公开(公告)号：WO2018112086A1

公开(公告)日：2018-06-21

申请号：PCT/US2017/066184

申请日：2017-12-13

Applicant: AMGEN INC.

Inventor： ALLEN, Jennifer R. ,  AMEGADZIE, Albert ,  BOURBEAU, Matthew P. ,  CHEN, Jian J. ,  FROHN, Michael J. ,  HARRINGTON, Paul E. ,  LOW, Jonathan D. ,  MA, Vu V. ,  NGUYEN, Thomas T. ,  PICKRELL, Alexander J. ,  REEVES, Corey

IPC: C07D417/10 ,  C07D417/14 ,  C07D279/08 ,  A61P25/28 ,  A61K31/5415

Abstract: The present disclosure 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, R 1 , R 2 , R 2' , R 3 , R 4 , and R 5 of Formula (I) are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Aβ 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, and other central nervous system conditions.

公开(公告)号：WO2021026099A1

公开(公告)日：2021-02-11

申请号：PCT/US2020/044798

申请日：2020-08-03

Applicant: AMGEN INC.

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

IPC: C07D241/28 ,  C07D401/04 ,  C07D401/14 ,  A61P35/00 ,  A61K31/497

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：WO2020132653A1

公开(公告)日：2020-06-25

申请号：PCT/US2019/068174

申请日：2019-12-20

Applicant: AMGEN INC.

Inventor： TAMAYO, Nuria A. ,  BANERJEE, Abhisek ,  FROHN, Michael J. ,  CHEN, Jian Jeffrey ,  LI, Kexue ,  BOURBEAU, Matthew Paul ,  JIA, Lei ,  KALLER, Matthew Richard ,  NGUYEN, Thomas T. ,  NISHIMURA, Nobuko ,  XUE, Qiufen May ,  ALLEN, John Gordon

IPC: C07D221/20 ,  C07D401/14 ,  C07D413/14 ,  A61P35/00 ,  A61K31/497 ,  C07D405/14 ,  C07D491/08 ,  C07D491/107

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.

公开(公告)号：WO2013188724A1

公开(公告)日：2013-12-19

申请号：PCT/US2013/045768

申请日：2013-06-14

Applicant: AMGEN INC.

Inventor： ALLEN, Jennifer R. ,  CHEN, Jian J. ,  FROHN, Michael J. ,  KALLER, Matthew Richard ,  LIU, Qingyian ,  NGUYEN, Thomas T. ,  PICKRELL, Alexander J. ,  QIAN, Wenyuan ,  RZASA, Robert M. ,  ZHONG, Wenge

IPC: C07D401/14 ,  C07D403/14 ,  A61K31/497 ,  A61P25/00

CPC classification number: C07D471/04 ,  A61K31/497 ,  A61K31/517 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

Abstract: Azetidine and piperidine compounds of formula (I) as defined in the specification, compositions containing them, and processes for preparing such compounds and intermediates thereof. Provided herein also are methods of treating cognitive disorders or diseases treatable by inhibition of PDE10, such as Huntington's Disease, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

Abstract translation: 说明书中定义的式（I）的氮杂环丁烷和哌啶化合物，含有它们的组合物，以及制备这些化合物的方法及其中间体。 本文还提供治疗认知障碍或通过抑制PDE10可治疗的疾病的方法，例如亨廷顿病，精神分裂症，双相障碍，强迫症等。

公开(公告)号：WO2020050890A3

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

IPC: C07D471/04 ,  C07D487/04 ,  A61K31/519 ,  A61K31/551 ,  A61P35/00 ,  A61K45/06

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：WO2018217651A1

公开(公告)日：2018-11-29

申请号：PCT/US2018/033714

申请日：2018-05-21

Applicant: AMGEN INC.

Inventor： LANMAN, Brian Alan ,  CHEN, Jian ,  REED, Anthony B. ,  CEE, Victor J. ,  LIU, Longbin ,  KOPECKY, David John ,  LOPEZ, Patricia ,  WURZ, Ryan Paul ,  NGUYEN, Thomas T. ,  BOOKER, Shon ,  NISHIMURA, Nobuko ,  SHIN, Youngsook ,  TAMAYO, Nuria A. ,  ALLEN, John Gordon ,  ALLEN, Jennifer Rebecca

IPC: C07D471/04 ,  A61K31/519 ,  A61P35/00 ,  C07D475/00

Abstract: 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：WO2013130660A1

公开(公告)日：2013-09-06

申请号：PCT/US2013/028087

申请日：2013-02-27

Applicant: AMGEN INC.

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

IPC: C07D471/04 ,  C07D487/04 ,  A61K31/4353 ,  A61P35/00

CPC classification number: C07D471/04 ,  C07D401/04 ,  C07D487/04

Abstract: 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.

Abstract translation: 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：EP2569302A1

公开(公告)日：2013-03-20

申请号：EP11724480.6

申请日：2011-05-12

Applicant: Amgen, Inc

Inventor： ALLEN, Jennifer ,  HORNE, Daniel B. ,  HARRINGTON, Essa Hu ,  KALLER, Matthew R. ,  MONENSCHEIN, Holger ,  NGUYEN, Thomas T. ,  REICHELT, Andreas ,  RZASA, Robert M.

IPC: C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/10 ,  A61K31/4709 ,  A61K31/454 ,  A61K31/4535 ,  A61P25/18

CPC classification number: C07D491/107 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10

Abstract: Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.

Abstract translation: 杂芳氧基杂环基化合物和含有它们的组合物，以及制备这些化合物的方法。 本文还提供了治疗可通过抑制PDE10治疗的疾病或疾病，例如肥胖症，非胰岛素依赖性糖尿病，精神分裂症，亨廷顿舞蹈病，双相型障碍，强迫性障碍等的方法。

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.