Details for Patent: 6,313,296
✉ Email this page to a colleague
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--. |