公开(公告)号：US20230295170A1

公开(公告)日：2023-09-21

申请号：US18072505

申请日：2022-11-30

Applicant: AMGEN INC. ,  Vigil Neuroscience, Inc.

Inventor： Lara C. CZABANIUK ,  Timothy Hopper ,  Jonathan B. Houze ,  Jane Panteleev ,  Gwenaella Rescourio ,  Vincent Santora ,  Haoxuan Wang ,  Ryan D. White ,  Alice R. Wong ,  Yongwei Wu ,  Maxence Bos ,  John Mancuso ,  Ivan Franzoni

IPC: C07D487/04 ,  A61P25/28 ,  C07D413/14 ,  C07D471/04

CPC classification number: C07D487/04 ,  A61P25/28 ,  C07D413/14 ,  C07D471/04

Abstract: The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2”).




This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

公开(公告)号：US11884675B2

公开(公告)日：2024-01-30

申请号：US18072501

申请日：2022-11-30

Applicant: AMGEN INC. ,  Vigil Neuroscience, Inc.

Inventor： Lara C. Czabaniuk ,  Timothy Hopper ,  Jonathan B. Houze ,  Jane Panteleev ,  Gwenaella Rescourio ,  Vincent Santora ,  Haoxuan Wang ,  Ryan D. White ,  Alice R. Wong ,  Yongwei Wu ,  Maxence Bos ,  John Mancuso ,  Ivan Franzoni

IPC: C07D487/04 ,  A61P25/28 ,  C07D413/14 ,  C07D471/04

CPC classification number: C07D487/04 ,  A61P25/28 ,  C07D413/14 ,  C07D471/04

Abstract: The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2”).




This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

公开(公告)号：US11718617B2

公开(公告)日：2023-08-08

申请号：US18072497

申请日：2022-11-30

Applicant: AMGEN INC. ,  Vigil Neuroscience, Inc.

Inventor： Lara C. Czabaniuk ,  Timothy Hopper ,  Jonathan B. Houze ,  Gwenaella Rescourio ,  Vincent Santora ,  Haoxuan Wang ,  Ryan D. White ,  Alice R. Wong ,  Yongwei Wu

IPC: C07D471/04 ,  C07D413/14

CPC classification number: C07D471/04 ,  C07D413/14

Abstract: The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2”).




This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

公开(公告)号：US11608344B2

公开(公告)日：2023-03-21

申请号：US17302502

申请日：2021-05-04

Applicant: AMGEN INC. ,  Vigil Neuroscience, Inc.

Inventor： Lara C. Czabaniuk ,  Timothy Hopper ,  Jonathan B. Houze ,  Jane Panteleev ,  Gwenaella Rescourio ,  Vincent Santora ,  Haoxuan Wang ,  Ryan D. White ,  Alice R. Wong ,  Yongwei Wu ,  Maxence Bos ,  John Mancuso ,  Ivan Franzoni

IPC: C07D487/04 ,  C07D413/14 ,  C07D471/04 ,  A61P25/28

Abstract: The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2”). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

公开(公告)号：US11912711B2

公开(公告)日：2024-02-27

申请号：US18072505

申请日：2022-11-30

Applicant: AMGEN INC. ,  Vigil Neuroscience, Inc.

Inventor： Lara C. Czabaniuk ,  Timothy Hopper ,  Jonathan B. Houze ,  Jane Panteleev ,  Gwenaella Rescourio ,  Vincent Santora ,  Haoxuan Wang ,  Ryan D. White ,  Alice R. Wong ,  Yongwei Wu ,  Maxence Bos ,  John Mancuso ,  Ivan Franzoni

IPC: C07D475/00 ,  A61P25/28 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04

CPC classification number: C07D487/04 ,  A61P25/28 ,  C07D413/14 ,  C07D471/04 ,  C07D475/00

Abstract: The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2”).




This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

公开(公告)号：US11572374B2

公开(公告)日：2023-02-07

申请号：US17266466

申请日：2019-08-13

Applicant: Amgen Inc. ,  Carmot Therapeutics, Inc.

Inventor： John R. Butler ,  Daniel Erlanson ,  Russell Graceffa ,  Jeffrey Iwig ,  Joon Won Jeong ,  Ryan D. White ,  Yongwei Wu ,  Shuyan Yi ,  Xiao Mei Zheng ,  Jesse M. McFarland ,  Abhisek Banerjee

IPC: C07D519/00 ,  C07D487/18

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.

