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1. 发明授权

US5399578A Acyl compounds 失效
标题翻译：酰基化合物
公开(公告)号：US5399578A
公开(公告)日：1995-03-21
申请号：US998755
申请日：1992-12-29
申请人： Peter Buhlmayer , Franz Ostermayer , Tibur Schmidlin
发明人： Peter Buhlmayer , Franz Ostermayer , Tibur Schmidlin
IPC分类号： A61K31/195 , A61K31/41 , A61K31/44 , A61K31/47 , A61K31/535 , A61K31/675 , A61P9/12 , C07C229/38 , C07C231/00 , C07C233/47 , C07C233/51 , C07C233/54 , C07C235/04 , C07C271/10 , C07C311/48 , C07D233/54 , C07D233/58 , C07D233/64 , C07D257/04 , C07D401/12 , C07D401/14 , C07D403/00 , C07D405/00 , C07D409/00 , C07F9/6524
CPC分类号： C07D233/64 , C07C229/38 , C07C233/54 , C07D257/04 , C07D401/12
摘要： Compounds of the formula ##STR1## in which R.sub.1 is an aliphatic hydrocarbon radical which is unsubstituted or substituted by halogen or hydroxyl, or a cycloaliphatic or araliphatic hydrocarbon radical; X.sub.1 is CO, SO.sub.2, or --O--C(.dbd.O)-- with the carbon atom of the carbonyl group being attached to the nitrogen atom shown in formula I; X.sub.2 is a divalent aliphatic hydrocarbon radical which is unsubstituted or substituted by hydroxyl, carboxyl, amino, guanidino or a cycloaliphatic or aromatic radical, or is a divalent cycloaliphatic hydrocarbon radical, it being possible for a carbon atom of the aliphatic hydrocarbon radical to be additionally bridged by a divalent aliphatic hydrocarbon radical; R.sub.2 is carboxyl which, if desired, is esterified or amidated, substituted or unsubstituted amino, formyl which, if desired, is acetalized, 1H-tetrazol-5-yl, pyridyl, hydroxyl which, if desired, is etherified, S(O).sub.m --R where m is 0, 1 or 2 and R is hydrogen or an aliphatic hydrocarbon radical, alkanoyl, unsubstituted or N-substituted sulfamoyl or PO.sub.n H.sub.2 where n is 2 or 3; X.sub.3 is a divalent aliphatic hydrocarbon; R.sub.3 is carboxyl, 5-tetrazolyl, SO.sub.3 H, PO.sub.2 H.sub.2, PO.sub.3 H.sub.2 or haloalkylsulfamoyl; and the rings A and B independently of one another are substituted or unsubstituted; in free form or in salt form, can be prepared in a manner known per se and can be used, for example, as medicament active ingredients.
摘要翻译：式（I）的化合物，其中R 1是未被取代或被卤素或羟基取代的脂族烃基，或脂环族或芳脂族烃基; X 1是CO，SO 2或-O-C（= O） - ，其中羰基的碳原子连接到式I所示的氮原子上; X2是未取代的或被羟基，羧基，氨基，胍基或脂环族或芳族基团取代的二价脂族烃基，或者是二价脂环族烃基，脂族烃基的碳原子可能另外由二价脂族烃基桥连; R 2是羧基，如果需要，其被酯化或酰胺化，取代或未取代的氨基，如果需要，缩醛化的甲酰基，1H-四唑-5-基，吡啶基，羟基，如果需要，其醚化，S（O） mR，其中m为0,1或2，R为氢或脂族烃基，烷酰基，未取代的或N-取代的氨磺酰基或POnH 2，其中n为2或3; X3是二价脂族烃; R3是羧基，5-四唑基，SO3H，PO2H2，PO3H2或卤代烷基氨磺酰; 环A和B彼此独立地是取代或未取代的; 游离形式或盐形式可以以本身已知的方式制备，并且可以用作例如药物活性成分。

