Method of producing a novel opioid peptide

摘要

The use of opioid peptides of a novel structure is claimed which, in addition to a pharmacophore, additionally contain structural elements reactive with tachykinin receptors. Due to the synergistic reactivity of the opioid with an additional element, an increased analgesic activity is obtained facilitating protracted effective use due to decreased drug tolerance effects. The drugs may particularly be of use in the treatment of chronic pain as effective analgesics during inflammation caused by rheumatism, gout, neurodegenerative states, post-surgical and post-traumatic inflammations or ones induced by tumors.

主权项

1. A compound having the general formula: where:
L, D denote an appropriate amino-acid chirality,R1 is an amino-acid residue selected from among: D-alanine, D-Leucine, D-arginine, D-lysine, D-serine or D-threonine,R2 is an amino-acid residue selected from among L-phenylalanine or L-tryptophan,
—CO—R3 denotes benzyloxycarbonyl or cynamoil, alpha-methyl-4-(2-metylopropyl)benzenoacetyl, salicyl-glycyl-, benzoyl-glycyl-, or its pharmaceutically permissible salt.