[EN] C5-C6-CARBOCYCLIC FUSED IMINOTHIADIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE<br/>[FR] DIOXYDES D'IMINOTHIADIAZINE CARBOXYLIQUES EN C5-C6 CONDENSÉS UTILISÉS COMME INHIBITEURS DE BACE, COMPOSITIONS, ET UTILISATION ASSOCIÉE
申请人:MERCK SHARP & DOHME
公开号:WO2017095759A1
公开(公告)日:2017-06-08
In its many embodiments, the present invention provides certain C5-C6-carbocyclic fused iminothiazine dioxide compounds, including compounds Formula (I): and tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, ring A, RA, m, -L1-, ring B, RB, n, q, ring C, RC, and p 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.
在其许多实施方式中,本发明提供了某些C5-C6-环融合咪唑硫酸亚胺二氧化物化合物,包括化合物式(I):及其互变异构体,以及所述化合物和所述互变异构体的药学上可接受的盐,其中R1、环A、RA、m、-L1-、环B、RB、n、q、环C、RC和p的定义如本文所述。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之相关的各种病理。还公开了包括一种或多种此类化合物(单独和与一种或多种其他活性剂的组合)的药物组合物,以及其制备和使用方法,包括可能用于治疗阿尔茨海默病的方法。