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1. 发明授权

US4882342A 5-alkylbenzimidazoles, method of use and pharmaceutical compositions 失效
标题翻译： 5-烷基苯并咪唑，使用方法和药物组合物
公开(公告)号：US4882342A
公开(公告)日：1989-11-21
申请号：US106413
申请日：1987-10-06
申请人： Wolfgang von der Saal , Jens-Peter Holck , Alfred Mertens , Bernd Muller-Beckmann , Lothar Kling
发明人： Wolfgang von der Saal , Jens-Peter Holck , Alfred Mertens , Bernd Muller-Beckmann , Lothar Kling
IPC分类号： C07D235/14 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/454 , A61K31/47 , A61K31/496 , A61K31/505 , A61P7/02 , A61P9/04 , A61P9/12 , C07D235/08 , C07D235/18 , C07D235/26 , C07D235/28 , C07D235/30 , C07D401/04 , C07D401/06 , C07D403/04 , C07D405/04 , C07D409/04
CPC分类号： C07D401/04 , C07D235/08 , C07D235/18 , C07D401/06 , C07D403/04 , C07D405/04 , C07D409/04
摘要： The present invention concerns new 5-alkylbenzimidazoles of the formula: ##STR1## wherein R.sub.1 is a phenyl ring of the formula: ##STR2## or R.sub.1 is naphthyl, heterocycle or a bicyclic heterocycle and R.sub.1 -R.sub.7 are described in claim 1.These compounds are useful for prophylaxis or treatment of heart and circulatory disease especially to increase contractility of the heart, lower blood pressure and/or influence the thrombocyte function and improve the microcirculation.
摘要翻译：本发明涉及下式的新的5-烷基苯并咪唑：其中R 1是下式的苯环：（II）或R 1是萘基，杂环或双环杂环，并且R 1 -R 7被描述这些化合物可用于预防或治疗心脏和血液循环疾病，特别是增加心脏的收缩力，降低血压和/或影响血小板功能并改善微循环。

2. 发明授权

US4925845A 2 heteroaryl 3,3 dialkyl-5-(3 oxo-2,3,4,5 tetrahydro-6 pyridazinyl)-3H-indoles 失效
标题翻译： 2杂芳基3,3二烷基-5-（3氧代-2,3,4,5四氢-6哒嗪基）-3H-吲哚
公开(公告)号：US4925845A
公开(公告)日：1990-05-15
申请号：US159744
申请日：1988-02-24
申请人： Alfred Mertens , Wolfgang von der Saal , Lothar Kling , Bernd Muller-Beckmann
发明人： Alfred Mertens , Wolfgang von der Saal , Lothar Kling , Bernd Muller-Beckmann
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/50 , A61P9/04 , C07D401/14 , C07D403/04 , C07D409/14
CPC分类号： C07D401/14 , C07D403/04 , C07D409/14
摘要： Gem 3 dialkyl or spiro 4 aryl or heteroaryl 5 heterocyclic 3 H indoles and their pharmaceutically acceptable salts are prepared. They are useful for reducing blood pressure producing a positive inotropic action influencing thrombocyte aggregation and improving microcirculation. Hydrazinophenyl heterocyclic intermeidates are also disclosed.
摘要翻译：制备Gem 3二烷基或螺环4芳基或杂芳基5杂环3 H吲哚及其药学上可接受的盐。它们可用于降低血压，产生影响凝血细胞聚集并改善微循环的正性肌力作用。还公开了肼基苯基杂环的中间体。

