公开(公告)号：US20200231601A1

公开(公告)日：2020-07-23

申请号：US16466207

申请日：2017-12-13

Applicant: AMGEN INC.

Inventor： Jennifer R. ALLEN ,  Matthew P. BOURBEAU ,  James A. BROWN ,  Ning CHEN ,  Michael J. FROHN ,  Zice FU ,  Longbin LIU ,  Qingyian LIU ,  Liping H. PETTUS ,  Wenyuan QIAN ,  Corey REEVES ,  Aaron C. SIEGMUND

IPC: C07D513/08 ,  C07D417/10 ,  A61P25/28

Abstract: The present disclosure provides a class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A, X, R2, R2′, R3, R4, R5, R6, and R7 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：US20180222876A1

公开(公告)日：2018-08-09

申请号：US15749895

申请日：2016-08-04

Applicant: AMGEN INC.

Inventor： Jennifer R. ALLEN ,  Albert AMEGADZIE ,  Matthew P. BOURBEAU ,  James A. BROWN ,  Ning CHEN ,  Michael J. FROHN ,  Longbin LIU ,  Qingyian LIU ,  Liping H. PETTUS ,  Wenyuan QIAN ,  Corey M. REEVES ,  Aaron C. SIEGMUND

IPC: C07D279/08 ,  A61P25/28 ,  A61P25/16 ,  A61P25/00 ,  C07D417/14 ,  C07D417/10 ,  C07D491/08 ,  C07F7/08 ,  C07D471/04 ,  C07D491/056 ,  C07D498/10 ,  C07D491/107

CPC classification number: C07D279/08 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D491/056 ,  C07D491/08 ,  C07D491/107 ,  C07D498/10 ,  C07F7/0812

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, A7, and each of Ra, Rb, R1, R2, R3, R8 R9 and R10 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 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, schizophrenia and other central nervous system conditions.