Succinamide derivative matrix-metalloprotease inhibitors

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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514212, 5142275, 5142278, 5142352, 5142358, 5142355, 5142372, 5142315, 5142378, 514252, 514253, 514255, 514318, 514315, 514343, 514357, 514397, 514400, 514414, 514419, 514422, 514424, 514438, 514319, 514326, 514428, 514562, 514616, 540597, 540602, 540603, 540596, 540610, 544 581, 544 585, 544 586, 544 587, 544 59, 544 60, 544 62, 544131, 544139, 544143, 544145, 544159, 544160, 544360, 544370, 544373, 544379, 544400, 546192, 546193, 546194, 546201, 546208, 546212, 546213, 546247, 546281, 546335, 548336, 5483

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active

052566579

ABSTRACT:
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.

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