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Details for Patent: 6,313,296

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Details for Patent: 6,313,296

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:Feb 23, 2000
Application Number:09/511,390
Claims:1. A compound of the formula: ##STR87##

wherein 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, cycloalkylalkyl, aryl or arylalkyl;

or a salt or activated ester derivative thereof;

with the proviso that when R.sub.3 is hydroxyalkyl, then R.sub.5 is other than ##STR89##

wherein n is 1, 2 or 3.

2. A compound according to claim 1 wherein R.sub.3 is loweralkyl and R.sub.5 is ##STR90##

wherein X, Y and n are defined as therein.

3. A compound according to claim 1 wherein 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 --CH.sub.2 -- or --NH--.

4. A compound according to claim 1 wherein 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--.

5. A compound according to claim 1 wherein 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--.

6. A compound according to claim 1 wherein R.sub.3 is isopropyl and R.sub.5 is ##STR94##

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

7. The compound according to claim 1 which is 2S-(1-Tetrahydropryimid-2-onyl)-3-methylbutanoic acid or a salt or an activated ester derivative thereof.

8. A compound according to claim 1 wherein R.sub.3 is loweralkyl and R.sub.5 is ##STR95##

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

9. 2S-(1-Tetrahydropryimid-2-onyl)-3-methylbutanoic acid or a salt thereof.

10. An activated ester derivative of 2S-(1-Tetrahydropryimid-2-onyl)-3-methylbutanoic acid.

11. A compound of the formula: ##STR96##

wherein R.sub.3 loweralkyl, hydroxyalkyl or cycloalkylalkyl; and

R.sub.5 is ##STR97##

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, loweralky, cycloalky, cycloalkylalky, aryl or arylalkyl;

or a salt thereof;

with the proviso that when R.sub.3 is hydroxyalkyl, then R.sub.5 is other than

wherein n is 1,2 or 3. ##STR98##

12. A compound according to claim 11 wherein R.sub.3 is loweralkyl and R.sub.5 is ##STR99##

wherein X, Y and n are defined as therein.

13. A compound according to claim 11 wherein R.sub.3 is loweralkyl and R.sub.5 is ##STR100##

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

14. A compound according to claim 11 wherein R.sub.3 is isopropyl and R.sub.5 is ##STR101##

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

15. A compound according to claim 11 wherein R.sub.3 is isopropyl and R.sub.5 is ##STR102##

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

16. A compound according to claim 11 wherein R.sub.3 is isopropyl and R.sub.5 is ##STR103##

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

17. A compound according to claim 11 wherein R.sub.3 is loweralky and R.sub.5 is ##STR104##

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