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Possess puroriruendopepuchida - ze inhibition activity chemical compound and its medicine application

机译:puroriruendopepuchidas-ze抑制活性化合物及其医药应用

摘要

A compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, wherein: R represents hydrogen or acyl; U represents -O-, -CHR1- or -NR2-, wherein R1 represents hydrogen or heterocycle, and R2 represents hydrogen or lower alkyl substituted by lower alkoxycarbonyl; V represents -O-, -S-, -CHR3- or -NR4-, wherein R3 represents hydrogen or lower alkoxycarbonyl, and R4 represents hydrogen, lower alkyl or acyl; W represents methyl, heterocycle or optionally substituted phenyl; X and Y, which may be the same or different from each other, represent each -CH¿2?- or -S-; m represents an integer of 0 to 6; and n represents an integer of 1 to 4. The compound has a specifically potent inhibitory activity against prolyl endopeptidase and suppresses the decomposition and deactivation of TRH, substance P, neurotensin, vasopressin, and so forth. Hence it can be used for preventing and/or treating dementia and amnesia including Alzheimer's disease.
机译:通式(I)代表的化合物或其药学上可接受的盐,其中:R代表氢或酰基; U代表-O-,-CHR1-或-NR2-,其中R1代表氢或杂环,R2代表氢或被低级烷氧羰基取代的低级烷基; V代表-O-,-S-,-CHR3-或-NR4-,其中R3代表氢或低级烷氧羰基,R4代表氢,低级烷基或酰基。 W代表甲基,杂环或任选取代的苯基; X和Y可以相同或不同,分别代表-CH 2-或-S。 m表示0〜6的整数。 n为1〜4的整数。该化合物对脯氨酰内肽酶具有特别有效的抑制活性,并且抑制TRH,P物质,神经降压素,加压素等的分解和失活。因此,它可以用于预防和/或治疗痴呆和健忘症,包括阿尔茨海默氏病。

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