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1. 发明授权

US4304912A Piperidine derivatives 失效
标题翻译：哌啶衍生物
公开(公告)号：US4304912A
公开(公告)日：1981-12-08
申请号：US102462
申请日：1979-12-10
申请人： Herbert Schroter , Kurt Eichenberger , Hans Kuhnis , Christian Egli , Oswald Schier , Franz Ostermayer
发明人： Herbert Schroter , Kurt Eichenberger , Hans Kuhnis , Christian Egli , Oswald Schier , Franz Ostermayer
IPC分类号： C07D401/04 , C07D209/12 , C07D217/22 , C07D241/18
CPC分类号： C07D401/04 , Y10S514/821
摘要： Piperidines of the formula ##STR1## in which R.sub.1 is a substituted or unsubstituted heteroaryl radical, alk.sub.1 and alk.sub.2 independently of one another are lower alkylene radicals, each of which separates by 2 carbon atoms the nitrogen atom bonded thereto from the methane group bonded thereto, R.sub.2 is a free or acylated hydroxyl group, Ph is a substituted or unsubstituted o-phenylene radical, n is 0 or 1, R.sub.3 is a hydrogen atom, a lower alkyl radical or a hydroxyl group and R.sub.5 is a lower alkyl radical or a hydrogen atom, or R.sub.3 and R.sub.5 together are a second bond and R.sub.4 and R.sub.6 are each a hydrogen atom, or R.sub.4 together with R.sub.3 is an oxo group, R.sub.5 is a lower alkyl radical or a hydrogen atom and R.sub.6 is a hydrogen atom, or R.sub.6 together with R.sub.5 is an oxo group, R.sub.3 is a hydrogen atom, a lower alkyl radical or a hydroxyl group and R.sub.4 is a hydrogen atom, or salts thereof are antihypertensive and antiarrhythmic agents.
摘要翻译：其中R1是取代或未取代的杂芳基，alk1和alk2彼此独立的式（I）的哌啶子是低级亚烷基，其各自分开2个碳原子，与甲烷基团键合的氮原子 R 2为游离或酰化羟基，Ph为取代或未取代的邻苯基，n为0或1，R3为氢原子，低级烷基或羟基，R5为低级烷基或氢原子，或者R 3和R 5一起为第二键，并且R 4和R 6各自为氢原子，或者R 4与R 3一起为氧基，R5为低级烷基或氢原子，R6为氢原子或R6与R5一起为氧基，R3为氢原子，低级烷基或羟基，R4为氢原子，或其盐为抗高血压药和抗心律失常药。

2. 发明授权

US4264599A Piperidino-propanols 失效
标题翻译：哌哌啶 - 丙醇
公开(公告)号：US4264599A
公开(公告)日：1981-04-28
申请号：US921521
申请日：1978-07-03
申请人： Kurt Eichenberger , Hans Kuhnis , Franz Ostermayer , Herbert Schroter
发明人： Kurt Eichenberger , Hans Kuhnis , Franz Ostermayer , Herbert Schroter
IPC分类号： C07D209/08 , C07D211/58 , C07D213/65 , C07D213/69 , C07D401/14 , A61K31/365 , A61K31/495
CPC分类号： C07D213/69 , C07D209/08 , C07D211/58 , C07D213/65
摘要： The invention relates to novel piperidino-propanols, especially 1-(3-heterocyclyloxy-2-hydroxy-propanol)-4-(N-diazcyclyl)-piperidines of the formula ##STR1## in which R.sub.1 is a substituted or unsubstituted heteroaryl radical, R.sub.2 is hydrogen or a substituted or unsubstituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic hydrocarbon radical or an acyl radical and alk is lower alkylene which separates the two nitrogen atoms from one another by 2 or 3 carbon atoms, or is a substituted or unsubstituted 1,2-phenylene radical, and salts thereof, as well as processes for their preparation, and also to pharmaceutical preparations containing these compounds and the use thereof, preferably in the form of pharmaceutical preparations as antihypertensive agents, antitachycardiac agents and .alpha.-sympathicolytic agents.
摘要翻译：本发明涉及新的哌啶子基 - 丙醇，特别是式（I）的1-（3-杂环氧基-2-羟基 - 丙醇）-4-（N-二氮杂环丙基） - 哌啶，其中R 1是取代或未取代的杂芳基，R2是氢或取代或未取代的脂族，脂环族，脂环族 - 脂族或芳脂族烃基或酰基，而烷基是两个氮原子彼此分开2或3个碳原子的低级亚烷基，或者是取代或未取代的1,2-亚苯基及其盐，以及其制备方法，以及含有这些化合物的药物制剂及其用途，优选以药物制剂的形式作为抗高血压药，抗心律失常药和α - 溶脂剂。

