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    Piperidine derivatives
    1.
    发明授权
    Piperidine derivatives 失效
    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。

    Piperidino-propanols
    2.
    发明授权
    Piperidino-propanols 失效
    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。

    4(2' Isoquinolin-1-one)piperidines
    3.
    发明授权
    4(2' Isoquinolin-1-one)piperidines 失效
    4（2 {40 {0-异喹啉-1-酮）哌啶

    公开(公告)号：US4029795A

    公开(公告)日：1977-06-14

    申请号：US595456

    申请日：1975-07-14

    申请人： Kurt Eichenberger ,  Christian Egli ,  Hans Kuhnis ,  Oswald Schier

    发明人： Kurt Eichenberger ,  Christian Egli ,  Hans Kuhnis ,  Oswald Schier

    IPC分类号： C07D213/74 ,  A61K31/47 ,  C07D217/00

    CPC分类号： C07D213/74 ,  Y10S514/821

    摘要： 1-(3-Aryloxy-2-hydroxypropyl)-4-(1-oxoisoquinolino)-piperidines, e.g. those of the formula ##STR1## R' = H, alkanoylaminoethenyl, carbamoyl, alkanoyl, CN, alkoxycarbonylamino-lower alkyl, halo, OH, alkanoylamino, alkyl, alkoxy, alkenyl, alkenyloxyR" = H, alkyl, alkoxy, alkenyl, alkenyloxy,R'" = alkanoylamino, NH.sub.2, NO.sub.2, alkyl, alkoxy, halo CF.sub.3, OH2-alkanoic acid esters and acid addition salts thereof are antihypertensive and antiarrhythmic agents.

    摘要翻译： 1-（3-芳氧基-2-羟丙基）-4-（1-氧代异喹啉） - 哌啶，例如 R'= H，烷酰基氨基乙烯基，氨基甲酰基，烷酰基，CN，烷氧基羰基氨基 - 低级烷基，卤素，OH，烷酰基氨基，烷基，烷氧基，烯基，链烯氧基，R“= H，烷基 ，烷氧基，烯基，烯氧基，R，烷酰氨基，NH 2，NO 2，烷基，烷氧基，卤代CF 3，OH 2 - 链烷酸酯及其酸加成盐是抗高血压药和抗心律失常剂。

    Antihypertensive compositions
    6.
    发明授权
    Antihypertensive compositions 失效
    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。

    3,5-diacyl-2,6-dialkyl-4-aryl-1,4-dihydropyridines, their use, and pharmaceutical compositions thereof
    7.
    发明授权
    3,5-diacyl-2,6-dialkyl-4-aryl-1,4-dihydropyridines, their use, and pharmaceutical compositions thereof 失效
    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。

    Dihydro pyridine compounds, compositions and use
    8.
    发明授权
    Dihydro pyridine compounds, compositions and use 失效
    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。

    Certain 1,4-dihydro-3-sulfinyl or sulfonyl-pyridines
    9.
    发明授权
    Certain 1,4-dihydro-3-sulfinyl or sulfonyl-pyridines 失效
    某些1,4-二氢-3-亚磺酰基或磺酰基吡啶

    公开(公告)号：US4017629A

    公开(公告)日：1977-04-12

    申请号：US581523

    申请日：1975-05-28

    申请人： Ernst Habicht ,  Hans Kuhnis

    发明人： Ernst Habicht ,  Hans Kuhnis

    IPC分类号： A61K31/455 ,  A61P9/08 ,  A61P9/12 ,  C07D211/02 ,  C07D211/84 ,  C07D211/90 ,  C07D211/86

    CPC分类号： C07D211/84 ,  C07D211/02 ,  C07D211/90

    摘要： The present invention relates to 1,4-dihydropyridines of the formula I ##STR1## and their tautomers, wherein R.sub.1 represents an aryl radical, R.sub.2 and R.sub.3 independently of one another represents hydrogen or a hydrocarbon radical, R.sub.4 represents an alkyl, aryl or aralkyl radical, R.sub.5 denotes an alkoxy radical, which is optionally substituted by an amino group, or denotes an amino group and n is 1 or 2, especially to the 2,6-dimethyl-3-carbomethoxy-5-methylsulphonyl-4-(2-trifluoromethylphenyl)-1,4-dihydro-pyridine and to the 2,6-dimethyl-3-carbomethoxy-5-methylsulphonyl-4-(2-nitrophenyl)-1,4-dihydropyridine.They have an antihypertensive activity.

