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公开(公告)号:US20140275055A1
公开(公告)日:2014-09-18
申请号:US14209997
申请日:2014-03-13
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: C07D471/04 , C07D498/04
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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42.
公开(公告)号:US20140213555A1
公开(公告)日:2014-07-31
申请号:US14163822
申请日:2014-01-24
Applicant: Rigel Pharmaceuticals, Inc.
Inventor: Esteban Masuda , Rajinder Singh , Vanessa Taylor , Donald G. Payan
IPC: C07D413/12 , C07F9/653
CPC classification number: C07D413/12 , A61K31/506 , A61K31/675 , A61K45/06 , C07F9/65324 , Y10T436/141111 , A61K2300/00
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.
Abstract translation: 公开了用于治疗和/或预防自身免疫疾病的方法的化合物和实施方案。 该方法包括向具有自身免疫性疾病如炎症性肠病的受试者施用治疗有效量的式I化合物,其中X和Y独立地为O或NR 1; 每个R 1独立地为H或C 1 -C 6烷基; 环A是芳基; 每个R 2独立地是与它们所连接的原子或原子一起形成的H,烷基,烷氧基,酰胺,氰基,卤素,卤代烷基,羟基烷基,杂烷基,杂环基,磺酰基,磺酰胺或两个R 2基团 4-10元环系; p为0,1,2,3或4; R3和R4独立地是H或C1-C6烷基; 且R 5为卤素,氰基或C 1 -C 6烷基。
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公开(公告)号:US11220496B2
公开(公告)日:2022-01-11
申请号:US16551431
申请日:2019-08-26
Applicant: Rigel Pharmaceuticals, Inc.
Inventor: Esteban Masuda , Rajinder Singh , Vanessa Taylor , Donald G. Payan
IPC: C07D413/12 , C07F9/653 , A61K31/675 , A61K45/06 , A61K31/506
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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44.
公开(公告)号:US20210379064A1
公开(公告)日:2021-12-09
申请号:US17351996
申请日:2021-06-18
Applicant: Rigel Pharmaceuticals, Inc.
Inventor: Yasumichi Hitoshi , Sacha Holland , Donald G. Payan
IPC: A61K31/502 , A61K45/06 , A61K31/4196 , A61K33/243 , C07D403/04 , C07D403/14
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.
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公开(公告)号:US10828301B2
公开(公告)日:2020-11-10
申请号:US16402912
申请日:2019-05-03
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: 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 , C07D239/48 , 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
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:US10314840B2
公开(公告)日:2019-06-11
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. Rossi
IPC: A61K31/505 , A61K31/519 , C07D239/48 , 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
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:US10005777B2
公开(公告)日:2018-06-26
申请号:US15588410
申请日:2017-05-05
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: C07D471/04 , C12Q1/48 , A61K31/506 , A61K31/538 , C12N9/12 , A61K31/5383 , A61K31/5386 , A61K31/553 , C07D519/00 , A61K31/5377
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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公开(公告)号:US09586908B2
公开(公告)日:2017-03-07
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 , 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 , A61K31/505 , 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.
Abstract translation: 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:US09162989B2
公开(公告)日:2015-10-20
申请号:US14626471
申请日:2015-02-19
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 , 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 , A61K31/505 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/551 , A61K45/06 , C07D498/04 , C07D265/36 , A61K31/5395 , C07D495/04 , C07F5/02 , C07D498/14
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.
Abstract translation: 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:US08927564B2
公开(公告)日:2015-01-06
申请号:US13789289
申请日:2013-03-07
Applicant: Rigel Pharmaceuticals, Inc.
Inventor: Dane Goff , Donald G. Payan , Sylvia Braselmann
IPC: C07D487/14 , C07D471/04 , C07D471/14 , C07D471/22 , C07D487/04 , C07D491/22 , A61K31/437 , C07D513/04 , C07D491/147 , C07D495/14 , C07D495/22 , C07D498/04 , C07D513/14
CPC classification number: C07D471/06 , C07D471/04 , C07D471/14 , C07D471/16 , C07D471/22 , C07D487/04 , C07D487/06 , C07D487/14 , C07D487/16 , C07D491/147 , C07D491/22 , C07D495/14 , C07D495/22 , C07D498/04 , C07D513/04 , C07D513/14
Abstract: Disclosed embodiments concern polycyclic alkaloid compounds and methods for their use and synthesis. Particular embodiments concern polycyclic alkaloids having a fused, six-membered ring, while other embodiments concern polycyclic alkaloids having a fused, five-membered ring. Methods for making the polycyclic alkaloids are disclosed, as well as methods for their use as prophylactics or treatments for certain diseases. Also disclosed are pharmaceutical compositions comprising the polycyclic alkaloids and their use.
Abstract translation: 公开的实施方案涉及多环生物碱化合物及其使用和合成方法。 具体实施方案涉及具有稠合六元环的多环生物碱,而其它实施方案涉及具有稠合五元环的多环生物碱。 公开了制备多环生物碱的方法,以及用作某些疾病的预防或治疗方法。 还公开了包含多环生物碱及其用途的药物组合物。
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