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1. 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。

2. 发明授权

US4727067A Derivatives of 3-aminopropane-1,2-diol 失效
标题翻译： 3-氨基丙烷-1,2-二醇的衍生物
公开(公告)号：US4727067A
公开(公告)日：1988-02-23
申请号：US785300
申请日：1985-10-07
申请人： Franz Ostermayer , Markus Zimmermann
发明人： Franz Ostermayer , Markus Zimmermann
IPC分类号： C07D209/32 , A61K31/165 , A61K31/60 , A61P9/06 , A61P9/12 , A61P25/02 , C07C67/00 , C07C229/38 , C07C231/00 , C07C231/06 , C07C231/12 , C07C231/14 , C07C233/00 , C07C233/12 , C07C235/46 , C07C237/30 , C07C253/00 , C07C255/54 , C07C313/00 , C07C323/18 , C07C323/20 , C07D207/32 , C07D207/325 , C07D207/333 , C07D209/08 , C07D213/64 , C07D215/22 , C07D215/227 , C07D235/26 , C07D265/22 , C07D285/08 , C07D295/192 , C07D303/22 , C07D303/26 , C07D409/10 , C07C103/26
CPC分类号： C07D207/325 , C07C229/38 , C07C265/12 , C07D209/08 , C07D213/64 , C07D215/227 , C07D235/26 , C07D265/22 , C07D285/08 , C07D295/192 , C07D303/22 , C07D303/26 , B65D2571/00018
摘要： Derivatives of 3-aminopropane-1,2-diol of the formula ##STR1## in which Ar represents optionally substituted aryl,n represents the number 0 or 1, andalk represents alkylene having 2 to 5 carbon atoms, the nitrogen atom and the oxygen atom, or, if n is zero, the phenyl radical, being separated from one another by at least two carbon atoms, andR.sub.1 and R.sub.2, independently of one another, each represents hydrogen or lower alkyl, or together they represent lower alkylene, oxa-lower alkylene, thia-lower alkylene, aza-lower alkylene or N-lower alkyl-aza-lower alkylene,and salts of such compounds, processes for their manufacture, medicaments containing the new compounds and their use for the treatment of Angina pectoris and cardiac arrhythmia, and as blood pressure-reducing agents, as well as for the treatment of reactive or endogenic states of depression.
摘要翻译：式（I）的3-氨基丙烷-1,2-二醇的衍生物，其中Ar表示任选取代的芳基，-n表示数字0或1，并且-a表示具有2至5个碳原子的亚烷基，氮原子或氧原子，或者如果_n为零，苯基通过至少两个碳原子彼此分开，并且R 1和R 2彼此独立地表示氢或低级烷基，或一起表示低级烷基亚烷基，氧杂低级亚烷基，硫杂低级亚烷基，氮杂低级亚烷基或N-低级烷基 - 氮杂 - 低级亚烷基，以及这些化合物的盐，其制备方法，含有新化合物的药物及其用于治疗心绞痛和心律失常以及作为减压剂，以及用于治疗抑郁症的反应性或内源性状态。

