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61. 发明授权

US08399472B2 Compositions and methods for inhibition of the JAK pathway 有权
公开(公告)号：US08399472B2
公开(公告)日：2013-03-19
申请号：US12193627
申请日：2008-08-18
申请人： Hui Li , Sambaiah Thota , David Carroll , Ankush Argade , Kin Tso , Arvinder Sran , Jeffrey Clough , Holger Keim , Somasekhar Bhamidipati , Vanessa Taylor , Robin Cooper , Rajinder Singh , Brian Wong
发明人： Hui Li , Sambaiah Thota , David Carroll , Ankush Argade , Kin Tso , Arvinder Sran , Jeffrey Clough , Holger Keim , Somasekhar Bhamidipati , Vanessa Taylor , Robin Cooper , Rajinder Singh , Brian Wong
IPC分类号： C07D239/48 , A61K31/506
CPC分类号： C07D413/12 , A61K31/343 , A61K31/436 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/541 , A61K31/695 , A61K38/13 , A61K39/3955 , A61K45/06 , C07D239/42 , C07D239/48 , C07D285/22 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D413/14 , C07D417/12 , C07D498/04 , C07F7/0812 , C07F7/10
摘要： The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.

62. 发明授权

US08377924B2 Protein kinase C inhibitors and uses thereof 有权
公开(公告)号：US08377924B2
公开(公告)日：2013-02-19
申请号：US12691607
申请日：2010-01-21
申请人： Rajinder Singh , Huí Li , Haoran Zhao , Rao Kolluri , Kin Tso , John Ramphal , Shihai Gu , Carlos Valdez , Jing Zhang , Emily Stauffer , Matthew Duncton , Salvador Alvarez
发明人： Rajinder Singh , Huí Li , Haoran Zhao , Rao Kolluri , Kin Tso , John Ramphal , Shihai Gu , Carlos Valdez , Jing Zhang , Emily Stauffer , Matthew Duncton , Salvador Alvarez
IPC分类号： A61K31/55 , A61K31/497 , A61K31/535 , A61K31/505 , C07D403/10 , C07D413/12 , C07D401/12
CPC分类号： A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/55 , C07D401/12 , C07D401/14 , C07D413/12
摘要： This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

63. 发明申请

US20130023660A1 Carboxamide Compounds and Methods for Using the Same 有权
公开(公告)号：US20130023660A1
公开(公告)日：2013-01-24
申请号：US13622078
申请日：2012-09-18
申请人： Jiaxin Yu , Hui Hong , Ihab S. Darwish , Xiang Xu , Rajinder Singh
发明人： Jiaxin Yu , Hui Hong , Ihab S. Darwish , Xiang Xu , Rajinder Singh
IPC分类号： C07D211/58 , C07D417/14 , C07D401/14 , C07D401/12 , C07D413/14 , C07D471/04
CPC分类号： C07D471/04 , A61K31/437 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/497 , C07D211/58 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D487/08
摘要： Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

64. 发明授权

US08314093B2 2,4-pyrimidinediamine compounds for treating or preventing autoimmune diseases 有权
标题翻译：用于治疗或预防自身免疫疾病的2,4-嘧啶二胺化合物
公开(公告)号：US08314093B2
公开(公告)日：2012-11-20
申请号：US12642406
申请日：2009-12-18
申请人： Jeffrey Wayne Clough , Somasekhar Bhamidipati , Rajinder Singh , Esteban Masuda , Haoran Zhao
发明人： Jeffrey Wayne Clough , Somasekhar Bhamidipati , Rajinder Singh , Esteban Masuda , Haoran Zhao
IPC分类号： C07D498/04 , A61K31/538
CPC分类号： C07D417/12 , C07D401/12 , C07D403/12 , C07D413/12 , C07D413/14 , C07D498/04
摘要： The present invention provides 3-hydroxyphenyl-2,4-pyrimidinediamine compounds of formula I, as well as related compositions and methods for treating a variety of autoimmune diseases.
摘要翻译：本发明提供式I的3-羟基苯基-2,4-嘧啶二胺化合物，以及用于治疗多种自身免疫疾病的相关组合物和方法。

