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公开(公告)号：US20130018051A1
公开(公告)日：2013-01-17
申请号：US13620010
申请日：2012-09-14
申请人： Rajinder Singh , Sacha Holland , Joane Litvak , Dane Goff , Jing Zhang , Thilo J. Heckrodt
发明人： Rajinder Singh , Sacha Holland , Joane Litvak , Dane Goff , Jing Zhang , Thilo J. Heckrodt
IPC分类号： C07D471/18 , A61K31/439 , C07D401/14 , A61K31/4545 , A61K31/4748 , A61K31/502 , C07D405/14 , C07D403/14 , A61K31/517 , A61K31/519 , C12P13/00 , C12P17/10 , A61P29/00 , A61P19/02 , A61P9/00 , A61P17/06 , A61P27/02 , A61P9/10 , A61P13/12 , A61P19/10 , A61P27/12 , A61P35/00 , A61P35/02 , A61P35/04 , A61K31/4709
CPC分类号： C07D403/04 , A61K31/502 , C07D221/22 , C07D237/26 , C07D237/34 , C07D401/14 , C07D403/14 , C07D471/18
摘要： Bridged bicyclic 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：US20110092502A1
公开(公告)日：2011-04-21
申请号：US12978260
申请日：2010-12-23
申请人： Dane Goff , Jing Zhang , Rajinder Singh , Sacha Holland
发明人： Dane Goff , Jing Zhang , Rajinder Singh , Sacha Holland
IPC分类号： A61K31/5377 , A61K31/517 , A61K31/4439 , A61K31/498 , A61K31/4725 , A61K31/428 , A61K31/519 , A61P15/00 , A61P35/00 , A61P29/00 , A61P19/00 , A61P27/02 , A61P17/06 , A61P13/12 , A61P9/00
CPC分类号： C07D417/04 , C07D495/04
摘要： Diaminothiazoles and pharmaceutical compositions containing them are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the diaminothiazoles in treating diseases or conditions associated with Axl activity are also disclosed.
摘要翻译： 公开了含有它们的二氨基噻唑和药物组合物可用于抑制受体蛋白酪氨酸激酶Ax1的活性。 还公开了使用二氨基噻唑治疗与Axl活性相关的疾病或病症的方法。
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公开(公告)号：US20110082131A1
公开(公告)日：2011-04-07
申请号：US12965545
申请日：2010-12-10
申请人： Rajinder Singh , Catherine Sylvain , Sacha Holland , Jing Zhang , John J. Partridge , Jeffrey Clough , Ankush Argade
发明人： Rajinder Singh , Catherine Sylvain , Sacha Holland , Jing Zhang , John J. Partridge , Jeffrey Clough , Ankush Argade
IPC分类号： A61K31/55 , A61K31/4196 , A61K31/5377 , A61K31/454 , A61K31/496 , A61K31/541 , A61K31/422 , A61K31/433 , A61K31/427 , A61K31/538 , A61K31/4709 , A61P35/00 , A61P19/02 , A61P17/06 , A61P3/10 , A61P13/12 , A61P27/12
CPC分类号： C07D403/12 , C07D249/14 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Methods of using triazole derivatives in treating diseases or conditions associated with Axl catalytic activity are disclosed.
摘要翻译： 公开了使用三唑衍生物治疗与Axl催化活性有关的疾病或病症的方法。
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4.发明申请AXL INHIBITORS FOR USE IN COMBINATION THERAPY FOR PREVENTING, TREATING OR MANAGING METASTATIC CANCER 有权用于组合治疗的AXL抑制剂用于预防，治疗或管理分子癌公开(公告)号：US20100196511A1
公开(公告)日：2010-08-05
申请号：US12688746
申请日：2010-01-15
CPC分类号： A61K31/502 , A61K31/4196 , A61K33/24 , A61K45/06 , C07D403/04 , C07D403/14 , A61K2300/00
摘要： This invention is directed to methods of preventing, treating or managing cancer, preferably metastatic cancer, in a patient. The methods comprise administering an effective amount of an Axl inhibitor in combination with the administration of an effective amount of one or more chemotherapeutic agents.
