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21.发明授权公开(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。
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22.发明授权Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds 有权用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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23.发明授权公开(公告)号：US08097630B2
公开(公告)日：2012-01-17
申请号：US11870362
申请日：2007-10-10
申请人： Rajinder Singh , Pingyu Ding , Sacha Holland , Dane Goff
发明人： Rajinder Singh , Pingyu Ding , Sacha Holland , Dane Goff
IPC分类号： A01N43/54 , C07D239/42 , C07D239/02
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12 , C07D413/12
摘要： Pinane-substituted pyrimidinediamine derivatives and pharmaceutical compositions containing the derivatives are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the derivatives in treating diseases or conditions associated with Axl catalytic activity are also disclosed.
摘要翻译： 公开了含有衍生物的蒎烷取代的嘧啶二胺衍生物和药物组合物可用于抑制受体蛋白酪氨酸激酶Ax1的活性。 还公开了使用衍生物治疗与Axl催化活性相关的疾病或病症的方法。
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24.发明申请BRIDGED BICYCLIC ARYL AND BRIDGED BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS 有权桥双环芳基和桥双环杂芳基取代三唑有用AS AXL抑制剂公开(公告)号：US20110281846A1
公开(公告)日：2011-11-17
申请号：US13191252
申请日：2011-07-26
申请人： Dane Goff , Jing Zhang , Rajinder Singh , Sacha Holland , Jiaxin Yu , Pingyu Ding , Joane Litvak
发明人： Dane Goff , Jing Zhang , Rajinder Singh , Sacha Holland , Jiaxin Yu , Pingyu Ding , Joane Litvak
IPC分类号： A61K31/55 , A61K31/5377 , A61K31/502 , A61K31/497 , A61K31/496 , A61K31/519 , A61K31/439 , A61P35/02 , A61P19/02 , A61P17/06 , A61P27/02 , A61P3/10 , A61P13/12 , A61P19/10 , A61P9/00 , A61P27/12 , A61P35/00 , A61K31/5513
CPC分类号： C07D495/04 , C07D249/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D409/14 , C07D453/06 , C07D471/18
摘要： Bridged bicyclic aryl or 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： 公开了桥连双环芳基或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。
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公开(公告)号：US08053434B2
公开(公告)日：2011-11-08
申请号：US12552125
申请日：2009-09-01
申请人： Pingyu Ding , Ankush Argade , Dane Goff , Rajinder Singh , Esteban Masuda , Vanessa Taylor , Sacha Holland
发明人： Pingyu Ding , Ankush Argade , Dane Goff , Rajinder Singh , Esteban Masuda , Vanessa Taylor , Sacha Holland
IPC分类号： C07D239/84 , C07D487/14 , C07D413/14 , A61K31/517 , A61K31/519 , A61K31/5355 , A61P35/00 , A61P19/02 , A61P9/10 , A61P17/06 , A61P3/14 , A61P37/08 , A61P1/18
CPC分类号： C07D519/00 , A61K31/517 , C07D239/94 , C07D239/95 , C07D471/04 , C07D473/16 , C07D487/04 , C07D495/04 , C07D495/12
摘要： The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity. The compounds of the present invention are according to structural formula (I): or a salt or N-oxide thereof, wherein B is selected from
摘要翻译： 本公开提供了抑制蛋白激酶（例如JAK，Ax1或Syk激酶）的化合物，包含该化合物的组合物和使用该化合物抑制蛋白激酶并治疗和/或预防与不适当激酶活性相关疾病的方法。 本发明的化合物是根据结构式（I）：或其盐或N-氧化物，其中B选自
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公开(公告)号：US20110144059A1
公开(公告)日：2011-06-16
申请号：US11943506
申请日：2007-11-20
IPC分类号： A61K31/675 , C07F9/6561 , A61P37/00 , A61P19/02 , A61P1/04 , A61P1/16 , A61P25/00
CPC分类号： A61K31/675 , A61K9/0053 , C07D498/04 , C07F9/6561
摘要： The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, salts and hydrates of the prodrugs, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.
