公开(公告)号：US20160222032A1

公开(公告)日：2016-08-04

申请号：US15021011

申请日：2014-09-08

申请人： Jack D. SCOTT ,  Wen-Lian WU ,  Jared N. CUMMING ,  MERCK SHARP & DOHME CORP.

发明人： Jack D. Scott ,  Wen-Lian Wu ,  Jared N. Cumming

IPC分类号： C07D513/10 ,  A61K45/06 ,  C07D417/12 ,  A61K31/547 ,  C07D519/00

CPC分类号： C07D513/10 ,  A61K31/547 ,  A61K45/06 ,  C07D279/16 ,  C07D417/12 ,  C07D471/04 ,  C07D519/00 ,  A61K2300/00

摘要： In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein RL, X, Y, R1A, R1B, R2, R3, m, and RA are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.

摘要翻译： 在其许多实施方案中，本发明提供某些C5-螺亚氨基二氮嗪二氧化物化合物，包括式（I）化合物：或其互变异构体和/或立体异构体，以及所述化合物，所述互变异构体和所述立体异构体的药学上可接受的盐，其中RL， X，Y，R 1A，R 1B，R 2，R 3，m和RA如本文所定义。 本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与其相关的各种病症。 还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括用于治疗阿尔茨海默氏病的药物组合物。