公开(公告)号：US20230012676A1

公开(公告)日：2023-01-19

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

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.

公开(公告)号：US11524955B2

公开(公告)日：2022-12-13

申请号：US16893981

申请日：2020-06-05

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Yan Chen ,  Rose Yen ,  Jiaxin Yu ,  Vanessa Taylor ,  Rajinder Singh

IPC: C07D239/48 ,  C07D403/12 ,  C07D401/14 ,  C07D405/14

Abstract: Compounds within the scope of the present invention have a Formula 1 or a salt or produg thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R2 and R3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC50 of from 0.003 μM to 3.7 μM; a TAK1 IC50 of from 0.008 μM to 132 μM; and/or an IRAK4/TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4/TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and/or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and/or IRAK4 over TAK1.

公开(公告)号：US20220185804A1

公开(公告)日：2022-06-16

申请号：US17687826

申请日：2022-03-07

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rose Yen ,  Yan Chen ,  Rajinder Singh ,  Vanessa Taylor

IPC: C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06

Abstract: Disclosed are novel benzazole compounds and compositions comprising the compounds. The compounds are useful as kinase inhibitors including interleukin receptor associated kinases (IRAK) inhibitors. 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：US20220098181A1

公开(公告)日：2022-03-31

申请号：US17517428

申请日：2021-11-02

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Hui Li ,  Sambaiah Thota ,  David Carroll ,  Ankush Argade ,  Kin Tso ,  Arvinder Sran ,  Jeffrey Clough ,  Holger Keim ,  Somasekhar Bhamidipati ,  Vanessa Taylor ,  Robin Cooper ,  Rajinder Singh ,  Brian Wong

IPC: C07D413/12 ,  C07D403/04 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D413/14 ,  C07D239/48 ,  A61K31/343 ,  A61K31/436 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/541 ,  A61K31/695 ,  A61K38/13 ,  A61K39/395 ,  C07D498/04 ,  C07F7/10 ,  A61K45/06 ,  C07D401/14 ,  C07D417/12 ,  C07F7/08

Abstract: The invention encompasses compounds having formula I-V 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, may be therapeutically useful.

公开(公告)号：US11198689B2

公开(公告)日：2021-12-14

申请号：US16551393

申请日：2019-08-26

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Hui Li ,  Sambaiah Thota ,  David Carroll ,  Ankush Argade ,  Kin Tso ,  Arvinder Sran ,  Jeffrey Clough ,  Holger Keim ,  Somasekhar Bhamidipati ,  Vanessa Taylor ,  Robin Cooper ,  Rajinder Singh ,  Brian Wong

IPC: C07D403/04 ,  C07D413/12 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D413/14 ,  C07D239/48 ,  A61K31/343 ,  A61K31/436 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/541 ,  A61K31/695 ,  A61K38/13 ,  A61K39/395 ,  C07D498/04 ,  C07F7/10 ,  A61K45/06 ,  C07D401/14 ,  C07D417/12 ,  C07F7/08 ,  C07D285/22

Abstract: The invention encompasses compounds having formula I-V 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, may be therapeutically useful.

公开(公告)号：US11174251B2

公开(公告)日：2021-11-16

申请号：US16656461

申请日：2019-10-17

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Hui Li ,  Thilo J. Heckrodt ,  Yan Chen ,  Darren John McMurtrie ,  Vanessa Taylor ,  Rajinder Singh ,  Pingyu Ding ,  Rose Yen

IPC: C07D413/12 ,  C07F9/6558 ,  C07B59/00

Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.

公开(公告)号：US20210276982A1

公开(公告)日：2021-09-09

申请号：US17324320

申请日：2021-05-19

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Marina Gelman ,  Pingyu Ding ,  Todd Kinsella ,  Rajinder Singh ,  Somasekhar Bhamidipati ,  Jeffrey Clough

IPC: C07D403/12 ,  A61P35/02 ,  C07D401/12 ,  C07D471/04

Abstract: Disclosed are aryl pyrimidine 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 A, Z, R and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits the activity of one or more members of the TGF-β superfamily, and can be used to treat disease by blocking such activity.

公开(公告)号：US20210130361A1

公开(公告)日：2021-05-06

申请号：US17087459

申请日：2020-11-02

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Marina Gelman ,  Todd Kinsella ,  Somasekhar Bhamidipati ,  Ihab Darwish ,  Rajinder Singh ,  Jiaxin Yu

IPC: C07D487/04 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D471/04 ,  C07D519/00

Abstract: Disclosed are pyrazole 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 A, X, Z, m, p, and R2 are as described herein. In certain embodiments, a compound disclosed herein inhibits the activity of one or more members of the TGF-β superfamily, and can be used to treat disease by blocking such activity.

公开(公告)号：US10941134B2

公开(公告)日：2021-03-09

申请号：US16451613

申请日：2019-06-25

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Dane Goff ,  Donald Payan ,  Rajinder Singh ,  Simon Shaw ,  David Carroll ,  Yasumichi Hitoshi

IPC: C07D401/14 ,  C07D213/82 ,  C07D401/06 ,  C07D401/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D451/06 ,  C07D471/10 ,  C07D487/04 ,  C07D495/04 ,  C07D405/12 ,  C07D213/81 ,  C07D213/56 ,  C07D401/04

Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

公开(公告)号：US10792282B2

公开(公告)日：2020-10-06

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 ,  C07D471/04 ,  C07D498/04

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.