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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

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。

7. 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。

8. 发明授权

US3998955A Antihypertensive compositions 失效
标题翻译：抗高血压药物
公开(公告)号：US3998955A
公开(公告)日：1976-12-21
申请号：US568483
申请日：1975-04-16
申请人： Hans Kuhnis , Christian Egli , Kurt Eichenberger , Phyllis Roberta Hedwall
发明人： Hans Kuhnis , Christian Egli , Kurt Eichenberger , Phyllis Roberta Hedwall
IPC分类号： C07D213/64 , C07D213/68 , C07D213/79 , C07D213/81 , A61K31/455
CPC分类号： C07D213/64 , C07D213/68 , C07D213/79 , C07D213/81
摘要： Pyridines of the formula I ##STR1## wherein R.sub.1 is free hydroxyl, lower alkoxy, cycloalkoxy, amino-lower alkoxy or lower alkoxy-lower alkoxy, free amino, hydroxyamino, lower alkyleneamino, oxa-, aza- or thia-lower alkyleneamino or mono- or di-lower alkylamino, R.sub.2 is oxygen or sulphur, R.sub.3 and R.sub.4 are each alkoxy, free amino, mono- or di-lower alkylamino, lower alkyleneamino, oxa-, aza- or thia-lower alkyleneamino, halogen or free hydroxyl, and either R.sub.3 or R.sub.4 can be hydrogen, and alk is an alkyl group with 3-10 carbon atoms, and their N-oxides, and salts are useful as dopamine-.beta.-hydroxylase inhibitors.
摘要翻译：式I的吡啶（I）其中R1是游离羟基，低级烷氧基，环烷氧基，氨基 - 低级烷氧基或低级烷氧基 - 低级烷氧基，游离氨基，羟基氨基，低级亚烷基氨基，氧杂 - ，氮杂 - 或低级亚烷基氨基或单 - 或二 - 低级烷基氨基，R2是氧或硫，R3和R4分别是烷氧基，游离氨基，一或二低级烷基氨基，低级亚烷基氨基，氧杂 - ，氮杂 - 或硫代 - 低级亚烷基氨基，卤素或游离羟基，R3或R4可以是氢，alk是具有3-10个碳原子的烷基，它们的N-氧化物和盐可用作多巴胺-β-羟化酶抑制剂。

9. 发明授权

US4616002A Dihydro pyridine compounds, compositions and use 失效
标题翻译：二氢吡啶化合物，组成和用途
公开(公告)号：US4616002A
公开(公告)日：1986-10-07
申请号：US816461
申请日：1986-01-06
申请人： Bruno Kamber , Thomas Leutert , Hans Kuhnis , Kurt Eichenberger
发明人： Bruno Kamber , Thomas Leutert , Hans Kuhnis , Kurt Eichenberger
IPC分类号： C07D211/90 , C07D401/06 , C07D405/12 , C07D417/12 , C07K5/065 , A61K31/535 , A61K37/02 , C07D413/12 , C07K5/06
CPC分类号： C07D401/06 , C07D211/90 , C07D405/12 , C07D417/12 , C07K5/06078
摘要： Compounds of the formula I ##STR1## in which n represents 1, 2 or 3, Ar represents a carbocyclic or heterocyclic aryl radical, Ac represents the acyl radical of an acid, Z represents a radical --OR.sub.7 or --NR.sub.8 R.sub.9, R.sub.1 represents hydrogen, unsubstituted or substituted lower alkyl, a carbocyclic or heterocyclic aryl radical or free, etherified or esterified hydroxy, R.sub.2 and R.sub.3, independently of one another, each represents hydrogen, unsubstituted or substituted lower alkyl, formyl or functionally modified formyl, carboxy or functionally modified carboxy, a carbocyclic or heterocyclic aryl radical or unsubstituted or mono- or di-substituted amino, R.sub.4 represents hydrogen or lower alkyl, R.sub.5 and R.sub.6, independently of one another, each represents hydrogen, unsubstituted or substituted lower alkyl or a carbocyclic or heterocyclic aryl radical, R.sub.7, R.sub.8 and R.sub.9, independently of one another, each represents hydrogen, unsubstituted or substituted alkyl or a carbocyclic or heterocyclic aryl radical; in which R.sub.1 and R.sub.2 together or R.sub.1 and R.sub.3 together may represent unsubstituted or substituted lower alkylene in which a carbon atom is optionally replaced by a hetero atom, in which R.sub.4 and R.sub.5 together, and likewise R.sub.5 and R.sub.6 together and/or R.sub.8 and R.sub.9 together, independently of one another, may represent unsubstituted or substituted lower alkylene in which a carbon atom may have been replaced by a hetero atom, optical isomers of compounds of the formula I, mixtures of these optical isomers and salts of such compounds that have a salt-forming grouping, are distinguished by cardiovascular, especially blood pressure-reducing, properties. They are manufactured in a manner known per se.
摘要翻译：式I的化合物（I）其中n表示1,2或3，Ar表示碳环或杂环芳基，Ac表示酸的酰基，Z表示基团-OR7或-NR8R9，R1 代表氢，未取代或取代的低级烷基，碳环或杂环芳基或游离的醚化或酯化的羟基，R 2和R 3彼此独立地表示氢，未取代或取代的低级烷基，甲酰基或官能改性的甲酰基，羧基或官能改性的羧基，碳环或杂环芳基或未取代的或单取代或二取代的氨基，R 4表示氢或低级烷基，R 5和R 6彼此独立地表示氢，未取代或取代的低级烷基或碳环或杂环芳基，R 7，R 8和R 9彼此独立地表示氢，未取代或取代的烷基或碳环或杂环芳基; 其中R 1和R 2一起或R 1和R 3一起可以表示未取代或取代的低级亚烷基，其中碳原子任选被杂原子取代，其中R 4和R 5一起以及R 5和R 6一起和/或R 8和R 9 一起彼此独立地表示未取代或取代的低级亚烷基，其中碳原子可以被杂原子取代，式I化合物的光学异构体，这些光学异构体的混合物和这些化合物的盐，其具有盐形成分组由心血管特别是降血压特性区分。它们以本身已知的方式制造。

