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1. 发明申请

US20070111991A1 Novel dibenzo [b, f] oxepine-10-carboxamides and pharmaceutical uses thereof 失效
标题翻译：新的二苯并[b，f]氧杂七环素-10-甲酰胺及其药物用途
公开(公告)号：US20070111991A1
公开(公告)日：2007-05-17
申请号：US10565456
申请日：2004-07-23
申请人： Yves Auberson , Claudia Betschart , Stefanie Flohr , Ralf Glatthar , Oliver Simic , Marina Tintelnot-Blomley , Thomas Troxler , Eric Vangrevelinghe , Siem Veenstra
发明人： Yves Auberson , Claudia Betschart , Stefanie Flohr , Ralf Glatthar , Oliver Simic , Marina Tintelnot-Blomley , Thomas Troxler , Eric Vangrevelinghe , Siem Veenstra
IPC分类号： A61K31/55 , A61K31/5375 , A61K31/5377 , A61K31/495 , A61K31/496 , A61K31/445 , A61K31/452 , A61K31/4025
CPC分类号： C07D405/12 , C07C235/82 , C07C2603/32 , C07D313/14 , C07D407/12 , C07D413/12 , C07D453/02 , C07D491/04
摘要： The present invention pertains to novel dibenzo[b,f]oxepine-10-carboxamides compound to a process for the preparation of such compounds of formula I, their use as a pharmaceuticals, especially in the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation, and to pharmaceutical compositions and combinations comprising such compounds of formula I.
摘要翻译：本发明涉及新的二苯并[b，f]氧杂七环素-10-甲酰胺化合物，其用于制备式I化合物的方法，它们作为药物的用途，特别是用于治疗与β-谷氨酸相关的神经和血管疾病，淀粉样蛋白生成和/或聚集，以及包含式I化合物的药物组合物和组合。

2. 发明申请

US20100168062A1 Quinoxaline Derivatives as Tyrosine Kinase Activity Inhibitors 失效
标题翻译：喹喔啉衍生物作为酪氨酸激酶抑制剂
公开(公告)号：US20100168062A1
公开(公告)日：2010-07-01
申请号：US12663698
申请日：2008-06-06
申请人： Marc Gerspacher , Pascal Furet , Eric Vangrevelinghe , Carole Pissot Sondermann , Christoph Gaul , Philipp Holzer
发明人： Marc Gerspacher , Pascal Furet , Eric Vangrevelinghe , Carole Pissot Sondermann , Christoph Gaul , Philipp Holzer
IPC分类号： A61K31/498 , C07D413/10 , A61K31/5377 , C07D241/42 , C07D417/10 , A61K31/541 , C07D403/10 , C07D413/12 , C07D413/14 , C07D417/14 , C07D401/14 , C07D405/14 , A61K31/69 , C07F5/02 , A61P35/00 , A61P37/00 , A61P37/06 , A61P17/06 , A61P17/00 , A61P3/10 , A61P1/00
CPC分类号： A61K31/498 , A61K31/5377 , A61K31/541 , C07D241/42 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14
摘要： The present invention relates to quinoxaline compound of the formula (I): wherein R1 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R7; R2 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R8; R3, R4, R5 and R8 are each independently hydrogen or R9; and R7, R8 and R9 are each independently selected from organic and inorganic substituents, their use in therapy of diseases, in particular diseases mediated by the tyrosine kinase activity of Janus kinases, including JAK-2 and JAK-3 kinases.
摘要翻译：本发明涉及式（I）的喹喔啉化合物：其中R 1是碳环基或杂环基，其任一个任选被1,2,3,4或5个R 7取代; R2是碳环基或杂环基，其任一个任选被1,2,3,4或5个R8取代; R3，R4，R5和R8各自独立地为氢或R9; R7，R8和R9各自独立地选自有机和无机取代基，它们用于治疗疾病，特别是由Janus激酶（包括JAK-2和JAK-3激酶）的酪氨酸激酶活性介导的疾病。

