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US 7,115,618 B2Granted
α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
AssigneeG.D. Searle & Co.
InventorsMichael J. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
Life of this patent
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Abstract
α- and β-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Claims13
A retroviral protease inhibiting compound represented by the formula
- or a pharmaceutically acceptable salt thereof, wherein:
- A represents a radical selected from the group consisting of cycloalkyl;
- heterocycloalkyl;
- aryl;
- heteroaryl;
- aroyl;
- and cycloalkyl, aryl, heteroaryl or aroyl that is substituted at one or more carbon atoms with a radical selected from the group consisting of alkyl, alkoxy, halogen, hydroxy, amino, alkylamino, dialkylamino, nitro, cyano, haloalkyl, carboxy, alkoxycarbonyl, cycloalkyl, heterocycloallcyl, alkylamido, dialkylamido, alkylsulfonyl, and alkylsulfonylalkyl;
- and
- R3 and R4 independently represent radicals selected from the group consisting of alkyl;
- haloalkyl;
- alkenyl;
- alkynyl;
- hydroxyalkyl;
- alkoxyalkyl;
- cycloalkyl;
- cycloalkylalkyl;
- heterocycloalkyl;
- heteroaryl;
- heterocycloalkylalkyl;
- aryl;
- aralkyl;
- heteroaralkyl;
- aminoalkyl;
- aminoalkyl substituted at one or more carbon atoms with a radical selected from the group consisting of alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroaralkyl, heterocycloalkyl, and heterocycloalkylalkyl;
- and aminoalkyl substituted at two carbon atoms with radicals that, together with the nitrogen atom to which they are attached, form a heterocycloalkyl or a heteroaryl radical.
22 more elements
A compound represented by the formula:
- or a pharmaceutically acceptable salt thereof, wherein
- P1 is a hydrogen radical;
- P2 represents a radical selected from the group consisting of alkoxycarbonyl, aralkoxycarbonyl, alkylcarbonyl, cycloalkylcarbonyl, cycloalkylalkoxycarbonyl, cycloalkylalkanoyl, alkanoyl, aralkanoyl, aroyl, aryloxycarbonyl, aryloxycarbonylalkyl, aryloxyalkanoyl, heterocyclylcarbonyl,heterocyclyloxycarbonyl,heterocyclylalkanoyl, heterocyclylalkoxycarbonyl, heteroaralkanoyl, heteroaralkoxycarbonyl, heteroaryloxycarbonyl, heteroaroyl, alkyl, alkenyl, cycloalkyl, aryl, aralkyl, aryloxyalkyl, heteroaryloxyalkyl, hydroxyalkyl, aminocarbonyl, and aminoalkanoyl;
- or a mono- or disubstituted aminocarbonyl radical or a mono- or disubstituted aminoalkanoyl radical, having substituents selected from the group consisting of alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroaralkyl, heterocycloalkyl and heterocycloalkyalkyl radicals;
- or, where said aminoalkanoyl radical is disubstituted, having substituents that, along with the nitrogen atom to which they are attached, form a heterocycloalkyl or heteroaryl radical;
- R3 is a radical selected from the group consisting of hydrogen, alkyl, haloalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heteroaryl, heterocycloalkylalkyl, aryl, aralkyl, heteroaralkyl, and aminoalkyl, or a mono- or disubstituted aminoalkyl radical, having substituents selected from the group consisting of alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroaralkyl, heterocycloalkyl and heterocycloalkylalkyl radicals;
- or where said aminoalkyl radical is disubstituted, said substituents along with the nitrogen atom to which they are attached, form a heterocycloalkyl or a heteroaryl radical;
- and
- R4 is a radical as defined by R3 except for hydrogen.
6 more elements
Dependencies are inferred from the claim text.