2. 发明授权

US5369110A Biphenylyl compounds 失效
标题翻译：联苯基化合物
公开(公告)号：US5369110A
公开(公告)日：1994-11-29
申请号：US89393
申请日：1993-07-09
申请人： Tibur Schmidlin , Franz Ostermayer , Peter Buhlmayer
发明人： Tibur Schmidlin , Franz Ostermayer , Peter Buhlmayer
IPC分类号： A61K31/18 , A61K31/185 , A61K31/19 , A61K31/215 , A61K31/255 , A61K31/41 , A61K31/66 , A61P9/12 , A61P43/00 , C07C233/05 , C07C233/58 , C07C311/06 , C07D257/04
CPC分类号： C07D257/04
摘要： Biphenylyl compounds of formula ##STR1## wherein the variables R.sub.1, R.sub.2, R.sub.3, p, q and X and the rings A and B are as defined in claim 1, in free form or in salt form, can be prepared in a manner known per se and can be used, for example, as active ingredients in medicaments.
摘要翻译：其中变量R1，R2，R3，p，q和X以及环A和B如权利要求1中所定义的式（I）的联苯基化合物以游离形式或盐形式可以制备在本身已知的方法，可以用作例如药物中的活性成分。

3. 发明授权

US5965592A Acyl compounds 失效
标题翻译：酰基化合物
公开(公告)号：US5965592A
公开(公告)日：1999-10-12
申请号：US124520
申请日：1998-07-29
申请人： Peter Buhlmayer , Franz Ostermayer , Tibur Schmidlin
发明人： Peter Buhlmayer , Franz Ostermayer , Tibur Schmidlin
IPC分类号： A61K31/195 , A61K31/41 , A61K31/44 , A61K31/47 , A61K31/535 , A61K31/675 , A61P9/12 , C07C229/38 , C07C231/00 , C07C233/47 , C07C233/51 , C07C233/54 , C07C235/04 , C07C271/10 , C07C311/48 , C07D233/54 , C07D233/58 , C07D233/64 , C07D257/04 , C07D401/12 , C07D401/14 , C07D403/00 , C07D405/00 , C07D409/00 , C07F9/6524 , A61K31/235
CPC分类号： C07D233/64 , C07C229/38 , C07C233/54 , C07D257/04 , C07D401/12
摘要： Compounds of the formula ##STR1## and their salts, in which R.sub.1, is a C.sub.1 -C.sub.7 aliphatic hydrocarbon radical; X.sub.1 is --CO; X.sub.2 is a divalent aliphatic hydrocarbon radical which comprises an ethyl group and an alkylene of 2 to 6 carbon atoms; R.sub.2 is hydroxy, carboxy or alkoxycarbonyl in which alkoxy is from 1 to 7 carbon atoms; X.sub.3 is a divalent aliphatic hydrocarbon; R.sub.3 is carboxyl or 5-tetrazolyl; and the rings A and B independently of one another are otherwise unsubstituted; can be prepared in a known manner and may be used as active ingredients for medicaments.
摘要翻译：式中的化合物及其盐，其中R 1为C 1 -C 7脂族烃基; X1是-CO; X 2是包含乙基和2至6个碳原子的亚烷基的二价脂族烃基; R2是羟基，羧基或烷氧基羰基，其中烷氧基是1至7个碳原子; X3是二价脂族烃; R3是羧基或5-四唑基; 环A和B彼此独立地是未取代的; 可以以已知的方式制备并且可以用作药物的活性成分。

