首页> 外国专利> MULTITARGET COMPOUNDS FOR THE TREATMENT OF ALZHEIMER'S DISEASE

MULTITARGET COMPOUNDS FOR THE TREATMENT OF ALZHEIMER'S DISEASE

机译:多目标化合物治疗老年痴呆症

摘要

The invention provides compounds of formula I wherein: m is 0, 1 or 2; n is 2, 3, 4 or 5; R0 and R1 are both H, or they form a bridge -CH2-C(R4 )=CH-, R4 being CH3 or CH2CH3; R2 and R3 independently are H, F, Cl or (C1-C4)-alkyl; R5 is H, F, Cl, Br, I, OCH3, OCF3, SF5, SO2F, SO2CH3, NO2, CF3 or (C1-C4)-alkyl; R6 and R7 independently are H, F, Cl, CH3 or CF3; and optionally R5 and R6 form a bridge -O-CH2 -O-, R7 being H, invitro assays show that compounds I are simultaneously inhibitors of acetylcholinesterase and inhibitors of soluble epoxide hydrolase, and that they have a good blood-brain barrier permeability. Thus, compounds I are multitarget active pharmaceutical ingredients for the treatment of Alzheimer's disease in humans.
机译:本发明提供了式I化合物,其中:m为0、1或2; m为0。 n为2、3、4或5; R 0 和R 1 均为H,或它们形成桥-CH 2 -C(R 4 )= CH-,R 4 为CH 3 或CH 2 CH 3 ; R 2 和R 3 分别是H,F,Cl或(C 1 -C 4 )-烷基; R 5 是H,F,Cl,Br,I,OCH 3 ,OCF 3 ,SF 5 , SO 2 F,SO 2 CH 3 ,NO 2 ,CF 3 或(C 1 -C 4 )-烷基; R 6 和R 7 分别为H,F,Cl,CH 3 或CF 3 ;以及可选的R 5 和R 6 形成桥-O-CH 2 -O-,R 7 为H, 体外分析中显示,化合物I同时是乙酰胆碱酯酶的抑制剂和可溶性环氧化物水解酶的抑制剂,并且它们具有良好的血脑屏障通透性。因此,化合物I是用于治疗人类阿尔茨海默氏病的多靶标活性药物成分。

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