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公开(公告)号：US20090099167A1
公开(公告)日：2009-04-16
申请号：US12177617
申请日：2008-07-22
申请人： Guido Bold , Andreas Floersheimer , Pascal Furet , Patricia Imbach , Keiichi Masuya , Joseph G. Schoepfer , Georg Martiny-Baron
发明人： Guido Bold , Andreas Floersheimer , Pascal Furet , Patricia Imbach , Keiichi Masuya , Joseph G. Schoepfer , Georg Martiny-Baron
IPC分类号： C07D487/04 , A61K31/519 , A61K31/496 , A61K31/5377 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention relates to the use of pyrazolo[1,5a]pyrimidin-7-yl amine compounds and salts thereof in the treatment of kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, novel pyrazolo[1,5a]pyrimidin-7-yl amine compounds, and a process for the preparation of the novel pyrazolo[1,5a]pyrimidin-7-yl amine compounds.
摘要翻译： 本发明涉及吡唑并[1,5a]嘧啶-7-基胺化合物及其盐在治疗激酶依赖性疾病中的用途以及用于制备用于治疗所述疾病的药物制剂，新颖的吡唑并[1,5a ]嘧啶-7-基胺化合物，以及制备新的吡唑并[1,5a]嘧啶-7-基胺化合物的方法。
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公开(公告)号：US20080096883A1
公开(公告)日：2008-04-24
申请号：US11573235
申请日：2005-08-10
申请人： Giorgio Caravatti , Pascal Furet , Patricia Imbach , Georg Martiny-Baron , Lawrence Blas Perez , Tao Sheng
发明人： Giorgio Caravatti , Pascal Furet , Patricia Imbach , Georg Martiny-Baron , Lawrence Blas Perez , Tao Sheng
IPC分类号： A61K31/5375 , A61K31/426 , A61K31/47 , A61K31/497 , C07D217/00 , C07D239/72 , C07D403/00 , C07D413/02 , C07D277/62 , C07D237/30 , A61P43/00 , A61K31/50 , A61K31/517
CPC分类号： C07D277/62 , C07D217/02 , C07D237/30 , C07D239/74 , C07D239/84
摘要： The invention relates to trifluoromethyl substituted benzamide compounds of the formula (I), pharmaceuticals comprising these compounds, their use as or for the manufacture of pharmaceuticals, particularly as inhibitors of protein kinases and/or the treatment of a condition, disorder or disease state mediated by a protein kinase activity and/or a proliferative disease, methods of treatment comprising administering the compounds, especially of therapeutic and prophylactic treatment, methods for the manufacture of the compounds and novel intermediates and partial steps for their synthesis.
摘要翻译： 本发明涉及式（I）的三氟甲基取代的苯甲酰胺化合物，包含这些化合物的药物，它们作为或用于制造药物的用途，特别是作为蛋白激酶的抑制剂和/或病症，病症或疾病状态介导的治疗 通过蛋白激酶活性和/或增殖性疾病，治疗方法包括施用化合物，特别是治疗和预防治疗的化合物和新中间体的制备方法及其合成的部分步骤。
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公开(公告)号：US20090131437A1
公开(公告)日：2009-05-21
申请号：US11813067
申请日：2006-01-03
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。
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4.发明申请Use of Pyrimidylaminobenzamides for the Treatment of Diseases that Respond to Modulation of Tie-2 Kinase Activity 审中-公开使用嘧啶氨基苯甲酰胺治疗响应调节Tie-2激酶活性的疾病公开(公告)号：US20080114001A1
公开(公告)日：2008-05-15
申请号：US11815046
申请日：2006-01-26
IPC分类号： A61K31/506
CPC分类号： A61K31/506
摘要： The present invention relates to the use of pyrimidylaminobenzamide compounds for the preparation of a drug for the treatment of diseases that respond to modulation of kinase, especially tie-2 kinase, activity, especially for the curative and/or prophylactic treatment of leukemia, myelodysplastic syndromes or pulmonary hypertension, and to a method of treating diseases that respond to modulation of kinase activity, especially tie-2 kinase activity.