3. 发明授权

US4497813A Derivatives of 3-aminopropane-1,2-diol 失效
标题翻译： 3-氨基丙烷-1,2-二醇的衍生物
公开(公告)号：US4497813A
公开(公告)日：1985-02-05
申请号：US378165
申请日：1982-05-14
申请人： Franz Ostermayer , Markus Zimmermann
发明人： Franz Ostermayer , Markus Zimmermann
IPC分类号： C07D209/32 , A61K31/165 , A61K31/60 , A61P9/06 , A61P9/12 , A61P25/02 , C07C67/00 , C07C229/38 , C07C231/00 , C07C231/06 , C07C231/12 , C07C231/14 , C07C233/00 , C07C233/12 , C07C235/46 , C07C237/30 , C07C253/00 , C07C255/54 , C07C313/00 , C07C323/18 , C07C323/20 , C07D207/32 , C07D207/325 , C07D207/333 , C07D209/08 , C07D213/64 , C07D215/22 , C07D215/227 , C07D235/26 , C07D265/22 , C07D285/08 , C07D295/192 , C07D303/22 , C07D303/26 , C07D409/10 , C07C103/26 , A61K31/605
CPC分类号： C07D207/325 , C07C229/38 , C07C265/12 , C07D209/08 , C07D213/64 , C07D215/227 , C07D235/26 , C07D265/22 , C07D285/08 , C07D295/192 , C07D303/22 , C07D303/26 , B65D2571/00018
摘要： Derivatives of 3-aminopropane-1,2-diol of the formula ##STR1## in which Ar represents optionally substituted aryl,n represents the number 0 or 1, andalk represents alkylene having 2 to 5 carbon atoms, the nitrogen atom and the oxygen atom, or, if n is zero, the phenyl radical, being separated from one another by at least two carbon atoms, andR.sub.1 and R.sub.2, independently of one another, each represents hydrogen or lower alkyl, or together they represent lower alkylene, oxa-lower alkylene, thia-lower alkylene, aza-lower alkylene or N-lower alkyl-aza-lower alkylene,and salts of such compounds, processes for their manufacture, medicaments containing the new compounds and their use for the treatment of Angina pectoris and cardiac arrhythmia, and as blood pressure-reducing agents, as well as for the treatment of reactive or endogenic states of depression.
摘要翻译：式（I）的3-氨基丙烷-1,2-二醇的衍生物，其中Ar表示任选取代的芳基，n表示数字0或1，alk表示具有2至5个碳原子的亚烷基，氮原子和氧原子，或者如果n为0，苯基通过至少两个碳原子彼此分开，并且R 1和R 2彼此独立地表示氢或低级烷基，或者它们一起表示低级烷基亚烷基，氧杂低级亚烷基，硫杂低级亚烷基，氮杂低级亚烷基或N-低级烷基 - 氮杂 - 低级亚烷基，以及这些化合物的盐，其制备方法，含有新化合物的药物及其用于治疗心绞痛和心律失常以及作为减压剂，以及用于治疗抑郁症的反应性或内源性状态。

4. 发明授权

US4460580A N-Alkylated aminoalcohols and their pharmaceutical compositions useful for the treatment of cardiac insufficiency 失效
标题翻译： N-烷基化氨基醇及其用于治疗心功能不全的药物组合物
公开(公告)号：US4460580A
公开(公告)日：1984-07-17
申请号：US391814
申请日：1982-06-24
申请人： Franz Ostermayer , Markus Zimmermann
发明人： Franz Ostermayer , Markus Zimmermann
IPC分类号： A61K31/165 , A61P9/04 , A61P25/02 , C07C67/00 , C07C229/38 , C07C231/00 , C07C231/12 , C07C231/14 , C07C235/46 , C07C237/30 , C07D213/38 , C07D265/22 , C07D307/52 , C07D333/20 , C07D213/56 , A61K31/44
CPC分类号： C07D265/22 , C07C229/38 , C07D213/38 , C07D307/52 , C07D333/20
摘要： The invention relates to novel N-alkylated aminoalcohols of the formula ##STR1## in which Ar is a radical of aromatic character which is unsubstituted or substituted by hydroxyl, n has the values nought or 1 and Alk is an alkylene radical having 2 to 5 carbon atoms and the nitrogen atom and the oxygen atom or, if n is nought, the salicylamide radical are separated from one another by at least two carbon atoms in the straight-chain, and their salts. The main action of the novel compounds consists in a stimulation of cardiac .beta.-receptors; the compounds also effect a blockage of adrenergic .alpha.-receptors and a lowering in the blood pressure. They can therefore be used as .beta.-stimulators, especially as agents having a positively inotropic action for the treatment of cardiac insufficiency. Compounds of the formula I in which Ar is phenyl, unsubstituted or substituted by 1 or 2 hydroxyl groups, Alk is an alkylene radical having 2 to 4 carbon atoms, n has the value 1, and the nitrogen atom and the oxygen atom are separated from one another by at least 2 carbon atoms in the straight-chain, or salts thereof, exhibit effects on the central nervous system, which are reflected for example in the suppression of the symptoms of impaired sympathetic functions and in the suppression of lack of initiative. Such compounds of the formula I therefore can be used for the treatment of reactive or endogenic states of depression of varying degrees of severity, and also for the treatment of neurotic or other psychic disturbances involving loss of initiative and depressive disorders. Such compounds can also be used for the short-term treatment of post-partum or postoperative depression, or of depression of different origin. Such compounds of the formula I can be used on their own or in combination with other antidepressants.
摘要翻译：本发明涉及式（I）的新型N-烷基化氨基醇，其中Ar是未被取代或被羟基取代的芳族基团，n的值不为1，Alk为具有2个的亚烷基至5个碳原子和氮原子和氧原子，或者如果n无效，则水杨酰胺基团通过直链中的至少两个碳原子和它们的盐彼此分离。新化合物的主要作用在于刺激心脏β受体; 该化合物还会影响肾上腺素α受体的阻断和降低血压。因此，它们可以用作β-刺激剂，特别是作为具有正性肌力作用的药物用于治疗心功能不全。其中Ar为未取代或被1或2个羟基取代的苯基的式I化合物，Alk为碳原子数2〜4的亚烷基，n为1，氮原子和氧原子与直链中至少有2个碳原子或其盐，彼此之间呈现对中枢神经系统的作用，例如反映在抑制交感神经功能受损症状和抑制缺乏主动性的作用。因此，式I的这种化合物可用于治疗不同程度的严重程度的抑郁症的反应性或内源性状态，并且还可用于治疗涉及主动性和抑郁障碍丧失的神经质或其他心理障碍。这些化合物也可用于短期治疗产后或术后抑郁症或不同来源的抑郁症。式I化合物可以单独使用或与其它抗抑郁药组合使用。

