3-Arylsulfonyl-2 (substituted methyl) propanoic acid derivatives as matrix metalloproteinase inhibitors

   
   

Compounds which are 3-arylsulfonyl-2-methyl propanoic acid derivatives of formula (I): wherein X is HO--NH-- or HO--, R1 is selected from phenyl, 4-chlorophenyl, 4-florophenyl, 4-cyanophenyl, benzamido (i.e., --NH--CO-Ph) and benzamido substituted on the terminal phenyl ring by C.sub.1 -C.sub.4 alkyl, fluoro, chloro, cyano or C.sub.1-4 alkoxy; R.sub.2 is selected from (a) --S--Ar or --S--CH.sub.2 --Ar wherein Ar is an aromatic moiety; (b) --O--Ar wherein Ar is as defined above; (c) --S-Het or --S--CH.sub.2 -Het wherein Het is a heterocyclic ring; and (d) 2,5-dioxo-1-imidazolidinyl or 2,4-dioxo-1-imidazolinyl; and the pharmaceutically acceptable salts thereof; have potent and selective inhibitory activity against matrix metalloproteinases (MMPs) and can thus be used in the treatment and prevention of diseases mediated by MMPs.

Samenstellingen die 3-arylsulfonyl-2-methyl propanoic zure derivaten van formule (I) zijn: waarin X HO -- NH -- of HO --, R1 wordt geselecteerd uit phenyl is, 4-4-chlorophenyl, 4-florophenyl, 4-cyanophenyl, benzamido (d.w.z.., -nh--Co-Ph) en benzamido die op de eind phenyl ring door C.sub.1 wordt gesubstitueerd - alkoxy alkyl C.sub.4, chloor, cyano fluoro, of c.sub.1-4; R.sub.2 wordt geselecteerd uit (a) -- S -- AR of -- S -- CH.sub.2 AR waarin AR een aromatisch deel is; (b) -- O -- AR waarin AR zoals hierboven bepaald is; (c) -- S-Het of -- S -- CH.sub.2 - Het waarin Het een heterocyclische ring is; en (d) 2.5-dioxo-1-imidazolidinyl of 2.4-dioxo-1-imidazolinyl; en de farmaceutisch aanvaardbare zouten daarvan; heb machtige en selectieve remmende activiteit tegen matrijsmetalloproteinases (MMPs) en kan zo in de behandeling en de preventie van ziekten worden gebruikt die door MMPs worden bemiddeld.

 
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