公开(公告)号：US10065946B2

公开(公告)日：2018-09-04

申请号：US15226625

申请日：2016-08-02

申请人： Rigel Pharmaceuticals, Inc.

发明人： Rose Yen ,  Yan Chen ,  Rajinder Singh ,  Vanessa Taylor

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

摘要： 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：US09834568B2

公开(公告)日：2017-12-05

申请号：US14754989

申请日：2015-06-30

申请人： Rigel Pharmaceuticals, Inc.

发明人： Pingyu Ding ,  Ankush Argade ,  Dane Goff ,  Rajinder Singh ,  Esteban Masuda ,  Vanessa Taylor ,  Sacha Holland

IPC分类号： C07D487/04 ,  C07D239/95 ,  A61K31/517 ,  A61P35/00 ,  C07D519/00 ,  C07D495/12 ,  C07D239/94 ,  C07D473/16 ,  C07D495/04 ,  C07D471/04

CPC分类号： C07D519/00 ,  A61K31/517 ,  C07D239/94 ,  C07D239/95 ,  C07D471/04 ,  C07D473/16 ,  C07D487/04 ,  C07D495/04 ,  C07D495/12

摘要： The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.

公开(公告)号：US20170137411A1

公开(公告)日：2017-05-18

申请号：US15419660

申请日：2017-01-30

申请人： Rigel Pharmaceuticals, Inc.

发明人： Yan Chen ,  Vanessa Taylor ,  Hui Li ,  Rajinder Singh

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

CPC分类号： 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

摘要： 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：US09566283B2

公开(公告)日：2017-02-14

申请号：US14793506

申请日：2015-07-07

申请人： Rigel Pharmaceuticals, Inc.

发明人： Yan Chen ,  Vanessa Taylor ,  Hui Li ,  Rajinder Singh

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

CPC分类号： 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

摘要： 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.

摘要翻译： 公开了式I化合物，含有它们的组合物，以及用于化合物和组合物用于治疗JAK途径的调节或JAK激酶，特别是JAK 2和JAK 3的抑制在治疗上有用的条件的方法。

公开(公告)号：US20160311839A1

公开(公告)日：2016-10-27

申请号：US15136508

申请日：2016-04-22

申请人： Rigel Pharmaceuticals, Inc.

发明人： Ryan Kelley ,  Hui Li ,  Thilo Heckrodt ,  Yan Chen ,  Darren McMurtrie ,  Kin Tso ,  Vanessa Taylor ,  Rajinder Singh ,  Rose Yen ,  Jack Maung

IPC分类号： C07F9/6558 ,  C07D417/14 ,  C07D471/04 ,  C07D405/14

CPC分类号： C07F9/65586 ,  C07D405/04 ,  C07D405/14 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04

摘要： Disclosed embodiments concern novel interleukin receptor associated kinases (IRAK) inhibitors and compositions comprising such 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.

摘要翻译： 公开的实施方案涉及新的白细胞介素受体相关激酶（IRAK）抑制剂和包含这种抑制剂的组合物。 还公开了制备和使用化合物和组合物的方法。 所公开的化合物和/或组合物可用于治疗或预防IRAK相关疾病或病症。

公开(公告)号：US09248190B2

公开(公告)日：2016-02-02

申请号：US14315073

申请日：2014-06-25

申请人： Rigel Pharmaceuticals, Inc.

发明人： 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分类号： A61K31/506 ,  A61K31/5415 ,  A61K45/06 ,  C07D239/42 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  A61K31/343 ,  A61K31/436 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/541 ,  A61K31/695 ,  A61K38/13 ,  A61K39/395 ,  C07D498/04 ,  C07F7/10 ,  C07D401/14 ,  C07D417/12 ,  C07F7/08 ,  C07D285/22

CPC分类号： C07D413/12 ,  A61K31/343 ,  A61K31/436 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/541 ,  A61K31/695 ,  A61K38/13 ,  A61K39/3955 ,  A61K45/06 ,  C07D239/42 ,  C07D239/48 ,  C07D285/22 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D413/14 ,  C07D417/12 ,  C07D498/04 ,  C07F7/0812 ,  C07F7/10

摘要： 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：US11564930B2

公开(公告)日：2023-01-31

申请号：US17013284

申请日：2020-09-04

申请人： Rigel Pharmaceuticals, Inc.

发明人： Jiaxin Yu ,  Ihab Darwish ,  Vanessa Taylor ,  Rao Kolluri ,  Yan Chen ,  Simon Shaw ,  Somasekhar Bhamidipati ,  Zhushou Luo

IPC分类号： A61K31/553 ,  C07D267/14 ,  C07D413/10 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00

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.

公开(公告)号：US11479543B2

公开(公告)日：2022-10-25

申请号：US17013034

申请日：2020-09-04

申请人： Rigel Pharmaceuticals, Inc.

发明人： Simon Shaw ,  Somasekhar Bhamidipati ,  Vanessa Taylor

IPC分类号： C07D401/14 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D471/08 ,  C07D487/04 ,  C07D491/107 ,  C07D413/12 ,  C07D413/14 ,  C07D267/02 ,  C07D493/04 ,  A61K31/553

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.

公开(公告)号：US20220306620A1

公开(公告)日：2022-09-29

申请号：US17747384

申请日：2022-05-18

申请人： Rigel Pharmaceuticals, Inc.

发明人： Lu Chou ,  Matt Duan ,  Ihab Darwish ,  Simon Shaw ,  Somasekhar Bhamidipati ,  Vanessa Taylor ,  Yan Chen ,  Dazhong Fan ,  Zhushou Luo

IPC分类号： C07D417/14

摘要： Disclosed herein are embodiments of a pyrazole compound according to formula I. Compositions comprising the compound, and a method for making the composition also are disclosed. The composition may comprise a carrier, such as a polymer and/or the composition may be a spray-dried formulation. Also disclosed is a method for using the compound and/or composition. The compound and/or composition may be useful to inhibit an IRAK protein and/or to ameliorate, treat and/or prevent an IRAK-associated disease or condition in a subject.

公开(公告)号：US20220218705A1

公开(公告)日：2022-07-14

申请号：US17547819

申请日：2021-12-10

申请人： Rigel Pharmaceuticals, Inc.

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

IPC分类号： A61K31/506 ,  A61K45/06 ,  A61P37/06

摘要： 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.