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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
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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
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公开(公告)号：EP3401314A1
公开(公告)日：2018-11-14
申请号：EP17206812.4
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： C07D401/06 , C07D417/06 , A61K31/496 , A61P35/00
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.
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公开(公告)号：EP3356354A1
公开(公告)日：2018-08-08
申请号：EP16778172.3
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： C07D403/14 , C07D417/14 , A61K31/496 , A61K31/498 , A61P35/00
CPC分类号： C07D417/14 , A61K9/0019 , A61K9/0053 , A61P35/04 , C07D403/14
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, tautomer, stereoisomer or prodrug thereof, wherein A, R3a, R3b, R4a, R4b, G1, 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.
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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
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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.-
7.发明公开
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.
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公开(公告)号：EP3197870A1
公开(公告)日：2017-08-02
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
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 R1, R2, R3a, R3b, R4a, R4b, G1, G2, L, 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.
摘要翻译： 提供了具有作为G12C突变KRAS蛋白抑制剂活性的化合物。 所述化合物具有以下结构（I）：或其药学上可接受的盐，互变异构体，立体异构体或前药，其中R1，R2，R3a，R3b，R4a，R4b，G1，G2，L，m1， 于此。 还提供了与这些化合物的制备和使用有关的方法，包含此类化合物的药物组合物以及调节G12C突变KRAS蛋白质活性以治疗疾病如癌症的方法。
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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
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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
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