Öfugar hýdroxamat afleiður sem málmpróteasa latar

Öfugar hýdroxamat afleiður sem málmpróteasa latar

A family of compounds having general structural formula (I) wherein W is a reverse hydroxamic acid group (a); R5 is hydrogen or lower alkyl; R6 is (b); where Z1 is heteroarylene; preferably: R1 is methyl, ethyl, isopropyl, n-propyl or 3,3,3-trifluoro-n-propyl; R2 is isobutyl or sec-butyl; R3 is hydr...

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Bibliographische Detailangaben
Hauptverfasser: JOSEPH HOWING CHAN, DARRYL LYNN MCDOUGALD, ROBERT WILLIAM WIETHE, JENNIFER BADIANG STANFORD, DAVID LEE MUSSO, MICHAEL DAVID GAUL, DULCIE GARRIDO BUBACZ, DAVID JOHN COWAN, MARC WERNER ANDERSEN, MICHAEL HOWARD RABINOWITZ, ROBERT CARL ANDREWS
Format: Patent
Sprache:ice
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:A family of compounds having general structural formula (I) wherein W is a reverse hydroxamic acid group (a); R5 is hydrogen or lower alkyl; R6 is (b); where Z1 is heteroarylene; preferably: R1 is methyl, ethyl, isopropyl, n-propyl or 3,3,3-trifluoro-n-propyl; R2 is isobutyl or sec-butyl; R3 is hydrogen; R4 is tert-butyl, sec-butyl, 1-methoxy-1-ethyl or 2-(2-pyridylcarbonylamino)-1-ethyl; R5 is hydrogen; and R6 is 2-thiazolyl or 2-pyridyl. Such compounds show potent inhibition of MMP's, cell-free TNF convertase enzyme and TNF release from cells, and in some cases inhibit TNF convertase and TNF release from cells in preference to matrix metalloproteases.