公开(公告)号：US20180051021A1

公开(公告)日：2018-02-22

申请号：US15554801

申请日：2016-03-02

Applicant: AMGEN INC.

Inventor： Matthew WEISS ,  Benjamin Charles MILGRAM ,  Thomas DINEEN ,  John STELLWAGEN ,  Angel GUZMAN-PEREZ ,  Alessandro BOEZIO ,  Issac E. MARX

IPC: C07D471/04

Abstract: The present invention provides compounds of Formula (I), wherein: as defined in the specification, an enantiomer, diastereomer, atropisomer thereof, or a mixture thereof, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders, cough, or itch. Also provided are pharmaceutical compositions containing compounds of the present invention.

公开(公告)号：US20200308145A1

公开(公告)日：2020-10-01

申请号：US16754349

申请日：2018-10-18

Applicant: Amgen Inc.

Inventor： Michael D. BARTBERGER ,  Nagasree CHAKKA ,  Hua GAO ,  Angel GUZMAN-PEREZ ,  Daniel B. HORNE ,  Zihao HUA ,  Madeleine KIEFFER ,  Daniel C. H. Lin ,  Benjamin Charles MILGRAM ,  Jane PANTELEEV ,  Laurie SCHENKEL ,  John STELLWAGEN ,  Matthew WEISS ,  Ryan D. WHITE ,  Wei ZHAO

IPC: C07D401/14 ,  C07D471/10 ,  C07D471/04 ,  C07D498/04 ,  C07D401/04 ,  C07D403/04 ,  C07D413/14

Abstract: The present invention relates to inhibitors of Transient Receptor Potential Channel 6 (TRPC6) protein activity. 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：US20190167682A1

公开(公告)日：2019-06-06

申请号：US16319783

申请日：2017-07-20

Applicant: AMGEN INC.

Inventor： Matthew WEISS ,  John R. BUTLER ,  Benjamin Charles MILGRAM ,  Gwenaella RESCOURIO ,  Alessandro BOEZIO ,  Brian Andrew SPARLING ,  Daniel LA

IPC: A61K31/506 ,  A61P25/00 ,  A61K31/4439

CPC classification number: A61K31/506 ,  A61K31/4439 ,  A61P25/00 ,  C07D213/75 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

Abstract: The present invention provides compounds of Formula (I), as defined in the specification, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders, cough, or itch. Also provided are pharmaceutical compositions containing compounds of the present invention.

公开(公告)号：US20160046626A1

公开(公告)日：2016-02-18

申请号：US14920833

申请日：2015-10-22

Applicant: AMGEN INC.

Inventor： Matthew WEISS ,  Alessandro BOEZIO ,  Christiane BOEZIO ,  John R. BUTLER ,  Margaret Yuhua CHU-MOYER ,  Erin F. DIMAURO ,  Thomas DINEEN ,  Russell GRACEFFA ,  Angel GUZMAN-PEREZ ,  Hongbing HUANG ,  Charles KREIMAN ,  Daniel LA ,  Isaac E. MARX ,  Benjamin Charles MILGRAM ,  Hanh Nho NGUYEN ,  Emily Anne PETERSON ,  Karina R. VAIDA ,  Brian SPARLING

IPC: C07D471/04 ,  C07D417/12 ,  C07D413/14 ,  C07D413/12 ,  C07D401/12

CPC classification number: C07D417/14 ,  C07C53/18 ,  C07D215/227 ,  C07D215/36 ,  C07D241/44 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

Abstract: The present invention provides compounds of Formula I, and pharmaceutically acceptable salts thereof, that are inhibitors of 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 and itch. Also provided are pharmaceutical compositions containing compounds of the present invention.

Abstract translation: 本发明提供式I化合物及其药学上可接受的盐，其是电压门控钠通道的抑制剂，特别是Nav1.7。 该化合物可用于治疗与钠通道活性相关的疾病，例如疼痛障碍和瘙痒。 还提供含有本发明化合物的药物组合物。