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Amino acid derivatives possessing prolyl endopeptidase-inhibitory activities

机译:具有脯氨酰内肽酶抑制活性的氨基酸衍生物

摘要

Amino acid derivatives of the formula ##STR1## wherein: Q is W- -(CH. sub.2).sub.m --(A).sub.n --CO--B-- whereinPPA is oxygen atom or --NH--;PPB is ##STR2## or --(CH.sub.2).sub. l -- wherein X is sulfur atom or --CH.sub.2 --, and l is an integer from 1 to 3;PPW is ##STR3## wherein Hal is halogen atom; n is an integer of 0 or 1; andPPm is an integer from 0 to 3; PPY is sulfur atom or --CH.sub.2 --; andP PR is hydrogen atom, formyl group, C.sub.1-5 alkoxycarbonyl group, -- C.tbd.N or ##STR4## wherein R.sup.1 is hydrogen atom, andP PR.sup. 2 is hydroxyl group, C.sub.1-5 alkylcarboxy group, phenylcarboxy group, C. sub.1-5 alkoxy group or phenyl C.sub.1-5 alkoxy group;PP with the proviso that when R is hydrogen atom, formyl group or C.sub.1-5 alkoxycarbonyl group, W is ##STR5## The compounds mentioned above specifically inhibit prolyl endopeptidase activity and are useful as agents for the treatment and prevention of dementia and amnesia.
机译:式## STR1 ##的氨基酸衍生物,其中:Q是W-(CH.sub.2).m .-(A).n.-CO-B-,其中

A是氧原子或--NH-;

B是## STR2 ##或-(CH.sub.2)sub。式中,X为硫原子或-CH 2-,l为1〜3的整数; P为W,其中Hal为卤素原子。 n是0或1的整数;并且

m是0到3的整数;

Y是硫原子或--CH.sub.2-;并且

R是氢原子,甲酰基,C 1-5烷氧羰基,-Ctbd.N或## STR4 ##,其中R 1是氢原子,并且< P>

R.sup。 2为羟基,C 1-5烷基羧基,苯基羧基,C 1-5烷氧基或苯基C 1-5烷氧基;

为条件R为氢原子,甲酰基或C 1-5烷氧羰基,W为## STR5 ##上述化合物特别抑制脯氨酰内肽酶活性,并可用作治疗和预防痴呆和健忘症的药物。

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