Back to results
US 6,552,203 B2Granted
Cyclic sulfone containing retroviral protease inhibitors
AssigneeMonsanto Company
InventorsDeborah E. Bertenshaw, Daniel Getman, Robert M. Heintz, John J. Talley, Kathryn L. Reed, Robert Alan Chrusciel, Michael Clare
Life of this patent
Estimating the term…
Abstract
The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.
Claims3
A compound represented by formula (II):
- or a pharmaceutically acceptable salt, prodrug, or ester thereof, wherein t represents 0, 1, or 2;
- Y′ represents O, S, and NR15, wherein R15 represents hydrogen;
- alkyl;
- haloalkyl;
- alkenyl;
- alkynyl;
- hydroxyalkyl;
- alkoxyalkyl;
- cycloalkyl;
- cycloalkylalkyl;
- heterocycloalkyl;
- heteroaryl;
- heterocycloalkylalkyl;
- aryl;
- aralkyl;
- heteroaralkyl;
- thioalkyl, alkylthioalkyl, arylthioalkyl, or the sulfone or sulfoxide derivatives thereof;
- aminoalkyl or a mono- or disubstituted aminoalkyl wherein said substituents are selected from alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroaralkyl, heterocycloalkyl, and heterocycloalkylalkyl, or, in the case of a disubsituted aminoalkyl radical, said substituents along with the nitrogen atom to which they are attached form a heterocycloalkyl or a heteroaryl;
- R2 represents an alkyl, aryl, cycloalkyl, cycloalkylalkyl, or aralkyl radical, which radical is optionally substituted with a substituent selected from the group consisting of alkyl, —NO2, CN, CF3, —OR9, —SR9, and halogen, wherein R9 represents hydrogen or alkyl;
- R6 represents hydrogen or alkyl;
- and, wherein
- represents
19 more elements
A compound of the following formula:
- or a pharmaceutically acceptable salt, prodrug, or ester thereof, wherein
- t represents 0, 1, or 2;
- R6 represents hydrogen or alkyl;
- R2 represents an alkyl, aryl, cycloalkyl, cycloalkylalkyl, or aralkyl radical, which radical is optionally substituted with a substituent selected from the group consisting of alkyl, —NO2, CN, CF3, —OR9, —SR9, and halogen, wherein R9 represents hydrogen or alkyl;
- R3 represents hydrogen;
- alkyl;
- haloalkyl;
- alkenyl;
- alkynyl;
- hydroxyalkyl;
- alkoxyalkyl;
- cycloalkyl;
- cycloalkylalkyl;
- heterocycloalkyl;
- heteroaryl;
- heterocycloalkylalkyl;
- aryl;
- aralkyl;
- heteroaralkyl;
- thioalkyl, alkylthioalkyl, arylthioalkyl, or the sulfone or sulfoxide derivatives thereof, aminoalkyl or a mono- or disubstituted aminoalkyl wherein said substituents are selected from alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroaralkyl, heterocycloalkyl, and heterocycloalkylalkyl, or, in the case of a disubsituted aminoalkyl, said substituents along with the nitrogen atom to which they are attached form a heterocycloalkyl or a heteroaryl;
- u represents 0, 1, 2, or 3;
- and,
- Y and Y′ independently represent O, S, and NR15, wherein R15 represents hydrogen and radicals as defined for R3.
20 more elements
A compound of the following formula:
- or a pharmaceutically acceptable salt, prodrug, or ester thereof, wherein
- t represents 0, 1, or 2;
- R6 represents hydrogen or alkyl;
- R2 represents an alkyl, aryl, cycloalkyl, cycloalkylalkyl, or aralkyl radical, which radical is optionally substituted with a substituent selected from the group consisting of alkyl, —NO2, CN, CF3, —OR9, —SR9, and halogen, wherein R9 represents hydrogen or alkyl;
- R3 represents hydrogen;
- alkyl;
- haloalkyl;
- alkenyl;
- alkynyl;
- hydroxyalkyl;
- alkoxyalkyl;
- cycloalkyl;
- cycloalkylalkyl;
- heterocycloalkyl;
- heteroaryl;
- heterocycloalkylalkyl;
- aryl;
- aralkyl;
- heteroaralkyl;
- thioalkyl, alkylthioalkyl, arylthioalkyl, or the sulfone or sulfoxide derivatives thereof;
- aminoalkyl or a mono- or disubstituted aminoalkyl wherein said substituents are selected from alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroaralkyl, heterocycloalkyl, and heterocycloalkylalkyl, or, in the case of a disubsituted aminoalkyl, said substituents along with the nitrogen atom to which they are attached form a heterocycloalkyl, or a heteroaryl;
- q represents 1 or 2;
- and,
- u represents 0, 1, 2, or 3.
21 more elements
Dependencies are inferred from the claim text.