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1. 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。

2. 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。

3. 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。

4. 发明授权

US4695567A Pyrrolobenzimidazoles, pharmaceutical compositions containing them and method of using them to treat certain heart and circulatory diseases 失效
标题翻译：吡咯并苯并咪唑，含有它们的药物组合物和使用它们治疗某些心脏和循环系统疾病的方法
公开(公告)号：US4695567A
公开(公告)日：1987-09-22
申请号：US820259
申请日：1986-01-17
申请人： Alfred Mertens , Jens-Peter Holck , Herbert Berger , Bernd Muller-Beckmann , Klaus Strein , Egon Roesch
发明人： Alfred Mertens , Jens-Peter Holck , Herbert Berger , Bernd Muller-Beckmann , Klaus Strein , Egon Roesch
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/50 , A61K31/505 , A61P9/00 , A61P9/04 , C07D403/12 , C07D405/12 , C07D487/04 , C07D403/06
CPC分类号： C07D403/12 , C07D405/12 , C07D487/04
摘要： The present invention provided pyrrolobenzimidazoles or tautomer thereof, of the general formula: ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.3 -C.sub.7 cycloalkyl;R.sub.2 is hydrogen, cyano, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or a carbonyl group substituted by hydroxyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkyoxy, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.12 dialkylamino or hydrazino, orR.sub.2 and R.sub.1 together with the carbon to which they are attached form a C.sub.3 -C.sub.8 spirocycloalkyl ring, or R.sub.1 and R.sub.2 together form C.sub.3 -C.sub.7 alkylidene or C.sub.3 -C.sub.7 cycloalkylkidene,X is a valency bond, C.sub.1 -C.sub.4 alkylene or vinylene andT is oxygen or sulphur;and Het is furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, pyrazinyl, pyrimidinyl or pyridazinyl wherein the heterocyclic five- and six-membered rings are unsubstituted or substituted by one or more C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, hydroxyl, oxo, nitro, amino, halo, carboxyl, C.sub.2 -C.sub.7 alkoxycarbonyl, aminocarbonyl or cyano groups; or a physiologically acceptable salt thereof with an inorganic or organic acid. These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.
摘要翻译：本发明提供了以下通式的吡咯并苯并咪唑或其互变异构体：其中R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基或C 3 -C 7环烷基; R2是氢，氰基，C1-C6烷基，C2-C6烯基或被羟基，C1-C6烷基，C1-C6烷氧基，氨基，C1-C6烷基氨基，C2-C12二烷基氨基或肼基取代的羰基或R2 并且R 1与它们所连接的碳一起形成C 3 -C 8螺环烷基环，或者R 1和R 2一起形成C 3 -C 7亚烷基或C 3 -C 7环烷基，X是价键，C 1 -C 4亚烷基或亚乙烯基，T是氧或硫; 并且Het是呋喃基，噻吩基，吡咯基，吡唑基，咪唑基，恶唑基，噻唑基，三唑基，恶二唑基，噻二唑基，吡嗪基，嘧啶基或哒嗪基，其中杂环五元和六元环是未取代的或被一个或多个C 1 -C 6烷基 C 1 -C 6烷氧基，C 1 -C 6烷硫基，羟基，氧代，硝基，氨基，卤素，羧基，C 2 -C 7烷氧基羰基，氨基羰基或氰基; 或其生理上可接受的盐与无机或有机酸反应。这些化合物可用于治疗心脏或循环系统疾病，特别是那些响应血压变化，心输出量增加和/或微循环变化的化合物。

