Arylsulfonamido-substituted hydrodxamic acids
AssigneeNovartis AG
InventorsLawrence J. MacPherson, David Thomas Parker
Life of this patent
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Abstract
Disclosed are the compounds of formula I ##STR1## wherein R and R.sub.1 together with the chain to which they are attached or R.sub.1 and R.sub.2 together with the carbon atom to which they are attached form a ring; pharmaceutically acceptable prodrug derivatives and pharmaceutically salts thereof; methods of preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.
Claims14
A compound of formula I ##STR13## (a) wherein R and R.sub.1 together with the chain to which they are attached form a 1,2,3,4-tetrahydro-isoquinoline, piperidine, oxazolidine, thiazolidine or pyrrolidine ring, each unsubstituted or substituted by lower alkyl;
- Ar is carbocyclic or heterocyclic aryl;
- and R.sub.2 is hydrogen or lower alkyl;
- or
- (b) wherein R.sub.1 and R.sub.2 together with the carbon atom to which they are attached form a ring system selected from C.sub.3 -C.sub.7 -cycloalkane which is unsubstituted or substituted by lower alkyl;
- oxa-cyclohexane, thia-cyclohexane, indane, tetralin, piperidine or piperidine substituted on nitrogen by acyl, lower alkyl, carbocyclic or heterocyclic aryl-lower alkyl, (carboxy, esterified or amidated carboxy)-lower alkyl or by lower alkylsulfonyl;
- Ar is carbocyclic or heterocyclic aryl;
- and R is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, (oxa or thia)-C.sub.3 -C.sub.6 -cycloalkyl, (oxa or thia)-C.sub.3 -C.sub.6 -cycloalkyl!-lower alkyl, hydroxy-lower alkyl, acyloxy-lower alkyl, lower alkoxy-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, (amino, mono- or di-lower alkylamino)-lower alkyl, acylamino-lower alkyl, (N-lower alkyl-piperazino or N-carbocyclic or heterocyclic aryl-lower alkylpiperazino)-lower alkyl, or (morpholino, thiomorpholino, piperidino, pyrrolidino, piperidyl or N-lower alkylpiperidyl)-lower alkyl;
- or a pharmaceutically acceptable prodrug derivative thereof;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.