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1. 发明授权

US4649196A Process for the manufacture of racemic (R,R; S,S) asocainol 失效
标题翻译：用于制备外消旋（R，R; S，S）asocainol的方法
公开(公告)号：US4649196A
公开(公告)日：1987-03-10
申请号：US730124
申请日：1985-05-03
申请人： Wolfgang Herrmann , Gerhard Satzinger
发明人： Wolfgang Herrmann , Gerhard Satzinger
IPC分类号： A61K31/395 , A61P9/06 , C07D225/08
CPC分类号： C07D225/08
摘要： A process for the preparation of racemic asocainol in the (R,R; S,S)-form and (-)-asocainol in the (S,S)-form as well as the pharmacologically compatible salts thereof is herein described on the basis of a thermal rearrangement of the inactive (R,S)-diastereomer to the (S,S)-form.Racemic (.+-.)-asocainol and the (-)-enantiomer are potent antiarrhythmic agents and local anesthetics.
摘要翻译：在（S，S）形式的（R，R; S，S）形式和（ - ） - 焦氨醇中制备外消旋asocainol以及其药理学上相容的盐的方法在此基于的非活性（R，S） - 非对映体与（S，S） - 形式的热重排。外消旋（+/-） - asocainol和（ - ） - 对映异构体是有效的抗心律失常药和局部麻醉药。

2. 发明授权

US5137918A N-(2'-aminophenyl)-benzamide derivatives process for the preparation thereof and pharmaceutical compositions containing them 失效
标题翻译： N-（2'-氨基苯基） - 苯甲酰胺衍生物的制备方法和含有它们的药物组合物
公开(公告)号：US5137918A
公开(公告)日：1992-08-11
申请号：US594592
申请日：1990-10-09
申请人： Ute Weiershausen , Gerhard Satzinger , Karl-Otto Vollmer , Wolfgang Herrmann
发明人： Ute Weiershausen , Gerhard Satzinger , Karl-Otto Vollmer , Wolfgang Herrmann
IPC分类号： C07C231/02 , A61K31/165 , A61P35/00 , A61P35/02 , C07C20060101 , C07C67/00 , C07C231/00 , C07C231/12 , C07C233/01 , C07C233/78 , C07C233/80 , C07C233/81 , C07C233/90 , C07C235/56 , C07C237/42
CPC分类号： C07C237/42 , Y02P20/55
摘要： The present invention provides substituted N-(2'-aminophenyl)-benzamide derivatives useful for combating neoplastic diseases. The present invention also provides a process for the preparation of these benzamide derivatives, as well as pharmaceutical compositions containing them and methods for using them.
摘要翻译：本发明提供了用于对抗肿瘤性疾病的取代的N-（2'-氨基苯基） - 苯甲酰胺衍生物。本发明还提供了制备这些苯甲酰胺衍生物的方法，以及含有它们的药物组合物以及使用它们的方法。

