HIV protease inhibitors useful for the treatment of AIDS
AssigneeMerck & Co., Inc.
InventorsCraig A. Coburn, Mark E. Fraley, M. Katharine Holloway, Randall W. Hungate, Kristine Prendergast
Life of this patent
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Abstract
Compounds such as ##STR1## or pharmaceutically acceptable salts thereof, are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in 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.
Claims13
A compound of the formula:
- ##STR83## wherein X is --O--, --NH--, --NR.sup.4 -- or --S--;
- Y is .dbd.O, or forms, with the carbon to which it is attached, ##STR84## Z is .dbd.O, or forms, with the carbon to which it is attached, ##STR85## R.sup.1 is a) H;
- b) C.sub.1-4 alkyl;
- c) C.sub.3-7 cycloalkyl;
- d) aryl, unsubstituted or substituted one or more times with hydroxy;
- e) CH.sub.2 R.sup.5 ;
- or
- f) 5-7 membered heterocycle;
- and
- R.sup.2 is
- a) C.sub.1-4 alkyl;
- b) aryl, unsubstituted or substituted with aryl;
- c) CH.sub.2 R.sup.6 ;
- or
- d) heterocycle;
- and
- R.sup.3 is
- a) CH(OH)R.sup.7 ;
- or
- b) CH(NH.sub.2)R.sup.7 ;
- and
- R.sup.4 is
- a) C.sub.1-4 alkyl;
- b) C.sub.3-6 cycloalkyl;
- c) aryl unsubstituted or substituted with halo or with C.sub.1-4 alkyl unsubstituted or substituted one or more times with hydroxy;
- d) CH.sub.2 R.sup.1 ;
- or
- e) 5-7 member ed heterocycle;
- and
- R.sup.5 is
- a) C.sub.1-4 alkyl;
- or
- b) aryl;
- and
- R.sup.6 is
- a) C.sub.1-4 alkyl;
- b) aryl unsubstituted or substituted with halo or with C.sub.1-4 alkyl unsubstituted or substituted one or more times with hydroxy;
- or
- c) 5-7 membered heterocycle;
- and
- R.sup.7 is
- a) H;
- b) C.sub.1-4 alkyl;
- c) aryl unsubstituted or substituted with amino;
- d) C.sub.1-3 alkylaryl unsubstituted or substituted with amino;
- or
- e) 5-7 membered heterocycle;
- or pharmaceutically acceptable salt thereof.
A compound of the formula ##STR86## wherein R.sup.2 is C.sub.1-4 alkylene-aryl;
- and
- R.sup.4 is C.sub.1-4 alkyl, unsubstituted or substituted with aryl, C.sub.3-6 cycloalkyl, or 5-7 membered heterocycle;
- R.sup.7 is H, benzyl unsubstituted or substituted with amino;
- or pharmaceutically acceptable salt thereof.
A combination of compounds, which is ##STR89## or pharmaceutically acceptable salts thereof, and any of AZT or ddI or ddC.
Dependencies are inferred from the claim text.