10. 发明授权

US4808603A 3,5-diacyl-2,6-dialkyl-4-aryl-1,4-dihydropyridines, their use, and pharmaceutical compositions thereof 失效
标题翻译： 3,5-二酰基-2,6-二烷基-4-芳基-1,4-二氢吡啶，其用途及其药物组合物
公开(公告)号：US4808603A
公开(公告)日：1989-02-28
申请号：US895604
申请日：1986-08-07
申请人： Kurt Eichenberger , Hans Kuhnis
发明人： Kurt Eichenberger , Hans Kuhnis
IPC分类号： A61K31/443 , A61K31/4433 , A61K31/455 , A61P7/02 , A61P9/08 , A61P9/10 , A61P9/12 , C07D211/90 , C07D317/00 , C07D333/00 , C07D405/12 , C07D409/12 , C07D213/55 , A61K31/44
CPC分类号： C07D409/12 , C07D211/90
摘要： Compounds of the formula ##STR1## in which R represents a carbocyclic or heterocyclic aryl radical, R.sub.1 represents lower alkyl, one of the groups R.sub.2 and R.sub.3 represents lower alkyl and the other represents lower alkyl, cyano aor amino, X represents oxygen or the group --NH--, Alk.sub.1 represents lower alkylene or optionally substituted phenyl-lower alkylene, which separates the group X from the nitrogen atom by at least two carbon atoms, R.sub.4 represents hydrogen, lower alkyl or optionally substituted phenyl-lower alkyl, Z represents the group --(C.dbd.O)-- or a single bond, Alk.sub.2 represents lower alkylene which separates the groups Z and Y preferably by from 2 to 4 carbon atoms, Y represents the group --(C.dbd.O)-- and Ar.sub.1 represents a monocyclic, carbocyclic or heterocyclic aryl radical, and salts of such compounds having salt-forming properties, have cardiovascular properties, especially coronary dilatory and anti-hypertensive properties.
摘要翻译：式（I）的化合物，其中R表示碳环或杂环芳基，R1表示低级烷基，R2和R3之一表示低级烷基，另一个表示低级烷基，氰基或氨基，X表示氧或基团-NH-，Alk1表示低级亚烷基或任选取代的苯基 - 低级亚烷基，其将基团X与氮原子分开至少两个碳原子，R 4表示氢，低级烷基或任选取代的苯基 - 低级烷基，Z 代表基团 - （C = O） - 或单键，Alk2表示将基团Z和Y优选分解为2至4个碳原子的低级亚烷基，Y表示 - （C = O） - 基团，Ar 1表示单环，碳环或杂环芳基，以及具有成盐性质的这些化合物的盐具有心血管特性，特别是冠状动脉介入和抗高血压性质。

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