    摘要翻译： 本发明涉及式I（I）的1,4-二氢吡啶及其互变异构体，其中R 1表示芳基，R 2和R 3彼此独立地表示氢或烃基，R 4表示烷基， 芳基或芳烷基，R5表示烷氧基，其任选被氨基取代，或表示氨基，n为1或2，特别是2,6-二甲基-3-甲酯基-5-甲基磺酰基-4 - （2-三氟甲基苯基）-1,4-二氢 - 吡啶和2,6-二甲基-3-甲酯基-5-甲基磺酰基-4-（2-硝基苯基）-1,4-二氢吡啶。

    N-Oxide compounds useful in the treatment of cardiovascular ailments
    10.
    发明授权
    N-Oxide compounds useful in the treatment of cardiovascular ailments 失效
    可用于治疗心血管疾病的N-氧化物化合物

    公开(公告)号：US4497808A

    公开(公告)日：1985-02-05

    申请号：US453393

    申请日：1982-12-27

    申请人： Markus Zimmermann ,  Hans Kuhnis

    发明人： Markus Zimmermann ,  Hans Kuhnis

    IPC分类号： A61K31/445 ,  C07D213/89 ,  C07D401/04 ,  C07D491/04 ,  C07D491/048 ,  A61K31/44

    CPC分类号： C07D213/89 ,  C07D401/04 ,  C07D491/04

    摘要： The present invention relates to novel N-oxide compounds that have cardiovascular properties, especially antihypertensive activity, and that correspond to the formula ##STR1## in which Py represents an unsubstituted or substituted N-oxidopyridyl radical, R.sub.1 represents hydrogen or unsubstituted or substituted lower alkyl, one of the radicals R.sub.2 and R.sub.3 represents lower alkyl and the other represents hydrogen; lower alkyl; lower alkyl containing free, etherified or esterified hydroxy, oxo, functionally modified carboxy or free or substituted amino or imino; functionally modified carboxy; or free or substituted amino, it being possible for an amino group R.sub.2 or R.sub.3 to be bonded to a lower alkyl radical R.sub.1 or, if R.sub.2 or R.sub.3 represents, for example, hydroxy-lower alkyl, for this hydroxy-lower alkyl, together with the adjacent acyl radical Ac.sub.1 or Ac.sub.2, to form a 2-oxa-1-oxo-lower alkylene radical, the carbonyl group of which is bonded to the 3- or 5-ring carbon atom of the 1,4-dihydropyridine ring, and each of the groups Ac.sub.1 and Ac.sub.2 represents, independently of the other, the acyl radical of an acid, and salts of compounds of the formula I having salt-forming groups, processes for the manufacture of these compounds, the use of these compounds and their salts, and pharmaceutical preparations which contain these compounds and salts, as antihypertensive agents and coronary dilators for the treatment of cardiovascular conditions, such as hypertonia, vascular constrictions, Angina pectoris and cardiac insufficiency.

    摘要翻译： 本发明涉及具有心血管特性，特别是抗高血压活性的新型N-氧化物化合物，其对应于其中Py表示未取代或取代的N-氧化吡啶基的式（I），R 1表示氢或未取代的或未取代的 取代的低级烷基，基团R2和R3之一表示低级烷基，另一个表示氢; 低级烷基 含有游离的醚化或酯化的羟基，氧代，官能改性的羧基或游离或取代的氨基或亚氨基的低级烷基; 官能改性羧基; 或游离或取代的氨基，氨基R2或R3可以与低级烷基R1键合，或者如果R2或R3表示例如羟基 - 低级烷基，对于该羟基 - 低级烷基，连同 相邻的酰基Ac1或Ac2形成2-氧杂-1-氧代 - 低级亚烷基，其羰基与1,4-二氢吡啶环的3-或5-环碳原子键合，以及 Ac1和Ac2各自独立地表示酸的酰基，以及具有成盐基团的式I化合物的盐，这些化合物的制备方法，这些化合物的用途及其制备方法 盐，以及含有这些化合物和盐的药物制剂作为抗高血压剂和用于治疗心血管疾病如高血压，血管收缩，心绞痛和心功能不全的冠状动脉扩张剂。