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US 5,552,419 AGranted
Arylsulfonamido-substituted hydroxamic acids
AssigneeCiba-Geigy Corporation
InventorsLawrence J. MacPherson, David T. Parker
Life of this patent
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Abstract
The invention relates to the compounds of formula I ##STR1## pharmaceutically acceptable prodrug derivatives and pharmaceutically acceptable salts thereof; methods for 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.
Claims17
A compound of formula I ##STR13## wherein Ar is carbocyclic or heterocyclic aryl;
- 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;
- R.sub.1 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.10 -cycloalkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, hydroxy-lower alkyl, acyloxy-lower alkyl, lower alkoxy-lower alkyl, (carbocyclic or heterocyclic aryl)-lower alkoxy-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, (amino, mono- or di-lower alkylamino)-lower alkyl, (N-lower alkyl-piperazino or N-carbocyclic or heterocyclic aryl-lower alkylpiperazino)-lower alkyl, (morpholino, thiomorpholino, piperidino, pyrrolidino, piperidyl, N-acyl or N-lower alkylpiperidyl)-lower alkyl, acylamino-lower alkyl, piperidyl, (morpholino, thiomorpholino, piperidino, pyrrolidino, piperidyl, N-acyl or N-lower alkylpiperidyl)-(hydroxy or lower alkoxy) lower alkyl, pyrrolidinyl, hexahydroazepinyl, N-lower alkyl or N-acyl(hexahydroazepinyl, piperidyl or pyrrolidinyl), C.sub.5 -C.sub.10 -oxacycloalkyl, C.sub.5 -C.sub.10 -thiacycloalkyl, (hydroxy-or oxo-) C.sub.5 -C.sub.10 -cycloalkyl, (hydroxy- or oxo-) C.sub.5 -C.sub.10 -thiacycloalkyl, (hydroxy- or oxo-) C.sub.5 -C.sub.10 -oxacycloalkyl, (amino, mono- or dialkylamino or acylamino)-C.sub.5 -C.sub.10 -cycloalkyl, 2-oxo(pyrrolidinyl, piperidyl or hexahydroazepinyl);
- (carbocyclic or heterocyclic aryl)-(thio, sulfinyl or sulfonyl)-lower alkyl;
- R.sub.2 is hydrogen or lower alkyl;
- or a pharmaceutically acceptable prodrug derivative thereof;
- or a pharmaceutically acceptable salt thereof.
3 more elements
Dependencies are inferred from the claim text.