Peptidyl derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...

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514740, 5142382, 514255, 514256, 514357, 514365, 514372, 514374, 514378, 514399, 514406, 514428, 514438, 514461, 544106, 544168, 544242, 544335, 544358, 544400, 546336, 546348, 548205, 548214, 548236, 548240, 5483351, 5483381, 5483751, 5483761, 548561, 548562, 548579, 549 76, 549496, 562442, 562450, 562553, 562561, 562567, 562621, 564123, 564152, A61K 3119, A61K 31195, C07C22904, C07C22924, C07C22928, C07C23305, C07C23308, C07C23706

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active

058890580

ABSTRACT:
Methods of use for compounds of formula (I) are described wherein R represent a --CONHOH, carboxyl (--CO.sub.2 H) or esterified carboxyl group; R.sup.1 represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R.sup.2 represents an optionally substituted phenylethyl, phenylpropyl or phenylbutyl group; R.sup.3 represents a hydrogen atom or an alkyl group; R.sup.4 represents a hydrogen atom or an alkyl group; R.sup.5 represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more --O-- or --S-- atoms or --N(R.sup.7)-- groups (where R.sup.7 is a hydrogen atom or a C.sub.1-6 alkyl group); X represents an amino (--NH.sub.2), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof. The compounds are metalloproteinase inhibitors and in particular have a selective gelatinase action, and may be of use in the treatment of cancer to control the development of tumour metastases. ##STR1##

REFERENCES:
patent: 5114953 (1992-05-01), Galardy et al.

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