alkyl, alkenyl, cyano or a substituted carbonyl or R.sub.1 and R.sub.2 together represent cycloalkylene or form alkylidene or cycloalkylidene, X is a valency bond, C.sub.1 -C.sub.4 alkylene or vinylene, T is oxygen or sulphur and Py is pyridyl or substituted pyridyl and including the tautomers thereof and the physiologically acceptable salts thereof.
摘要翻译：吡咯并苯并咪唑，其制备方法及其药物组合物，用于治疗冠状动脉不全，心力衰竭，血液循环障碍和闭塞性疾病。新的吡咯并苯并咪唑具有下式（Ⅰ）其中R1是氢，烷基，烯基或环烷基，R2是氢，烷基，烯基，氰基或取代的羰基，或者R1和R2一起代表亚环烷基或亚烷基或亚环烷基， X是价键，C1-C4亚烷基或亚乙烯基，T是氧或硫，Py是吡啶基或取代的吡啶基，并包括其互变异构体及其生理上可接受的盐。

3. 发明授权

US4146630A Blood pressure lowering and adrenergic .beta.-receptor inhibiting 3-(4-phenoxymethylpiperidino)-propyl-phenyl ethers 失效
标题翻译：血压降低和ADRENERGIC“ - 抑制3-（4-苯甲酰氨基哌啶）丙基苯基醚
公开(公告)号：US4146630A
公开(公告)日：1979-03-27
申请号：US846057
申请日：1977-10-27
申请人： Wolfgang Kampe , Walter-Gunar Friebe , Fritz Wiedemann , Gisbert Sponer , Wolfgang Bartsch , Karl Dietmann
发明人： Wolfgang Kampe , Walter-Gunar Friebe , Fritz Wiedemann , Gisbert Sponer , Wolfgang Bartsch , Karl Dietmann
IPC分类号： C07D401/12 , A61K31/403 , A61K31/4184 , A61K31/44 , A61K31/4427 , A61K31/445 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , C07D209/90 , C07D211/22 , C07D231/56
CPC分类号： C07D211/22 , C07D231/56
摘要： A 3-(4-phenoxymethylpiperidino)-propyl-phenyl-ether of the formula ##STR1## wherein R.sub.1 and R.sub.2 each independently is hydrogen, lower alkyl, hydroxyalkyl, lower alkanoyloxyalkyl or --CO--Z,Z is hydroxy, lower alkyloxy or ##STR2## R.sub.6 and R.sub.7 each independently is hydrogen, lower alkyl or hydroxyalkyl,R.sub.3 is hydrogen or --O--R.sub.8,R.sub.8 is hydrogen, lower alkanoyl or aroyl optionally substituted by halogen, lower alkyl, lower alkoxy, alkoxycarbonyl, hydroxyl, alkylthio, nitrile, nitro or trifluoromethyl,R.sub.4 and R.sub.5 each independently is hydrogen, halogen, hydroxy, benzyloxy, lower alkyl, lower alkoxy, lower alkylthio, carboxy, benzyloxycarbonyl or lower alkoxycarbonyl,X and Y each independently is nitrogen or ##STR3## R.sub.9 is hydrogen, lower allkyl optionally substituted by --O--R.sub.8, or --CO--Z,or a pharmacologically acceptable salt thereof. The compounds lower blood pressure and inhibit adrenergic .beta.-receptors.

4. 发明授权

US4468520A 3-Cyano-indoles as cardioselective agents 失效
标题翻译： 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。