摘要翻译： 本发明涉及在患者体内预防，治疗或控制癌症，优选转移性癌症的方法。 所述方法包括与施用有效量的一种或多种化学治疗剂组合施用有效量的Axl抑制剂。
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公开(公告)号：US07550460B2
公开(公告)日：2009-06-23
申请号：US11782581
申请日：2007-07-24
申请人： Rajinder Singh , Ankush Argade , Donald Payan , Susan Molineaux , Sacha Holland , Jeffrey Clough , Holger Keim , Somasekhar Bhamidipati , Catherine Sylvain , Hui Li , Alexander Rossi
发明人： Rajinder Singh , Ankush Argade , Donald Payan , Susan Molineaux , Sacha Holland , Jeffrey Clough , Holger Keim , Somasekhar Bhamidipati , Catherine Sylvain , Hui Li , Alexander Rossi
IPC分类号： A61K31/535
CPC分类号： A61K31/505 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/5395 , A61K31/551 , A61K45/06 , C07D239/48 , C07D265/36 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/12 , C07D409/14 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D495/04 , C07D498/04 , C07D498/14 , C07F5/027
摘要： The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
摘要翻译： 本发明提供了抑制导致释放化学介质，中间体和合成化合物的方法的IgE和/或IgG受体信号级联的2,4-嘧啶二胺化合物和在多种情况下使用化合物的方法，包括 在治疗和预防以IgE和/或IgG受体信号传导级联的活化作用通过脱颗粒和其它方法释放化学介质引起或与之相关的疾病。
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公开(公告)号：US20070293523A1
公开(公告)日：2007-12-20
申请号：US11539049
申请日：2006-10-05
申请人： Rajinder Singh , Ankush Argade , Donald Payan , Susan Molineaux , Sacha Holland , Jeffrey Clough , Holger Keim , Somasekhar Bhamidipati , Catherine Sylvain , Hui Li , Alexander Rossi
发明人： Rajinder Singh , Ankush Argade , Donald Payan , Susan Molineaux , Sacha Holland , Jeffrey Clough , Holger Keim , Somasekhar Bhamidipati , Catherine Sylvain , Hui Li , Alexander Rossi
IPC分类号： A61K31/505 , A61K31/506 , A61P43/00 , C07D239/02 , C12N5/02 , C12N9/99
CPC分类号： A61K31/505 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/5395 , A61K31/551 , A61K45/06 , C07D239/48 , C07D265/36 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/12 , C07D409/14 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D495/04 , C07D498/04 , C07D498/14 , C07F5/027
摘要： The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
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公开(公告)号：US20070293522A1
公开(公告)日：2007-12-20
申请号：US11539041
申请日：2006-10-05
申请人： Rajinder SINGH , Ankush Argade , Donald Payan , Susan Molineaux , Sacha Holland , Jeffrey Clough , Holger Keim , Somasekhar Bhamidipati , Catherine Sylvain , Hui Li , Alexander Rossi
发明人： Rajinder SINGH , Ankush Argade , Donald Payan , Susan Molineaux , Sacha Holland , Jeffrey Clough , Holger Keim , Somasekhar Bhamidipati , Catherine Sylvain , Hui Li , Alexander Rossi
IPC分类号： A61K31/505 , A61K31/506 , A61P43/00 , C07D239/02 , C12N5/02 , C12N9/99
CPC分类号： A61K31/505 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/5395 , A61K31/551 , A61K45/06 , C07D239/48 , C07D265/36 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/12 , C07D409/14 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D495/04 , C07D498/04 , C07D498/14 , C07F5/027
摘要： The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
摘要翻译： 本发明提供了抑制导致释放化学介质，中间体和合成化合物的方法的IgE和/或IgG受体信号级联的2,4-嘧啶二胺化合物和在各种情况下使用化合物的方法，包括 在治疗和预防以IgE和/或IgG受体信号传导级联的活化作用通过脱颗粒和其它方法释放化学介质引起或与之相关的疾病。
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公开(公告)号：US20050250163A1
公开(公告)日：2005-11-10
申请号：US11060659
申请日：2005-02-16
申请人： James Lorens , Sacha Holland , Weiduan Xu
发明人： James Lorens , Sacha Holland , Weiduan Xu
IPC分类号： A61K31/7105 , A61K39/395 , G01N33/50 , G01N33/53 , G01N33/574
CPC分类号： G01N33/5029 , G01N33/5011 , G01N33/5064
摘要： The present invention relates to regulation of angiogenesis and tumorigenesis. The invention further relates to methods for identifying and using agents, including small organic molecules, antibodies, peptides, cyclic peptides, nucleic acids, antisense nucleic acids, RNAi, and ribozymes, that modulate angiogenesis via modulation of endothelial cell haptotaxis; as well as to the use of expression profiles and compositions in diagnosis and therapy of angiogenesis and cancer.
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9.发明授权Method for identifying compounds that inhibit or enhance activation of a transmembrane ligand for a receptor tyrosine kinase 失效用于鉴定抑制或增强受体酪氨酸激酶跨膜配体活化的化合物的方法公开(公告)号：US06413730B1
公开(公告)日：2002-07-02
申请号：US09214631
申请日：1999-03-12
申请人： Sacha Holland , Geraldine Mbamalu , Tony Pawson
发明人： Sacha Holland , Geraldine Mbamalu , Tony Pawson
IPC分类号： G01N3353
CPC分类号： C12N9/1205 , A61K38/00 , C07K14/4702 , C07K14/705 , C07K2319/00 , C12Q1/6897
摘要： A method of modulating the biological activity of a transmembrane ligand for an Elk-related receptor tyrosine kinase in a cell expressing the transmembrane ligand, comprising forming a complex between a purified and isolated oligomerized Elk-related receptor tyrosine kinase, or an isoform or an extracellular domain of the kinase, and a transmembrane ligand expressed on the cell, thereby affecting a pathway in the cell which is regulated by the transmembrane ligand.
摘要翻译： 一种调节表达跨膜配体的细胞中Elk相关受体酪氨酸激酶的跨膜配体的生物学活性的方法，包括在纯化和分离的寡聚化的Elk相关受体酪氨酸激酶或同种型或细胞外 激酶的结构域和在细胞上表达的跨膜配体，从而影响由跨膜配体调节的细胞中的途径。
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10.发明授权公开(公告)号：US08658669B2
公开(公告)日：2014-02-25
申请号：US13620010
申请日：2012-09-14
申请人： Rajinder Singh , Sacha Holland , Joane Litvak , Dane Goff , Jing Zhang , Thilo J. Heckrodt
发明人： Rajinder Singh , Sacha Holland , Joane Litvak , Dane Goff , Jing Zhang , Thilo J. Heckrodt
CPC分类号： C07D403/04 , A61K31/502 , C07D221/22 , C07D237/26 , C07D237/34 , C07D401/14 , C07D403/14 , C07D471/18
摘要： Bridged bicyclic 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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