公开(公告)号：US20240101570A1

公开(公告)日：2024-03-28

申请号：US18255575

申请日：2021-11-22

申请人： AMGEN INC.

发明人： 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分类号： C07D491/048 ,  A61K35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D491/147 ,  C07D495/04 ,  C07D498/04 ,  C07D519/00

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

摘要： 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

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：US20220395504A1

公开(公告)日：2022-12-15

申请号：US17363878

申请日：2021-06-30

申请人： Amgen Inc.

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

IPC分类号： A61K31/517 ,  A61P35/00 ,  A61K31/4985 ,  A61K39/395 ,  C07D403/04 ,  C07D471/04

摘要： Provided herein are KRAS G12C inhibitors, 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：US20240317715A1

公开(公告)日：2024-09-26

申请号：US18680558

申请日：2024-05-31

申请人： AMGEN INC.

发明人： 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分类号： C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  C07D413/14 ,  C07D419/14 ,  C07D491/107

CPC分类号： C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  C07D413/14 ,  C07D419/14 ,  C07D491/107

摘要： 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：US20220175782A1

公开(公告)日：2022-06-09

申请号：US17579359

申请日：2022-01-19

申请人： AMGEN INC.

发明人： 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分类号： A61K31/519 ,  A61K31/551 ,  A61K39/395 ,  A61P35/00

摘要： 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

申请人： AMGEN INC.

发明人： 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分类号： C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  C07D413/14 ,  C07D419/14 ,  C07D491/107

摘要： 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：US20240092794A1

公开(公告)日：2024-03-21

申请号：US18502780

申请日：2023-11-06

申请人： AMGEN INC.

发明人： 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分类号： C07D491/06 ,  A61P35/00 ,  C07D471/06 ,  C07D471/16 ,  C07D491/16

CPC分类号： C07D491/06 ,  A61P35/00 ,  C07D471/06 ,  C07D471/16 ,  C07D491/16

摘要： 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：US20150329538A1

公开(公告)日：2015-11-19

申请号：US14380918

申请日：2013-02-27

申请人： AMGEN INC.

发明人： Victor CEE ,  Frank CHAVEZ, JR. ,  Jian J. CHEN ,  Essa Hu HARRINGTON ,  Bradley HERBERICH ,  Claire L.M. JACKSON ,  Brian A. LANMAN ,  Thomas T. NGUYEN ,  Mark H. NORMAN ,  Liping H. PETTUS ,  Anthony B. REED ,  Adrian L. SMITH ,  Nuria A. TAMAYO ,  Andrew TASKER ,  Hui-Ling WANG ,  Bin WU ,  Ryan WURZ

IPC分类号： C07D471/04 ,  C07D401/04 ,  C07D487/04

CPC分类号： C07D471/04 ,  C07D401/04 ,  C07D487/04

摘要： The invention relates to amide-containing compounds of formula (1), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.

摘要翻译： 本发明涉及式（1）的含酰胺化合物及其盐。 在一些实施方案中，本发明涉及Pim-1和/或Pim-2和/或Pim-3蛋白激酶活性或酶功能的抑制剂或调节剂。 在另外的实施方案中，本发明涉及包含本文公开的化合物的药物组合物及其在预防和治疗Pim激酶相关病症和疾病，优选癌症中的用途。

公开(公告)号：US20140213581A1

公开(公告)日：2014-07-31

申请号：US14166012

申请日：2014-01-28

申请人： AMGEN INC.

发明人： Ryan WHITE ,  Jennifer R. ALLEN ,  Oleg EPSTEIN ,  Fang-Tsao HONG ,  Zihao HUA ,  Jason Brooks HUMAN ,  Patricia LOPEZ ,  Philip R. OLIVIERI ,  Karina ROMERO ,  Laurie SCHENKEL ,  John STELLWAGEN ,  Nuria A. TAMAYO ,  Xiao Mei ZHENG

IPC分类号： C07D513/04 ,  C07D513/14

CPC分类号： C07D513/04 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/10 ,  C07D513/14 ,  C07D513/20 ,  C07D519/00

摘要： 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 A5, A6, A8, R1, R2, R3, R7, X, Y, n and o of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding 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 Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.

摘要翻译： 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的变量A5，A6，A8，R1，R2，R3，R7，X，Y，n和o独立地在本文中定义。 本发明还提供包含该化合物的药物组合物，以及用于治疗由BACE的生物学活性产生的A-β斑块形成和沉积相关的病症和/或病症的化合物和组合物的相应用途。 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。 本发明进一步提供式II化合物及其次式实施方案，式III化合物，可用于制备式I-III化合物的中间体和方法和方法及其分式。

公开(公告)号：US20240254100A1

公开(公告)日：2024-08-01

申请号：US17632333

申请日：2020-08-03

申请人： AMGEN INC.

发明人： Nuria A. TAMAYO ,  Matthew Richard KALLER ,  Thomas T. NGUYEN ,  Nobuko NISHIMURA ,  Qiufen May XUE ,  John Gordon ALLEN

IPC分类号： C07D401/04 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/541 ,  C07D241/20 ,  C07D417/14

CPC分类号： C07D401/04 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/541 ,  C07D241/20 ,  C07D417/14

摘要： 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.