公开(公告)号：WO2022083569A1

公开(公告)日：2022-04-28

申请号：PCT/CN2021/124598

申请日：2021-10-19

Applicant: AMGEN INC. ,  ZHANG, Wenhan

Inventor： LANMAN, Brian Alan ,  BANERJEE, Abhisek ,  CHU-MOYER, Margaret ,  DAI, Dongcheng ,  ESHON, Josephine ,  HUANG, David ,  KALLER, Matthew R. ,  LEE, Heejun ,  LOPEZ, Patricia ,  MA, Vu Van ,  MANONI, Francesco ,  MEDINA, Jose M. ,  PICKRELL, Alexander J. ,  STELLWAGEN, John C. ,  SUN, Zhen ,  TAMAYO, Nuria A. ,  ZHANG, Wenhan ,  ZHU, Kai

IPC: C07D401/14 ,  C07D471/10 ,  C07D487/10 ,  A61K31/517 ,  A61P35/00

Abstract: Provided are compounds of Formula (I) having activity as inhibitors of G12C mutant KRAS protein, pharmaceutical compositions comprising the compounds, and uses and methods of treating certain disorders, such as cancer, including but not limited to lung, pancreatic and colorectal cancers.

公开(公告)号：WO2021026098A1

公开(公告)日：2021-02-11

申请号：PCT/US2020/044797

申请日：2020-08-03

Applicant: AMGEN INC.

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

IPC: C07D221/20 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  A61P35/00 ,  A61K31/438

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：WO2020132651A1

公开(公告)日：2020-06-25

申请号：PCT/US2019/068172

申请日：2019-12-20

Applicant: AMGEN INC.

Inventor： TAMAYO, Nuria A. ,  BANERJEE, Abhisek ,  BROWN, James Alexander ,  FROHN, Michael J. ,  CHEN, Jian Jeffrey ,  LI, Kexue ,  LIU, Qingyian ,  LOW, Jonathan Dante ,  MA, Vu ,  PETTUS, Liping H. ,  WALTON, Mary Catherine ,  MINATTI, Ana Elena ,  BOURBEAU, Matthew Paul ,  JIA, Lei ,  NGUYEN, Thomas T. ,  NISHIMURA, Nobuko ,  XUE, Qiufen May ,  ALLEN, John Gordon

IPC: A61P35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  A61K31/497 ,  A61K31/444

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：WO2020050890A2

公开(公告)日：2020-03-12

申请号：PCT/US2019/036626

申请日：2019-06-11

Applicant: AMGEN INC.

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

Abstract: Provided herein are KRAS G12C inhibitors, such as [Insert Compound Here] 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：WO2014134341A1

公开(公告)日：2014-09-04

申请号：PCT/US2014/019100

申请日：2014-02-27

Applicant: AMGEN INC.

Inventor： MINATTI, Ana Elena ,  LOW, Jonathan D. ,  ALLEN, Jenifer R. ,  CHEN, Jian ,  CHEN, Ning ,  CHENG, Yuan ,  JUDD, Ted ,  LIU, Qingyian ,  LOPEZ, Patricia ,  QIAN, Wenyuan ,  RUMFELT, Shannon ,  RZASA, Robert M. ,  TAMAYO, Nuria A. ,  XUE, Qiufen ,  YANG, Bryant ,  ZHONG, Wenge

IPC: C07D413/14 ,  A61K31/535 ,  A61K31/5355 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D471/04 ,  C07D265/08 ,  C07D498/04 ,  C07D513/04 ,  A61P25/00

CPC classification number: C07D413/14 ,  C07D265/08 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  C07F7/0812

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 A 4 , A 5 , A 6 , A 8 , each of R 1 and R 2 , R 3 and R 7 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 Formulas II and III, and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.

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中的各个R 1和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。 本发明还提供式II和III的化合物及其分式实施方案，可用于制备式I-III化合物的中间体和方法和方法。

公开(公告)号：WO2009085230A1

公开(公告)日：2009-07-09

申请号：PCT/US2008/013940

申请日：2008-12-18

Applicant: AMGEN INC. ,  BOOKER, Shon ,  KIM, Tae-seong ,  LIAO, Hongyu ,  LIU, Longbin ,  NORMAN, Mark H. ,  PETERSON, Emily Anne ,  STEC, Markian ,  TAMAYO, Nuria A.

Inventor： BOOKER, Shon ,  KIM, Tae-seong ,  LIAO, Hongyu ,  LIU, Longbin ,  NORMAN, Mark H. ,  PETERSON, Emily Anne ,  STEC, Markian ,  TAMAYO, Nuria A.