65. 发明申请

US20120263737A1 METHODS FOR INHIBITING ALLOGRAFT REJECTION 有权
标题翻译：抑制ALLOGRAFT抑制剂的方法
公开(公告)号：US20120263737A1
公开(公告)日：2012-10-18
申请号：US13444684
申请日：2012-04-11
申请人： Vanessa Taylor , Esteban Masuda
发明人： Vanessa Taylor , Esteban Masuda
IPC分类号： A61K31/506 , A61K39/00 , A61P37/06 , A61K39/395
CPC分类号： A61K31/506 , A61K31/436 , A61K31/4545 , A61K38/13 , A61K45/06 , A61K2300/00
摘要： Disclosed herein are methods for treating or inhibiting allograft rejection in a transplant recipient. In some embodiments, the methods include administering to the transplant recipient a first amount of a JAK1/3 inhibitor comprising 5-(2-(4-fluoro-3-methoxy-5-methylphenylamino)-5-methylpyrimidin-4-ylamino)benzo[d]oxazol-2(3H)-one (Compound I) or a prodrug thereof and administering to the transplant recipient a second amount of a non-JAK1/3 inhibitor immunosuppressant, wherein the combined effect of the first amount and the second amount is greater than the effect of the first amount or the second amount individually, wherein the JAK1/3 inhibitor acts in combination with the non-JAK1/3 inhibitor immunosuppressant to inhibit or treat allograft rejection. In some embodiments at least one of the first amount or the second amount is individually a suboptimal dose for inhibiting or treating allograft rejection. In some examples, the combined effect of the first amount and the second amount to inhibit or treat allograft rejection in the transplant recipient is synergistic.
摘要翻译：本文公开了用于在移植受体中治疗或抑制同种异体移植排斥的方法。在一些实施方案中，所述方法包括向移植受体施用第一量的包含5-（2-（4-氟-3-甲氧基-5-甲基苯基氨基）-5-甲基嘧啶-4-基氨基）苯并[ [d]恶唑-2（3H） - 酮（化合物I）或其前药，向移植受体施用第二量的非JAK1 / 3抑制剂免疫抑制剂，其中第一量和第二量的组合效应大于第一量或第二量的作用，其中JAK1 / 3抑制剂与非JAK1 / 3抑制剂免疫抑制剂联合用于抑制或治疗同种异体移植排斥反应。在一些实施方案中，第一量或第二量中的至少一种量单独为抑制或治疗同种异体移植物排斥反应的次优剂量。在一些实例中，第一量和第二量在移植受体中抑制或治疗同种异体移植排斥的组合作用是协同的。

66. 发明申请

US20120230984A1 Methods of Treating or Preventing Autoimmune Diseases With 2,4-Pyrimidinediamine Compounds 有权
标题翻译：用2,4-嘧啶二胺化合物治疗或预防自身免疫性疾病的方法
公开(公告)号：US20120230984A1
公开(公告)日：2012-09-13
申请号：US13418696
申请日：2012-03-13
申请人： Rajinder Singh , Ankush Argade , Donald G. Payan , Jeffrey Clough , Holger Keim , Somasekhar Bhamidipati , Catherine Sylvain , Hui Li
发明人： Rajinder Singh , Ankush Argade , Donald G. Payan , Jeffrey Clough , Holger Keim , Somasekhar Bhamidipati , Catherine Sylvain , Hui Li
IPC分类号： A61K31/506 , A61K31/5383 , A61K31/56 , A61K31/616 , A61K31/519 , A61P37/06 , A61P37/08 , A61K39/395 , A61P7/06 , A61P25/00 , A61P7/00 , A61P27/02 , A61P21/04 , A61P1/16 , A61P13/12 , A61P29/00 , A61P19/02 , A61P19/04 , A61K31/538
CPC分类号： A61K31/506 , A61K31/519 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D413/12 , C07D413/14 , C07D471/04 , C07D498/04 , Y10S514/825 , Y10S514/903
摘要： The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.
摘要翻译：本发明提供了用2,4-嘧啶二胺化合物治疗或预防自身免疫疾病的方法，以及治疗，预防或改善与这些疾病相关的症状的方法。可以用化合物治疗或预防的自身免疫性疾病的具体实例包括类风湿性关节炎和/或其相关症状，系统性红斑狼疮病和/或其相关症状和多发性硬化症和/或其相关症状。

