Back to results
US 5,508,407 AGranted
Retroviral protease inhibitors
AssigneeEli Lilly and Company
InventorsStephen W. Kaldor, Marlys Hammond
Life of this patent
Estimating the term…
Abstract
The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of their use.
Claims30
A compound having the Formula:
- ##STR12## where:
- R is quinolyl, tetrahydroquinolyl, or quinolyl substituted by oxo, chloro, methoxy, 2-methylpropyl, isopropyl, or one or two fluoro, or methyl groups;
- X is a bond, (--CH.sub.2).sub.q --, --O--(--CH.sub.2 --).sub.q --, --(--CH.sub.2 --).sub.q --O-- or --N(R.sup.5) (CH.sub.2 --).sub.m --;
- q is 1, 2, 3 or 4;
- n is 0, 1, or2;
- R.sup.1 is aryl or C.sub.5 -C.sub.7 cycloalkyl;
- R.sup.2 is an amino acid side chain,
- C.sub.1 -C.sub.4 alkylaminocarbonyl(C.sub.1 -C.sub.4 alkanediyl), or a group having the structure --CH.sub.2 --C(O)--NR.sup.4 --X--R' or --CH.sub.2 --R" where
- R' is pyridyl, imidazolyl, phenyl, benzimidazolyl or indolyl;
- and
- R" is imidazolyl;
- Y is aryl or furyl, thienyl, or benzofuryl;
- R.sup.3 is a group having the structure:
- ##STR13## where:
- l is 3, 4 or 5;
- m at each occurrence is independently 0, 1, 2, or 3;
- p is 4 or 5;
- R.sup.4 at each occurrence is independently hydrogen, C.sub.1 -C.sub.6 alkyl, or hydroxy(C.sub.1 -C.sub.4)alkanediyl;
- R.sup.5 and R.sup.6 are independently selected from hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, amino, C.sub.1 -C.sub.4 alkylamino, hydroxy(C.sub.1 -C.sub.4)-alkanediyl, carboxy, C.sub.1 -C.sub.4 alkoxy)carbonyl, aminocarbonyl, C.sub.1 -C.sub.4 alkylaminocarbonyl, or aryl;
- or a pharmaceutically acceptable salt or solrate thereof.
17 more elements
Dependencies are inferred from the claim text.