N-substituted mercaptopropanamide derivatives

Details N-substituted mercaptopropanamide derivatives N-substituted mercaptopropanamide derivatives

1990-11-05

1993-05-11

Higel, Floyd D.

Organic compounds -- part of the class 532-570 series

Organic compounds

Esters having the thiocarboxylate group, -cx-, wherein the...

544169, 546224, 548557, 541 77, 541493, C07C32360, C07C32732, A61K 3195

Patent

active

052102661

ABSTRACT:
Novel N-substituted mercaptopropanamide derivatives of the formula: ##STR1## wherein R.sub.1 is mercapto or a group convertible into mercapto when cleaved within the biobody, W is hydrogen atom, an alkyl or an aralkyl, R.sub.2 is an aryl which may optionally have substituent(s), a heterocyclic group which may optionally have substituent(s), or an alkyl which may optionally have substituent(s), X is a cycloalkylene, a cycloalkylidene, or a phenylene which may optionally have substituent(s) or may optionally be fused with other ring, and R.sub.3 is carboxyl or a group convertible into carboxyl when cleaved within the biobody, or a pharmaceutically acceptable salt thereof, and a solid solution of said N-substituted mercaptopropanamide derivative with an amino acid, which have excellent enkephalinase inhibitory activity and are useful for the treatment of mild to moderate pain, and a pharmaceutical composition containing said compounds as an active ingredient, and processes for preparing these compounds.

REFERENCES:
patent: 4299842 (1981-11-01), Cavazza
patent: 4722810 (1988-02-01), Delaney et al.
B. P. Roques et al., The Enkephalinase Inhibitor Thiorphan Shows Anti-nociceptive Activity in Mice, Nature vol. 288, Nov. 20, 1980, pp. 286-288.
Derwet Abstract to Roussel-UCLAF, Omega Amino Acid Omega Mercaptopropanamide(s), are Enkephalinase Inhibitors, Useful as Analgesics (Dec. 14, 1983).

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