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81. 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。

82. 发明授权

US07956053B2 Inhibitors of tyrosine kinases 有权
标题翻译：酪氨酸激酶抑制剂
公开(公告)号：US07956053B2
公开(公告)日：2011-06-07
申请号：US12489049
申请日：2009-06-22
申请人： Werner Breitenstein , Pascal Furet , Sandra Jacob , Paul W Manley
发明人： Werner Breitenstein , Pascal Furet , Sandra Jacob , Paul W Manley
IPC分类号： C07D401/04 , A61K31/506
CPC分类号： C07D401/14 , C07D405/14
摘要： The invention relates to compounds of formula wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, in particular leukaemia, and a method for the treatment of such a disease.
摘要翻译：本发明涉及下式的化合物，其中取代基R 1，R 2和R 4具有本发明说明书中阐述和解释的含义，制备这些化合物的方法，含有它们的药物组合物，其任选组合的用途与一种或多种用于治疗对蛋白激酶活性，特别是肿瘤性疾病，特别是白血病的抑制作出反应的疾病的其它药学活性化合物，以及治疗这种疾病的方法。

83. 发明申请

US20100125064A1 3-Imidazolyl-Indoles for the Treatment of Proliferative Diseases 失效
标题翻译：用于治疗增生性疾病的3-咪唑基 - 吲哚
公开(公告)号：US20100125064A1
公开(公告)日：2010-05-20
申请号：US12593721
申请日：2008-03-27
申请人： Andreas Boettcher , Nicole Buschmann , Pascal Furet , Jean-Marc Groell , Jorg Kallen , Joanna Hergovich Lisztwan , Keiichi Masuya , Lorenz Mayr , Andrea Vaupel
发明人： Andreas Boettcher , Nicole Buschmann , Pascal Furet , Jean-Marc Groell , Jorg Kallen , Joanna Hergovich Lisztwan , Keiichi Masuya , Lorenz Mayr , Andrea Vaupel
IPC分类号： A61K31/55 , C07D403/04 , C07D413/12 , C07D403/12 , C07D401/14 , A61K31/4178 , A61K31/497 , A61K31/5377 , A61P35/00
CPC分类号： C07D403/04
摘要： The invention relates to 3-heterocyclyl indolyl compounds capable of inhibiting the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively, said compounds having the formula I, wherein R1, R2, R3, R4, RA, Y and Y are as defined in the specification. Due to their activity, the compounds are useful in the treatment of various disorders and diseases mediated by the activity of MDM2 and/or MDM4, or variants thereof, such as inflammatory or proliferative diseases or in the protection of cells.
摘要翻译：本发明涉及能够分别抑制p53或其变体和MDM2和/或MDM4或其变体之间的相互作用的3-杂环基吲哚基化合物，所述化合物具有式I，其中R 1，R 2，R 3，R 4， RA，Y和Y如说明书中所定义。由于它们的活性，所述化合物可用于治疗由MDM2和/或MDM4或其变体如炎性或增殖性疾病或保护细胞的活性介导的各种疾病和疾病。

84. 发明申请

US20100075980A1 Phenylacetamides being FLT3 Inhibitors 失效
标题翻译：苯乙酰胺是FLT3抑制剂
公开(公告)号：US20100075980A1
公开(公告)日：2010-03-25
申请号：US12445545
申请日：2007-10-15
申请人： Pascal Furet , Vito Guagnano
发明人： Pascal Furet , Vito Guagnano
IPC分类号： A61K31/437 , C07D471/04 , C07D401/14 , A61K31/496 , A61P35/00
CPC分类号： C07D471/04 , C07D235/06
摘要： Compounds of formula wherein the residues R1, R2, R3, R9, R10 and Q and X, Y and Z are as defined in the specification, salts thereof; their use, methods of their use, processes for their production, pharmaceutical compositions comprising them, their combinations with second drug substances and the use thereof and the like. The compounds are protein kinase inhibitors and can be used for the treatment of diseases mediated by protein kinase inhibitors, e.g. for the treatment of various proliferative diseases.
摘要翻译：其中残基R 1，R 2，R 3，R 9，R 10和Q和X，Y和Z如说明书中所定义，其盐; 其用途，使用方法，其制备方法，包含它们的药物组合物，其与第二药物物质的组合及其用途等。这些化合物是蛋白激酶抑制剂，可用于治疗由蛋白激酶抑制剂介导的疾病，例如，用于治疗各种增殖性疾病。

