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Acylated N-hydroxy methyl thalidomide prodrugs with immunomodulator action

机译:具有免疫调节作用的酰化N-羟甲基沙利度胺前药

摘要

Thalidomide prodrugs of the formula I:in which R is -CHR1-NHR2 or -(CH2)nCOOH; R1 is H or C1-4 alkyl; R2 is H, C1-3 alkyl, C(O)-CH2-NHR3 or an amino-protective group, R3 is H or an amino-protective group, and n is an integer from 2 to 4, in the form of their free bases or of salts with physiologically acceptable acids, as well as a process for preparation of such prodrugs and the use of such prodrugs as an active drug substance.
机译:式I的沙利度胺前药:其中R为-CHR1-NHR2或-(CH2)nCOOH; R1是H或C1-4烷基; R 2为H,C 1-3烷基,C(O)-CH 2 -NHR 3或氨基保护基,R 3为H或氨基保护基,n为2至4的整数,其形式为游离碱或与生理上可接受的酸形成的盐,以及此类前药的制备方法和此类前药作为活性药物的用途。

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