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US 6,444,829 B1Granted
Pyrrolidine compounds
AssigneeHoffmann-La Roche Inc.
InventorsJohannes Aebi, Henrietta Dehmlow, Eric Argirios Kitas
Life of this patent
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Abstract
The present invention relates to a pyrrolidine compound and pharmaceutically acceptable esters and/or salts thereof. The compounds are useful as inhibitors of metalloproteases, e.g. zinc proteases, particularly zinc hydrolases, and which are effective in treating disease states are associated with vasoconstriction of increasing occurrences.
Claims42
A compound of formula (I)
- wherein
- R1 is hydrogen, alkylcarbonyl, or arylcarbonyl;
- R2 is alkyl, alkylcycloalkyl, alkylcycloalkylalkyl, cycloalkyl, halogenalkyl, carboxyalkyl, aminoalkyl, (mono- and dialkyl)aminoalkyl, alkoxyalkyl, alkoxycarbonylalkyl, alkinyl, aryl, arylalkyl, arylalkyl(alkoxycarbonyl)alkyl, arylcarbonylalkyl, aryloxyalkyl, arylalkenyl, aryl(alkoxycarbonyl)alkyl, heteroaryl, heteroarylalkyl, heterocyclyl or hetercycylalkyl;
- R3 is hydrogen, aryl, alkyl, or arylalkyl, arylsulfonyl, heteroarylsulfonyl;
- R4 is hydrogen, arylalkyl, alkyl, aryl, cycloalkyl, cycloalkylalkyl, alkylsulfonyl, arylsulfonyl, arylalkylsulfonyl, heteroarylsulfonyl, carboxyalkyl, carboxyalkylsulfonyl, or alkoxycarbonylalkyl;
- or the groups —NR3R4 or R5—[N—N(R4)]—R3 form a saturated or unsaturated 5- or 6-membered aliphatic ring;
- R5 is hydrogen, alkylsulfonyl, arylsulfonyl, heteroarylsulfonyl, alkoxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, alkylcarbonyl, arylcarbonyl, heteroarylcarbonyl, heteroarylalkylcarbonyl, heterocyclyl, (mono- or di-alkylamino)-alkylcarbonyl, (mono- and dialkyl)aminosulfonyl, arylaminocarbonyl, alkyl, alkylcarbonyl, alkoxycarbonyl, aryl, arylalkyl, arylalkoxycarbonyl, or heteroaryl;
- R6 is hydrogen, alkyl, aryl, or carboxyalkyl;
- X is —S(O)2—, —S(O)2—NH—, —C(O)—, —C(O)NR6 or C(O)—O—
- or a pharmaceutically acceptable ester, or a pharmaceutically acceptable salt thereof.
7 more elements
Dependencies are inferred from the claim text.