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公开(公告)号:US20180002297A1
公开(公告)日:2018-01-04
申请号:US15617900
申请日:2017-06-08
Applicant: Rigel Pharmaceuticals, Inc.
Inventor: Matthew Duncton , Rajinder Singh
IPC: C07D257/04 , A61K31/41 , C07D487/04 , C07D471/04 , C07D413/10 , C07D403/14 , C07D403/12 , C07D403/06 , C07D401/14 , C07D401/12 , C07D401/10 , C07D401/04 , A61K31/58 , A61K31/55 , A61K31/546 , A61K31/519 , A61K31/506 , A61K31/496 , A61K31/4709 , A61K31/4245 , A61K31/4184 , C07D501/16 , C07J43/00
CPC classification number: C07D257/04 , A61K31/41 , A61K31/4155 , A61K31/4184 , A61K31/4245 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/5383 , A61K31/546 , A61K31/55 , A61K31/58 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D413/10 , C07D471/04 , C07D487/04 , C07D498/06 , C07D501/16 , C07D501/46 , C07J9/005 , C07J43/003
Abstract: The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
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公开(公告)号:US20170360786A1
公开(公告)日:2017-12-21
申请号:US15395606
申请日:2016-12-30
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
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.
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公开(公告)号:US09845307B2
公开(公告)日:2017-12-19
申请号:US15423436
申请日:2017-02-02
Applicant: Rigel Pharmaceuticals, Inc.
Inventor: Matthew Duncton , Rajinder Singh
IPC: C07D401/04 , C07D255/02 , C07D257/04
CPC classification number: C07D401/04 , C07D249/12 , C07D255/02 , C07D257/04
Abstract: Aspects of the present disclosure include compounds that activate Nrf2. Such compounds find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate to pharmaceutical compositions that include 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:US20170217932A1
公开(公告)日:2017-08-03
申请号:US15422246
申请日:2017-02-01
Applicant: RIGEL PHARMACEUTICALS, INC.
Inventor: Matthew Duncton , Rajinder Singh
IPC: C07D401/14 , C07D401/04
CPC classification number: C07D401/14 , C07D401/04
Abstract: Aspects of the present disclosure include compounds that activate Nrf2. Such compounds may find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate to pharmaceutical compositions that include 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:US20170129862A1
公开(公告)日:2017-05-11
申请号:US15233676
申请日:2016-08-10
Applicant: RIGEL PHARMACEUTICALS, INC.
Inventor: Matthew Duncton , Rajinder Singh
IPC: C07D257/04 , C07D403/14 , C07D401/12 , C07D403/12 , C07D401/10 , C07D413/10 , C07D501/16 , C07D401/14 , C07J43/00 , C07D401/04 , C07D487/04 , C07D471/04 , A61K31/41 , A61K31/4184 , A61K31/4709 , A61K31/4245 , A61K31/546 , A61K31/55 , A61K31/496 , A61K31/58 , A61K31/506 , A61K31/519 , C07D403/06
CPC classification number: C07D257/04 , A61K31/41 , A61K31/4155 , A61K31/4184 , A61K31/4245 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/5383 , A61K31/546 , A61K31/55 , A61K31/58 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D413/10 , C07D471/04 , C07D487/04 , C07D498/06 , C07D501/16 , C07D501/46 , C07J9/005 , C07J43/003
Abstract: The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
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公开(公告)号:US09439888B2
公开(公告)日:2016-09-13
申请号:US15005773
申请日:2016-01-25
Applicant: RIGEL PHARMACEUTICALS, INC.
Inventor: Matthew Duncton , Rajinder Singh
IPC: A61K31/4155 , A61K31/519 , A61K31/5383 , A61K31/4725 , A61K31/517 , C07D403/12 , C07D471/12 , C07D401/12 , C07D498/06 , C07D403/10 , C07D471/04
CPC classification number: C07D257/04 , A61K31/41 , A61K31/4155 , A61K31/4184 , A61K31/4245 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/5383 , A61K31/546 , A61K31/55 , A61K31/58 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D413/10 , C07D471/04 , C07D487/04 , C07D498/06 , C07D501/16 , C07D501/46 , C07J9/005 , C07J43/003
Abstract: The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
Abstract translation: 本公开提供了包含活性剂的羧基的四唑酮衍生物的化合物。 本公开还涉及包括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,以及制备这些化合物的方法。
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公开(公告)号:US20160257681A1
公开(公告)日:2016-09-08
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: C07D471/04 , A61K31/5383 , C07D519/00 , C12N9/12 , A61K31/5386 , A61K31/553 , A61K31/5377 , C12Q1/48 , A61K31/506 , A61K31/538
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: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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公开(公告)号:US08754251B2
公开(公告)日:2014-06-17
申请号:US13912000
申请日:2013-06-06
Applicant: Rigel Pharmaceuticals, Inc.
Inventor: Matthew Duncton , Martin D. Burke
CPC classification number: C07F5/025 , C07C17/263 , C07C2601/02 , C07J1/0059 , C07J31/006 , Y02P20/55 , C07C22/08
Abstract: Provided are protected cyclopropylboronic acids that include a substituted cyclopropyl group and a boronic ester group having a protecting group. The protecting group is a pinene-derived iminodiacetic acid (PIDA) group or PIDA-based group.
Abstract translation: 提供包括取代的环丙基和具有保护基的硼酸酯基的保护的环丙基硼酸。 保护基是蒎烯衍生的亚氨基二乙酸(PIDA)组或基于PIDA的组。
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公开(公告)号:US20130210810A1
公开(公告)日:2013-08-15
申请号:US13718632
申请日:2012-12-18
Applicant: Rigel Pharmaceuticals, Inc.
Inventor: Rajinder Singh , Hui Li , Haoran Zhao , Rao Kolluri , Kin Tso , John Ramphal , Shihai Gu , Carlos Valdez , Jing Zhang , Emily Stauffer , Matthew Duncton , Salvador Alvarez
IPC: A61K31/506 , A61K31/55 , A61K31/538 , A61K31/5377
CPC classification number: A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/55 , C07D401/12 , C07D401/14 , C07D413/12
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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