3. 发明授权

US4477661A Process for the preparation of 4-hydroxy-3-(heterocyclocarbamoyl)-2H-1,2-benzothiazine-1,1-dioxides 失效
标题翻译：制备4-羟基-3-（杂环氨基甲酰基）-2H-1,2-苯并噻嗪-1,1-二氧化物的方法
公开(公告)号：US4477661A
公开(公告)日：1984-10-16
申请号：US478763
申请日：1983-03-25
申请人： Wolfgang Herrmann , Wolfram Geibel , Gerhard Satzinger
发明人： Wolfgang Herrmann , Wolfram Geibel , Gerhard Satzinger
IPC分类号： C07D417/12 , C07D401/12
CPC分类号： C07D417/12
摘要： The present invention provides a process for the preparation of 4-hydroxy-3-(heterocyclocarbamoyl)-2H-1,2-benzothiazine-1,1-dioxides of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a methyl radical, R.sub.2 is a nitrogen-containing heterocyclic radical and R.sub.3 is a hydrogen or halogen atom or a methyl radical, and of the alkali metal, alkaline earth metal and amine salts thereof, by the reaction of an amine-substituted, nitrogen-containing heterocyclic compound with a halo-acetyl halide, reaction of the intermediate thus obtained with sodium benzoic acid sulphimide, ring expansion of the benzoisothiazole ring to give a benzothiazine ring and, in case R.sub.2 is to be an isoxazolyl radical, reverse rearrangement of the oxadiazole-ring formed by ring expansion to the isoxazolyl ring, wherein (in a one-pot reaction A) the reaction of an amine-substituted, nitrogen-containing heterocyclic compound with a halo-acetyl halide is carried out, without the addition of a base, in boiling ethyl acetate, the intermediate formed is, without isolation, reacted with sodium benzoic acid sulphimide and the reaction product isolated, whereafter, in a one-pot reaction B, the reaction product from the one-pot reaction A is reacted in a dipolar aprotonic solvent under an atmosphere of a protection gas with a strongly basic alkali-alkohole and thereafter with so much acid that about 2 equivalents of base remained unneutralized in the reaction solution and, if desired, the benzothiazine ring is N-methylated in the usual manner and the product obtained is, if desired, converted in known manner into an alkali metal, alkaline earth metal or amine salt.
摘要翻译：本发明提供了制备下列通式的4-羟基-3-（杂环氨基甲酰基）-2H-1,2-苯并噻嗪-1,1-二氧化物的方法：其中R 1是氢原子或甲基自由基，R2是含氮杂环基，R3是氢或卤素原子或甲基，以及其碱金属，碱土金属和胺盐，通过胺取代的含氮杂环与卤代 - 乙酰卤的化合物，由此获得的中间体与苯甲酸亚磺酰亚胺的反应，苯并异噻唑环的环扩展得到苯并噻嗪环，并且在R2为异恶唑基的情况下，恶二唑环的反向重排通过环扩展形成异恶唑环，其中（在一锅反应A）中，胺取代的含氮杂环化合物与卤代 - 乙酰卤的反应在不加碱的情况下进行沸腾等乙酸乙酯，形成的中间体不经分离，与苯甲酸亚磺酰亚胺反应，分离出反应产物，然后在一锅反应B中，来自一锅反应A的反应产物在偶极非质子溶剂在具有强碱性碱性碱性气体的保护气体的气氛下，然后用如此多的酸使约2当量的碱在反应溶液中保持未中和，如果需要，苯并噻嗪环以常规方式进行N-甲基化，并且如果需要，获得的产物以已知的方式转化为碱金属，碱土金属或胺盐。

4. 发明授权

US4255433A (+)-(3-Methyl-4-oxo-5N-piperidinothiazolidin-2-ylidene)acetic acid esters, method of preparation and use 失效
标题翻译：（+） - （3-甲基-4-氧代-5N-哌啶子基异噻唑烷-2-亚基）乙酸酯，制备和使用方法
公开(公告)号：US4255433A
公开(公告)日：1981-03-10
申请号：US132577
申请日：1980-03-21
申请人： Wolfgang Herrmann , Gerhard Satzinger , Manfred Herrmann , Wolfgang Steinbrecher , Heinrich Bahrmann
发明人： Wolfgang Herrmann , Gerhard Satzinger , Manfred Herrmann , Wolfgang Steinbrecher , Heinrich Bahrmann
IPC分类号： C07D417/04 , A61K31/4453 , A61K31/4523 , A61P9/12 , C07D277/42 , A61K31/445
CPC分类号： C07D277/42
摘要： The invention discloses (+)-(3-methyl-4-oxo-5N-piperidinothiazolidin-2-ylidene)acetic acid esters and a process for their preparation. The process provides the dextrorotatory isomers substantially free from the corresponding levorotatory isomers. Antihypertensive pharmaceutical compositions comprising the dextrorotatory esters and methods for using said compositions are also disclosed.
摘要翻译：本发明公开了（+） - （3-甲基-4-氧代-5N-哌啶子基异噻唑烷-2-亚基）乙酸酯及其制备方法。该方法提供基本上不含相应左旋异构体的右旋异构体。还公开了包含右旋酯的抗高血压药物组合物和使用所述组合物的方法。