5. 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。

6. 发明授权

US4870077A Heterocyclic substituted indolinones 失效
标题翻译：杂环取代的二氢吲哚酮
公开(公告)号：US4870077A
公开(公告)日：1989-09-26
申请号：US94871
申请日：1987-09-10
申请人： Wolfgang Von Der Saal , Walter-Gunar Friebe , Alfred Mertens , Bernd Muller-Beckmann , Lothar Kling
发明人： Wolfgang Von Der Saal , Walter-Gunar Friebe , Alfred Mertens , Bernd Muller-Beckmann , Lothar Kling
IPC分类号： A61K31/50 , A61K31/535 , A61K31/54 , A61P9/00 , C07D209/34 , C07D209/46 , C07D403/04 , C07D413/04 , C07D417/04
CPC分类号： C07D403/04 , C07D209/34 , C07D413/04 , C07D417/04
摘要： Heterocyclic substituted indolinones of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl or hydroxyalkyl radical, R.sub.2 is a carboxyl group or an alkoxy-carbonyl, hydroxyalkyl or alkylcarbonyloxyalkyl radical or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a lactone having 4, 5 or 6 ring atoms, A-B is --CH.sub.2 --CH(R.sub.3)--, --CH.dbd.CR.sub.3 --, --CH.sub.2 --NH--, --NH--CH.sub.2 --, --CH.sub.2 --O--, --O--CH.sub.2 --, --CH.sub.2 --S-- or --S--CH.sub.2 -- radical, R.sub.3 being a hydrogen atom or an alkyl or hydroxyalkyl radical, or A is a valency bond and B is a methylene radical ##STR2## or an imino group ##STR3## R.sub.4, R.sub.5, and R.sub.6 independently being hydrogen atoms or alkyl radicals wherein the alkyl groups independently contain 1 to 6 carbon atoms; as well as the tautomers thereof and the physiologically acceptable salt thereof and the physiologically acceptable salts thereof with inorganic and organic acids, are disclosed, such as, for instance, the compound 5-(2,3,4,5-tetrahydro-3-oxopyridazin-6-yl)-3-ethoxycarbonyl-3-methyl-1H-indol n-2-one. The compounds of the invention are useful in the treatment of heart and circulatory diseases, for example, by producing a positive inotropic action in a patient to whom the compounds are administered.
摘要翻译：式（I）的杂环取代的二氢吲哚酮：其中R 1是氢原子或烷基或羟烷基，R 2是羧基或烷氧羰基，羟基烷基或烷基羰基氧基烷基或R 1和R 2与碳它们连接的原子形成具有4,5或6个环原子的内酯，AB是-CH 2 -CH（R 3） - ， - CH = CR 3 - ， - CH 2 -NH-，-NH-CH 2 - ， - CH 2 -O-，-O-CH 2 - ， - CH 2 -S-或-S-CH 2 - 基，R 3是氢原子或烷基或羟烷基，或A是价键，B是亚甲基。或亚氨基基团R4，R5和R6独立地为氢原子或烷基，其中烷基独立地含有1至6个碳原子; 以及其与无机和有机酸的互变异构体及其生理上可接受的盐及其生理上可接受的盐，例如化合物5-（2,3,4,5-四氢-3- 氧基哒嗪-6-基）-3-乙氧基羰基-3-甲基-1H-吲哚-2-酮。本发明的化合物可用于治疗心脏和循环系统疾病，例如通过在施用化合物的患者中产生正性肌力作用。