85. 发明授权

US07638523B2 Diarylamine-containing compounds and compositions, and their use as modulators of c-kit receptors 有权
标题翻译：含二芳基胺的化合物和组合物，以及它们作为c-kit受体调节剂的用途
公开(公告)号：US07638523B2
公开(公告)日：2009-12-29
申请号：US11933030
申请日：2007-10-31
申请人： Valentina Molteni , Shuli You , Juliet Nabakka , Yi Liu , Xiaolin Li , Donatella Chianelli , Jon Loren , Xiaodong Liu , Shifeng Pan , Donald S. Karanewsky , Pascal Furet , Vito Guagnano
发明人： Valentina Molteni , Shuli You , Juliet Nabakka , Yi Liu , Xiaolin Li , Donatella Chianelli , Jon Loren , Xiaodong Liu , Shifeng Pan , Donald S. Karanewsky , Pascal Furet , Vito Guagnano
IPC分类号： A61K31/505 , A61K31/506 , A61P19/02 , A61P37/08 , A61P9/02 , A61P17/06 , A61P1/04 , A61P1/16 , A61P25/20 , C07D239/42 , C07D403/10 , C07D403/14
CPC分类号： C07D403/04 , C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D413/12 , C07D417/12 , C07D471/04 , C07D491/10
摘要： Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.
摘要翻译：本文描述的是包括二芳基胺结构特征的化合物。本文还描述了制备这种化合物的方法，使用这些化合物调节c-kit受体的活性的方法，以及包含这些化合物的药物组合物和药物。本文还描述了使用这些化合物，药物组合物和药物来治疗和/或预防和/或抑制和/或改善与c-kit受体活性相关的病理学和/或症状学疾病或病症的方法。

86. 发明授权

US07563894B2 Diarylamine-containing compounds and compositions, and their use as modulators of c-kit receptors 有权
公开(公告)号：US07563894B2
公开(公告)日：2009-07-21
申请号：US11932945
申请日：2007-10-31
申请人： Valentina Molteni , Shuli You , Juliet Nabakka , Yi Liu , Xiaolin Li , Donatella Chianelli , Jon Loren , Xiaodong Liu , Shifeng Pan , Donald S. Karanewsky , Pascal Furet , Vito Guagnano
发明人： Valentina Molteni , Shuli You , Juliet Nabakka , Yi Liu , Xiaolin Li , Donatella Chianelli , Jon Loren , Xiaodong Liu , Shifeng Pan , Donald S. Karanewsky , Pascal Furet , Vito Guagnano
IPC分类号： C07D403/10 , C07D403/14 , C07D239/42 , A61K31/505
CPC分类号： C07D403/04 , C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D413/12 , C07D417/12 , C07D471/04 , C07D491/10
摘要： Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.

87. 发明申请

US20090131437A1 DISUBSTITUTED UREAS AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的消除性尿路炎
公开(公告)号：US20090131437A1
公开(公告)日：2009-05-21
申请号：US11813067
申请日：2006-01-03
申请人： Pascal Furet , Georg Martiny-Baron , Clive McCarthy , Vittorio Rasetti , Andrea Vaupel
发明人： Pascal Furet , Georg Martiny-Baron , Clive McCarthy , Vittorio Rasetti , Andrea Vaupel
IPC分类号： A61K31/5377 , C07D413/14
CPC分类号： C07D403/12 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14
摘要： The invention relates to compounds of the formula (I), their use as kinase inhibitors, new pharmaceutical formulations comprising said compounds, said compounds for use in the diagnostic or therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of diseases or for the manufacture of pharmaceutical formulations useful in the treatment of diseases that respond to modulation of kinase activity, methods of treatment comprising administration of said compounds to a warm-blooded animal, especially a human, and processes for the manufacture of said compounds.
摘要翻译：本发明涉及式（I）化合物，其作为激酶抑制剂的用途，包含所述化合物的新药物制剂，用于诊断或治疗温血动物，特别是人的所述化合物，其用于治疗疾病或用于制造可用于治疗对激酶活性调节作出反应的疾病的药物制剂，包括将所述化合物施用于温血动物，特别是人的治疗方法，以及所述化合物的制备方法。

