公开(公告)号：EP3630745A2

公开(公告)日：2020-04-08

申请号：EP18769873.3

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： C07D401/14 ,  C07D413/14 ,  C07D403/14 ,  C07D417/14 ,  A61P35/00 ,  A61K31/517

公开(公告)号：EP3055290B1

公开(公告)日：2019-10-02

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

公开(公告)号：EP3870585A1

公开(公告)日：2021-09-01

申请号：EP19802439.0

申请日：2019-10-23

申请人： Araxes Pharma LLC

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

IPC分类号： C07D487/10 ,  C07D471/10 ,  A61K31/407 ,  A61K31/438 ,  A61K31/416 ,  A61K31/5377 ,  A61K31/444 ,  A61P35/00 ,  A61P35/04

公开(公告)号：EP3636639A1

公开(公告)日：2020-04-15

申请号：EP19195037.7

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

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 R 1 , R 2a , R 3a , R 3b , R 4a , R 4b , G 1 , G 2 , L 1 , L 2 , m 1 , m 2 , 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.

公开(公告)号：EP3325447A1

公开(公告)日：2018-05-30

申请号：EP16747678.7

申请日：2016-07-22

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： C07D215/42 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D239/88 ,  A61K31/517 ,  A61K31/496 ,  A61P35/00

CPC分类号： C07D215/42 ,  C07D239/88 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14

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, stereoisomer or prodrug thereof, wherein R, R1, R2a, R2b, R2c, A, B, L1 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：EP3523289A1

公开(公告)日：2019-08-14

申请号：EP17797780.8

申请日：2017-10-06

申请人： Araxes Pharma LLC

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

IPC分类号： C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  A61K31/4035 ,  A61K31/437 ,  A61P35/00 ,  C07D513/04

公开(公告)号：EP3519402A1

公开(公告)日：2019-08-07

申请号：EP17781353.2

申请日：2017-09-29

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 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  A61K31/407 ,  A61P35/00

公开(公告)号：EP3356339A1

公开(公告)日：2018-08-08

申请号：EP16778179.8

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： C07D401/04 ,  C07D471/04 ,  A61K31/4375 ,  A61P35/00

CPC分类号： C07D401/04 ,  C07D471/04

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, R1, R3a, R3b, R4a, R4b, G2, G3, G4, m1, m2, m3, m4, 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：EP3280708A1

公开(公告)日：2018-02-14

申请号：EP16716802.0

申请日：2016-04-08

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： C07D403/12 ,  C07D401/14 ,  C07D405/14 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12 ,  C07D239/74 ,  C07D239/94 ,  C07D239/95 ,  C07D413/12 ,  C07D417/04 ,  C07D471/08

CPC分类号： C07D239/74 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/04 ,  C07D471/08 ,  C07D487/10 ,  C07D491/10 ,  C07F9/65583

摘要： or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, R5a, R5b, R6, A, B, G1, G2, L1, L2, m1, m2, n, x, y, X 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：EP3887373A1

公开(公告)日：2021-10-06

申请号：EP19824126.7

申请日：2019-11-27

申请人： Araxes Pharma LLC

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

IPC分类号： C07D471/10 ,  C07D487/10 ,  A61P35/00