7. 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。

8. 发明授权

US4847251A Pyridazinone derivatives, and pharmaceutical compositions containing them 失效
标题翻译：哒嗪酮衍生物和含有它们的药物组合物
公开(公告)号：US4847251A
公开(公告)日：1989-07-11
申请号：US80998
申请日：1987-08-03
申请人： Alfred Mertens , Wolfgang Von Der Saal , Bernd Muller-Beckmann , Gisbert Sponer
发明人： Alfred Mertens , Wolfgang Von Der Saal , Bernd Muller-Beckmann , Gisbert Sponer
IPC分类号： A61K31/50 , A61K31/53 , A61K31/535 , A61P1/10 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D417/14
摘要： The present invention provides pyridazinone derivatives of the general formula: ##STR1## wherein Het is a mono- or bicyclic heterocycle with one or two nitrogen atoms, B-C is a --CHR.sub.1 --CH.sub.2 --, --CR.sub.1 .dbd.CH--, --CHR.sub.1 --O--, --O--CHR.sub.1 --, --CHR.sub.1 --NH-- or --NH--CHR.sub.1 -- group, R.sub.1 being a hydrogen atom or an alkyl radical, and A is an amiono, alkylcarbonylamino, aminocarbonylamino, aminothiocarbonylamino, alkylaminothiocarbonylamino, alkylamionocarbonylamino, N'-cyanoguanidino or N'-cyano-N"-alkylguanidino group, a substituted phenyl ring or heterocycle attached via a nitrogen or sulphur atom, or a mono- or bicyclic substituted heterocycle with 1 to 3 nitrogen atoms, one ring nitrogen atom being directly attached to Het; as well as the physiologically acceptable salts thereof.The present invention also provides processes for the preparation of these pyridazinone drivatives and pharmaceutical compositions containing them for the treatment of heart and circulatory diseases.
摘要翻译：本发明提供以下通式的哒嗪酮衍生物：其中Het是具有一个或两个氮原子的单环或双环杂环，BC是-CHR 1 -CH 2 - ，-CR 1 = CH-，-CHR 1 -O-，-O-CHR 1 - ， - CHR 1 -NH-或-NH-CHR 1 - 基，R 1为氢原子或烷基，A为酰胺基，烷基羰基氨基，氨基羰基氨基，氨基硫代羰基氨基，烷基氨基硫代羰基氨基，烷基氨基羰基氨基，N “氰基胍基”或“氰基-N” - 烷基胍基，经氮或硫原子连接的取代苯环或杂环，或具有1至3个氮原子的单环或双环取代杂环，一个环氮原子为直接附于Het; 以及其生理上可接受的盐。本发明还提供了制备这些哒嗪酮驱动剂和含有它们用于治疗心脏和循环系统疾病的药物组合物的方法。

9. 发明授权

US4835167A Tricyclic benzotriazoles, processes for the preparation thereof and pharmaceutical compositions containing them 失效
标题翻译：三环苯并三唑，其制备方法和含有它们的药物组合物
公开(公告)号：US4835167A
公开(公告)日：1989-05-30
申请号：US80658
申请日：1987-08-03
申请人： Wolfgang Von Der Saal , Walter-Gunar Friebe , Alfred Mertens , Bernd Muller-Beckmann , Gisbert Sponer
发明人： Wolfgang Von Der Saal , Walter-Gunar Friebe , Alfred Mertens , Bernd Muller-Beckmann , Gisbert Sponer
IPC分类号： C07D487/04 , C07D487/10 , C07D498/04 , C07D513/04
CPC分类号： C07D487/04 , C07D487/10 , C07D513/04
摘要： The present invention provides new tricyclic benzotriazoles of the general formula: ##STR1## wherein Z is a hydrogen atom or an acyl radical, Y is an oxygen or sulphur atom or two hydrogen atoms and X is an oxygen or sulphur atom or a >CR.sub.1 R.sub.2 or >NR.sub.3 group, R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical, R.sub.2 is a hydrogen atom or an alkyl, alkenyl or cyano group or a carbonyl group substituted by a hydroxyl, alkyl, alkoxy, amino, alkylamino, dialkylamino or hydrazino group or R.sub.2, together with R.sub.1, represents a cycloalkylene radical or R.sub.1 and R.sub.2 together form an alkylidene or cycloalkylidene radical and R.sub.3 is a hydrogen atom or an alkyl radical; the tautomers thereof and the physiologically acceptable acid-addition salts thereof with inorganic and organic acids.The present invention also provides processes for the preparation of these tricyclic benzotriazoles and pharmaceutical compositions containing them for the treatment of heart and circulatory diseases.
摘要翻译：本发明提供了新的具有以下通式的三环苯并三唑：其中Z是氢原子或酰基，Y是氧或硫原子或两个氢原子，X是氧或硫原子或 > CR1R2或> NR3基团，R1是氢原子或烷基，烯基或环烷基，R2是氢原子或烷基，烯基或氰基或被羟基，烷基，烷氧基，氨基，烷基氨基取代的羰基，二烷基氨基或肼基或R 2与R 1一起代表亚环烷基或R 1和R 2一起形成亚烷基或亚环烷基，R 3为氢原子或烷基; 其互变异构体及其与无机和有机酸的生理上可接受的酸加成盐。本发明还提供了制备这些三环苯并三唑的方法和含有它们用于治疗心脏和循环系统疾病的药物组合物。

10. 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。

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