88. 发明授权

US07482369B2 Anthranilic acid amides and their use as VEGF receptor tyrosine kinase inhibitors 失效
标题翻译：邻氨基苯甲酸酰胺及其作为VEGF受体酪氨酸激酶抑制剂的用途
公开(公告)号：US07482369B2
公开(公告)日：2009-01-27
申请号：US11374720
申请日：2006-03-14
申请人： Guido Bold , Pascal Furet , Paul W Manley
发明人： Guido Bold , Pascal Furet , Paul W Manley
IPC分类号： A01N43/40 , A61K31/44
CPC分类号： C07D213/64 , C07D213/70
摘要： The invention relates to anthranilic acid amide derivatives of formula I, wherein R1 represents H or lower alkyl, R2 represents H or lower alkyl, R3 represents perfluoro lower alkyl, and X is O or S, or an N-oxide or a tautomer thereof, to salts of such anthranilic acid amides, their N-oxides and their tautomers; processes for the preparation thereof, the application thereof for the treatment of the human or animal body, the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment especially of a neoplastic disease, such as a tumor disease, of retinopathy or age-related macular degeneration; a method for the treatment of such a disease in animals, especially in humans, and the use of such a compound—alone or in combination with one or more other pharmaceutically active compounds—for the manufacture of a pharmaceutical preparation for the treatment of a neoplastic disease, of retinopathy or age-related macular degeneration.
摘要翻译：本发明涉及式I的邻氨基苯甲酰胺衍生物，其中R1表示H或低级烷基，R2表示H或低级烷基，R3表示全氟低级烷基，X表示O或S，或其N-氧化物或互变异构体，这种邻氨基苯甲酸酰胺的盐，它们的N-氧化物及其互变异构体; 其制备方法，其用于治疗人或动物体的应用，其单独使用或与一种或多种其它药学活性化合物组合用于特别是肿瘤性疾病如肿瘤疾病的治疗，视网膜病变或年龄相关性黄斑变性; 用于治疗动物，特别是人类中的这种疾病的方法，以及使用这样的化合物 - 单独或与一种或多种其它药学活性化合物组合 - 用于制备用于治疗肿瘤的药物制剂视网膜病变或年龄相关性黄斑变性疾病。

89. 发明申请

US20080167308A1 DIARYLAMINE-CONTAINING COMPOUNDS AND COMPOSITIONS, AND THEIR USE AS MODULATORS OF C-KIT RECEPTORS 有权
公开(公告)号：US20080167308A1
公开(公告)日：2008-07-10
申请号：US11932945
申请日：2007-10-31
申请人： Valentina Molteni , Xiaolin Li , Donatella Chianelli , Juliet Nabakka , Jon Loren , Xiaodong Liu , Shifeng Pan , Yi Liu , Donald S. Karanewsky , Pascal Furet , Vito Guagnano , Shuli You
发明人： Valentina Molteni , Xiaolin Li , Donatella Chianelli , Juliet Nabakka , Jon Loren , Xiaodong Liu , Shifeng Pan , Yi Liu , Donald S. Karanewsky , Pascal Furet , Vito Guagnano , Shuli You
IPC分类号： A61K31/5377 , C07D239/42 , A61K31/505 , A61K31/506 , C12N9/12 , C07D403/12 , C07D413/12
CPC分类号： C07D403/04 , C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D413/12 , C07D417/12 , C07D471/04 , C07D491/10
摘要： Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.

90. 发明申请

US20070093506A1 Inhibitors of tyrosine kinases 审中-公开
公开(公告)号：US20070093506A1
公开(公告)日：2007-04-26
申请号：US11607542
申请日：2006-12-01
申请人： Werner Breitenstein , Pascal Furet , Sandra Jacob , Paul Manley
发明人： Werner Breitenstein , Pascal Furet , Sandra Jacob , Paul Manley
IPC分类号： A61K31/506 , C07D403/14
CPC分类号： C07D401/14 , C07D405/14
摘要： The invention relates to compounds of formula wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, in particular leukaemia, and a method for the treatment of such a disease.

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