摘要翻译： 本公开提供了前体药物的生物活性2,4-嘧啶二胺化合物，盐和水合物的前药，包含前体药物的组合物，用于合成前药的中间体和方法以及在各种应用中使用前药的方法。
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公开(公告)号：US20110124599A1
公开(公告)日：2011-05-26
申请号：US12950612
申请日：2010-11-19
IPC分类号： A61K31/5383 , C07D498/04 , A61P29/00 , A61P17/02 , A61P37/06 , A61K31/675 , C12N9/99 , C12N5/071
CPC分类号： C07D498/04 , C07F9/6561
摘要： The present disclosure provides biologically active 2,4-pyrimidinediamine compounds of formulae (I)-(III): and salts thereof, compositions comprising these compounds, and methods of using these compounds in a variety of applications.
摘要翻译： 本公开提供式（I） - （III）的生物活性2,4-嘧啶二胺化合物及其盐，包含这些化合物的组合物，以及在各种应用中使用这些化合物的方法。
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公开(公告)号：US20110098274A1
公开(公告)日：2011-04-28
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： A61K31/55 , C07D249/14 , C07D237/26 , C07D223/18 , C07D285/36 , A61K31/4196 , A61K31/502 , A61P35/00
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.
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公开(公告)号：US07915293B2
公开(公告)日：2011-03-29
申请号：US10858537
申请日：2004-06-01
IPC分类号： A61K31/4545 , C07D41/02
CPC分类号： C07C323/49 , C07C233/75 , C07C275/34 , C07C311/21 , C07C311/29 , C07C311/48 , C07C311/51 , C07C311/64 , C07C317/34 , C07C335/42 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07D207/16 , C07D207/26 , C07D207/325 , C07D209/08 , C07D211/46 , C07D211/58 , C07D213/42 , C07D213/64 , C07D213/76 , C07D213/78 , C07D215/40 , C07D217/02 , C07D231/56 , C07D235/30 , C07D239/34 , C07D239/42 , C07D261/16 , C07D265/36 , C07D295/13 , C07D295/26 , C07D307/14 , C07D307/91 , C07D317/66 , C07D319/20 , C07D333/36 , C07D401/12
摘要： This invention describes compounds useful as ubiquitin ligase inhibitors. The compounds of the invention are useful as inhibitors of the biochemical pathways of organisms in which ubiquitination is involved. The invention also provides for pharmaceutical compositions comprising the compounds described in the invention for the treatment of conditions that require inhibition of ubiquitin ligases. Furthermore, the invention provides for methods of inhibiting ubiquitination in a cell comprising contacting a cell in which inhibition of ubiquitination is desired with a compound according to the invention.
摘要翻译： 本发明描述了可用作泛素连接酶抑制剂的化合物。 本发明的化合物可用作涉及泛素化的生物体的生物化学途径的抑制剂。 本发明还提供了包含本发明所述化合物用于治疗需要抑制泛素连接酶的病症的药物组合物。 此外，本发明提供了抑制细胞泛素化的方法，包括使需要泛素化抑制的细胞与根据本发明的化合物接触。
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30.发明申请BICYCLIC ARYL AND BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS 有权双相ARYL和双相异构体取代三唑类有用的AXL抑制剂公开(公告)号：US20110071133A1
公开(公告)日：2011-03-24
申请号：US12957822
申请日：2010-12-01
申请人： Dane Goff , Jing Zhang , Rajinder Singh , Sacha Holland , Jiaxin Yu , Pingyu Ding , Thilo J. Heckrodt , Joane Litvak
发明人： Dane Goff , Jing Zhang , Rajinder Singh , Sacha Holland , Jiaxin Yu , Pingyu Ding , Thilo J. Heckrodt , Joane Litvak
IPC分类号： A61K31/551 , A61K31/502 , A61K31/496 , A61K31/517 , A61K31/5377 , A61K31/55 , A61P29/00 , A61P9/00 , A61P17/06 , A61P19/10 , A61P35/00 , A61P13/12
CPC分类号： A61K31/519 , A61K31/395 , C07D401/14 , C07D403/04 , C07D403/14 , C07D417/14 , C07D495/04
摘要： Bicyclic aryl substituted triazoles or 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： 公开了双环芳基取代的三唑或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。
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