公开(公告)号：US20240092794A1

公开(公告)日：2024-03-21

申请号：US18502780

申请日：2023-11-06

Applicant: AMGEN INC.

Inventor： Shon BOOKER ,  Matthew Paul BOURBEAU ,  John R. BUTLER ,  Sanne Ormholt Schroder GLAD ,  Brian Alan LANMAN ,  Patricia LOPEZ ,  Francesco MANONI ,  Liping H. PETTUS ,  Ian SARVARY ,  Nuria A. TAMAYO ,  Mikkel VESTERGAARD ,  Nicholas Anthony WEIRES

IPC: C07D491/06 ,  A61P35/00 ,  C07D471/06 ,  C07D471/16 ,  C07D491/16

CPC classification number: C07D491/06 ,  A61P35/00 ,  C07D471/06 ,  C07D471/16 ,  C07D491/16

Abstract: Described herein are novel PRMT5 inhibitors of Formula I and pharmaceutically acceptable salts thereof, as well as the 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:

公开(公告)号：US20240101570A1

公开(公告)日：2024-03-28

申请号：US18255575

申请日：2021-11-22

Applicant: AMGEN INC.

Inventor： Albert AMEGADZIE ,  Diane Jennifer BEYLKIN ,  Shon BOOKER ,  Matthew Paul BOURBEAU ,  John R. BUTLER ,  Sanne Ormholt Schroder GLAD ,  Todd J. KOHN ,  Brian Alan LANMAN ,  Kexue LI ,  Qingyian LIU ,  Patricia LOPEZ ,  Francesco MANONI ,  Primali Vasundera NAVARATNE ,  Liping H. PETTUS ,  Rene RAHIMOFF ,  Nuria A. TAMAYO ,  Mikkel VESTERGAARD ,  Hui-Ling WANG ,  Nicholas Anthony WEIRES

IPC: C07D491/048 ,  A61K35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D491/147 ,  C07D495/04 ,  C07D498/04 ,  C07D519/00

CPC classification number: C07D491/048 ,  A61K35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D491/147 ,  C07D495/04 ,  C07D498/04 ,  C07D519/00

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

公开(公告)号：US20230159510A1

公开(公告)日：2023-05-25

申请号：US17799077

申请日：2021-02-11

Applicant: AMGEN INC.

Inventor： 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: C07D413/14 ,  C07D471/04 ,  C07D401/14 ,  C07D401/12 ,  C07D405/14

CPC classification number: C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04

Abstract: 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：US20220194955A1

公开(公告)日：2022-06-23

申请号：US17552016

申请日：2021-12-15

Applicant: AMGEN INC.

Inventor： Shon BOOKER ,  Matthew Paul BOURBEAU ,  John R. BUTLER ,  Sanne Ormholt Schroder GLAD ,  Brian Alan LANMAN ,  Patricia LOPEZ ,  Francesco MANONI ,  Liping H. PETTUS ,  Ian SARVARY ,  Nuria A. TAMAYO ,  Mikkel VESTERGAARD ,  Nicholas Anthony WEIRES

IPC: C07D491/06 ,  C07D491/16 ,  C07D471/06 ,  C07D471/16 ,  A61P35/00

Abstract: Described herein are novel PRMT5 inhibitors of Formula I and pharmaceutically acceptable salts thereof, as well as the 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:

公开(公告)号：US20220106293A1

公开(公告)日：2022-04-07

申请号：US17551105

申请日：2021-12-14

Applicant: AMGEN INC.

Inventor： Nuria A. TAMAYO ,  Abhisek BANERJEE ,  James Alexander BROWN ,  Michael J FROHN ,  Jian Jeffrey CHEN ,  Kexue LI ,  Qingyian LIU ,  Jonathan Dante LOW ,  Vu MA ,  Liping H. PETTUS ,  Mary Catherine WALTON ,  Ana Elena MINATTI ,  Matthew Paul BOURBEAU ,  Lei JIA

IPC: C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  C07D413/14 ,  C07D419/14 ,  C07D491/107

Abstract: Compounds of formula (I): as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

公开(公告)号：US20220289724A1

公开(公告)日：2022-09-15

申请号：US17632330

申请日：2020-08-03

Applicant: AMGEN INC.