摘要翻译： 本发明涉及嘧啶氨基苯甲酰胺化合物在制备用于治疗对激酶调节，特别是tie-2激酶，特别是用于治疗和/或预防性治疗白血病，骨髓增生异常综合征的活性的疾病的药物中的用途 或肺动脉高压，以及治疗对激酶活性调节，特别是tie-2激酶活性作出反应的疾病的方法。
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5.发明授权Monoclonal antibodies against the extracellular domain of human VEGF-receptor protein (KDR) 失效针对人VEGF受体蛋白（KDR）细胞外结构域的单克隆抗体公开(公告)号：US06344339B1
公开(公告)日：2002-02-05
申请号：US09254640
申请日：1999-05-19
IPC分类号： G01N3353
CPC分类号： C07K16/2863 , A61K38/00 , A61K51/103
摘要： Monoclonal antibodies, secreted by hybridoma cell lines, that are directed against an epitope of the extracellular domain of human VEGF-receptor KDR, methods of determining human VEGF-receptor KDR in cell lysates or tissue analysates and the use of the antibodies in analytical assays, in diagnostics and as carrier molecules for therapeutic substances, are described.
摘要翻译： 通过杂交瘤细胞系分泌的针对人类VEGF-受体KDR的细胞外结构域的表位的单克隆抗体，在细胞裂解物或组织分析中测定人VEGF-受体KDR的方法以及在分析测定中使用抗体， 描述了诊断和作为治疗物质的载体分子。
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公开(公告)号：US20100022569A1
公开(公告)日：2010-01-28
申请号：US12301690
申请日：2007-05-23
IPC分类号： A61K31/506 , A61P35/04
CPC分类号： A61K31/506
摘要： The present invention relates to the use of pyrimidylaminobenzamide compounds for the preparation of a drug for the treatment of diseases that respond to modulation of Ephrin receptor kinase, especially EphB4, activity, especially for the curative and/or prophylactic treatment of proliferative diseases, and to a method of treating diseases that respond to modulation of kinase activity, especially Ephrin receptor kinase activity.
摘要翻译： 本发明涉及嘧啶氨基苯甲酰胺化合物用于制备用于治疗对调节Ephrin受体激酶，特别是EphB4的活性的药物的药物的用途，特别是用于治疗性和/或预防性治疗增殖性疾病的活性，以及 治疗对激酶活性调节作用的疾病的方法，特别是Ephrin受体激酶活性。
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![4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-N-[5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl]-benzamide for treatment of melanoma](/abs-image/US/2012/01/10/US08093259B2/abs.jpg.150x150.jpg)
7.发明授权4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-N-[5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl]-benzamide for treatment of melanoma 失效4-甲基-3 - [[4-（3-吡啶基）-2-嘧啶基]氨基] -N- [5-（4-甲基-1H-咪唑-1-基）-3-（三氟甲基）苯基] 苯甲酰胺治疗黑色素瘤公开(公告)号：US08093259B2
公开(公告)日：2012-01-10
申请号：US12301690
申请日：2007-05-23
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： A61K31/506
摘要： The present invention relates to the use of pyrimidylaminobenzamide compounds for the preparation of a drug for the treatment of diseases that respond to modulation of Ephrin receptor kinase, especially EphB4, activity, especially for the curative and/or prophylactic treatment of proliferative diseases, and to a method of treating diseases that respond to modulation of kinase activity, especially Ephrin receptor kinase activity.
摘要翻译： 本发明涉及嘧啶氨基苯甲酰胺化合物用于制备用于治疗对调节Ephrin受体激酶，特别是EphB4的活性的药物的药物的用途，特别是用于治疗性和/或预防性治疗增殖性疾病的活性，以及 治疗对激酶活性调节作用的疾病的方法，特别是Ephrin受体激酶活性。
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![Pyrazolo[1,5-a]Pyrimidin-7-Yl Amine Derivatives as Protein Kinase Inhibitors](/abs-image/US/2008/09/25/US20080234284A1/abs.jpg.150x150.jpg)
8.发明申请Pyrazolo[1,5-a]Pyrimidin-7-Yl Amine Derivatives as Protein Kinase Inhibitors 审中-公开吡唑并[1,5-a]嘧啶-7-基胺衍生物作为蛋白激酶抑制剂公开(公告)号：US20080234284A1
公开(公告)日：2008-09-25
申请号：US11996337
申请日：2006-07-19
IPC分类号： A61K31/519 , A61P35/00 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to pyrazolo[1,5a]pyrimidin-7-yl amine derivatives of formula (I) and salts thereof, their use in the treatment of protein kinase dependent diseases.
