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1. 发明申请

WO2010083207A3 PROTEIN KINASE C INHIBITORS AND USES THEREOF 审中-公开
标题翻译：蛋白激酶C抑制剂及其用途
公开(公告)号：WO2010083207A3
公开(公告)日：2010-11-04
申请号：PCT/US2010020888
申请日：2010-01-13
申请人： RIGEL PHARMACEUTICALS INC , ZHAO HAORAN , KOLLURI RAO , VALDEZ CARLOS , TSO KIN , SINGH RAJINDER , RAMPHAL JOHN
发明人： ZHAO HAORAN , KOLLURI RAO , VALDEZ CARLOS , TSO KIN , SINGH RAJINDER , RAMPHAL JOHN
IPC分类号： C07D413/14 , A61K31/407 , A61K31/506 , A61P3/00 , A61P9/00 , A61P29/00 , C07D413/12
CPC分类号： C07D498/04 , A61K31/5383 , C07D498/14
摘要： 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.
摘要翻译：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。

2. 发明专利

AU2020378407A1 Heterocyclic RIP1 inhibitory compounds 未知
公开(公告)号：AU2020378407A1
公开(公告)日：2022-06-02
申请号：AU2020378407
申请日：2020-11-06
申请人： RIGEL PHARMACEUTICALS INC
发明人： CHEN YAN , YU JIAXIN , SHAW SIMON , DARWISH IHAB , TAYLOR VANESSA , BHAMIDIPATI SOMASEKHAR , LUO ZHUSHOU , KOLLURI RAO
IPC分类号： C07D491/10 , A61K31/553 , A61P29/00 , A61P37/00 , C07D401/14 , C07D403/14 , C07D413/14 , C07D471/08 , C07D471/10
摘要： Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The compounds may have a structure according to Formula (I). The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

3. 发明专利

CA3149926A1 RIP1 INHIBITORY COMPOUNDS AND METHODS FOR MAKING AND USING THE SAME 未知
公开(公告)号：CA3149926A1
公开(公告)日：2021-03-11
申请号：CA3149926
申请日：2020-09-04
申请人： RIGEL PHARMACEUTICALS INC
发明人： CHEN YAN , YU JIAXIN , SHAW SIMON , DARWISH IHAB , TAYLOR VANESSA , BHAMIDIPATI SOMASEKHAR , LUO ZHUSHOU , KOLLURI RAO
IPC分类号： A61K31/553 , A61P37/00 , C07D413/12 , C07D413/14
摘要： Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

4. 发明专利

CA2892677A1 PROTEIN KINASE C INHIBITORS AND USES THEREOF 未知
公开(公告)号：CA2892677A1
公开(公告)日：2014-06-12
申请号：CA2892677
申请日：2013-12-03
申请人： RIGEL PHARMACEUTICALS INC
发明人： MCMURTRIE DARREN , KOLLURI RAO , MASUDA ESTEBAN , TSO KIN , ALVAREZ SALVADOR , HECKRODT THILO , HOLLAND SACHA , KELLEY RYAN , DUNCTON MATTHEW , SINGH RAJINDER
IPC分类号： C07D455/02
摘要： 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 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.

5. 发明专利

AU2008275918B2 Cyclic amine substituted pyrimidinediamines as PKC inhibitors 未知
公开(公告)号：AU2008275918B2
公开(公告)日：2014-01-30
申请号：AU2008275918
申请日：2008-07-17
申请人： RIGEL PHARMACEUTICALS INC
发明人： RAMPHAL JOHN , TSO KIN , LI HUI , PAYAN DONALD G , GU SHIHAI , KOLLURI RAO , SINGH RAJINDER , ZHAO HAORAN
IPC分类号： C07D239/48 , A61K31/506 , A61P35/00 , C07D401/12 , C07D401/14 , C07D407/14 , C07D413/14 , C07D417/14 , C07D498/04
摘要： The invention encompasses Pyrimidine compounds and the compositions and methods using these compounds in the treatment of conditions in which inhibition of PKC and PKD is therapeutically useful.