4. 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。

5. 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。

6. 发明授权

US3984436A Pyrrolyl compounds and processes for their manufacture 失效
标题翻译：吡咯基化合物及其制备方法
公开(公告)号：US3984436A
公开(公告)日：1976-10-05
申请号：US447118
申请日：1974-02-28
申请人： Knut A. Jaeggi , Franz Ostermayer , Herbert Schroter
发明人： Knut A. Jaeggi , Franz Ostermayer , Herbert Schroter
IPC分类号： C07D207/06 , A61K31/40 , A61P9/06 , A61P9/08 , A61P9/10 , A61P25/00 , A61P25/02 , C07D207/32 , C07D207/325
CPC分类号： C07D207/325 , Y10S514/821
摘要： Pyrrolyl compounds of the formula I ##EQU1## wherein Py is optionally lower-alkylated 1-pyrrolyl, Ph is phenylene, R.sub.1 is hydrogen or lower alkyl and R.sub.2 is hydrogen, lower alkyl, aryl-lower alkyl or optionally functionally modified carboxy-lower alkyl or R.sub.1 and R.sub.2 together are lower alkylene, oxa-lower alkylene, thia-lower alkylene or aza-lower alkylene, their antipodes and salts, which are valuable blockers of adrenergic .beta.-receptors.
摘要翻译：式I的吡咯基化合物R1 Py-Ph-O-CH2-CHOH-CH2-N（I）R2 R1 Py-Ph-O-CH2-CHOH-CH2-N（I）R2其中Py是任选低级 - 烷基化的1-吡咯基，Ph是亚苯基，R 1是氢或低级烷基，R 2是氢，低级烷基，芳基 - 低级烷基或任选的官能改性的羧基 - 低级烷基或R 1和R 2一起是低级亚烷基，氧杂低级亚烷基，硫杂 - 低级亚烷基或氮杂 - 低级亚烷基，它们的对映体和盐，它们是肾上腺素β受体的有价值的阻断剂。

7. 发明授权

US4818766A Novel phenoxyaliphatylphenyleneoxyalkyl esters and amides 失效
标题翻译：新型苯氧基亚芳基苯基氧基烷基酯和酰胺
公开(公告)号：US4818766A
公开(公告)日：1989-04-04
申请号：US75156
申请日：1987-07-20
申请人： Franz Ostermayer , Markus Zimmermann
发明人： Franz Ostermayer , Markus Zimmermann
IPC分类号： A61K31/44 , A61K31/4427 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , C07D211/90 , C07D401/12 , C07D413/12 , A61K31/455
CPC分类号： C07D211/90
摘要： The invention relates to novel 1,4-dihydropyridine-3-carboxylic acid phenoxyaliphatylphenyleneoxyalkyl esters of the formula ##STR1## in which Ac represents an acyl group, X represents oxy or optionally substituted imino, A represents a divalent aliphatic hydrocarbon radical interrupted by a group --X.sub.1 --Ph--X.sub.2 -- in which at least one of the radicals X.sub.1 and X.sub.2 represents oxy and a radical X.sub.1 or X.sub.2 that is other than oxy represents a direct bond, and Ph represents an optionally substituted phenylene radical, and R represents an optionally substituted phenyl, pyridyl or 1-oxidopyridyl, (1,3-dioxa)indanyl or benzofurazanyl radical, R.sub.1 represents an optionally substituted phenyl or indolyl radical, R.sub.2 represents an aliphatic hydrocarbon radical and R.sub.3 represents an aliphatic radical, cyano or amino, and acid addition salts thereof.
摘要翻译：本发明涉及式（Ⅰ）的新颖的1,4-二氢吡啶-3-羧酸苯氧基苯基苯基氧基烷基酯，其中Ac代表酰基，X代表氧基或任意取代的亚氨基，A代表二价脂族烃基中断基团-X1-Ph-X2-，其中基团X1和X2中的至少一个表示氧，并且除氧以外的基团X 1或X 2表示直接键，并且Ph表示任选取代的亚苯基，R 表示任选取代的苯基，吡啶基或1-氧化吡啶基，（1,3-二氧杂）茚满基或苯并呋喃基，R1表示任选取代的苯基或吲哚基，R 2表示脂族烃基，R 3表示脂族基，氰基或氨基，及其酸加成盐。

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

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。

10. 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。

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