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.

公开(公告)号：US09266912B2

公开(公告)日：2016-02-23

申请号：US14310312

申请日：2014-06-20

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rajinder Singh ,  Somasekhar Bhamidipati ,  Esteban Masuda ,  Thomas Sun ,  Valentino J. Stella

IPC: C07D498/04 ,  C07F9/6561 ,  C07F9/6574 ,  C07F9/6558

CPC classification number: C07D498/04 ,  A61K31/5383 ,  A61K31/675 ,  C07F9/65583 ,  C07F9/6561 ,  C07F9/65742

Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.

公开(公告)号：US20150313899A1

公开(公告)日：2015-11-05

申请号：US14750794

申请日：2015-06-25

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Esteban Masuda ,  Rajinder Singh ,  Vanessa Taylor ,  Donald G. Payan

IPC: A61K31/506 ,  A61K31/675

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。

公开(公告)号：US20150158824A1

公开(公告)日：2015-06-11

申请号：US14624301

申请日：2015-02-17

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Hui Li ,  Ankush Argade ,  Kin Tso ,  Sambaiah Thota ,  David Carroll ,  Arvinder Sran ,  Robin Cooper ,  Rajinder Singh ,  Somasekhar Bhamidipati ,  Vanessa Taylor ,  Esteban Masuda

IPC: C07D239/50 ,  C07D417/12 ,  A61K45/06 ,  A61K31/505 ,  A61K31/506 ,  C07D409/12 ,  C07D401/12

CPC classification number: C07D239/50 ,  A61K31/505 ,  A61K31/506 ,  A61K45/06 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12

Abstract: The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.

Abstract translation: 本发明包括具有式I的化合物和使用这些化合物的组合物和方法用于治疗JAK途径的调节或JAK激酶，特别是JAK3的抑制在治疗上有用的条件。

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。

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。

公开(公告)号：US20130310341A1

公开(公告)日：2013-11-21

申请号：US13861650

申请日：2013-04-12

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Somasekhar Bhamidipati ,  Rajinder Singh ,  Thomas Sun ,  Esteban Masuda

IPC: A61K31/675

CPC classification number: A61K31/675 ,  A61K9/0053 ,  C07D498/04 ,  C07F9/6561

Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, salts and hydrates of the prodrugs, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.

公开(公告)号：US12263180B2

公开(公告)日：2025-04-01

申请号：US17323901

申请日：2021-05-18

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Esteban Masuda ,  Vadim Markovtsov

IPC: A61K31/5383 ,  A61K31/155 ,  A61K31/245 ,  A61K31/427 ,  A61K31/4706 ,  A61K31/4748 ,  A61K31/519 ,  A61K31/573 ,  A61K31/675 ,  A61K31/7048 ,  A61K39/42 ,  A61P31/14 ,  C07K16/10

Abstract: Provided herein are a variety of methods that involve administering fostamatinib, an active component thereof or a pharmaceutically acceptable salt thereof to a patient. In some embodiments, the method may comprise administering fostamatinib, an active component thereof or a pharmaceutically acceptable salt thereof to a patient having or suspected of having a COVID-19 infection. In some embodiments, the method may comprise administering fostamatinib, an active component thereof or a pharmaceutically acceptable salt thereof to a patient having, suspected of having or expected to develop acute respiratory distress syndrome, acute kidney injury, and/or thrombosis. In some embodiments, the method may comprise administering fostamatinib, an active component thereof or a pharmaceutically acceptable salt thereof to a patient having, suspected of having or expected to develop symptoms associated with a cytokine response. Aspects of the methods may further include identifying a patient with kidney malfunction, e.g., acute kidney injury, and/or thrombosis.

公开(公告)号：US20230303555A1

公开(公告)日：2023-09-28

申请号：US18187789

申请日：2023-03-22

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Jack Maung ,  Yan Chen ,  Simon Shaw ,  David Sweeny ,  Esteban Masuda

IPC: C07D417/14

CPC classification number: C07D417/14

Abstract: Disclosed embodiments concern novel interleukin receptor associated kinases (IRAK) inhibitor compounds and compositions comprising such compounds. The compounds may have a structure according to Formula I




Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent an IRAK-associated disease or condition.

公开(公告)号：US11672791B2

公开(公告)日：2023-06-13

申请号：US17465662

申请日：2021-09-02

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Sacha Holland ,  Rajinder Singh ,  Somasekhar Bhamidipati ,  Pingyu Ding ,  Rao Kolluri ,  Ihab Darwish ,  Esteban Masuda ,  Jiaxin Yu

IPC: C07D471/04 ,  A61K31/4545 ,  C07D519/00 ,  A61K31/519

CPC classification number: A61K31/4545 ,  A61K31/519 ,  C07D471/04 ,  C07D519/00

Abstract: Disclosed are imidazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure




and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, Y and Z are as described herein. In certain embodiments, a compound disclosed herein inhibits a cellular TAM receptor, and can be used to treat disease mediated by or involving the TAM receptor family.