3. 发明授权

US4144344A Antihypertensive 1-substituted-4-(2-oxo-1-imidazolidinyl) piperidines 失效
标题翻译：抗高血压1-取代-4-（2-氧代-1-咪唑烷基）哌啶
公开(公告)号：US4144344A
公开(公告)日：1979-03-13
申请号：US761510
申请日：1977-01-21
申请人： Kurt Eichenberger , Hans Kuhnis , Franz Ostermayer , Herbert Schroter
发明人： Kurt Eichenberger , Hans Kuhnis , Franz Ostermayer , Herbert Schroter
IPC分类号： A61K31/4409 , A61K31/4427 , A61K31/445 , A61K31/4468 , A61K31/505 , A61P9/06 , A61P9/12 , A61P25/02 , C07D211/58 , C07D211/72 , C07D211/74 , C07D213/74 , C07D401/04 , C07D401/14
CPC分类号： C07D213/74 , C07D211/58 , C07D211/72
摘要： A process known per se for the manufacture of oxygenated N-aryl-diazacyclic compounds of the formula ##STR1## wherein EACH OF R.sub.1 and R.sub.2 represents a substituted or unsubstituted aryl group and alk represents a lower alkylene group which separates both nitrogen atoms from each other by 2 or 3 carbon atoms, or salts thereof.The novel compounds can be used as antihypertensives, antitachycardiac agents and .alpha.-receptor blockers.
摘要翻译：本领域已知的用于制备式（I）的氧化N-芳基 - 二氮环化合物的方法，其中R 1和R 2各自表示取代或未取代的芳基，而alk表示分开两个氮原子的低级亚烷基彼此间有2或3个碳原子，或其盐。

4. 发明授权

US4217350A Oxygenated N-aryl-diazacyclic compounds 失效
标题翻译：氧化N-芳基 - 二氮环化合物
公开(公告)号：US4217350A
公开(公告)日：1980-08-12
申请号：US972589
申请日：1978-12-22
申请人： Kurt Eichenberger , Hans Kuhnis , Franz Ostermayer , Herbert Schroter
发明人： Kurt Eichenberger , Hans Kuhnis , Franz Ostermayer , Herbert Schroter
IPC分类号： C07D211/58 , C07D211/74 , C07D213/74 , A61K31/495 , C07D401/14
CPC分类号： C07D213/74 , C07D211/58 , C07D211/74
摘要： A process known per se for the manufacture of oxygenated N-aryl-diazacyclic compounds of the formula ##STR1## wherein each of R.sub.1 and R.sub.2 represents a substituted or unsubstituted aryl group and alk represents a lower alkylene group which separates both nitrogen atoms from each other by 2 or 3 carbon atoms, or salts thereof.The novel compounds can be used as antihypertensives, antitachycardiac agents and .alpha.-receptor blockers.
摘要翻译：本领域已知的用于制备式（I）的氧化N-芳基 - 二氮环化合物的方法，其中R 1和R 2各自表示取代或未取代的芳基，而alk表示分开两个氮原子的低级亚烷基彼此间有2或3个碳原子，或其盐。新型化合物可用作抗高血压药，抗心律失常药和α-受体阻断剂。