3. 发明授权

US4851406A Heterocyclic-substituted indoles and pharmaceutical compositions containing them 失效
标题翻译：杂环取代的吲哚和含有它们的药物组合物
公开(公告)号：US4851406A
公开(公告)日：1989-07-25
申请号：US904092
申请日：1986-09-04
申请人： Alfred Mertens , Wolfgang von der Saal , Walter-Gunar Friebe , Bernd Muller-Beckmann , Gisbert Sponer
发明人： Alfred Mertens , Wolfgang von der Saal , Walter-Gunar Friebe , Bernd Muller-Beckmann , Gisbert Sponer
IPC分类号： C07D409/14 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/50 , A61K31/53 , A61K31/535 , A61P9/00 , C07D237/00 , C07D333/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/14 , C07D417/14
CPC分类号： C07D401/14
摘要： The present invention provides indole derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl, cycloalkyl, cycloalkenyl, carboxyl, cyano, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl or aryl radical, R.sub.2 is a hydrogen atom or an alkyl, trihalogenomethyl, hydroxyl, cycloalkyl, cyano, carboxyl, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl radical; R.sub.2 is a heterocyclic five-membered ring containing 1 to 4 heteroatoms or a heterocyclic six-membered ring containing 1 to 5 heteroatoms, the heteroatoms of the five- and six-membered rings being the same or different and being nitrogen, oxygen or sulphur and one or more of the nitrogen atoms optionally carrying an oxygen atom, the said five- and six-membered rings optionally being substituted by one or more alkyl, alkoxy, alkylthio, oxo, hydroxyl, nitro, amino, halogen or cyano groups; or R.sub.2 is ##STR2## the tautomers thereof and the physiologically acceptable salts thereof with inorganic and organic acids.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.Furthermore, the present invention provides intermediates of the general formula: ##STR3## in which R.sub.1, R.sub.2, A and X have the same meanings as above, and processes for the preparation of these intermediates.
摘要翻译：本发明提供以下通式的吲哚衍生物：其中R 1是氢原子或烷基，烯基，环烷基，环烯基，羧基，氰基，烷基羰基，烷氧基羰基，氨基羰基，烷基氨基羰基，二烷基氨基羰基或芳基， R2是氢原子或烷基，三卤代甲基，羟基，环烷基，氰基，羧基，烷氧基羰基，烷基羰基，氨基羰基，烷基氨基羰基或二烷基氨基羰基; R2是含有1至4个杂原子的杂环五元环或含有1至5个杂原子的杂环六元环，五元和六元环的杂原子相同或不同，为氮，氧或硫，一个或多个氮原子任选地带有氧原子，所述五元和六元环任选被一个或多个烷基，烷氧基，烷硫基，氧代，羟基，硝基，氨基，卤素或氰基取代; 或者R2是其互变异构体及其与无机和有机酸的生理上可接受的盐。本发明还提供了制备这些化合物的方法和含有它们的药物组合物。此外，本发明提供通式如下的中间体：其中R1，R2，A和X具有与上述相同的含义，以及制备这些中间体的方法。

4. 发明授权

US4831032A Cardiotonic benzimidazoles 失效
标题翻译：强心苯并咪唑
公开(公告)号：US4831032A
公开(公告)日：1989-05-16
申请号：US881983
申请日：1986-07-03
申请人： Wolfgang von der Saal , Alfred Mertens , Herbert Berger , Bernd Muller-Beckmann , Klaus Strein
发明人： Wolfgang von der Saal , Alfred Mertens , Herbert Berger , Bernd Muller-Beckmann , Klaus Strein
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61P9/04 , A61P9/12 , C07D235/26 , C07D235/28 , C07D235/30 , C07D263/58 , C07D277/62 , C07D413/12 , C07D417/12 , C07D487/04 , C07D498/04 , C07D513/04
CPC分类号： C07D263/58 , C07D413/12 , C07D417/12 , C07D487/04 , C07D513/04
摘要： The present invention provides benzimidazoles of the general formula: ##STR1## wherein R.sub.1, X, A, and R.sub.2 are as defined in the specification. The present invention also provides processes for the preparation of these new benzimidazoles and pharmaceutical compositions containing them, as well as intermediates for the preparation thereof.The new benzimidazoles are useful to treat heart or circulatory diseases which respond to a lowering of blood pressure, a positive inotropic action and/or an improvement in microcirculation.
摘要翻译：本发明提供以下通式的苯并咪唑：其中R1，X，A和R2如说明书中所定义。本发明还提供制备这些新的苯并咪唑和含有它们的药物组合物的方法，以及制备它们的中间体。新的苯并咪唑可用于治疗对降低血压，正性肌力作用和/或微循环改善作出反应的心脏或循环系统疾病。

