Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1990-04-04
1993-01-12
Lee, Mary C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
562427, 562432, A61K 31195, C07C31500, C07C32100
Patent
active
051791250
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.
patent: 4879309 (1989-11-01), Doll 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.
Deguchi Takashi
Mimura Tetsutaro
Nakamura Hideo
Nakamura Yasuhisa
Nishino Junko
Dainippon Pharmaceutical Co., Ltd.
Lee Mary C.
Whittenbaugh Robert C.
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