5. 发明授权

US4075208A 1-Substituted-4-(2-oxo-hexahydro-1-pyrimidinyl)-piperidine 失效
标题翻译： 1-取代的-4-（2-氧代 - 六氢-1-嘧啶基） - 哌啶
公开(公告)号：US4075208A
公开(公告)日：1978-02-21
申请号：US652965
申请日：1976-01-28
申请人： Max Wilhelm , Kurt Eichenberger , Herbert Schroter , Franz Ostermayer
发明人： Max Wilhelm , Kurt Eichenberger , Herbert Schroter , Franz Ostermayer
IPC分类号： A61K31/445 , A61K31/495 , A61K31/635 , C07D213/75 , A61K31/505 , C07D401/04
CPC分类号： C07D213/75 , A61K31/445 , A61K31/495 , A61K31/635
摘要： Piperidines of the formula ##STR1## in which R.sub.1 stands for optionally substituted aryl, R.sub.2 for hydrogen, lower alkyl, lower alkenyl, acyl or .alpha.-aryl-lower alkyl, R.sub.3 for a free or substituted hydroxyl group, alk for lower alkylene which separates the two nitrogen atoms by 2 or 3 carbon atoms, R.sub.4 represents hydrogen or lower alkyl and n represents an integer from 1 to 4, and their salts as well as processes for their manufacture and pharmaceutical compositions comprising such compounds, and a process for lowering the blood pressure wherein such compositions are administered to a warm-blooded host.
摘要翻译：其中R1代表任选取代的芳基，R2代表氢，低级烷基，低级烯基，酰基或α-芳基 - 低级烷基，R3代表游离或取代的羟基，用于低级亚烷基的烷基， 2个或3个碳原子的氮原子，R4代表氢或低级烷基，n代表1至4的整数，它们的盐以及它们的制备方法和包含这些化合物的药物组合物，以及降低血压，其中将这样的组合物施用于温血主体。

6. 发明授权

US4075335A Pharmaceutical piperidine derivatives 失效
标题翻译：制药哌啶衍生物
公开(公告)号：US4075335A
公开(公告)日：1978-02-21
申请号：US652966
申请日：1976-01-28
申请人： Max Wilhelm , Kurt Eichenberger , Herbert Schroter , Franz Ostermayer
发明人： Max Wilhelm , Kurt Eichenberger , Herbert Schroter , Franz Ostermayer
IPC分类号： A61K31/445 , A61K31/495 , A61K31/635 , C07D213/75 , A61K31/33
CPC分类号： C07D213/75 , A61K31/445 , A61K31/495 , A61K31/635
摘要： Piperidines of the formula ##STR1## in which R.sub.1 stands for optionally substituted aryl, R.sub.2 for hydrogen, lower alkyl, lower alkenyl, acyl or .alpha.-aryl-lower alkyl, R.sub.3 for a free or substituted hydroxyl group, alk for lower alkylene which separates the two nitrogen atoms by 2 or 3 carbon atoms, R.sub.4 represents hydrogen or lower alkyl and n represents an integer from 1 to 4, and their salts as well as processes for their manufacture and pharmaceutical compositions comprising such compounds, and a process for lowering the blood pressure wherein such compositions are administered to a warm-blooded host.
摘要翻译：其中R1代表任选取代的芳基，R2代表氢，低级烷基，低级烯基，酰基或α-芳基 - 低级烷基，R3代表游离或取代的羟基，用于低级亚烷基的烷基， 2个或3个碳原子的氮原子，R4代表氢或低级烷基，n代表1至4的整数，它们的盐以及它们的制备方法和包含这些化合物的药物组合物，以及降低血压，其中将这样的组合物施用于温血主体。

