Carbocyclic HIV protease inhibitors
AssigneeHoffmann-La Roche Inc.
InventorsEmmanuel Demont, Joseph Armstrong Martin, Sally Redshaw, Steven Swallow
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Abstract
The present invention is concerned with novel HIV protease Inhibitors of formula I as individual isomers, racemates, non-racemic mixtures or mixtures of diastereoisomers; wherein n, R1 and R4 are as described herein. The compounds of formula I are peptide mimetics which act as inhibitors of the HIV aspartyl protease, an essential enzyme in the replicative life cycle of HIV.
Claims8
A compound having the following formula I
- as individual isomers, racemates, non-racemic mixtures or mixtures of diastereoisomers;
- wherein
- n is 0, 1 or 2;
- R1 is naphthyl, quinolinyl or phenyl, optionally substituted by halogen;
- R4 is (C1-C7)-alkyl;
- A is a group
- wherein
- R2 is hydrogen or (C1-C7) lower alkoxy;
- and
- R3 is (C1-C7)-alkyl;
- or pharmaceutically acceptable salts thereof.
A method of treating or preventing a disease mediated by the human immunodeficiency virus (HIV) comprising administering to a patient in need of such treatment, an effective amount of a compound of the following formula I
- as individual isomers, racemates, non-racemic mixtures or mixtures of diastereoisomers;
- wherein
- n is 0, 1 or 2;
- R1 is naphthyl, quinolinyl or phenyl, optionally substituted by halogen;
- R4 is (C1-C7)-alkyl;
- A is a group
- wherein
- R2 is hydrogen or (C1-C7) lower alkoxy;
- and
- R3 is (C1-C7)-alkyl;
- or pharmaceutically acceptable salts thereof.
A pharmaceutical composition comprising a pharmaceutically effective amount of a compound of the following formula I
- as individual isomers, racemates, non-racemic mixtures or mixtures of diastereoisomers;
- wherein
- n is 0, 1 or 2;
- R1 is naphthyl, quinolinyl or phenyl, optionally substituted by halogen;
- R4 is (C1-C7)-alkyl;
- A is a group
- wherein
- R2 is hydrogen or (C1-C7) lower alkoxy;
- and
- R3 is (C1-C7)-alkyl;
- or pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.