5. 发明授权

US4730003A Tricyclic compounds for treating heart and circulatory diseases 失效
标题翻译：用于治疗心脏和循环系统疾病的三环化合物
公开(公告)号：US4730003A
公开(公告)日：1988-03-08
申请号：US904094
申请日：1986-09-04
申请人： Wolfgang von der Saal , Alfred Mertens , Herbert Berger , Bernd Muller-Beckmann
发明人： Wolfgang von der Saal , Alfred Mertens , Herbert Berger , Bernd Muller-Beckmann
IPC分类号： A61K31/41 , A61K31/415 , A61K31/42 , A61P9/00 , C07D487/04 , C07D487/10 , C07D498/04 , C07D498/10 , C07D513/04 , C07D513/10
CPC分类号： C07D487/04 , C07D487/10 , C07D513/04 , C07D513/10
摘要： The present invention provides compounds of the general formula: ##STR1## wherein the various substituents are defined hereinbelow. The compounds are used for the treatment and/or prophylaxis of heart and circulatory diseases.
摘要翻译：本发明提供以下通式的化合物：其中各种取代基如下文所定义。该化合物用于治疗和/或预防心脏和循环系统疾病。

6. 发明授权

US4874756A Benzodipyrroles, processes for the preparation thereof and pharmaceutical compositions containing them 失效
标题翻译：苯并二吡咯，其制备方法和含有它们的药物组合物
公开(公告)号：US4874756A
公开(公告)日：1989-10-17
申请号：US902182
申请日：1986-08-29
申请人： Alfred Mertens , Wolfgang von der Saal , Herbert Berger , Bernd Muller-Beckmann , Klaus Strein
发明人： Alfred Mertens , Wolfgang von der Saal , Herbert Berger , Bernd Muller-Beckmann , Klaus Strein
IPC分类号： A61K31/40 , A61K31/415 , A61K31/44 , A61K31/50 , A61P9/00 , C07D209/34 , C07D487/04
CPC分类号： C07D487/04 , C07D209/34
摘要： The present invention provides compounds of the general formula ##STR1## wherein the variables are as defined herein. The present invention also provides processes for the preparation thereof, pharmaceutical compositions containing them and intermediates for the preparation thereof.
摘要翻译：本发明提供了通式（I）（I）的化合物，其中变量如本文所定义。本发明还提供其制备方法，含有它们的药物组合物和其制备中间体。

7. 发明申请

US20070123513A1 Pyridylsulfonamide derivatives 失效
标题翻译：吡啶基磺酰胺衍生物
公开(公告)号：US20070123513A1
公开(公告)日：2007-05-31
申请号：US11594297
申请日：2006-11-08
申请人： Lothar Kling , Ulrike Reiff , Manfred Schwaiger , Georg Tiefenthaler , Wolfgang von der Saal , Thomas von Hirschheydt
发明人： Lothar Kling , Ulrike Reiff , Manfred Schwaiger , Georg Tiefenthaler , Wolfgang von der Saal , Thomas von Hirschheydt
IPC分类号： A61K31/55 , A61K31/4439 , A61K31/4412 , A61K31/4545 , C07D213/63
CPC分类号： C07D213/71
摘要： The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of such compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.
摘要翻译：本发明涉及式I化合物：其药学上可接受的盐，对映体形式，非对映异构体和外消旋体，这些化合物的制备，含有它们的药物组合物及其制备，以及这些化合物在控制或预防中的用途的疾病，如癌症。