Inventor： Nuria A. TAMAYO ,  Abhisek BANERJEE ,  Jian Jeffrey CHEN ,  Matthew Paul BOURBEAU ,  Matthew Richard KALLER ,  Jonathan Dante LOW ,  Ana Elena MINATTI ,  Thomas T. NGUYEN ,  Nobuko NISHIMURA ,  Liping H. PETTUS ,  Mary Catherine WALTON ,  Qiufen May XUE ,  John Gordon ALLEN

IPC: C07D405/12 ,  C07D221/20 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12

Abstract: Amide compounds of formula (I): and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of Kinesin Motor Protein KIF18A, such as cancer, psoriasis, atopic dermatitis, an autoimmune disorder, or inflammatory bowel disease, and the like.

公开(公告)号：US20220281843A1

公开(公告)日：2022-09-08

申请号：US17632338

申请日：2020-08-03

Applicant: AMGEN INC.

Inventor： Nuria A. TAMAYO ,  Abhisek BANERJEE ,  Matthew Paul BOURBEAU

IPC: C07D401/14 ,  C07D401/04 ,  C07D413/14 ,  C07D471/04 ,  C07D405/14 ,  C07D471/08

Abstract: Compounds of formula (I): (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

公开(公告)号：US20240317715A1

公开(公告)日：2024-09-26

申请号：US18680558

申请日：2024-05-31

Applicant: AMGEN INC.

Inventor： Nuria A. TAMAYO ,  Abhisek BANERJEE ,  James Alexander BROWN ,  Michael J. FROHN ,  Jian Jeffrey CHEN ,  Kexue LI ,  Qingyian LIU ,  Jonathan Dante LOW ,  Vu MA ,  Liping H. PETTUS ,  Mary Catherine WALTON ,  Ana Elena MINATTI ,  Matthew Paul BOURBEAU ,  Lei JIA

IPC: C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  C07D413/14 ,  C07D419/14 ,  C07D491/107

CPC classification number: C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  C07D413/14 ,  C07D419/14 ,  C07D491/107

Abstract: Compounds of formula (I):




as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

公开(公告)号：US20240124442A1

公开(公告)日：2024-04-18

申请号：US18264216

申请日：2022-02-03

Applicant: AMGEN INC.

Inventor： Albert AMEGADZIE ,  Diane Jennifer BEYLKIN ,  Shon BOOKER ,  Matthew Paul BOURBEAU ,  John R. BUTLER ,  Kevin Lloyd GREENMAN ,  Todd J. KOHN ,  Kexue LI ,  Qingyian LIU ,  Ana Elena MINATTI ,  Primali Vasundera NAVARATNE ,  Liping H. PETTUS ,  Rene RAHIMOFF ,  Hui-Ling WANG ,  Nicholas Anthony WEIRES

IPC: C07D471/04 ,  A61P35/00 ,  C07D471/14 ,  C07D491/048 ,  C07D491/147 ,  C07D495/04 ,  C07D498/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61P35/00 ,  C07D471/14 ,  C07D491/048 ,  C07D491/147 ,  C07D495/04 ,  C07D498/04 ,  C07D519/00

Abstract: Described herein are novel PRMT5 inhibitors of Formula I and pharmaceutically acceptable salts thereof, as well as the 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:

公开(公告)号：US20200239441A1

公开(公告)日：2020-07-30

申请号：US16724119

申请日：2019-12-20

Applicant: AMGEN INC.

Inventor： Nuria A. TAMAYO ,  Abhisek BANERJEE ,  James Alexander BROWN ,  Michael J. FROHN ,  Jian Jeffrey CHEN ,  Kexue LI ,  Qingyian LIU ,  Jonathan Dante LOW ,  Vu MA ,  Liping H. PETTUS ,  Mary Catherine WALTON ,  Ana Elena MINATTI ,  Matthew Paul BOURBEAU ,  Lei JIA

IPC: C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  C07D413/14 ,  C07D419/14 ,  C07D491/107

Abstract: Compounds of formula (I): as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.