Invention Grant
US09550762B2 Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
有权
环丙基稠合噻嗪-2-胺化合物作为β-分泌酶抑制剂和使用方法
- Patent Title: Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
- Patent Title (中): 环丙基稠合噻嗪-2-胺化合物作为β-分泌酶抑制剂和使用方法
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Application No.: US14819256Application Date: 2015-08-05
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Publication No.: US09550762B2Publication Date: 2017-01-24
- Inventor: Jennifer R. Allen , Albert Amegadzie , Matthew P. Bourbeau , James A. Brown , Jian J. Chen , Yuan Cheng , Michael J. Frohn , Angel Guzman-Perez , Paul E. Harrington , Longbin Liu , Qingyian Liu , Jonathan D. Low , Vu Van Ma , James Manning , Ana Elena Minatti , Thomas T. Nguyen , Nobuko Nishimura , Mark H. Norman , Liping H. Pettus , Alexander J. Pickrell , Wenyuan Qian , Shannon Rumfelt , Robert M. Rzasa , Aaron C. Siegmund , Markian M. Stec , Ryan D. White , Qiufen Xue
- Applicant: AMGEN INC.
- Applicant Address: US CA Thousand Oaks
- Assignee: Amgen, Inc.
- Current Assignee: Amgen, Inc.
- Current Assignee Address: US CA Thousand Oaks
- Agent Bernard P. Friedrichsen; Markus Bergauer
- Main IPC: C07D417/12
- IPC: C07D417/12 ; C07D417/14 ; C07D471/04 ; C07D513/10 ; C07D417/04 ; C07D279/08

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, and 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.
Public/Granted literature
- US20160046618A1 Cyclopropyl Fused Thiazin-2-Amine Compounds as Beta-Secretase Inhibitors and Methods of Use Public/Granted day:2016-02-18
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