8. 发明授权

US07625896B2 Pyridylsulfonamide derivatives 失效
标题翻译：吡啶基磺酰胺衍生物
公开(公告)号：US07625896B2
公开(公告)日：2009-12-01
申请号：US11594297
申请日：2006-11-08
申请人： Lothar Kling , Ulrike Reiff , Manfred Schwaiger , Georg Tiefenthaler , Wolfgang von der Saal , Thomas von Hirschheydt
发明人： Lothar Kling , Ulrike Reiff , Manfred Schwaiger , Georg Tiefenthaler , Wolfgang von der Saal , Thomas von Hirschheydt
IPC分类号： A61K31/535 , C07D413/00 , A61K31/445 , C07D211/68 , C07D401/00 , A61K31/44
CPC分类号： C07D213/71
摘要： The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of such compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.
摘要翻译：本发明涉及式I化合物：其药学上可接受的盐，对映体形式，非对映异构体和外消旋体，这些化合物的制备，含有它们的药物组合物及其制备，以及这些化合物在控制或预防中的用途的疾病，如癌症。

9. 发明申请

US20100292247A1 HETEROCYCLYL PYRIDYL SULFONAMIDE DERIVATIVES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS 失效
标题翻译：间苯二酚吡啶酰胺衍生物及其制备和用作药物代理
公开(公告)号：US20100292247A1
公开(公告)日：2010-11-18
申请号：US12377911
申请日：2007-10-24
申请人： Frederick Brookfield , Jonathan Gridley , Lothar Kling , Michael Prime , Ulrike Reiff , Wolfgang von der Saal , Thomas von Hirschheydt
发明人： Frederick Brookfield , Jonathan Gridley , Lothar Kling , Michael Prime , Ulrike Reiff , Wolfgang von der Saal , Thomas von Hirschheydt
IPC分类号： A61K31/496 , C07D401/14 , C07D401/04 , C07D491/113 , A61K31/438 , A61P35/00
CPC分类号： C07D295/04
摘要： Objects of the present invention are the compounds of formula I, their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.
摘要翻译：本发明的目的是式I化合物，其药学上可接受的盐，对映体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的药物及其制备，以及上述化合物在对照中的用途或预防癌症等疾病。

10. 发明授权

US4954498A Tricyclic benzimidazole compounds, pharmaceutical compositions and methods of use 失效
标题翻译：三环苯并咪唑化合物，药物组合物和使用方法
公开(公告)号：US4954498A
公开(公告)日：1990-09-04
申请号：US144514
申请日：1988-01-15
申请人： Alfred Mertens , Wolfgang von der Saal , Erwin Boehm , Klaus Strein
发明人： Alfred Mertens , Wolfgang von der Saal , Erwin Boehm , Klaus Strein
IPC分类号： A61K31/47 , A61K31/495 , A61P7/02 , C07D471/04 , C07D471/10 , C07D487/04 , C07D498/04 , C07D513/04
CPC分类号： C07D471/04 , C07D471/10 , C07D487/04 , C07D513/04
摘要： The present invention provides tricyclic benzimidazoles of the formula: ##STR1## wherein R.sub.1 is a phenyl radical of the general formula: ##STR2## wherein R.sub.2, R.sub.3 and R.sub.4 can be the same or diferent as in claim 1. For A, B, C and D are understood those compounds where one or two of A, B, C or D are nitrogen. These compounds are useful to inhibit the aggregation of thrombocytes and erythrocytes, lower blood pressure and can increase the power of the heart.
摘要翻译：本发明提供下式的三环苯并咪唑：其中R 1是下列通式的苯基：其中R 2，R 3和R 4可以与权利要求1中相同或不同。对于A，B，C和D，理解为A，B，C或D中的一个或两个为氮的化合物。这些化合物可用于抑制凝血细胞和红细胞的聚集，降低血压并可增加心脏的功能。

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