公开(公告)号：US10005767B2

公开(公告)日：2018-06-26

申请号：US15419660

申请日：2017-01-30

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Yan Chen ,  Vanessa Taylor ,  Hui Li ,  Rajinder Singh

IPC: A01N43/54 ,  A61K31/505 ,  C07D413/12 ,  A61K31/155 ,  C07D401/14 ,  C07D403/12 ,  C07D413/04 ,  C07D487/08 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/54 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D419/14 ,  C07D471/08 ,  C07D487/04 ,  C07D491/08 ,  A61K31/538 ,  A61K31/55 ,  A61K31/675 ,  C07D413/14 ,  C07D471/04 ,  C07D487/10 ,  C07D498/04 ,  C07F9/6558 ,  A61K31/5415 ,  A61K31/635 ,  C07D451/02

CPC classification number: C07D413/12 ,  A61K31/155 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/54 ,  A61K31/541 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/551 ,  A61K31/635 ,  A61K31/675 ,  A61K45/06 ,  C07D401/14 ,  C07D403/12 ,  C07D413/04 ,  C07D413/14 ,  C07D419/14 ,  C07D451/02 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/08 ,  C07D498/04 ,  C07F9/65583

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.

公开(公告)号：US20180141938A1

公开(公告)日：2018-05-24

申请号：US15875897

申请日：2018-01-19

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D413/12 ,  A61K31/675 ,  A61K45/06 ,  C07F9/653 ,  A61K31/506

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.

公开(公告)号：US20180051006A1

公开(公告)日：2018-02-22

申请号：US15677809

申请日：2017-08-15

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Simon Shaw ,  Xiang Xu ,  Sarkiz Issakani ,  Rajinder Singh ,  Yasumichi Hitoshi ,  Matthew Duncton ,  Nan Lin

IPC: C07D403/04 ,  C07D235/26 ,  C07D403/14 ,  C07D403/12

CPC classification number: C07D403/04 ,  C07D235/26 ,  C07D403/12 ,  C07D403/14

Abstract: Disclosed are benzimidazole 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 R1, R2, R3, R4, Y and X are as described herein. In certain embodiments, a compound disclosed herein activates AMPK, and can be used to treat disease by activating the AMPK pathway.

公开(公告)号：US09890144B2

公开(公告)日：2018-02-13

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 ,  C07D413/12 ,  C07F9/653 ,  A61K45/06

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.

公开(公告)号：US09884868B2

公开(公告)日：2018-02-06

申请号：US15054895

申请日：2016-02-26

Applicant: Rigel Pharmaceuticals, Inc. ,  Bristol-Myers Squibb Company

Inventor： Todd Kinsella ,  Marina Gelman ,  Hui Hong ,  Ihab S. Darwish ,  Rajinder Singh ,  Jiaxin Yu ,  Robert M. Borzilleri ,  Upender Velaparthi ,  Peiying Liu ,  Chetan Darne ,  Hasibur Rahaman ,  Jayakumar Sankara Warrier

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

CPC classification number: C07D487/04 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D471/04

Abstract: Disclosed are imidazole and thiazole 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, A, Z, R1 and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.

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.

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.

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.

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.

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.