7. 发明授权

US3956335A 1-Substituted-4-(2-oxo-1-imidazolidinyl) piperidines 失效
标题翻译： 1-取代的-4-（2-氧代-1-咪唑烷基）哌啶
公开(公告)号：US3956335A
公开(公告)日：1976-05-11
申请号：US483742
申请日：1974-06-27
申请人： Max Wilhelm , Kurt Eichenberger , Herbert Schroter , Franz Ostermayer
发明人： Max Wilhelm , Kurt Eichenberger , Herbert Schroter , Franz Ostermayer
IPC分类号： A61K31/445 , A61K31/505 , A61K31/635 , C07D213/75 , C07D211/58
CPC分类号： C07D213/75 , A61K31/445 , A61K31/505 , A61K31/635
摘要： Piperidines of the formula ##SPC1##In which R.sub.1 stands for optionally substituted aryl, R.sub.2 for hydrogen, lower alkyl, lower alkenyl, acyl or .alpha.-aryl-lower alkyl, R.sub.3 for a free or substituted hydroxyl group, alk for lower alkylene which separates the two nitrogen atoms by 2 or 3 carbon atoms, R.sub.4 represents hydrogen or lower alkyl and n represents an integer from 1 to 4, and their salts as well as processes for their manufacture and pharmaceutical compositions comprising such compounds, and a process for lowering the blood pressure wherein such compositions are administered to a warm-blooded host.
摘要翻译：式I的哌啶代表任选取代的芳基，R 2表示氢，低级烷基，低级烯基，酰基或α-芳基 - 低级烷基，R3表示游离或取代的羟基，alk表示分开两个氮的低级亚烷基 2个或3个碳原子的原子，R4代表氢或低级烷基，n代表1至4的整数，以及它们的盐及其制备方法和包含这些化合物的药物组合物，以及降低血压的方法，其中将这样的组合物施用于温血的宿主。

8. 发明授权

US4310527A Etherified hydroxy quinazolone compounds 失效
标题翻译：醚化羟基喹唑啉酮化合物
公开(公告)号：US4310527A
公开(公告)日：1982-01-12
申请号：US18397
申请日：1979-03-08
申请人： Knut A. Jaeggi , Franz Ostermayer , Herbert Schroter
发明人： Knut A. Jaeggi , Franz Ostermayer , Herbert Schroter
IPC分类号： A61K31/415 , A61K31/416 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5355 , A61K31/536 , A61K31/5377 , A61K31/538 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , C07C205/37 , C07C205/42 , C07C205/43 , C07D235/26 , C07D239/80 , C07D239/96 , C07D241/44 , C07D263/58 , C07D265/18 , C07D265/36 , C07D277/26 , C07D285/10 , C07D303/22 , C07D303/24 , C07D309/12 , A61K31/505
CPC分类号： C07D263/58 , C07D235/26 , C07D239/80 , C07D239/96 , C07D241/44 , C07D265/18 , C07D265/36 , C07D285/10 , C07D303/22 , C07D303/24 , C07D309/12 , Y10S514/821
摘要： A compound of the formula ##STR1## in which R.sub.1 denotes optionally substituted lower alkyl which is optionally branched at the linking carbon atom, R.sub.2 represents hydrogen or lower alkanoyl and R.sub.3 is a group of the formula --R.sub.3.sup.a --(R.sub.3.sup.b).sub.n -- (Ia), in which R.sub.3.sup.a represents the radical of the formula --N(R.sub.4)-- or --O-- and R.sub.4 represents hydrogen or lower alkyl, R.sub.3.sup.b denotes the radical of the formula --CH.sub.2 -- or, if R.sub.3.sup.a represents --N(R.sub.4)--, denotes the radical of the formula --C(.dbd.O)-- and n represents nought or 1, and a group of the formula Ia, in which n represents 1, can be linked to the carbonyl group of the carbamoyl grouping either via the group R.sub.3.sup.a or the group R.sub.3.sup.b, or acid addition salts thereof, which can be used pharmaceutically can be used as beta-receptor blocking agents for the treatment of disorders in the cardiac rhythm and coronary heart diseases. These compounds also possess a cardio-stimulating action; some of them also display alpha-receptor-blocking properties.
摘要翻译：式（I）的化合物，其中R 1表示在连接碳原子上任选支链的任选取代的低级烷基，R 2表示氢或低级烷酰基，R 3是式-R 3 a（R 3 b）n - （Ia），其中R 3a表示式-N（R 4） - 或-O-的基团，R 4表示氢或低级烷基，R 3b表示式-CH 2 - 或如果R 3a表示-N（ R 4） - 表示式-C（= O） - 且n表示无或者1的基团，并且其中n表示1的式Ia的基团可以与氨基甲酰基的羰基连接，或者可以通过组R3a或R3b或其酸加成盐或其酸加成盐，其可以用作β-受体阻断剂，用于治疗心律和冠心病疾病。这些化合物还具有心脏刺激作用; 其中一些还显示α-受体阻断性质。

