公开(公告)号：EP2970121B1

公开(公告)日：2017-12-13

申请号：EP14720375.6

申请日：2014-03-14

申请人： Araxes Pharma LLC

发明人： REN, Pingda ,  LIU, Yi ,  LI, Liansheng ,  FENG, Jun ,  WU, Tao

IPC分类号： C07D211/60 ,  C07D205/04 ,  C07D285/14 ,  C07D211/62 ,  C07D295/16 ,  C07D213/64 ,  C07D403/12 ,  G01N33/58 ,  C07D213/74 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D237/04 ,  C07D403/06 ,  C07D405/06 ,  C07D419/12

CPC分类号： C07D205/04 ,  A61P35/00 ,  C07D211/56 ,  C07D211/58 ,  C07D211/60 ,  C07D211/62 ,  C07D213/64 ,  C07D213/74 ,  C07D231/40 ,  C07D237/04 ,  C07D285/14 ,  C07D285/16 ,  C07D295/16 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D417/06 ,  C07D419/12 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  G01N33/58

摘要： Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.

公开(公告)号：EP3193851A1

公开(公告)日：2017-07-26

申请号：EP15771461.9

申请日：2015-09-18

申请人： Araxes Pharma LLC

发明人： JANES, Matthew, Robert ,  PATRICELLI, Matthew, Peter ,  LI, Liansheng ,  REN, Pingda ,  LIU, Yi

IPC分类号： A61K31/00 ,  A61K31/496 ,  A61K31/517 ,  A61P35/00

摘要： Combination therapies for treatment of cancers associated with mutations in the KRAS gene are provided. Compositions comprising therapeutic agents for treatment of cancers associated with mutations in the KRAS gene are also provided.

摘要翻译： 提供了用于治疗与KRAS基因突变相关的癌症的组合疗法。 还提供了包含用于治疗与KRAS基因中的突变相关的癌症的治疗剂的组合物。

公开(公告)号：EP3829580A1

公开(公告)日：2021-06-09

申请号：EP19752880.5

申请日：2019-08-01

申请人： Araxes Pharma LLC

发明人： LI, Liansheng ,  FENG, Jun ,  WU, Tao ,  LIU, Yuan ,  WANG, Yi ,  BORUM, Alana K. ,  REN, Pingda ,  LIU, Yi

IPC分类号： A61K31/4427 ,  A61K31/506 ,  A61P35/00 ,  C07D487/10

公开(公告)号：EP3193851B1

公开(公告)日：2020-10-21

申请号：EP15771461.9

申请日：2015-09-18

申请人： Araxes Pharma LLC

发明人： JANES, Matthew, Robert ,  PATRICELLI, Matthew, Peter ,  LI, Liansheng ,  REN, Pingda ,  LIU, Yi

IPC分类号： A61K31/00 ,  A61K31/496 ,  A61K31/517 ,  A61P35/00

公开(公告)号：EP3197870B1

公开(公告)日：2020-08-19

申请号：EP15784184.2

申请日：2015-09-25

申请人： Araxes Pharma LLC

发明人： LI, Liansheng ,  FENG, Jun ,  REN, Pingda ,  LIU, Yi

IPC分类号： C07D213/75 ,  C07D231/56 ,  C07D401/04 ,  C07D239/42 ,  C07D295/185 ,  A61K31/506 ,  A61K31/495 ,  A61K31/4468 ,  A61K31/445 ,  A61K31/496 ,  A61P35/00

公开(公告)号：EP3630747A1

公开(公告)日：2020-04-08

申请号：EP18731661.7

申请日：2018-05-24

申请人： Araxes Pharma LLC

发明人： LI, Liansheng ,  FENG, Jun ,  WU, Tao ,  LIU, Yuan ,  WANG, Yi ,  REN, Pingda ,  LIU, Yi

IPC分类号： C07D403/04 ,  C07D403/14 ,  A61P35/00 ,  A61K31/517

公开(公告)号：EP3356351A1

公开(公告)日：2018-08-08

申请号：EP16781608.1

申请日：2016-09-27

申请人： Araxes Pharma LLC

发明人： LI, Liansheng ,  FENG, Jun ,  LONG, Yun, Oliver, ,  REN, Pingda ,  LIU, Yi

IPC分类号： C07D403/12 ,  A61P35/00 ,  A61K31/496

CPC分类号： C07D403/12 ,  A61P35/00 ,  C07D417/12

摘要： Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein A, X, R3a, R3b, R4a, R4b, G1, G2, G3, G4, L1, L2, m1, m2, m3, m4, and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

公开(公告)号：EP3356349A1

公开(公告)日：2018-08-08

申请号：EP16778628.4

申请日：2016-09-28

申请人： Araxes Pharma LLC

发明人： LI, Liansheng ,  FENG, Jun ,  LONG, Yun, Oliver ,  LIU, Yuan ,  REN, Pingda ,  LIU, Yi

IPC分类号： C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D417/04 ,  C07D243/14 ,  C07D471/04 ,  C07D307/82 ,  A61K31/4355 ,  A61K31/428 ,  A61P35/00

CPC分类号： C07D471/04 ,  C07D243/14 ,  C07D307/82 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D417/04

摘要： Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein A, B R1, R2a, R2b, R3a, R3b, R4a, R4b, G1, G2, m1, m2, L1, L2 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

公开(公告)号：EP3283462A1

公开(公告)日：2018-02-21

申请号：EP16718179.1

申请日：2016-04-15

申请人： Araxes Pharma LLC

发明人： LI, Liansheng ,  FENG, Jun ,  LONG, Yun, Oliver ,  LIU, Yuan ,  WU, Tao ,  REN, Pingda ,  LIU, Yi

IPC分类号： C07D219/10 ,  C07D219/12 ,  C07D471/04 ,  C07D491/056 ,  C07D498/04 ,  C07D513/04 ,  A61K31/4375 ,  A61P35/00

CPC分类号： C07D471/04 ,  C07D219/10 ,  C07D219/12 ,  C07D491/056 ,  C07D498/04 ,  C07D513/04

摘要： Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I):(I) or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A is a heterocyclic or heteroaryl ring, and R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, A, G1, G2, L1, L2, m1, m2, and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

公开(公告)号：EP3055290A1

公开(公告)日：2016-08-17

申请号：EP14799915.5

申请日：2014-10-10

申请人： Araxes Pharma LLC

发明人： LI, Liansheng ,  FENG, Jun ,  WU, Tao ,  REN, Pingda ,  LIU, Yi ,  LIU, Yuan ,  LONG, Yun, Oliver

IPC分类号： C07D239/94 ,  C07D403/12 ,  C07D215/46 ,  C07D215/54 ,  C07D231/56 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D237/28 ,  C07D409/04 ,  C07D409/14 ,  C07D417/10 ,  A61K31/517 ,  A61P35/00

CPC分类号： C07D239/94 ,  C07D215/46 ,  C07D215/54 ,  C07D231/56 ,  C07D237/28 ,  C07D239/84 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D417/10 ,  C07D417/12 ,  C07D487/04 ,  C07D495/04

摘要： Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.