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.

公开(公告)号：US20160102075A1

公开(公告)日：2016-04-14

申请号：US14973491

申请日：2015-12-17

Applicant: AMGEN INC.

Inventor： Jennifer R. ALLEN ,  Jian J. CHEN ,  Michael J. FROHN ,  Essa Hu HARRINGTON ,  Qingyian LIU ,  Alexander J. PICKRELL ,  Shannon RUMFELT ,  Robert M. RZASA ,  Wenge ZHONG

IPC: C07D401/14 ,  C07D409/14 ,  C07D403/14 ,  C07D491/107 ,  C07D487/10 ,  C07C53/18 ,  C07D405/14 ,  C07D413/14 ,  C07D487/04 ,  C07D491/08 ,  C07D487/08 ,  C07D471/04 ,  C07D491/056 ,  C07D513/04 ,  C07D417/14

CPC classification number: C07D401/14 ,  C07C53/18 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/056 ,  C07D491/08 ,  C07D491/107 ,  C07D513/04

Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

Abstract translation: 式（I）的不饱和氮杂环化合物：如说明书中所定义，含有它们的组合物，以及制备这些化合物的方法。 本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，亨廷顿舞蹈病，非胰岛素依赖性糖尿病，精神分裂症，双相障碍，强迫症等。