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Imino group thiadiazine dioxide compound, composition and their purposes as BACE inhibitor
专利权人:
Merck Sharp & Dohme Corp.;默沙东公司;默沙東公司
发明人:
J.D.斯科特,A.W.斯坦福德,E.J.吉尔伯特,E.J.吉爾伯特,J.N.卡明,U.伊泽洛,U.伊澤洛,J.A.米西亚塞克,J.A.米西亞塞克,李国青,李國青,J.D.斯科特,A.W.斯坦福德,E.J.吉尔伯特,E.J.吉爾伯特,J.N.卡明,U.伊泽洛,U.伊澤洛,J.A.米西亚塞克,J.A.米西亞塞克
申请号:
MOJ001739
公开号:
MOJ001739B
申请日:
2015.04.29
申请国别(地区):
MO
年份:
2015
代理人:
摘要:
In its many embodiments, the present invention provides certain imino group thiadiazine dioxide compounds, including formula (I) compound: (I) includes its stereoisomer, with the officinal salt of the compound, stereoisomer, R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p ,-L1- ,-L2- and-L3- is wherein selected independently, and as defined herein. It is surprised to find that, new imino group thiadiazine dioxide compound of the invention shows following performance, which makes them that can advantageously act as BACE inhibitor and/or treat and prevent various lesions relevant to beta-amyloid protein (" A β ") generation with what. It also discloses pharmaceutical composition (individually and to one or more other activating agents being combined) and their preparation method comprising one or more this compounds and is treating the purposes in lesion relevant with amyloid (A β) albumen, including alzheimer's disease.在它的許多實施方案中,本發明提供了某些亞氨基噻二嗪二氧化物化合物,包括式(I)化合物:(I)包括其立體異構體,和所述化合物、立體異構體的可藥用鹽,其中獨立地選擇R1、R2、R3、R4、R5、R9、環A、環B、m、n、p、-L1-、-L2-和-L3-,並且如本文所定義。意外地發現,本發明的新的亞氨基噻二嗪二氧化物化合物顯示出如下性能,該性能使得它們可有利地作爲BACE抑制劑和/或用於治療和預防與β-澱粉樣蛋白(“Aβ”)産生相關的各種病變。還公開了包含一或多種這種化合物的藥物組合物(單獨和與一或多種其它活性劑聯用)和它們的製備方法和在治療與澱粉樣β(Aβ)蛋白相關的病變中的用途,包括阿爾茨海默氏疾病。
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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