公开(公告)号：WO2014035872A1

公开(公告)日：2014-03-06

申请号：PCT/US2013/056593

申请日：2013-08-26

Applicant: AMGEN INC.

Inventor： ASHTON, Kate ,  FOTSCH, Christopher H. ,  KUNZ, Roxanne K. ,  LIU, Longbin ,  NISHIMURA, Nobuko ,  NORMAN, Mark H. ,  SIEGMUND, Aaron C. ,  ST. JEAN, JR., David J. ,  TAMAYO, Nuria A. ,  YANG, Kevin C.

IPC: C07D403/12 ,  C07D401/14 ,  C07D413/14 ,  C07D401/12 ,  C07D417/14 ,  A61K31/501 ,  A61K31/496 ,  A61P3/00

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to tricyclic alkyne compounds of formula I that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.

Abstract translation: 本发明涉及与葡萄糖激酶调节蛋白相互作用的式I的三环炔化合物。 此外，本发明还涉及治疗2型糖尿病的方法，以及使用该化合物或其药学上可接受的盐涉及葡萄糖激酶调节蛋白的其它疾病和/或病症，以及含有该化合物或其药学上可接受的盐的药物组合物 它们。

公开(公告)号：WO2006069258A1

公开(公告)日：2006-06-29

申请号：PCT/US2005/046652

申请日：2005-12-20

Applicant: AMGEN INC

Inventor： HONG, Fang-tsao ,  LIAO, Hongyu ,  LOPEZ, Patricia ,  TADESSE, Seifu ,  TAMAYO, Nuria A.

IPC: C07D471/04 ,  C07D498/04 ,  A61K31/4375 ,  A61K31/5383 ,  A61P29/00

CPC classification number: C07D471/04

Abstract: The present invention relates to nitrogen-containing compounds according to formula (I) and pharmaceutically acceptable salts thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic ß cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.

Abstract translation: 本发明涉及式（I）的含氮化合物及其药学上可接受的盐。 还包括治疗炎症，类风湿性关节炎，佩吉特病，骨质疏松症，多发性骨髓瘤，葡萄膜炎，急性或慢性骨髓性白血病，胰腺β细胞破坏，骨关节炎，类风湿性脊椎炎，痛风性关节炎，炎性肠病，成人呼吸窘迫综合征 （ARDS），牛皮癣，克罗恩病，过敏性鼻炎，溃疡性结肠炎，过敏反应，接触性皮炎，哮喘，肌肉退化，恶病质，赖特综合征，I型糖尿病，II型糖尿病，骨吸收疾病，移植物抗宿主反应，阿尔茨海默病 ，中风，心肌梗塞，缺血再灌注损伤，动脉粥样硬化，脑外伤，多发性硬化，脑疟疾，败血症，败血性休克，中毒性休克综合征，发热，HIV-1，HIV-2，HIV-3，巨细胞病毒 ），流感病毒，腺病毒，哺乳动物中的疱疹病毒或带状疱疹感染，包括给予有效量的如上所述的化合物。

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：WO2012027261A1

公开(公告)日：2012-03-01

申请号：PCT/US2011/048596

申请日：2011-08-22

Applicant: AMGEN INC. ,  ASHTON, Kate ,  BARTBERGER, Michael David ,  BO, Yunxin ,  BRYAN, Marian C. ,  CROGHAN, Michael ,  FOTSCH, Christopher Harold ,  HALE, Clarence Henderson ,  KUNZ, Roxanne Kay ,  LIU, Longbin ,  NISHIMURA, Nobuko ,  NORMAN, Mark H. ,  PENNINGTON, Lewis Dale ,  POON, Steve Fong ,  STEC, Markian Myroslaw ,  ST. JEAN, David, Joseph, Jr. ,  TAMAYO, Nuria A. ,  TEGLEY, Christopher Michael ,  YANG, Kevin Chao

