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1. 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。

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

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。

4. 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。

5. 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。

6. 发明授权

US07879884B2 Aryl pyridyl sulfonamide derivatives, their manufacture and use as pharmaceutical agents 失效
标题翻译：芳基吡啶基磺酰胺衍生物，其制造和用作药剂
公开(公告)号：US07879884B2
公开(公告)日：2011-02-01
申请号：US12599699
申请日：2008-05-14
申请人： Frederick Brookfield , Lothar Kling , Ulrike Reiff , Wolfgang Von der Saal , Thomas Von Hirschheydt
发明人： Frederick Brookfield , Lothar Kling , Ulrike Reiff , Wolfgang Von der Saal , Thomas Von Hirschheydt
IPC分类号： A61K31/44 , C07D213/00
CPC分类号： C07D213/71
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）化合物的药学上可接受的盐，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，以及上述化合物在控制或预防癌症等疾病。

7. 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。

8. 发明授权

US07939532B2 Heterocyclyl pyridyl sulfonamide derivatives, their manufacture and use as pharmaceutical agents 失效
标题翻译：杂环基吡啶磺酰胺衍生物，其制造和用作药剂
公开(公告)号：US07939532B2
公开(公告)日：2011-05-10
申请号：US12377911
申请日：2006-10-24
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： A61K31/438 , A61K31/4545 , A61K31/496 , C07D213/74 , C07D401/12 , C07D491/13 , 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。

9. 发明申请

US20100256200A1 ARYL PYRIDYL SULFONAMIDE DERIVATIVES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS 失效
标题翻译： ARYL PYRIDYL磺胺衍生物，其制造和用作药物代理
公开(公告)号：US20100256200A1
公开(公告)日：2010-10-07
申请号：US12599699
申请日：2008-05-14
申请人： Frederick Brookfield , Lothar Kling , Ulrike Reiff , Wolfgang Von der Saal , Thomas Von Hirschheydt
发明人： Frederick Brookfield , Lothar Kling , Ulrike Reiff , Wolfgang Von der Saal , Thomas Von Hirschheydt
IPC分类号： A61K31/4418 , C07D213/71 , A61P35/00
CPC分类号： C07D213/71
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）化合物的药学上可接受的盐，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，以及上述化合物在控制或预防癌症等疾病。

10. 发明申请

US20050267179A1 NOVEL THIOETHER DERIVATIVES 失效
标题翻译：新型三氯乙烯衍生物
公开(公告)号：US20050267179A1
公开(公告)日：2005-12-01
申请号：US11132082
申请日：2005-05-18
申请人： Birgit Bossenmaier , Walter-Gunar Friebe , Thomas Friess , Lothar Kling , Ulrike Reiff , Edgar Voss
发明人： Birgit Bossenmaier , Walter-Gunar Friebe , Thomas Friess , Lothar Kling , Ulrike Reiff , Edgar Voss
IPC分类号： A61K31/422 , A61P35/00 , C07D413/02 , C07D413/12
CPC分类号： C07D413/12
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, pharmaceutical compositions 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）化合物的药学上可接受的盐，对映体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的药物组合物及其制备方法，以及上述化合物在控制或预防癌症等疾病。

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