5. 发明授权

US4636511A Derivatives of 3-aminopropane-1,2-diol 失效
标题翻译： 3-氨基丙烷-1,2-二醇的衍生物
公开(公告)号：US4636511A
公开(公告)日：1987-01-13
申请号：US687093
申请日：1984-12-28
申请人： Franz Ostermayer , Markus Zimmermann
发明人： Franz Ostermayer , Markus Zimmermann
IPC分类号： C07D209/32 , A61K31/165 , A61K31/60 , A61P9/06 , A61P9/12 , A61P25/02 , C07C67/00 , C07C229/38 , C07C231/00 , C07C231/06 , C07C231/12 , C07C231/14 , C07C233/00 , C07C233/12 , C07C235/46 , C07C237/30 , C07C253/00 , C07C255/54 , C07C313/00 , C07C323/18 , C07C323/20 , C07D207/32 , C07D207/325 , C07D207/333 , C07D209/08 , C07D213/64 , C07D215/22 , C07D215/227 , C07D235/26 , C07D265/22 , C07D285/08 , C07D295/192 , C07D303/22 , C07D303/26 , C07D409/10 , C07C103/26 , A61K31/605
CPC分类号： C07D207/325 , C07C229/38 , C07C265/12 , C07D209/08 , C07D213/64 , C07D215/227 , C07D235/26 , C07D265/22 , C07D285/08 , C07D295/192 , C07D303/22 , C07D303/26 , B65D2571/00018
摘要： Derivatives of 3-aminopropan-1,2-diol of the formula ##STR1## in which Ar represents optionally substituted aryl,n represents the number 0 or 1, andalk represents alkylene having 2 to 5 carbon atoms, the nitrogen atom and the oxygen atom, or, if n is zero, the phenyl radical, being separated from one another by at least two carbon atoms, andR.sub.1 and R.sub.2, independently of one another, each represents hydrogen or lower alkyl, or together they represent lower alkylene, oxa-lower alkylene, thia-lower alkylene, aza-lower alkylene or N-lower alkyl-aza-lower alkylene,and salts of such compounds, processes for their manufacture, medicaments containing the new compounds and their use for the treatment of Angina pectoris and cardiac arrhythmia, and as blood pressure-reducing agents, as well as for the treatment of reactive or endogenic states of depression.
摘要翻译：式（I）的3-氨基丙-1,2-二醇的衍生物，其中Ar表示任选取代的芳基，n表示数字0或1，且-a表示具有2至5个碳原子的亚烷基，氮原子或氧原子，或者如果_n为零，苯基通过至少两个碳原子彼此分开，并且R 1和R 2彼此独立地表示氢或低级烷基，或一起表示低级烷基亚烷基，氧杂低级亚烷基，硫杂低级亚烷基，氮杂低级亚烷基或N-低级烷基 - 氮杂 - 低级亚烷基，以及这些化合物的盐，其制备方法，含有新化合物的药物及其用于治疗心绞痛和心律失常以及作为减压剂，以及用于治疗抑郁症的反应性或内源性状态。

