To obtain a compound inhibiting matrix metaprotease, esp. interstitial collagenase, and useful for treating diseases involved in excessive decomposition of the matrix and connective tissue in mammals (e.g. arthritis).
This compound (a pharmaceutically permissible salt or ester thereof) is expressed by formula I ](n) is 0, 1 or 2; Y is hydroxyl or XONH (X is H or a lower alkyl); R1 is H or lower alkyl; R2 is H, a lower alkyl, heteroalkyl, aryl, etc.; R3 is H, a lower alkyl, cycloalkyl, aralkyl, etc.; R4 is H, a lower alkyl, cycloalkyl, etc.; R5 is a lower alkyl, aryl, aralkyl, etc.], e.g. N-hydroxy-2-[4-(4-phenoxyphenylsulfonyl)-tetrahydropyran-4-yl]-acetamide. The compound of formula I is obtained by bringing a compound of formula II into contact with an oxidizing agent.
BROKA CHRIS ALLEN (US)
CAMPBELL JEFFREY ALLEN (US)
CASTELHANO ARLINDO LUCAS (US)
FISHER LAWRENCE EMERSON (US)
HENDRICKS ROBERT THAN (US)
SARMA KESHAB (US)
AGOURON PHARMA (US)
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