3. 发明授权

US08629168B2 Benzoxazoles and oxazolopyridines being useful as janus kinases inhibitors 失效
标题翻译：苯并恶唑和恶唑啉吡啶可用作甘油激酶抑制剂
公开(公告)号：US08629168B2
公开(公告)日：2014-01-14
申请号：US12440298
申请日：2007-09-13
申请人： Marc Gerspacher , Pascal Furet , Eric Vangrevelinghe
发明人： Marc Gerspacher , Pascal Furet , Eric Vangrevelinghe
IPC分类号： C07D263/58 , C07D263/60 , C07D413/00 , C07D498/00 , A01N43/76 , A61K31/42
CPC分类号： C07D263/58 , C07D413/04
摘要： The invention relates to 2,7-disubstituted benzoxazole and 2,4-disubstituted oxazolo[5,4-c]pyridine compounds of the formula I given below, as well as salts thereof, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, these compounds for use in the treatment (including prophylaxis) of the animal, especially human, body (especially with regard to a proliferative disease), the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment especially of a protein tyrosine kinase mediated disease (such as a tumor disease) or for the manufacture of a pharmaceutical preparation for use in the treatment of such a disease, a method for the treatment of such a disease and a pharmaceutical preparation for the treatment of a disease as mentioned. The compounds are of the formula I, wherein the symbols are as defined in the description. The compounds inhibit, for example, JAK2 and JAK3.
摘要翻译：本发明涉及以下给出的式I的2,7-二取代苯并恶唑和2,4-二取代的恶唑并[5,4-c]吡啶化合物及其盐，其制备方法及其在用于治疗人或动物体的方法，这些化合物用于动物，特别是人体（特别是关于增殖性疾病）的治疗（包括预防）中，单独使用或与一种或更多其它药物活性化合物 - 用于治疗特别是蛋白质酪氨酸激酶介导的疾病（例如肿瘤疾病）或用于制备用于治疗这种疾病的药物制剂的治疗方法用于治疗所述疾病的疾病和药物制剂。所述化合物具有式I，其中符号如说明书中所定义。该化合物抑制例如JAK2和JAK3。

4. 发明授权

US08193189B2 Quinoxaline derivatives as tyrosine kinase activity inhibitors 失效
标题翻译：喹喔啉衍生物作为酪氨酸激酶活性抑制剂
公开(公告)号：US08193189B2
公开(公告)日：2012-06-05
申请号：US12663698
申请日：2008-06-06
申请人： Marc Gerspacher , Pascal Furet , Eric Vangrevelinghe , Carole Pissot Sondermann , Christoph Gaul , Philipp Holzer
发明人： Marc Gerspacher , Pascal Furet , Eric Vangrevelinghe , Carole Pissot Sondermann , Christoph Gaul , Philipp Holzer
IPC分类号： A61K31/495
CPC分类号： A61K31/498 , A61K31/5377 , A61K31/541 , C07D241/42 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14
摘要： The present invention relates to quinoxaline compound of the formula (I): wherein R1 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R7; R2 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R8; R3, R4, R5 and R6 are each independently hydrogen or R9; and R7, R8 and R9 are each independently selected from organic and inorganic substituents, their use in therapy of diseases, in particular diseases mediated by the tyrosine kinase activity of Janus kinases, including JAK-2 and JAK-3 kinases.
摘要翻译：本发明涉及式（I）的喹喔啉化合物：其中R 1是碳环基或杂环基，其任一个任选被1,2,3,4或5个R 7取代; R2是碳环基或杂环基，其任一个任选被1,2,3,4或5个R8取代; R3，R4，R5和R6各自独立地为氢或R9; R7，R8和R9各自独立地选自有机和无机取代基，它们用于治疗疾病，特别是由Janus激酶（包括JAK-2和JAK-3激酶）的酪氨酸激酶活性介导的疾病。

5. 发明申请

US20080194629A1 3-Mono-and 3,5-Disubstituted Piperidine Derivatives as Renin Inhibitors 审中-公开
标题翻译： 3-单和3,5-二取代的哌啶衍生物作为肾素抑制剂
公开(公告)号：US20080194629A1
公开(公告)日：2008-08-14
申请号：US11913492
申请日：2006-05-02
申请人： Daniel Kaspar Baeschlin , Werner Breitenstein , Claus Ehrhardt , Juergen Klaus Maibaum , Nils Ostermann , Juerg Zimmermann , Simon Rudisser , Eric Vangrevelinghe , Osamu Irie , Ichiro Umemura , Masaki Suzuki , Muneto Mogi , Takanori Kanazawa , Fumiaki Yokokawa , Atsuko Nihonyanagi
发明人： Daniel Kaspar Baeschlin , Werner Breitenstein , Claus Ehrhardt , Juergen Klaus Maibaum , Nils Ostermann , Juerg Zimmermann , Simon Rudisser , Eric Vangrevelinghe , Osamu Irie , Ichiro Umemura , Masaki Suzuki , Muneto Mogi , Takanori Kanazawa , Fumiaki Yokokawa , Atsuko Nihonyanagi
IPC分类号： A61K31/453 , C07D401/12
CPC分类号： C07D405/14 , C07D211/60 , C07D401/12 , C07D405/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The invention relates to 3,5-piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-piperidine compound, and/or a method of treatment comprising administering a 3,5-piperidine compound, a method for the manufacture of a 3,5-piperidine compound, and novel intermediates and partial steps for their synthesis. Especially, the 3,5-piperidine compounds have the formula I, wherein the symbols have the meanings described in the specification.
摘要翻译：本发明涉及3,5-哌啶化合物，这些化合物用于诊断和治疗温血动物，特别是用于治疗依赖于肾素活性的疾病（=病症）; 使用该类化合物制备用于治疗依赖于肾素活性的疾病的药物制剂; 使用该类化合物治疗依赖于肾素活性的疾病; 包括3,5-哌啶化合物的药物制剂和/或治疗方法，包括施用3,5-哌啶化合物，制备3,5-哌啶化合物的方法，以及新的中间体和部分步骤合成。特别地，3,5-哌啶化合物具有式I，其中符号具有说明书中描述的含义。

