公开(公告)号：US11021493B2

公开(公告)日：2021-06-01

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 ,  A61P25/28 ,  C07D417/10

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：US09663476B2

公开(公告)日：2017-05-30

申请号：US14264731

申请日：2014-04-29

Applicant: AMGEN INC.

Inventor： Stephen A. Hitchcock ,  Albert Amegadzie ,  Wenyuan Qian ,  Xiaoyang Xia ,  Scott S. Harried

IPC: C07D295/108 ,  C07D241/04 ,  C07D295/15 ,  C07D241/08

CPC classification number: C07D241/04 ,  A61K31/495 ,  A61K31/551 ,  A61K33/00 ,  C07D213/36 ,  C07D241/08 ,  C07D243/08 ,  C07D295/15 ,  C07D333/20

Abstract: The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

公开(公告)号：US09611261B2

公开(公告)日：2017-04-04

申请号：US14932787

申请日：2015-11-04

Applicant: AMGEN INC.

Inventor： Ana Elena Minatti ,  Jonathan D. Low ,  Jennifer R. Allen ,  Albert Amegadzie ,  James Brown ,  Michael J. Frohn ,  Angel Guzman-Perez ,  Paul E. Harrington ,  Patricia Lopez ,  Vu Van Ma ,  Nobuko Nishimura ,  Wenyuan Qian ,  Shannon Rumfelt ,  Robert M. Rzasa ,  Kelvin Sham ,  Adrian L. Smith ,  Ryan White ,  Qiufen Xue

IPC: C07D471/04 ,  C07D265/12 ,  C07D413/14 ,  C07D413/12 ,  C07D417/14 ,  C07D417/12 ,  C07D413/10 ,  C07D491/048 ,  C07D413/04

CPC classification number: C07D413/12 ,  C07D265/12 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048

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, 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.

公开(公告)号：US09493459B2

公开(公告)日：2016-11-15

申请号：US15058023

申请日：2016-03-01

Applicant: AMGEN INC.

Inventor： Jennifer R. Allen ,  Jian J. Chen ,  Michael J. Frohn ,  Matthew R. Kaller ,  Qingyian Liu ,  Thomas T. Nguyen ,  Alexander J. Pickrell ,  Wenyuan Qian ,  Robert M. Rzasa ,  Wenge Zhong

IPC: C07D401/04 ,  C07D403/04 ,  C07D471/04 ,  C07D401/14 ,  A61K31/497 ,  A61K45/06 ,  A61K31/517 ,  C07D403/14

CPC classification number: C07D471/04 ,  A61K31/497 ,  A61K31/517 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

Abstract: Azetidine and piperidine compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds and intermediates thereof. Provided herein also are methods of treating cognitive disorders or diseases treatable by inhibition of PDE10, such as Huntington's Disease, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

公开(公告)号：US20150307457A1

公开(公告)日：2015-10-29

申请号：US14264731

申请日：2014-04-29

Applicant: AMGEN INC.

Inventor： Stephen A. Hitchcock ,  Albert Amegadzie ,  Wenyuan Qian ,  Xiaoyang Xia ,  Scott S. Harried

IPC: C07D241/04 ,  C07D241/08 ,  C07D295/15

CPC classification number: C07D241/04 ,  A61K31/495 ,  A61K31/551 ,  A61K33/00 ,  C07D213/36 ,  C07D241/08 ,  C07D243/08 ,  C07D295/15 ,  C07D333/20

Abstract: The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.