摘要翻译： 本发明涉及式（I）的吡唑并[1,5a]嘧啶-7-基胺衍生物及其盐，它们用于治疗蛋白激酶依赖性疾病。
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9.发明申请公开(公告)号：US20070092527A1
公开(公告)日：2007-04-26
申请号：US10560322
申请日：2004-06-18
申请人： Birgit Baumgarten , Carol Jones , Marie-Gabrielle Ludwig , Georg Martiny-Baron , Klaus Seuwen , Romain Wolf , Lorenza Wyder , Thomas Suply
发明人： Birgit Baumgarten , Carol Jones , Marie-Gabrielle Ludwig , Georg Martiny-Baron , Klaus Seuwen , Romain Wolf , Lorenza Wyder , Thomas Suply
IPC分类号： G01N33/567 , A61K39/00 , A61K38/17
CPC分类号： C12N15/8509 , A01K2217/075 , A01K2227/105 , A01K2267/03 , A01K2267/0368 , A61K38/1709 , A61K48/00 , G01N33/74 , G01N33/84 , G01N2333/726
摘要： This invention relates to the newly identified utility of certain G protein-coupled receptors (GPCRs), in particular to OGR1, GPR4 and TDAG8 (TDAG8 is also named GPR65) polypeptides, and polynucleotides encoding such GPCR polypeptides, to their use in diagnosis and to methods of identifying compounds that are agonists or antagonists to said GPCRs, and to the production of such polypeptides and polynucleotides.
摘要翻译： 本发明涉及新鉴定的某些G蛋白偶联受体（GPCR），特别是OGR1，GPR4和TDAG8（TDAG8也称为GPR65）多肽以及编码这种GPCR多肽的多核苷酸在临床诊断中的用途和 识别作为所述GPCR的激动剂或拮抗剂的化合物的方法，以及这些多肽和多核苷酸的产生。
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公开(公告)号：US20060035897A1
公开(公告)日：2006-02-16
申请号：US11201348
申请日：2005-08-10
申请人： Giorgio Caravatti , Pascal Furet , Patricia Imbach , Georg Martiny-Baron , Lawrence Perez , Tao Sheng
发明人： Giorgio Caravatti , Pascal Furet , Patricia Imbach , Georg Martiny-Baron , Lawrence Perez , Tao Sheng
IPC分类号： A61K31/502 , A61K31/517 , A61K31/47 , A61K31/428
CPC分类号： C07D277/62 , C07D217/02 , C07D237/30 , C07D239/74 , C07D239/84
摘要： The invention relates to trifluoromethyl substituted benzamide compounds of the formula I, pharmaceuticals comprising these compounds, their use as or for the manufacture of pharmaceuticals, particularly as inhibitors of protein kinases, especially of ephrin receptor kinases, and/or the treatment of a condition, disorder or disease state mediated by a protein kinase activity and/or a proliferative disease, methods of treatment comprising administering the compounds, especially of therapeutic and prophylactic treatment, methods for the manufacture of the compounds and novel intermediates and partial steps for their synthesis.
摘要翻译： 本发明涉及式I的三氟甲基取代的苯甲酰胺化合物，包含这些化合物的药物，它们作为药物的用途或用于制造药物，特别是作为蛋白激酶抑制剂，特别是ephrin受体激酶的抑制剂和/或治疗病症， 由蛋白激酶活性和/或增殖性疾病介导的紊乱或疾病状态，治疗方法包括施用化合物，特别是治疗和预防性治疗化合物和新中间体的制备方法及其合成的部分步骤。
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