Pharmacologically active peptides

C - Chemistry – Metallurgy – 07 – K

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530/5.04

C07K 5/107 (2006.01) C07K 5/087 (2006.01)

Patent

CA 1142514

X-5208 -1- Abstract of the Disclosure Compounds of the formula Image (I) 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 Image and m is 1 or 2; R3 is hydrogen, C1-C4 primary or secondary alkyl, cyclopropylmethyl, allyl or propargyl; and Z is -CH2OR4, Image , or Image , in which R4 is hydrogen, acetyl, or acetoxymethyl and R5 is C1-C3 alkyl; are useful analgesic agents. These compounds are prepared by deblocking the correspondingly blocked compound of formula I with a deblocking agent,

366542

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