6. 发明专利

CA2780759A1 PROTEIN KINASE C INHIBITORS AND USES THEREOF 未知
公开(公告)号：CA2780759A1
公开(公告)日：2011-06-09
申请号：CA2780759
申请日：2010-12-01
申请人： RIGEL PHARMACEUTICALS INC
发明人： SINGH RAJINDER , TSO KIN , ZHANG JING , DUNCTON MATTHEW , ALVAREZ SALVADOR , KOLLURI RAO , RAMPHAL JOHN , HOLLAND SACHA
IPC分类号： C07D401/14 , A61K31/41 , A61P29/00 , C07D405/14
摘要： This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseThis 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.ases 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.

7. 发明专利

AU2008275918A1 Cyclic amine substituted pyrimidinediamines as PKC inhibitors 未知
公开(公告)号：AU2008275918A1
公开(公告)日：2009-01-22
申请号：AU2008275918
申请日：2008-07-17
申请人： RIGEL PHARMACEUTICALS INC
发明人： SINGH RAJINDER , KOLLURI RAO , PAYAN DONALD G , TSO KIN , ZHAO HAORAN , GU SHIHAI , RAMPHAL JOHN , LI HUI
IPC分类号： C07D239/48 , A61K31/506 , A61P35/00 , C07D401/12 , C07D401/14 , C07D407/14 , C07D413/14 , C07D417/14 , C07D498/04

8. 发明专利

PE20221762A1 COMPUESTOS INHIBIDORES DE RIP1 Y METODOS PARA PREPARARLOS Y USARLOS 未知
公开(公告)号：PE20221762A1
公开(公告)日：2022-11-11
申请号：PE2022000317
申请日：2020-09-04
申请人： RIGEL PHARMACEUTICALS INC
发明人： CHEN YAN , YU JIAXIN , SHAW SIMON , DARWISH IHAB , TAYLOR VANESSA , BHAMIDIPATI SOMASEKHAR , LUO ZHUSHOU , KOLLURI RAO
IPC分类号： C07D471/04 , A61K31/55 , A61P37/00 , C07D487/04
摘要： En la presente descripcion se describen compuestos inhibidores de quinasa, tales como compuestos inhibidores de quinasa de proteina 1 que interactua con el receptor (RIP1), Referido a compuestos inhibidores de quinasa de proteina 1 que interactuan con el receptor (RIP1); en donde X es C o N; Y se selecciona de O, S y CH2; L es un heteroatomo, -CH2CH2-, cicloalquilo C3-6 o un resto divalente de Ra, caracterizado por ser alifatico C1-10, haloalifatico C1-10, entre otros; Z es alifatico C1-10, heteroaromatico o aromatico; R1 es independientemente un halogeno o un grupo enlazador R6, cuyo enlazador es Ra, siempre y cuando no represente H o D; R2 es Ra; R4 es independientemente oxo, heterociclilo C3-6, entre otros; el sistema de anillos A y B se sustituye opcionalmente con uno o mas grupos R4; y n es 0,1 o 2. Un compuesto seleccionado es (S)-3-(2-bencil-3-cloro-7-oxo-2,4,5,7-tetrahidro-6H-pirazolo[3,4-c]piridin-6-il)-8-(3-hidroxi-3-metilbut-1-in-1-il)-5-metil-2,3-dihidrobenzo[b][1,4]oxazepin-4(5H)-ona; ademas, estos compuestos pueden usarse para tratar o prevenir una enfermedad o afeccion asociada a RIP1.

9. 发明专利

BR112022002378A2 Compostos inibitórios de rip1 e métodos para preparação e uso dos mesmos 未知
公开(公告)号：BR112022002378A2
公开(公告)日：2022-06-14
申请号：BR112022002378
申请日：2020-09-04
申请人： RIGEL PHARMACEUTICALS INC
发明人： DARWISH IHAB , YU JIAXIN , KOLLURI RAO , SHAW SIMON , BHAMIDIPATI SOMASEKHAR , TAYLOR VANESSA , CHEN YAN , LUO ZHUSHOU
IPC分类号： C07D471/04 , A61K31/55 , A61P37/00 , C07D487/04
摘要： compostos inibitórios de rip1 e métodos para preparação e uso dos mesmos. a presente invenção refere-se a compostos inibitórios de cinase, tais como, compostos inibidores de proteína-1 cinase de interação com o receptor (rip1), bem como, as composições farmacêuticas e combinações compreendendo tais compostos inibitórios. os compostos descritos, composições farmacêuticas e/ou combinações podem ser usados para tratar ou prevenir uma doença ou condição associada à cinase, particularmente, uma doença ou condição associada à rip1.