5. 发明授权

US4208526A Process for the preparation of thiazolidin-4-one-acetic acid derivatives 失效
标题翻译：噻唑烷-4-酮乙酸衍生物的制备方法
公开(公告)号：US4208526A
公开(公告)日：1980-06-17
申请号：US004797
申请日：1979-01-19
申请人： Wolfgang Herrmann , Gerhard Satzinger
发明人： Wolfgang Herrmann , Gerhard Satzinger
IPC分类号： C07D277/20 , A61K31/427 , A61K31/4453 , A61K31/4523 , A61P1/16 , A61P7/10 , C07D277/34 , C07D277/54 , C07D417/04
CPC分类号： C07D277/34 , C07D277/54
摘要： A new and chemically unique one-pot process for the preparation of thiazolidin-4-one-acetic acid derivatives of the general formula: ##STR1## wherein R.sub.1 is a lower alkyl radical.
摘要翻译：用于制备通式如下的噻唑烷-4-酮 - 乙酸衍生物的新的和化学上独特的一锅法：其中R1是低级烷基。

6. 发明授权

US4933368A N-phenylbenzamide derivatives 失效
标题翻译： N-苯基苯甲酰胺衍生物
公开(公告)号：US4933368A
公开(公告)日：1990-06-12
申请号：US359189
申请日：1989-05-31
申请人： Gerhard Satzinger , Manfred Herrmann , Edgar Fritschi , Ute Weiershausen
发明人： Gerhard Satzinger , Manfred Herrmann , Edgar Fritschi , Ute Weiershausen
IPC分类号： A61K31/165 , A61K20060101 , A61P31/12 , A61P35/00 , A61P37/06 , C07C20060101 , C07C231/00 , C07C231/02 , C07C233/65 , C07C237/40 , C07K1/113 , C07K5/08
CPC分类号： C07C237/40 , A61K31/165 , C07C231/02 , C07C231/12 , Y10S514/885
摘要： N-phenylbenzamide derivatives of the general formula I ##STR1## wherein the radicals R.sup.1, R.sup.2, and R.sup.3, which can be the same or different, are a hydrogen atom or a methyl radical, as well as the pharmacologically acceptable salts thereof for controlling refractory tumors in mammals are described.

7. 发明授权

US4857662A N-phenylbenzamide derivatives 失效
公开(公告)号：US4857662A
公开(公告)日：1989-08-15
申请号：US578466
申请日：1984-02-09
申请人： Gerhard Satzinger , Manfred Hermann , Edgar Fritschi , Ute Weiershausen
发明人： Gerhard Satzinger , Manfred Hermann , Edgar Fritschi , Ute Weiershausen
IPC分类号： A61K31/165 , A61K20060101 , A61P31/12 , A61P35/00 , A61P37/06 , C07C20060101 , C07C231/00 , C07C231/02 , C07C233/65 , C07C237/40 , C07K1/113 , C07K5/08
CPC分类号： C07C237/40 , A61K31/165 , C07C231/02 , C07C231/12 , Y10S514/885
摘要： N-phenylbenzamide derivatives of the general formula I ##STR1## wherein the radicals R.sup.1, R.sup.2, and R.sup.3, which can be the same or different, are a hydrogen atom or a methyl radical, as well as the pharmacologically acceptable salts thereof for controlling malignant, proliferative and auto-immune diseases and for immunosuppressive therapy upon grafting are described.