IPC: C07D471/04 ,  C07D487/04 ,  A61K31/4162 ,  A61P35/00

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof, that inhibit phosphoinositide 3-kinase; Formula (I) methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds.

Abstract translation: 本发明涉及抑制磷酸肌醇3-激酶的式I化合物或其药学上可接受的盐; 式（I）使用该化合物治疗疾病或病症如癌症的方法; 和含有这些化合物的药物组合物。

公开(公告)号：WO2009017822A2

公开(公告)日：2009-02-05

申请号：PCT/US2008/009312

申请日：2008-08-01

Applicant: AMGEN INC. ,  BOOKER, Shon ,  D'ANGELO, Noel ,  D'AMICO, Derin C. ,  KIM, Tae-seong ,  LIU, Longbin ,  MEAGHER, Kristin ,  NORMAN, Mark H. ,  PANTER, Kathleen ,  SCHENKEL, Laurie B. ,  SMITH, Adrian L. ,  TAMAYO, Nuria A. ,  WHITTINGTON, Douglas A. ,  XI, Ning ,  YANG, Kevin

Inventor： BOOKER, Shon ,  D'ANGELO, Noel ,  D'AMICO, Derin C. ,  KIM, Tae-seong ,  LIU, Longbin ,  MEAGHER, Kristin ,  NORMAN, Mark H. ,  PANTER, Kathleen ,  SCHENKEL, Laurie B. ,  SMITH, Adrian L. ,  TAMAYO, Nuria A. ,  WHITTINGTON, Douglas A. ,  XI, Ning ,  YANG, Kevin

IPC: C07D277/82 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D513/04 ,  A61K31/423 ,  A61K31/424 ,  A61K31/428 ,  A61K31/429 ,  A61P35/00

CPC classification number: C07D277/82 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D513/04

Abstract: The present invention comprises a new class of compounds capable of modulating the activity of PI3 kinase and, accordingly, useful for treatment of PI3 kinase mediated diseases, including melanomas, carcinomas and other cancer-related conditions. The compounds have a general Formula I wherein each of A 1 , A 2 , A 3 , A 4 , X, R 1 and R 2 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of PI3 kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

Abstract translation: 本发明包括能够调节PI3激酶活性的新一类化合物，因此可用于治疗PI3激酶介导的疾病，包括黑素瘤，癌和其它癌症相关病症。 所述化合物具有通式I，其中A1，A2，A3，A4，X，R1和R2各自在本文中定义。 本发明还包括药物组合物，治疗PI3激酶介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。

公开(公告)号：WO2022115377A1

公开(公告)日：2022-06-02

申请号：PCT/US2021/060332

申请日：2021-11-22

Applicant: AMGEN INC.

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

IPC: C07D471/04 ,  A61K31/4355 ,  A61K31/437 ,  A61K31/501 ,  A61P35/00 ,  C07D491/048 ,  C07D491/147 ,  C07D471/14 ,  C07D498/04 ,  C07D401/14 ,  C07D401/12 ,  C07D495/04

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 Formule (I).

公开(公告)号：WO2022093856A1

公开(公告)日：2022-05-05

申请号：PCT/US2021/056702

申请日：2021-10-26

Applicant: AMGEN INC.

Inventor： LANMAN, Brian Alan ,  BANERJEE, Abhisek ,  CHU-MOYER, Margaret ,  DAI, Dongcheng ,  KALLER, Matthew R. ,  LOPEZ, Patricia ,  MA, Vu Van ,  MANONI, Francesco ,  MEDINA, Jose M. ,  PICKRELL, Alexander J. ,  TAMAYO, Nuria A. ,  ZHU, Kai

IPC: A61P35/00 ,  C07D487/10 ,  C07D491/04 ,  C07D513/04 ,  A61K31/506 ,  A61K31/519 ,  A61K31/541 ,  A61K31/517 ,  A61K31/5395

Abstract: The present disclosure provides compounds of Formula (I) having activity as inhibitors of G12C mutant KRAS protein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses and methods of treating certain disorders, such as cancer, including but not limited to lung, pancreatic and colorectal cancers.

公开(公告)号：WO2020132649A1

公开(公告)日：2020-06-25

申请号：PCT/US2019/068170

申请日：2019-12-20

Applicant: AMGEN INC.

Inventor： TAMAYO, Nuria A. ,  BANERJEE, Abhisek ,  CHEN, Jian Jeffrey ,  LI, Kexue ,  PETTUS, Liping H. ,  BOURBEAU, Matthew Paul ,  JIA, Lei

IPC: C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  A61P35/00 ,  A61K31/506

Abstract: The present invention relates to chemical compounds having a general 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.