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公开(公告)号：US10414758B2
公开(公告)日：2019-09-17
申请号：US15875897
申请日：2018-01-19
Applicant: Rigel Pharmaceuticals, Inc.
Inventor： Esteban Masuda , Rajinder Singh , Vanessa Taylor , Donald G. Payan
IPC: A61K31/506 , A61K31/675 , C07D413/12 , C07F9/653 , A61K45/06
Abstract: Compounds and embodiments of a method for treating and/or preventing autoimmune diseases are disclosed. The method includes administering to a subject having an autoimmune disease, such as an inflammatory bowel disease, a therapeutically effective amount of a compound according to formula I wherein X and Y independently are O or NR1; each R1 is independently H or C1-C6 alkyl; ring A is aryl; each R2 independently is H, alkyl, alkoxy, amide, cyano, halo, haloalkyl, hydroxyalkyl, heteroalkyl, heterocyclyl, sulfonyl, sulfonamide, or two R2 groups, taken together with the atom or atoms to which they are attached, combine to form a 4-10 membered ring system; p is 0, 1, 2, 3, or 4; R3 and R4 independently are H or C1-C6 alkyl; and R5 is halo, cyano, or C1-C6 alkyl.
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公开(公告)号：US20190060310A1
公开(公告)日：2019-02-28
申请号：US15918929
申请日：2018-03-12
Applicant: Rigel Pharmaceuticals, Inc.
Inventor： Rajinder Singh , Matthew Duncton , Jing Zhang , Salvador Alvarez , Kin Tso , Sacha Holland , Rose Yen , Rao Kolluri , Thilo Heckrodt , Yan Chen , Esteban Masuda , Hui Li , Donald G. Payan
IPC: A61K31/506 , C07D498/04 , C07D471/04
Abstract: 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.
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公开(公告)号：US20170246167A1
公开(公告)日：2017-08-31
申请号：US15443145
申请日：2017-02-27
Applicant: Rigel Pharmaceuticals, Inc
Inventor： Rajinder Singh , Ankush Argade , Donald G. Payan , Susan Molineaux , Sacha J. Holland , Jeffrey Clough , Holger Keim , Somasekhar Bhamidipati , Catherine Sylvain , Hui Li , Alexander B. Rossii
IPC: A61K31/505 , A61K31/5377 , A61K31/506
CPC classification number: 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
Abstract: 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：US09682976B2
公开(公告)日：2017-06-20
申请号：US15056535
申请日：2016-02-29
Applicant: Rigel Pharmaceuticals, Inc.
Inventor： Rajinder Singh , Matthew Duncton , Jing Zhang , Salvador Alvarez , Kin Tso , Sacha Holland , Rose Yen , Rao Kolluri , Thilo Heckrodt , Yan Chen , Esteban Masuda , Hui Li , Donald G. Payan , Ryan Kelley
IPC: A61K31/5383 , A61K31/5386 , A61K31/506 , A61K31/553 , A61K31/538 , A61K31/5377 , C07D519/00 , C07D471/04 , C12Q1/48 , C12N9/12
CPC classification number: C07D471/04 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/5386 , A61K31/553 , C07D519/00 , C12N9/12 , C12Q1/485 , C12Y207/11013
Abstract: 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.
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25.发明申请AXL INHIBITORS FOR USE IN COMBINATION THERAPY FOR PREVENTING, TREATING OR MANAGING METASTATIC CANCER 审中-公开用于组合治疗的AXL抑制剂用于预防，治疗或管理分子癌公开(公告)号：US20170042891A1
公开(公告)日：2017-02-16
申请号：US15077648
申请日：2016-03-22
Applicant: Rigel Pharmaceuticals, Inc.
Inventor： Yasumichi Hitoshi , Sacha Holland , Donald G. Payan
IPC: A61K31/502 , A61K33/24 , A61K45/06
CPC classification number: A61K31/502 , A61K31/4196 , A61K33/24 , A61K45/06 , C07D403/04 , C07D403/14 , A61K2300/00
Abstract: 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.
Abstract translation: 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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Patent Agency Ranking
公开(公告)号：US09566278B2
公开(公告)日：2017-02-14
申请号：US14849376
申请日：2015-09-09
Applicant: Rigel Pharmaceuticals, Inc.