5. 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。

6. 发明授权

US4378363A Certain heterocyclic-carboxamido-phenoxy-aminopropanols, compositions containing same and methods of using same 失效
标题翻译：某些杂环 - 甲酰胺基 - 苯氧基 - 氨基丙醇，含有它们的组合物及其使用方法
公开(公告)号：US4378363A
公开(公告)日：1983-03-29
申请号：US207527
申请日：1980-11-17
申请人： Walter-Gunar Friebe , Wolfgang Kampe , Wolfgang Bartsch , Gisbert Sponer , Karl Dietmann
发明人： Walter-Gunar Friebe , Wolfgang Kampe , Wolfgang Bartsch , Gisbert Sponer , Karl Dietmann
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/4406 , A61K31/4418 , A61K31/455 , A61P9/00 , A61P25/02 , C07D207/26 , C07D207/27 , C07D207/34 , C07D209/18 , C07D209/42 , C07D209/43 , C07D213/81 , C07D213/82 , C07D215/48 , C07D235/24 , C07D307/85
CPC分类号： C07D207/27 , C07D207/34 , C07D209/18 , C07D209/42 , C07D213/81 , C07D213/82 , C07D215/48 , C07D235/24 , C07D307/85 , Y10S514/821
摘要： This invention relates to new aminopropanol compounds having beta-adrenergic activity. In addition, the invention is directed to pharmaceutical compositions containing such compounds for the treatment of cardiac and circulatory infirmities and to methods for treating such infirmities.More particularly, the invention relates to new aminopropanol compound of the formula ##STR1## wherein R.sub.1 is a low alkyl moiety, which can be substituted, if desired, by a group Z-R.sub.5 ;R.sub.2 is hydrogen or a low alkanoyl group;R.sub.3 is a mono- or bicyclic heterocyclic compound having 1 to 2 hetero atoms, which can be mono- or polysubstituted, if desired, by halogen, amino, hydroxyl, low alkoxyl, low alkyl;R.sub.4 is hydrogen, a low alkanoyl group or an aroyl group;R.sub.5 is hydrogen or a carbocyclic or heterocyclic aryl moiety, which can be mono- or polysubstituted, if desired, by hydroxyl, low alkyl, low alkenyl, low alkoxyl or low alkenyloxyl;X is a valence bond or a methylene group; andZ is a valence bond, an oxygen atom, or a sulfur atom, and their pharmacologically compatible salts.
摘要翻译：本发明涉及具有β-肾上腺素能活性的新的氨基丙醇化合物。此外，本发明涉及含有用于治疗心脏和循环系统疾病的化合物的药物组合物以及用于治疗这些病症的方法。更具体地，本发明涉及式（I）的新的氨基丙醇化合物，其中R 1是低级烷基部分，如果需要，可以被Z-R5基团取代; R2是氢或低烷酰基; R3是具有1至2个杂原子的单环或双环杂环化合物，如果需要，可以被卤素，氨基，羟基，低烷氧基，低级烷基单取代或多取代; R4是氢，低级烷酰基或芳酰基; R5是氢或碳环或杂环芳基部分，如果需要，可以被羟基，低级烷基，低级链烯基，低烷氧基或低链烯氧基单取代或多取代; X是价键或亚甲基; Z是价键，氧原子或硫原子，以及它们的药理学上相容的盐。

7. 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。

8. 发明授权

US4963686A Certain pyridinoylamino-indolin-2-one derivatives 失效
标题翻译：某些吡啶基氨基 - 二氢吲哚-2-酮衍生物
公开(公告)号：US4963686A
公开(公告)日：1990-10-16
申请号：US217143
申请日：1988-07-05
申请人： Jens-Peter Holck , Alfred Mertens , Wolfgang Kampe , Bernd Muller-Beckmann , Gisbert Sponer , Klaus Strein
发明人： Jens-Peter Holck , Alfred Mertens , Wolfgang Kampe , Bernd Muller-Beckmann , Gisbert Sponer , Klaus Strein
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/44 , A61P9/00 , A61P9/04 , A61P9/12 , C07D209/34 , C07D209/42 , C07D209/96 , C07D401/12 , C07D403/14 , C07D487/04 , C07D487/10 , C07D487/14
CPC分类号： C07D487/04 , C07D209/34 , C07D209/42 , C07D209/96 , C07D401/12 , C07D487/10
摘要： The new pyrrolobenzimidazoles according to the present invention are compounds 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, an alkyl or alkenyl radical or a cyano group or a carbonyl group substituted by a hydroxyl or hydrazino group or by an alkyl, alkoxy, amino, alkylamino or dialkylamino group or together with R.sub.1 represents a cycloalkylene radical or R.sub.1 and R.sub.2 together form an alkylidene or cycloalkylidene radical, X is a valency bond, a C.sub.1 -C.sub.4 alkylene radical or a vinylene radical, T is an oxygen or sulphur atom and Py is a 2-, 3- or 4-pyridyl radical which optionally carries an oxygen atom on the ring heteroatom and/or can be substituted one or more times by alkyl, alkoxy, hydroxyl, cyano or nitro, as well as by halogen; the tautomers thereof and the physiologically acceptable salts thereof with inorganic and organic acids.

