Protease inhibitors

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Tripeptides – e.g. – tripeptide thyroliberin – etc.

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530330, A61K 3702, C07K 508, C07K 510

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active

049354930

ABSTRACT:
A compound having the structure ##STR1## where T is of the fomrula ##STR2## where each D.sup.1 and D.sup.2, independently, is a hydroxyl group of a group which is capable of being hydrolysed to a hydroxyl group in aqueous solution at physiological pH; a group of the formula ##STR3## where G is either H,F or an alkyl group containing 1 to about 20 carbon atoms and optional heteroatoms which can be N, S, or O; or a phosphonate group of the formula ##STR4## where J is O-alkyl, N-alkyl, or alkyl, each comprising about 1-20 carbon atoms and, optionally, heteroatoms which can be N, S, or O; T being able to form a complex with the catalytic site of an enzyme, X is a group having at least one amino acid, ##STR5## and each R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.8 is separately a group which does not interfere significantly (i.e., does not lower than Ki of the compound to less than 10.sup.-7 M) with site-specific recognition of the compound by the enzyme, and allows a complex to be formed with the enzyme.

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Report of the National Heart Lung and Blood Institute Workshop on Elastase Inhibitors for Treatment of Emphysema held in Rockville, Md. (Jun. 10-11, 1985).

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