New HIV protease inhibitors
AssigneeMerck & Co., Inc.
InventorsRandall W. Hungate, Joseph P. Vacca
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Abstract
Oligopeptide analogs containing sulfonamide, urea or carbamate linkages in the backbone are described. These compounds are useful in the inhibition of HIV protease, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
Claims4
A compound of the formula ##STR165## Wherein R is
- a) --V--R.sup.3 ;
- wherein V is --C(O)--Q--, or --SO.sub.2 --Q--;
- Q is
- a) absent, --O--, or --NH--,
- R.sup.1 is
- a) hydrogen, or
- b) --C.sub.1-5 alkyl unsubstituted or substituted with one or more of
- i) halo,
- ii) hydroxy,
- iii) C.sub.1-3 alkoxy,
- iv) aryl unsubstituted or substituted with one or more of C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitro, amino, amido, carboxy, hydroxy, halo or aryl;
- v) carboxyl;
- --C.sub.3-5 cycloalkyl, unsubstituted or substituted at the 3-position with C.sub.1-4 alkyl;
- or
- d) aryl unsubstituted or substituted with one or more of C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitro, amino, amido, carboxy, hydroxy, halo or aryl;
- and
- R.sup.2 is
- a) phenyl unsubstituted or substituted with one or more of --OH or C.sub.1-3 alkoxy;
- or
- b) C.sub.5-7 cycloalkyl, unsubstituted or substituted with one or more of --OH or C.sub.1-3 alkoxy;
- R.sup.3 is
- a) aryl unsubstituted or substituted with one or more of --C.sub.1-4 alkyl, oxo, amino or halo;
- b) C.sub.1-4 alkyl, unsubstituted or substituted once with aryl;
- c) C.sub.3-5 cycloalkyl, unsubstituted or substituted at the 3-position with C.sub.1-4 alkyl;
- J is ##STR166## or pharmaceutically acceptable salt thereof.
The compound ##STR168## named N-(2'(R)-hydroxy-1'(S)-indanyl)-2(R)-phenylmethyl-4(S)-hydroxy-5-[((2'''-m ethyl)propyl)-benzyloxycarbonyl]-aminopentaneamide, or pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.