9. 发明授权

US4438128A Cardioactive aryloxypropanolamines 失效
公开(公告)号：US4438128A
公开(公告)日：1984-03-20
申请号：US273543
申请日：1981-06-15
申请人： Fritz Wiedemann , Wolfgang Kampe , Karl Dietmann , Gisbert Sponer
发明人： Fritz Wiedemann , Wolfgang Kampe , Karl Dietmann , Gisbert Sponer
IPC分类号： A61K31/38 , A61K31/045 , A61K31/135 , A61K31/138 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/435 , A61K31/47 , A61K31/472 , A61K31/473 , A61K31/495 , A61K31/498 , A61K31/50 , A61K31/505 , A61K31/52 , A61K31/522 , A61P9/00 , A61P9/04 , C07C217/32 , C07C217/72 , C07C217/78 , C07C219/06 , C07C219/08 , C07C219/14 , C07D209/48 , C07D213/74 , C07D215/46 , C07D217/22 , C07D219/12 , C07D231/06 , C07D231/20 , C07D231/32 , C07D231/38 , C07D231/46 , C07D231/52 , C07D231/56 , C07D237/20 , C07D239/42 , C07D239/54 , C07D239/545 , C07D239/557 , C07D239/56 , C07D239/84 , C07D239/95 , C07D241/44 , C07D249/18 , C07D333/36 , C07D473/16 , C07D473/32 , C07D473/34 , C07D487/00 , C07D487/04 , C07D231/54
CPC分类号： C07D473/16 , C07D209/48 , C07D213/74 , C07D215/46 , C07D217/22 , C07D219/12 , C07D231/06 , C07D231/20 , C07D231/32 , C07D231/38 , C07D231/52 , C07D231/56 , C07D237/20 , C07D239/42 , C07D239/545 , C07D239/557 , C07D239/56 , C07D239/84 , C07D239/95 , C07D333/36 , C07D473/34 , C07D487/04
摘要： The present invention provides aryloxypropanolamines of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, are hydrogen or halogen atoms or lower alkyl, cyano, carboxamido, hydroxyl, lower acyloxy, lower alkoxy, lower alkenyloxy or aryl lower alkoxy radicals, R.sub.5 and R.sub.6, which may be the same or different, are hydrogen atoms or lower alkyl radicals, X is a straight or branched alkylene chain containing 2 to 6 carbon atoms, A is a mono-, bi- or tricyclic heteroaromatic or hydroheteroaromatic radical or, when at least one of the symbols R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is other than a hydrogen atom, may also be a phenyl radical, with the proviso that when A is a uracil-6-yl radical, the 5-position of the uracil moiety does not contain a hydrogen atom, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11, which may be the same or different, are mono- or divalent substituents selected from hydrogen, halogen, nitro, hydroxylamino, amino, lower acylamino, lower alkylamino, di-(lower alkyl)-amino, hydroxyethylamino, di-(hydroxyethyl)-amino, hydroxyl, lower alkoxy, allyloxy, methoxy lower alkoxy, cyano, carboxamido, carboxy, lower alkoxycarbonyl, hydroxymethyl, lower alkoxymethyl, halomethyl, aminomethyl, lower acylaminomethyl, di-(lower alkyl)-aminomethyl, pyrrolidinomethyl, piperidinomethyl, di-(hydroxyethyl)-aminomethyl, morpholinomethyl, piperazinomethyl, 4-lower acylpiperazinomethyl, 4-lower alkylpiperazinomethyl, lower alkyl, lower alkenyl, 2-cyanoethyl, 2-(lower alkoxycarbonyl)-ethyl, 2-carboxyethyl, 2-hydroxyethyl, phenyl lower alkyl and phenyl, the phenyl radicals being optionally substituted with 1 or 2 hydroxyl or methoxy radicals, or from oxygen or sulphur; the optically-active forms and the racemic mixtures thereof, and the pharmacologically compatible salts thereof.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.