6. 发明申请

US20100009978A1 Benzoxazoles and Oxazolopyridines Being Useful as Janus Kinases Inhibitors 失效
标题翻译：苯并恶唑和唑吡吉因作为Janus激酶抑制剂有用
公开(公告)号：US20100009978A1
公开(公告)日：2010-01-14
申请号：US12440298
申请日：2007-09-13
申请人： Marc Gerspacher , Pascal Furet , Eric Vangrevelinghe
发明人： Marc Gerspacher , Pascal Furet , Eric Vangrevelinghe
IPC分类号： A61K31/423 , C07D263/58 , C07D413/14 , C07D417/14 , A61K31/5377 , A61K31/541 , A61P35/00
CPC分类号： C07D263/58 , C07D413/04
摘要： The invention relates to 2,7-disubstituted benzoxazole and 2,4-disubstituted oxazolo[5,4-c]pyridine compounds of the formula I given below, as well as salts thereof, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, these compounds for use in the treatment (including prophylaxis) of the animal, especially human, body (especially with regard to a proliferative disease), the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment especially of a protein tyrosine kinase mediated disease (such as a tumor disease) or for the manufacture of a pharmaceutical preparation for use in the treatment of such a disease, a method for the treatment of such a disease and a pharmaceutical preparation for the treatment of a disease as mentioned. The compounds are of the formula I, wherein the symbols are as defined in the description. The compounds inhibit, for example, JAK2 and JAK3.
摘要翻译：本发明涉及以下给出的式I的2,7-二取代苯并恶唑和2,4-二取代的恶唑并[5,4-c]吡啶化合物及其盐，其制备方法及其在用于治疗人或动物体的方法，这些化合物用于动物，特别是人体（特别是关于增殖性疾病）的治疗（包括预防）中，单独使用或与一种或更多其它药物活性化合物 - 用于治疗特别是蛋白质酪氨酸激酶介导的疾病（例如肿瘤疾病）或用于制备用于治疗这种疾病的药物制剂的治疗方法用于治疗所述疾病的疾病和药物制剂。所述化合物具有式I，其中符号如说明书中所定义。该化合物抑制例如JAK2和JAK3。

7. 发明授权

US07612054B2 Dibenzo[b,f]oxepine-10-carboxamides and pharmaceutical uses thereof 失效
标题翻译：二苯并[b，f]氧杂七环-10-甲酰胺及其药物用途
公开(公告)号：US07612054B2
公开(公告)日：2009-11-03
申请号：US10565456
申请日：2004-07-23
申请人： Yves Auberson , Claudia Betschart , Stefanie Flohr , Ralf Glatthar , Oliver Simic , Marina Tintelnot-Blomley , Thomas J. Troxler , Eric Vangrevelinghe , Siem Jacob Veenstra
发明人： Yves Auberson , Claudia Betschart , Stefanie Flohr , Ralf Glatthar , Oliver Simic , Marina Tintelnot-Blomley , Thomas J. Troxler , Eric Vangrevelinghe , Siem Jacob Veenstra
IPC分类号： A01N43/00 , A61K31/33 , C07D313/00
CPC分类号： C07D405/12 , C07C235/82 , C07C2603/32 , C07D313/14 , C07D407/12 , C07D413/12 , C07D453/02 , C07D491/04
摘要： The present invention pertains to novel dibenzo[b,f]oxepine-10-carboxamides compound to a process for the preparation of such compounds of formula I, their use as a pharmaceuticals, especially in the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation, and to pharmaceutical compositions and combinations comprising such compounds of formula I.
摘要翻译：本发明涉及新的二苯并[b，f]氧杂七环素-10-甲酰胺化合物，其用于制备式I化合物的方法，它们作为药物的用途，特别是用于治疗与β-谷氨酸相关的神经和血管疾病，淀粉样蛋白生成和/或聚集，以及包含式I化合物的药物组合物和组合。

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