10. 发明专利

ES2658395T3 Inhibidores de proteína cinasa C y usos de los mismos 未知
公开(公告)号：ES2658395T3
公开(公告)日：2018-03-09
申请号：ES13773141
申请日：2013-04-04
申请人： RIGEL PHARMACEUTICALS INC
发明人： SINGH RAJINDER , DUNCTON MATTHEW , ZHANG JING , ALVAREZ SALVADOR , TSO KIN , HOLLAND SACHA , YEN ROSE , KOLLURI RAO , HECKRODT THILO , CHEN YAN , MASUDA ESTEBAN , LI HUI , PAYAN DONALD G , KELLEY RYAN
IPC分类号： C07D471/04 , A61K31/437 , A61K31/506 , A61P29/00
摘要： Un compuesto de fórmula (VI): **(Ver fórmula)** en la que R1, R2, R3, R4, R5, y R6 se seleccionan independientemente de hidrógeno, alquilo, alquilo sustituido, alcoxi, alcoxi sustituido, acilo, acilamino, aciloxi, amino, amino sustituido, aminoacilo, aminoaciloxi, oxiaminoacilo, azido, ciano, halógeno, hidroxilo, carboxilo, carboxilalquilo, tiol, tioalcoxi, tioalcoxi sustituido, arilo, ariloxi, hidroxiamino, alcoxiamino, nitro, -SO-alquilo, -SO-alquilo sustituido, -SO-arilo, -SO-heteroarilo, -SO2-alquilo, -SO2-alquilo sustituido, -SO2-arilo y -SO2-heteroarilo; o R1 y R2 juntos forman un grupo oxo; o R3 y R4 juntos forman un grupo oxo; o R5 y R6 juntos forman un grupo oxo; R7, R8, R9, y R10 se seleccionan independientemente de hidrógeno, alquilo, alquilo sustituido, alcoxi, alcoxi sustituido, acilo, acilamino, aciloxi, amino, amino sustituido, aminoacilo, aminoaciloxi, oxiaminoacilo, azido, ciano, halógeno, hidroxilo, carboxilo, carboxilalquilo, tiol, tioalcoxi, tioalcoxi sustituido, arilo, ariloxi, hidroxiamino, alcoxiamino, nitro, -SO-alquilo, -SO-alquilo sustituido, -SO-arilo, -SO-heteroarilo, -SO2-alquilo, -SO2-alquilo sustituido, -SO2-arilo y -SO2-heteroarilo; o R7 y R8 juntos forman un grupo oxo; o R9 y R10 juntos forman un grupo oxo; R11 se selecciona de alquilo, alquilo sustituido, cicloalquilo, cicloalquilo sustituido, hidroxi, alcoxi, alcoxi sustituido, amino, amino sustituido, carboxilo, éster carboxílico, ciano, halógeno, tiol, tioalcoxi, tioalcoxi sustituido, acilo, aminoacilo, nitro, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, -SO-alquilo, -SO-alquilo sustituido, - SO-arilo, -SO-heteroarilo, -SO2-alquilo, -SO2-alquilo sustituido, -SO2-arilo y -SO2-heteroarilo; R20 se selecciona de hidrógeno, alquilo y alquilo sustituido; G es -NY2Ar1; Y1 e Y2 se seleccionan independientemente de hidrógeno, alquilo y alquilo sustituido; y Ar1 se selecciona de arilo, arilo sustituido, heteroarilo, y heteroarilo sustituido; o una sal o estereoisómero del mismo; en la que: "alquilo" es un grupo hidrocarbilo alifático saturado monovalente que tiene de 1 a 6 átomos de carbono; "alcoxi" es un grupo -O-alquilo; "alquenilo" es un grupo hidrocarbilo de cadena lineal o ramificada que tiene de 2 a 6 átomos de carbono y que tiene al menos 1 sitio de insaturación de doble enlace; y "alquinilo" es un grupo hidrocarbilo lineal o ramificado que tiene de 2 a 6 átomos de carbono y que tiene al menos 1 sitio de insaturación de triple enlace.

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