公开(公告)号：US20200231601A1

公开(公告)日：2020-07-23

申请号：US16466207

申请日：2017-12-13

申请人： AMGEN INC.

发明人： 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分类号： C07D513/08 ,  C07D417/10 ,  A61P25/28

摘要： 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：US20210171529A1

公开(公告)日：2021-06-10

申请号：US17103350

申请日：2020-11-24

申请人： Amgen Inc.

发明人： Jennifer R. ALLEN ,  Albert AMEGADZIE ,  Matthew P. BOURBEAU ,  Ning CHEN ,  Clifford GOODMAN ,  Giulia LATTANZI ,  Iain LINGARD ,  Qingyian LIU ,  Jonathan D. LOW ,  Vu Van MA ,  Ana E. MINATTI ,  Alfonso POZZAN ,  Corey REEVES ,  Aaron C. SIEGMUND ,  Sabrina TASSINI ,  Federica TONELLI ,  Mary WALTON

IPC分类号： C07D487/04 ,  A61P3/04 ,  C07D471/04 ,  C07D498/04

摘要： The present disclosure provides compounds useful for the inhibition of Delta-5 Desaturase (“D5D”). The compounds have a general Formula 1: wherein the variables of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a metabolic or cardiovascular disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

公开(公告)号：US20200231585A1

公开(公告)日：2020-07-23

申请号：US16466199

申请日：2017-12-13

申请人： AMGEN INC.

发明人： Jennifer R. ALLEN ,  Albert AMEGADZIE ,  Matthew P. BOURBEAU ,  Jian J. CHEN ,  Michael J. FROHN ,  Paul E. HARRINGTON ,  Jonathan D. LOW ,  Vu V. MA ,  Thomas T. NGUYEN ,  Alexander PICKRELL ,  Corey REEVES

IPC分类号： C07D417/14 ,  C07D417/10

摘要： The present disclosure 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 A, R1, R2, R2′, R3, R4, and R5 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：US20200207747A1

公开(公告)日：2020-07-02

申请号：US16466211

申请日：2017-12-13

申请人： AMGEN INC.

发明人： Jennifer R. ALLEN ,  Matthew P. BOURBEAU ,  Ning CHEN ,  Michael J. FROHN ,  Paul E. HARRINGTON ,  Qingyian LIU ,  Corey REEVES

IPC分类号： C07D413/10 ,  C07D413/14 ,  A61P25/28

摘要： 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: (insert Formula I structure) wherein variables W, X, Y, 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 beta amyloid (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.