67. 发明授权

US08178671B2 Methods of treating or preventing autoimmune diseases with 2, 4-pyrimidinediamine compounds 有权
标题翻译：用2,4-嘧啶二胺化合物治疗或预防自身免疫性疾病的方法
公开(公告)号：US08178671B2
公开(公告)日：2012-05-15
申请号：US10903263
申请日：2004-07-30
申请人： Rajinder Singh , Ankush Argade , Hui Li , Somasekhar Bhamidipati , David Carroll , Catherine Sylvain , Jeffrey Clough , Holger Keim
发明人： Rajinder Singh , Ankush Argade , Hui Li , Somasekhar Bhamidipati , David Carroll , Catherine Sylvain , Jeffrey Clough , Holger Keim
IPC分类号： C07D239/48 , C07D403/12 , C07D403/14 , C07D413/12 , C07D417/12 , A61K31/506 , A61K31/498 , A61K31/5375 , A61K31/5383 , A61K31/5415 , A61P19/02
CPC分类号： C07D498/04 , A61K31/506 , A61K31/541 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/06
摘要： The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.
摘要翻译：本发明提供了用2,4-嘧啶二胺化合物治疗或预防自身免疫疾病的方法，以及治疗，预防或改善与这些疾病相关的症状的方法。可以用化合物治疗或预防的自身免疫性疾病的具体实例包括类风湿性关节炎和/或其相关症状，系统性红斑狼疮和/或其相关症状和多发性硬化症和/或其相关症状。

68. 发明申请

US20120108810A1 Prodrugs of 2,4-Pyrimidinediamine Compounds and Their Uses 有权
公开(公告)号：US20120108810A1
公开(公告)日：2012-05-03
申请号：US13349194
申请日：2012-01-12
申请人： Rajinder Singh , Somasekhar Bhamidipati , Thomas Sun , Valentino J. Stella
发明人： Rajinder Singh , Somasekhar Bhamidipati , Thomas Sun , Valentino J. Stella
IPC分类号： C07D498/04
CPC分类号： C07D498/04 , A61K31/5383 , A61K31/675 , C07F9/65583 , C07F9/6561 , C07F9/65742
摘要： The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.

69. 发明授权

US08168636B2 Polycyclic heteroaryl substituted triazoles useful as Axl inhibitors 有权
标题翻译：可用作Axl抑制剂的多环杂芳基取代的三唑
公开(公告)号：US08168636B2
公开(公告)日：2012-05-01
申请号：US12986951
申请日：2011-01-07
申请人： Dane Goff , Jing Zhang , Rajinder Singh , Sacha Holland , Jiaxin Yu , Thilo J. Heckrodt , Pingyu Ding , Joane Litvak
发明人： Dane Goff , Jing Zhang , Rajinder Singh , Sacha Holland , Jiaxin Yu , Thilo J. Heckrodt , Pingyu Ding , Joane Litvak
IPC分类号： A61K31/502 , C07D237/26
CPC分类号： C07D401/14 , A61K31/502 , C07D403/04 , C07D403/14 , C07D405/14 , C07D417/04 , C07D417/14 , C07D451/04 , C07D471/04 , C07D487/04 , C07D487/10 , C07D491/04 , C07D491/20 , C07D495/04 , C07D519/00
摘要： Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
摘要翻译：公开了多环杂芳基取代的三唑和含有这些化合物的药物组合物可用于抑制受体蛋白酪氨酸激酶Ax1的活性。还公开了使用该化合物治疗与Axl活性相关的疾病或病症的方法。

70. 发明授权

US08158621B2 Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds 有权
标题翻译：用2,4-嘧啶二胺化合物治疗或预防自身免疫性疾病的方法
公开(公告)号：US08158621B2
公开(公告)日：2012-04-17
申请号：US12691657
申请日：2010-01-21
申请人： Rajinder Singh , Ankush Argade , Jeffrey Clough , Holger Keim , Somasekhar Bhamidipati , Catherine Sylvain , Hui Li
发明人： Rajinder Singh , Ankush Argade , Jeffrey Clough , Holger Keim , Somasekhar Bhamidipati , Catherine Sylvain , Hui Li
IPC分类号： C07D498/04 , A61K31/538
CPC分类号： A61K31/506 , A61K31/519 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D413/12 , C07D413/14 , C07D471/04 , C07D498/04 , Y10S514/825 , Y10S514/903
摘要： The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.
摘要翻译：本发明提供了用2,4-嘧啶二胺化合物治疗或预防自身免疫疾病的方法，以及治疗，预防或改善与这些疾病相关的症状的方法。可以用化合物治疗或预防的自身免疫性疾病的具体实例包括类风湿性关节炎和/或其相关症状，系统性红斑狼疮病和/或其相关症状和多发性硬化症和/或其相关症状。

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