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：US20220175782A1

公开(公告)日：2022-06-09

申请号：US17579359

申请日：2022-01-19

Applicant: AMGEN INC.

Inventor： John Gordon ALLEN ,  Brian Alan LANMAN ,  Jian CHEN ,  Anthony B. REED ,  Victor J. CEE ,  Longbin LIU ,  Patricia LOPEZ ,  Ryan Paul WURZ ,  Thomas T. NGUYEN ,  Shon BOOKER ,  Jennifer Rebecca ALLEN ,  Margaret CHU-MOYER ,  Albert AMEGADZIE ,  Ning CHEN ,  Clifford GOODMAN ,  Jonathan D. LOW ,  Vu Van MA ,  Ana Elena MINATTI ,  Nobuko NISHIMURA ,  Alexander J. PICKRELL ,  Hui-Ling WANG ,  Youngsook SHIN ,  Aaron C. SIEGMUND ,  Kevin C. YANG ,  Nuria A. TAMAYO ,  Mary WALTON ,  Qiufen XUE

IPC: A61K31/519 ,  A61K31/551 ,  A61K39/395 ,  A61P35/00

Abstract: Provided herein are KRAS G12C inhibitors, such as composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

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.

公开(公告)号：US20140275058A1

公开(公告)日：2014-09-18

申请号：US14199844

申请日：2014-03-06

Applicant: AMGEN INC.

Inventor： Ana Elena MINATTI ,  Jonathan D. LOW ,  Jennifer R. ALLEN ,  Albert AMEGADZIE ,  James BROWN ,  Michael J. FROHN ,  Angel GUZMAN-PEREZ ,  Paul E. HARRINGTON ,  Patricia LOPEZ ,  Vu Van MA ,  Nobuko NISHIMURA ,  Wenyuan QIAN ,  Shannon RUMFELT ,  Robert M. RZASA ,  Kelvin SHAM ,  Adrian L. SMITH ,  Ryan WHITE ,  Qiufen XUE

IPC: C07D471/04 ,  C07D265/12 ,  C07D417/12 ,  C07D417/14 ,  C07D413/12 ,  C07D413/14

CPC classification number: C07D413/12 ,  C07D265/12 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048

Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.

Abstract translation: 本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。 化合物具有通式I：其中式I中的每个R a，R b，R 1，R 2，R 3和R 7各自独立地定义的变量A4，A5，A6，A8在本文中定义。 本发明还提供包含该化合物的药物组合物，以及该化合物和组合物用于治疗由BACE的生物学活性产生的与A-β斑块形成和沉积有关的病症和/或病症的用途。 这种BACE介导的疾病包括例如阿尔茨海默病，认知缺陷，认知障碍，精神分裂症和其他中枢神经系统疾病。 本发明还提供式II和III的化合物及其分子式实施方案，用于制备本发明化合物的中间体和方法。