10. 发明授权

US5760069A Method of treatment for decreasing mortality resulting from congestive heart failure 失效
标题翻译：减少充血性心力衰竭引起的死亡率的治疗方法
公开(公告)号：US5760069A
公开(公告)日：1998-06-02
申请号：US483635
申请日：1995-06-07
申请人： Mary Ann Lukas-Laskey , Robert Ruffolo, Jr. , Neil Howard Shusterman , Gisbert Sponer , Klaus Strein
发明人： Mary Ann Lukas-Laskey , Robert Ruffolo, Jr. , Neil Howard Shusterman , Gisbert Sponer , Klaus Strein
IPC分类号： C07D207/16 , A61K31/196 , A61K31/34 , A61K31/40 , A61K31/401 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/54 , A61K31/549 , A61K31/662 , A61K31/70 , A61K31/702 , A61K38/00 , A61K45/00 , A61K45/06 , A61P9/00 , A61P9/04 , C07D209/88 , A61K31/585
CPC分类号： A61K31/403 , A61K31/7048
摘要： A method of treatment using a compound of Formula I: ##STR1## wherein: R.sub.1 is hydrogen, lower alkanoyl of up to 6 carbon atoms or aroyl selected from benzoyl and naphthoyl; R.sub.2 is hydrogen, lower alkyl of up to 6 carbon atoms or arylalkyl selected from benzyl, phenylethyl and phenylpropyl; R.sub.3 is hydrogen or lower alkyl of up to 6 carbon atoms; R.sub.4 is hydrogen or lower alkyl of up to 6 carbon atoms, 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 selected from phenyl, naphthyl, indanyl and tetrahydronaphthyl; R.sub.5 and R.sub.6 are individually selected from hydrogen, fluorine, chlorine, bromine, hydroxyl, lower alkyl of up to 6 carbon atoms, a --CONH.sub.2 -- group, lower alkoxy of up to 6 carbon atoms, benzyloxy, lower alkylthio of up to 6 carbon atoms, lower alkysulphinyl of up to 6 carbon atoms and lower alkylsulphonyl of up to 6 carbon atoms; or R.sub.5 and R.sub.6 together represent methylenedioxy; or a pharmaceutically acceptable salt thereof, alone or in conjunction with one or more other therapeutic agents, said agents being selected from the group consisting of ACE inhibitors, diuretics, and digoxin for decreasing mortality resulting from congestive heart failure (CHF) in mammals, particularly humans.
摘要翻译：使用式I化合物的方法：其中：R1是氢，至多6个碳原子的低级烷酰基或选自苯甲酰基和萘甲酰基的芳酰基; R2是氢，至多6个碳原子的低级烷基或选自苄基，苯基乙基和苯基丙基的芳基烷基; R3是氢或至多6个碳原子的低级烷基; R4是氢或至多6个碳原子的低级烷基，或当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选自苯基，萘基，茚满基和四氢萘基; R 5和R 6分别选自氢，氟，氯，溴，羟基，至多6个碳原子的低级烷基，-CONH 2 - 基，至多6个碳原子的低级烷氧基，苄氧基，至多6个碳的低级烷硫基原子，低至6个碳原子的低级烷基亚磺酰基和至多6个碳原子的低级烷基磺酰基; 或R5和R6一起表示亚甲二氧基; 特别是用于降低哺乳动物充血性心力衰竭（CHF）引起的死亡率的ACE抑制剂，利尿剂和地高辛，所述药物单独或与一种或多种其它治疗剂联合使用，或其药学上可接受的盐，人类。

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