Inventor： Rajinder Singh , Matthew Duncton , Jing Zhang , Salvador Alvarez , Kin Tso , Sacha Holland , Rose Yen , Rao Kolluri , Thilo Heckrodt , Yan Chen , Esteban Masuda , Hui Li , Donald G. Payan
IPC: C12N9/99 , C07D471/04 , C07D498/04 , A61K31/506
CPC classification number: A61K31/506 , C07D471/04 , C07D498/04 , Y02A50/411
Abstract: 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.
Abstract translation: 本公开涉及可用作蛋白激酶C（PKC）的抑制剂的化合物，因此可用于治疗通过PKC的活性介导或维持的多种疾病和病症。 本公开还涉及包含这些化合物的药物组合物，使用这些化合物治疗各种疾病和病症的方法，制备这些化合物的方法和可用于这些方法的中间体。
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公开(公告)号：US09540334B2
公开(公告)日：2017-01-10
申请号：US14812829
申请日：2015-07-29
Applicant: Rigel Pharmaceuticals, Inc.
Inventor： Rajinder Singh , Ankush Argade , Donald G. Payan , Susan Molineaux , Sacha J. Holland , Jeffrey Clough , Holger Keim , Somasekhar Bhamidipati , Catherine Sylvain , Hui Li , Alexander B. Rossi
IPC: C07D239/48 , A61K31/505 , A61K31/519 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/551 , A61K45/06 , C07D498/04 , C07D265/36 , A61K31/5395 , C07D495/04 , C07F5/02 , C07D498/14 , C07D407/14
CPC classification number: 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
Abstract: 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：US20160009660A1
公开(公告)日：2016-01-14
申请号：US14858661
申请日：2015-09-18
Applicant: Rigel Pharmaceuticals, Inc
Inventor： Rajinder Singh , Ankush Argade , Donald G. Payan , Susan Molineaux , Sacha J. Holland , Jeffrey Clough , Holger Keim , Somasekhar Bhamidipati , Catherine Sylvain , Hui Li , Alexander B. Rossi
IPC: C07D239/48
CPC classification number: 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
Abstract: 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：US08853397B2
公开(公告)日：2014-10-07
申请号：US13759835
申请日：2013-02-05
Applicant: Rigel Pharmaceuticals, Inc.
Inventor： Rajinder Singh , Ankush Argade , Donald G. Payan , Susan Molineaux , Sacha J. Holland , Jeffrey Clough , Holger Keim , Somasekhar Bhamidipati , Catherine Sylvain , Hui Li , Alexander B. Rossi
IPC: C07D239/48 , A61K31/506 , C07D413/12 , C07D401/12 , A61K31/551 , C07D409/12 , C07D409/14 , A61K31/538 , C07D417/12 , A61K31/519 , C07D405/14 , C07D401/14 , C07D403/14 , C07D265/36 , A61K31/5383 , A61K31/505 , A61K45/06 , C07D413/10 , C07D413/14 , A61K31/5377 , C07D498/04 , C07D405/12 , C07D417/14 , C07D403/12
CPC classification number: 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
Abstract: 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：US08822685B2
公开(公告)日：2014-09-02
申请号：US13961780
申请日：2013-08-07
Applicant: Rigel Pharmaceuticals, Inc.
Inventor： Rajinder Singh , Ankush Argade , Donald G. Payan , Susan Molineaux , Sacha J. Holland , Jeffrey Clough , Holger Keim , Somasekhar Bhamidipati , Catherine Sylvain , Hui Li , Alexander B. Rossi
IPC: C07D239/48 , A61K31/505 , C07D405/14 , A61K31/551 , C07D403/12 , C07D409/14 , A61K31/5383 , C07D413/14 , C07D413/10 , A61K31/5377 , C07D405/12 , C07D265/36 , C07D401/14 , C07D498/04 , C07D409/12 , A61K31/519 , C07D401/12 , C07D417/14 , C07D403/14 , C07D413/12 , A61K31/506 , A61K31/538 , C07D417/12 , A61K45/06
CPC classification number: 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
Abstract: 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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