9. 发明授权

US4049797A Composition and method for treatment of heart and circulatory ailments 失效
标题翻译：治疗心脏和循环系统疾病的组合物和方法
公开(公告)号：US4049797A
公开(公告)日：1977-09-20
申请号：US669078
申请日：1976-03-22
申请人： Knut A. Jaeggi , Herbert Schroter , Franz Ostermayer
发明人： Knut A. Jaeggi , Herbert Schroter , Franz Ostermayer
IPC分类号： C07H15/20 , A61K31/70
CPC分类号： C07H15/20
摘要： 1-Phenoxy-2-hydroxy-3-amino-propanes of the formula I ##STR1## wherein R.sub.1 is a sugar residue and R.sub.2 is isopropyl, tert.-butyl or .alpha.-methyl-phenethyl optionally substituted in the phenyl part, and salts thereof are useful as positively inotropic agents, especially in the treatment of insufficiency of the cardiac muscle.
摘要翻译：式I（I）的1-苯氧基-2-羟基-3-氨基 - 丙烷其中R1是糖残基，R2是异丙基，叔丁基或α-甲基 - 苯乙基，其在苯基部分任选被取代及其盐可用作正性肌力药，特别是用于治疗心肌功能不全。

10. 发明授权

US4195090A 2-(3-Amino-2-hydroxy-propoxy)pyridine derivatives and pharmaceutical compositions therewith 失效
标题翻译： 2-（3-氨基-2-羟基 - 丙氧基）吡啶衍生物及其药物组合物
公开(公告)号：US4195090A
公开(公告)日：1980-03-25
申请号：US883434
申请日：1978-03-03
申请人： Jurg Frei , Knut A. Jaeggi , Franz Ostermayer , Herbert Schroter
发明人： Jurg Frei , Knut A. Jaeggi , Franz Ostermayer , Herbert Schroter
IPC分类号： C07D213/38 , C07D213/40 , C07D213/57 , C07D213/61 , C07D213/63 , C07D213/69 , C07D213/75 , C07D213/81 , C07D213/82 , C07D213/85 , C07D213/89 , C07D239/30 , C07D239/34 , C07D239/36 , C07D239/42 , C07D239/46 , C07D239/54 , C07D239/56 , C07D241/18 , C07D263/06 , A61K31/44 , C07D213/46
CPC分类号： C07D213/40 , C07D213/38 , C07D213/57 , C07D213/61 , C07D213/63 , C07D213/69 , C07D213/75 , C07D213/81 , C07D213/82 , C07D213/85 , C07D213/89 , C07D239/34 , C07D239/36 , C07D239/42 , C07D239/47 , C07D239/54 , C07D239/56 , C07D241/18 , C07D263/06
摘要： Heterocyclic compounds of the formula ##STR1## wherein Het denotes optionally substituted pyridazinyl, pyrimidinyl, pyrazinyl or substituted pyridyl, R.sub.1 is hydrogen or methyl and R.sub.2 is lower alkyl, optionally substituted phenyl-lower alkyl, carboxy-lower alkyl or functionally modified carboxy-lower alkyl, their condensation products with aldehydes, ketones or carbonic acid and their N-oxides, which are valuable (cardioselective) .beta.-rezeptor blocking agents, and/or (cardioselective) .beta.-rezeptor-stimulants.
摘要翻译：式（I）的杂环化合物，其中Het表示任选取代的哒嗪基，嘧啶基，吡嗪基或取代的吡啶基，R 1为氢或甲基，R 2为低级烷基，任选取代的苯基 - 低级烷基，羧基 - 低级烷基或官能改性羧基 - 低级烷基，它们与醛，酮或碳酸及其N-氧化物的缩合产物，它们是有价值的（心脏选择性）β-受体阻断剂和/或（心脏选择性）β-受体激动剂。

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