摘要 |
A family of molecules of formula (A) in which R<1> is a 5- or 6-membered carbocyclo, heterocyclo, aryl or heteroaryl radical such that its size defined by certain parameters; R<20> is -O-R<21>, -NR<13>-O-R<22> or -NR<13>-O-R<14>; and the other variables are as defined in the claims, is disclosed that inhibit matrix metalloproteinase (MMP) activity, and particularly inhibit the activity of one or more of MMP-2, MMP-9, or MMP-13, while generally exhibiting little activity against MMP-1. A contemplated compound also exhibits little inhibition of the production of TNF. Also disclosed are process for preparing a contemplated compound and for treating a mammal having a condition associated with pathological matrix metalloproteinase activity.
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申请人 |
G.D. SEARLE & CO.;BARTA, THOMAS, E.;BECKER, DANIEL, P.;BEDELL, LOUIS, J.;DE CRESCENZO, GARY, A.;FRESKOS, JOHN, N.;GETMAN, DANIEL, P.;HEINTZ, ROBERT, M.;HOCKERMAN, SUSAN, L.;LI, HUI;MISCHKE, BRENT, V.;VILLAMIL, CLARA, I. |
发明人 |
BARTA, THOMAS, E.;BECKER, DANIEL, P.;BEDELL, LOUIS, J.;DE CRESCENZO, GARY, A.;FRESKOS, JOHN, N.;GETMAN, DANIEL, P.;HEINTZ, ROBERT, M.;HOCKERMAN, SUSAN, L.;LI, HUI;MISCHKE, BRENT, V.;VILLAMIL, CLARA, I. |