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：US12252489B2

公开(公告)日：2025-03-18

申请号：US17923160

申请日：2021-05-04

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 ,  A61K31/519 ,  A61K31/5377 ,  C07D413/14 ,  C07D519/00

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 (1).

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：US12240839B2

公开(公告)日：2025-03-04

申请号：US17633151

申请日：2021-06-10

Applicant: AMGEN INC.

Inventor： Benjamin C Milgram ,  Isaac E Marx ,  Haoxuan Wang ,  Alan H Cherney

IPC: C07D413/12 ,  A61P25/04 ,  C07D215/36 ,  C07D401/12

Abstract: The present invention provides a cyclobutyl dihydroquinoline sulfonamide compound of Formula (I), an enantiomer, diastereoisomer, atropisomer thereof, a mixture thereof, or a pharmaceutically acceptable salt thereof, that inhibits voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders, cough, and itch. Also provided are pharmaceutical compositions containing the compounds of the present invention. Also further provided is an atropi-selective preparation of said compounds of Formula (I), and intermediate thereof.

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.