Inventor： ASHTON, Kate ,  BARTBERGER, Michael David ,  BO, Yunxin ,  BRYAN, Marian C. ,  CROGHAN, Michael ,  FOTSCH, Christopher Harold ,  HALE, Clarence Henderson ,  KUNZ, Roxanne Kay ,  LIU, Longbin ,  NISHIMURA, Nobuko ,  NORMAN, Mark H. ,  PENNINGTON, Lewis Dale ,  POON, Steve Fong ,  STEC, Markian Myroslaw ,  ST. JEAN, David, Joseph, Jr. ,  TAMAYO, Nuria A. ,  TEGLEY, Christopher Michael ,  YANG, Kevin Chao

IPC: C07D213/30 ,  C07D213/71 ,  C07D213/74 ,  C07D231/18 ,  C07D239/42 ,  C07D241/04 ,  C07D277/36 ,  C07D333/34 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/12 ,  C07D491/08 ,  C07D498/08

CPC classification number: C07D333/34 ,  C07C317/22 ,  C07D213/30 ,  C07D213/32 ,  C07D213/71 ,  C07D213/72 ,  C07D213/74 ,  C07D231/18 ,  C07D239/42 ,  C07D241/04 ,  C07D277/36 ,  C07D285/135 ,  C07D295/26 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/08 ,  C07D498/08

Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.

Abstract translation: 本发明涉及与葡萄糖激酶调节蛋白相互作用的式I化合物或其药学上可接受的盐。 此外，本发明还涉及治疗2型糖尿病的方法，以及使用该化合物或其药学上可接受的盐涉及葡萄糖激酶调节蛋白的其它疾病和/或病症，以及含有该化合物或其药学上可接受的盐的药物组合物 它们。

公开(公告)号：WO2021163344A1

公开(公告)日：2021-08-19

申请号：PCT/US2021/017682

申请日：2021-02-11

Applicant: AMGEN INC.

Inventor： ALLEN, Jennifer Rebecca ,  AMEGADZIE, Albert ,  BEYLKIN, Diane Jennifer ,  BOOKER, Shon ,  BOURBEAU, Matthew Paul ,  BUTLER, John R. ,  FROHN, Michael J. ,  GLAD, Sanne Ormholt Schroder ,  HUSEMOEN, Birgitte Weinreich ,  KALLER, Matthew R. ,  KOHN, Todd J. ,  LANMAN, Brian Alan ,  LI, Kexue ,  LIU, Qingyian ,  LOPEZ, Patricia ,  MA, Vu Van ,  MANONI, Francesco ,  MEDINA, Jose ,  MINATTI, Ana Elena ,  PEIRO CADAHIA, Jorge ,  PETTUS, Liping ,  PICKRELL, Alexander J. ,  SARVARY, Ian ,  TAMAYO, Nuria A. ,  VESTERGAARD, Mikkel

IPC: C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  A61P35/00 ,  A61K31/435

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：WO2021026101A1

公开(公告)日：2021-02-11

申请号：PCT/US2020/044800

申请日：2020-08-03

Applicant: AMGEN INC.

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

IPC: C07D401/04 ,  C07D401/14 ,  A61P35/00 ,  A61K31/498

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：WO2021026100A1

公开(公告)日：2021-02-11

申请号：PCT/US2020/044799

申请日：2020-08-03

Applicant: AMGEN INC.

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

IPC: A61P35/00 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D498/08 ,  A61K31/444

Abstract: Amide 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：WO2019213516A1

公开(公告)日：2019-11-07

申请号：PCT/US2019/030593

申请日：2019-05-03

Applicant: AMGEN INC.

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

IPC: C07D403/04 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  A61P35/00 ,  A61K31/519

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：WO2022132914A1

公开(公告)日：2022-06-23

申请号：PCT/US2021/063540

申请日：2021-12-15

Applicant: AMGEN INC.

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

IPC: C07D487/14 ,  C07D491/04 ,  C07D491/14 ,  A61K31/4353

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