SCOTT, JACK D.,史考特 杰克Ｄ,史考特 傑克Ｄ,STAMFORD, ANDREW W.,史丹佛 安德鲁Ｗ,史丹佛 安德魯Ｗ,GILBERT, ERIC J.,吉伯特 艾力克Ｊ,CUMMING, JARED N.,卡门 杰瑞Ｎ,卡門 傑瑞Ｎ,ISERLOH, ULRICH,爱森华 奥勒历奇,愛森華 奧勒歷奇,MISIASZEK, JEFFREY A.,米西亚兹克 杰佛,史考特 杰克D,史考特 傑克D,史丹佛 安德鲁W,史丹佛 安德魯W,吉伯特 艾力克J,卡门 杰瑞N,卡門 傑瑞N,爱森华 奥勒历奇,愛森華 奧勒歷奇,米西亚兹克 杰佛
申请号：
TW100118230
公开号：
TWI477502B
申请日:
2010.10.06
申请国别(地区):
TW
年份:
2015
代理人:
摘要：
In its many embodiments, the present invention provides provides certain iminothiadiazine dioxide compounds, including compounds Formula (I):and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-,-L2-, and -L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to β-amyloid (“Aβ”) production. 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 in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimer’s disease, are also disclosed.在本發明之許多實施例中，本發明提供某些亞胺噻二二氧化物化合物，包括式(I)化合物：且包括其立體異構體、及該等化合物之立體異構體的醫藥學上可接受之鹽，其中各R1、R2、R3、R4、R5、R9、環A、環B、m、n、p、-L1-、-L2-及-L3-經獨立選擇且如本文所定義。已驚訝地發現本發明之新穎亞胺噻二二氧化物化合物展現預期宜作為BACE抑制劑及/或用於治療及預防與β-類澱粉蛋白(「Aβ」)之產生相關之各種病變的性質。亦揭示包含一或多種此類化合物(單獨及與一或多種其他活性劑組合)之醫藥組合物、及其製備方法以及治療與類澱粉β(Aβ)蛋白相關之病變(包括阿茲海默氏病(Alzheimer's disease))的用途。