6. 发明授权

US4559354A Certain antihypertensive 1-[2-[3-carbamoyl-4-hydroxy phenoxy]alkylene amino]-heterocyclic phenoxy-propanol derivatives 失效
标题翻译：某些抗高血压的1- [2- [3-氨基甲酰基-4-羟基苯氧基]亚烷基氨基] - 杂环苯氧基 - 丙醇衍生物
公开(公告)号：US4559354A
公开(公告)日：1985-12-17
申请号：US490211
申请日：1983-05-06
申请人： Walter Fuhrer , Franz Ostermayer , Markus Zimmermann
发明人： Walter Fuhrer , Franz Ostermayer , Markus Zimmermann
IPC分类号： A61K31/165 , A61K31/22 , A61P25/02 , C07C67/00 , C07C235/46 , C07C235/60 , C07C237/30 , C07C253/00 , C07C255/54 , C07C313/00 , C07C317/22 , C07C323/12 , C07C323/20 , C07D207/32 , C07D207/333 , C07D209/12 , C07D213/64 , C07D213/80 , C07D233/64 , C07D239/26 , C07D239/36 , C07D249/08 , C07D249/12 , C07D257/04 , C07D277/24 , C07D303/22 , C07D307/46 , C07D213/38 , A61K31/44 , C07D307/52 , C07D333/20
CPC分类号： C07D207/333 , C07D209/12 , C07D213/64 , C07D213/80 , C07D239/26 , C07D239/36 , C07D249/08 , C07D249/12 , C07D257/04 , C07D277/24 , C07D303/22 , C07D307/46
摘要： The invention relates to novel substituted phenyl ethers of the formula ##STR1## in which Ar represents a mono- or bi-cyclic carbocyclic aryl radical, or a mono- or bi-cyclic heterocyclic aryl radical bonded to a phenylene radical by way of a ring carbon atom,Ph represents a phenylene radical,n has the value 0 to 1 andalk represents alkylene having from 2 to 5 carbon atoms, the nitrogen atom and the oxygen atom or, if n is 0, the aromatic radical being separated from each other by at least two carbon atoms in the unbranched chain, andR.sub.1 and R.sub.2 each represents, independently of the other, hydrogen or lower alkyl, or together represent lower alkylene, oxa-lower alkylene, thia-lower alkylene, aza-lower alkylene or N-lower alkyl-aza-lower alkylene,and salts thereof, especially pharmaceutically acceptable non-toxic acid addition salts. Such compounds possess, on the one hand, blocking properties towards .beta.-adrenergic receptors and can therefore be used as .beta.-receptor-blockers with or without cardioselectivity for the treatment of Angina pectoris, hypertrophic cardiomyopathy and heart rhythm disorders and also as blood-pressure-reducing agents. On the other hand, such compounds possess .beta.-receptor-stimulating properties and can therefore be used as positively inotropically active agents, especially as cardiotonics, for the treatment of heart muscle insufficiency.
摘要翻译：本发明涉及式（I）的新的取代苯基醚，其中Ar表示单环或双环碳环芳基，或通过方式键合至亚苯基的单环或双环杂环芳基的环碳原子，Ph表示亚苯基，n的数值为0〜1，alk表示2〜5个碳原子的亚烷基，氮原子和氧原子，或者n为0时，芳香族基团分离在不分支链中彼此具有至少两个碳原子，R 1和R 2各自独立地表示氢或低级烷基，或一起代表低级亚烷基，氧杂低级亚烷基，硫杂低级亚烷基，低级氮原子亚烷基或N-低级烷基 - 氮杂 - 低级亚烷基及其盐，特别是药学上可接受的无毒酸加成盐。这样的化合物一方面具有阻止β-肾上腺素能受体的性质，因此可用作具有或不具有心脏选择性的β-受体阻滞剂用于治疗心绞痛，肥厚性心肌病和心律失常以及血压减免剂。另一方面，这些化合物具有β-受体刺激性能，因此可用作积极的换向活性剂，特别是作为强心剂，用于治疗心肌功能不全。

7. 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。

8. 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。

9. 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。

10. 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。

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