公开(公告)号：US20150266824A1

公开(公告)日：2015-09-24

申请号：US14633936

申请日：2015-02-27

Applicant: AMGEN INC. ,  Teijin Pharma Limited

Inventor： Hilary Plake Beck ,  Shon Keith Booker ,  Howard Bregman ,  Victor J. Cee ,  Nagasree Chakka ,  Timothy D. Cushing ,  Oleg Epstein ,  Brian M. Fox ,  Stephanie Geuns-Meyer ,  Xiaolin Hao ,  Kenta Hibiya ,  Jun Kirata ,  Zihao Hua ,  Jason Human ,  Shinji Kakuda ,  Patricia Lopez ,  Ryota Nakajima ,  Kazuhisa Okada ,  Steven H. Olson ,  Hiroyuki Oono ,  Lewis D. Pennington ,  Kosuke Sasaki ,  Keiko Shimada ,  Youngsook Shin ,  Ryan D. White ,  Ryan P. Wurz ,  Shuyan Yi ,  Xiao Mei Zheng

IPC: C07D231/14 ,  C07D409/12 ,  C07D413/12 ,  C07D405/14 ,  C07D401/14 ,  C07D493/08 ,  C07D401/12 ,  C07D403/12

CPC classification number: C07D231/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/14 ,  C07D493/08

Abstract: The present invention relates to a novel compound having a function of inhibiting RORγ activity. The present invention also relates to pharmaceutical composition comprising the compound, a use of the compound in treating or preventing autoimmune diseases, inflammatory diseases, metabolic diseases, or cancer diseases.

Abstract translation: 本发明涉及具有抑制RORγ活性的新型化合物。 本发明还涉及包含该化合物的药物组合物，该化合物在治疗或预防自身免疫疾病，炎性疾病，代谢疾病或癌症疾病中的用途。

公开(公告)号：US09550762B2

公开(公告)日：2017-01-24

申请号：US14819256

申请日：2015-08-05

Applicant: AMGEN INC.

Inventor： Jennifer R. Allen ,  Albert Amegadzie ,  Matthew P. Bourbeau ,  James A. Brown ,  Jian J. Chen ,  Yuan Cheng ,  Michael J. Frohn ,  Angel Guzman-Perez ,  Paul E. Harrington ,  Longbin Liu ,  Qingyian Liu ,  Jonathan D. Low ,  Vu Van Ma ,  James Manning ,  Ana Elena Minatti ,  Thomas T. Nguyen ,  Nobuko Nishimura ,  Mark H. Norman ,  Liping H. Pettus ,  Alexander J. Pickrell ,  Wenyuan Qian ,  Shannon Rumfelt ,  Robert M. Rzasa ,  Aaron C. Siegmund ,  Markian M. Stec ,  Ryan D. White ,  Qiufen Xue

IPC: C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D513/10 ,  C07D417/04 ,  C07D279/08

CPC classification number: C07D417/12 ,  C07D279/08 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D513/10

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, and 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。 所述化合物具有通式I：其中式I中的变量A4，A5，A6，A8以及R 1，R b，R 1，R 2，R 3和R 7各自独立地定义。 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。

公开(公告)号：US09365522B2

公开(公告)日：2016-06-14

申请号：US14633936

申请日：2015-02-27

Applicant: AMGEN INC. ,  TEIJIN PHARMA LIMITED

Inventor： Hilary Plake Beck ,  Shon Keith Booker ,  Howard Bregman ,  Victor J. Cee ,  Nagasree Chakka ,  Timothy D. Cushing ,  Oleg Epstein ,  Brian M. Fox ,  Stephanie Geuns-Meyer ,  Xiaolin Hao ,  Kenta Hibiya ,  Jun Hirata ,  Zihao Hua ,  Jason Human ,  Shinji Kakuda ,  Patricia Lopez ,  Ryota Nakajima ,  Kazuhisa Okada ,  Steven H. Olson ,  Hiroyuki Oono ,  Lewis D. Pennington ,  Kosuke Sasaki ,  Keiko Shimada ,  Youngsook Shin ,  Ryan D. White ,  Ryan P. Wurz ,  Shuyan Yi ,  Xiao Mei Zheng

IPC: C07D231/14 ,  C07D403/12 ,  C07D401/14 ,  C07D405/14 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/14 ,  C07D493/08 ,  C07D413/12 ,  A61K31/4155 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/422

CPC classification number: C07D231/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/14 ,  C07D493/08

Abstract: The present invention relates to a novel compound having a function of inhibiting RORγ activity. The present invention also relates to pharmaceutical composition comprising the compound, a use of the compound in treating or preventing autoimmune diseases, inflammatory diseases, metabolic diseases, or cancer diseases.

Abstract translation: 本发明涉及具有抑制RORγ活性的新型化合物。 本发明还涉及包含该化合物的药物组合物，该化合物在治疗或预防自身免疫疾病，炎性疾病，代谢疾病或癌症疾病中的用途。