PHARMACOLOGICALLY ACTIVE PEPTIDES THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

摘要

Compounds of the formula and pharmaceutically acceptable non-toxic acid addition salts thereof, in which L and D define the chirality; R1 is hydrogen or C1-C3 primary alkyl; R2 is C1-C4 primary or secondary alkyl, allyl, cyclopropylmethyl, C1-C2 hydroxyalkyl, or -(CH2)m-U-CH3 in which U is -S- or @S-O and m is 1 or 2; R3 is hydrogen, C1-C4 primary or secondary alkyl, cyclopropylmethyl, or allyl; X is hydrogen, halo, hydroxy, C1-C3 alkoxy, nitro, C1-C3, alkyl, or trifluoromethyl; and Z is -CH2OR4, -@-NHR4, or -@-OR5, in which R4 is hydrogen or C1-C3 alkyl and R5 is C1-C3 alkyl; are useful analgesic agents. These compounds of formula I are prepared by deblocking the corresponding blocked compound of formula I by conventional methods.