Sterling Winthrop Inc.

Sterling Drug Inc.

Jasbir Singh

Barry A Morgan

Thomas D Gordon

Robert C Wahl

Philip E Hansen

James A Gainor

Azole-fused peptides useful as Substance P antagonists and analgesics, for example ##STR1## wherein ##STR2## represents ##STR3## wherein X is O, S or NH and * is D, or as intermediates therefor are prepared by azole and peptide forming methods.

Azole-fused peptides and processes for preparation thereof

Compounds having the structural formula ##STR1## wherein X is HONH or HO and especially wherein the carbon atom bearing CH.sub.2 R.sup.1 has the R-configuration, the carbon atom bearing CH.sub.2 R.sup.2 has the S-configuration, R.sup.1 is isopropyl, R.sup.2 is 3-indolyl, m is 2, n is 0, p is 2 and R.sup.3 and R.sup.4 taken alone are each methyl or R.sup.3 and R.sup.4 taken together with N are morpholino and pharmaceutically acceptable acid addition salts or solvates or acid addition salts-solvates thereof, which are matrix-metalloprotease inhibitors useful in treatment of disease in which matrix-metalloprotease promoted connective tissue remodelling is a causative factor, for example, rheumatoid arthritis and cancer, and a method of preparation and method of use thereof and methods of preparation of intermediates therefor are disclosed.

Succinamide derivative matrix-metalloprotease inhibitors

Di(D-tryptophyl and/or tetrahydropyridoindolylcarbonyl)-containing peptide amides useful as Substance P agonists and/or antagonists and as antihypertensives and/or analgesics and a process for preparing them are disclosed.

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Albany, NY, United States of America

Jasbir Singh