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Details for Patent: 6,472,529

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Details for Patent: 6,472,529

Title: Retroviral protease inhibiting compounds
Abstract:A compound of the formula: ##STR1## is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
Inventor(s): Sham; Hing Leung (Mundelein, IL), Norbeck; Daniel W. (Crystal Lake, IL), Chen; Xiaoqi (Libertyville, IL), Betebenner; David A. (Gurnee, IL), Kempf; Dale J. (Libertyville, IL), Herrin; Thomas R. (Waukegan, IL), Kumar; Gondi N. (Round Lake Beach, IL), Condon; Stephen L. (Kenosha, WI), Cooper; Arthur J. (Lake Villa, IL), Dickman; Daniel A. (Grayslake, IL), Hannick; Steven M. (Highland Park, IL), Kolaczkowski; Lawrence (Gurnee, IL), Oliver; Patricia A. (Lindenhurst, IL), Plata; Daniel J. (Waukegan, IL), Stengel; Peter J. (Waukegan, IL), Stoner; Eric J. (Kenosha, WI), Tien; Jieh-Heh J. (Libertyville, IL), Liu; Jih-Hua (Greek Oaks, IL), Patel; Ketan M. (Arlington Heights, IL)
Assignee: Abbott Laboratories (Abbott Park, IL)
Filing Date:Apr 18, 2001
Application Number:09/837,280
Claims:1. A compound of the formula: ##STR87## wherein P.sub.3 and P.sub.4 are independently selected from hydrogen and an N-protecting group; R.sub.1 and R.sub.2 ae independently selected from the group consisting of loweralkyl, cycloalkylalkyl and ary lalkyl; and R.sub.3 is loweralkyl, hydroxyalkyl or cycloalkylalkyl; and R.sub.5 is ##STR88## wherein n is 1, 2 or 3, X is O, S, or NH and Y is --CH.sub.2 --, --O--, --S-- or --N(R.sub.6)-- wherein R.sub.6 is hydrogen, loweralkyl, cycloalkyl, cycloalkylakyl, aryl or arylalkyl; or a salt thereof.

2. A compound according to claim 1 wherein P.sub.3 and P.sub.4 are hydrogen or benzyl, R.sub.1 and R.sub.2 are arylalkyl, R.sub.3 is loweralkyl and R.sub.5 is ##STR89##

wherein X, Y and n are defned as therein.

3. A compound according to claim 1 wherein P.sub.3 and P.sub.4 are hydrogen or benzyl, R.sub.1 and R.sub.2 are benzyl or R.sub.1 is benzyl and R.sub.2 is loweralkyl, R.sub.3 is loweralkyl and R.sub.5 is ##STR90## wherein n is 1 or 2, X is O or S and Y is --CH.sub.2 -- or --NH.

4. A compound according to claim 1 wherein P.sub.3 and P.sub.4 are hydrogen or benzyl, R.sub.1 and R.sub.2 are benzyl or R.sub.1 is benzyl and R.sub.2 is isopropyl, R.sub.3 is loweralkyl and R.sub.5 is ##STR91## wherein n is 1 or 2, X is O or S and Y is --NH--.

5. A compound according to claim 1 wherein P.sub.3 and P.sub.4 are hydrogen or benzyl, R.sub.1 and R.sub.2 are benzyl or R.sub.1 is benzyl and R.sub.2 is isopropyl, R.sub.3 is isopropyl and R.sub.5 is ##STR92## wherein n is 1 or 2, X is O or S and Y is --CH.sub.2 -- or --NH.

6. A compound according to claim 1 wherein P.sub.3 and P.sub.4 are hydrogen or benzyl, R.sub.1 and R.sub.2 are benzyl and R.sub.2 is isopropyl, R.sub.3 is isopropyl and R.sub.5 is ##STR93##

wherein n is 1 or 2, X is O or S and Y is --NH--.

7. A compound selected from the group consisting of: (2S, 3S, 5S)-2-N,N-dibenzylamino-3-hydroxy-5-(2S-(1-tetrahydro-pyrimid-2-onyl)-3- methylbutanoyl) amino-1,6-diphenylhexane; and (2S, 3S, 5S)-2-Amino-3-hydroxy-5-(2S-(1-tetrahydro-pyrimid-2-onyl)-3-methylbutanoy) amino-1,6- diphenylhexane; or a salt thereof.

8. A compound selected from the group consisting of: (2S, 3S, 5S)-2-(t-butyloxycarbonyl)amino-3-hydroxy-5-(2S-(1-imidazolidin-2-onyl)-3- methyl- butanoyl)amino-1,6-diphenylhexane and (2S, 3S, 5S)-2-amino-3-HYDROXY -5-(2 S-(1-imidazolidin-2-onyl)-3-methyl-butanoy)amino-1,6- diphenylhexane; or a salt thereof.

9. The compound (2S, 3S, 5S)-2-amino-3-hydroxy-5-(2S-(1-tetrahydro-pyrimid- 2-onyl)-3-methylbutanoyl)amino-1,6-diphenylhexane (S)-Pyroglutamic acid salt.
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