8. 发明授权

US4698341A Use of 1,6-naphthyridinone derivatives in treating pulmonary thrombosis 失效
标题翻译：使用1,6-萘啶酮衍生物治疗肺血栓形成
公开(公告)号：US4698341A
公开(公告)日：1987-10-06
申请号：US753758
申请日：1985-07-11
申请人： Gerhard Satzinger , Johannes Hartenstein , Karl Mannhardt , Jurgen Kleinschroth , Manfred Herrmann , Edgar Fritschi , Horst-Dietmar Tauschel , Bernd Wagner , Gunter Wolf
发明人： Gerhard Satzinger , Johannes Hartenstein , Karl Mannhardt , Jurgen Kleinschroth , Manfred Herrmann , Edgar Fritschi , Horst-Dietmar Tauschel , Bernd Wagner , Gunter Wolf
IPC分类号： C07D211/90 , C07D471/04 , A61K31/455 , A61K31/535
CPC分类号： C07D471/04 , C07D211/90
摘要： New 1,6-naphthyridinone derivatives of the formula I ##STR1## are herein described wherein R.sup.1 represents an unsubstituted or substituted aromatic or heteroaromatic ring;R.sup.2 is hydrogen, a straight-chained or branched alkyl, alkoxyalkyl, or a substituted or unsubstituted aminoalkyl group with up to ten carbon atoms;R.sup.3 is hydrogen, a straight-chained or branched alkyl group, or an alkoxycarbonyl radical with up to four carbon atoms;R.sup.4 is hydrogen, or a morpholinoethyl group;R.sup.5 is a straight-chained or branched alkyl group with up to four carbon atoms, or an amino group; andR.sup.6 is a carboxyl group, or an alkyl- or alkyloxyalkyl carbonyl radical, containing up to 12 carbon atoms and optionally interrupted by an oxygen, sulphur, or nitrogen atom;as well as optionally the pharmacologically acceptable salts thereof; processes for the preparation of these derivatives and their use in the control of vascular diseases.
摘要翻译：本文描述了式I（I）的新的1,6-萘啶酮衍生物，其中R 1表示未取代或取代的芳族或杂芳族环; R2是氢，直链或支链烷基，烷氧基烷基或具有至多10个碳原子的取代或未取代的氨基烷基; R3是氢，直链或支链烷基或具有至多四个碳原子的烷氧基羰基; R4是氢或吗啉代乙基; R5是具有至多4个碳原子的直链或支链烷基或氨基; 并且R 6是含有至多12个碳原子并任选被氧，硫或氮原子中断的羧基或烷基 - 或烷氧基烷基羰基; 以及任选地其药理学上可接受的盐; 这些衍生物的制备方法及其在血管疾病控制中的应用。

9. 发明授权

US4587263A Cycloaliphatic aminosulfonic acid derivatives 失效
标题翻译：环脂族氨基磺酸衍生物
公开(公告)号：US4587263A
公开(公告)日：1986-05-06
申请号：US634839
申请日：1984-07-26
申请人： Gerhard Satzinger , Johannes Hartenstein , Edgar Fritschi , Wolf-Dieter Vigelius
发明人： Gerhard Satzinger , Johannes Hartenstein , Edgar Fritschi , Wolf-Dieter Vigelius
IPC分类号： A61K31/185 , A61P9/06 , A61P9/12 , C07C67/00 , C07C301/00 , C07C303/02 , C07C303/24 , C07C309/19 , C07C143/21
CPC分类号： C07C309/19 , C07C2101/08 , C07C2101/14 , C07C2101/18
摘要： New aminosulfonic acids of the general formula I ##STR1## wherein n represents the figures 4, 5, or 6, prepared according to previously known processes and characterized by very good tolerance and valuable cardiovascular properties, serve for the therapy of dysrhythmia and are superior to procaine.
摘要翻译：通式I的新的氨基磺酸（I）其中n代表按照先前已知的方法制备并以非常好的耐受性和有价值的心血管特性为特征的图4,5或6，用于治疗心律失常和优于普鲁卡因。

10. 发明授权

US4152326A Cyclic sulphonyloxyimides 失效
标题翻译：循环磺酰亚胺
公开(公告)号：US4152326A
公开(公告)日：1979-05-01
申请号：US775336
申请日：1977-03-07
申请人： Johannes Hartenstein , Gerhard Satzinger
发明人： Johannes Hartenstein , Gerhard Satzinger
IPC分类号： C07D209/54 , C07D221/20 , C07D211/94
CPC分类号： C07D221/20 , C07D209/54
摘要： The present invention is concerned with new cyclic sulphonyloxyimides and their preparation.

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