公开(公告)号：US20230159510A1

公开(公告)日：2023-05-25

申请号：US17799077

申请日：2021-02-11

申请人： AMGEN INC.

发明人： Jennifer Rebecca ALLEN ,  Albert AMEGADZIE ,  Diane Jennifer BEYLKIN ,  Shon BOOKER ,  Matthew Paul BOURBEAU ,  John R. BUTLER ,  Michael J. FROHN ,  Sanne Ormholt Schroder GLAD ,  Birgitte Weinreich HUSEMOEN ,  Matthew R. KALLER ,  Todd J. KOHN ,  Brian Alan LANMAN ,  Kexue LI ,  Qingyian LIU ,  Patricia LOPEZ ,  Vu Van MA ,  Francesco MANONI ,  Jose MEDINA ,  Ana Elena MINATTI ,  Jorge PEIRO CADAHIA ,  Liping PETTUS ,  Alexander J. PICKRELL ,  Ian SARVARY ,  Nuria A. TAMAYO ,  Mikkel VESTERGAARD

IPC分类号： C07D413/14 ,  C07D471/04 ,  C07D401/14 ,  C07D401/12 ,  C07D405/14

CPC分类号： C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04

摘要： Described herein are compounds of Formula I and pharmaceutically acceptable salt thereof, stereoisomers, tautomers as well as pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, metabolic and blood disorders. Compounds of Formula I have the following structure: (I)

公开(公告)号：US20240294551A1

公开(公告)日：2024-09-05

申请号：US18614911

申请日：2024-03-25

申请人： AMGEN INC.

发明人： Ryan Paul Wurz ,  Yunxiao LI ,  Primali Vasundera NAVARATNE ,  Jose M. MEDINA ,  Ning CHEN ,  Liping PETTUS ,  Xiaofen LI ,  John STELLWAGEN ,  Kexue LI ,  Brian Alan LANMAN ,  Michael M. YAMANO ,  Wei ZHAO ,  Benjamin WIGMAN ,  Fabien EMMETIERE ,  Albert K. AMEGADZIE ,  Christopher P. MOHR ,  Aaron C. SIEGMUND ,  Rene RAHIMOFF ,  Zhichen WU ,  Adriano BAUER ,  Andrew SMALIGO ,  Quentin Tercenio ,  Qingyian Liu ,  Shon K. Booker

IPC分类号： C07D519/00 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  C07D471/22 ,  C07D498/22 ,  C07D513/22

CPC分类号： C07D519/00 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  C07D471/22 ,  C07D498/22 ,  C07D513/22

摘要： The present disclosure provides compounds useful for the inhibition of KRAS G12D, G12V, G12A, G12S, G13D, Q61H, Q61L or G12C. The compounds have a general Formula I′:




wherein the variables of Formula I′ are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, cancer.