.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 7,968,707

« Back to Dashboard

Details for Patent: 7,968,707

Title:Retroviral protease inhibiting compounds
Abstract: A compound of the formula: ##STR00001## 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. (Wads Worth, 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 27, 2007
Application Number:11/679,227
Claims:1. A process for the preparation of a compound of Formula I or a pharmaceutically acceptable salt, ester or prodrug thereof, ##STR00088## said process comprising reacting a compound of the formula: ##STR00089## with a compound of the formula: ##STR00090## or a salt or activated ester derivative thereof, wherein: R.sub.1 and R.sub.2 are independently selected from the group consisting of loweralkyl, cycloalkylalkyl and arylalkyl; R.sub.3 is loweralkyl, hydroxyalkyl or cycloalkylalkyl; R.sub.4 is aryl; R.sub.5 is ##STR00091## wherein n is 1, 2 or 3, X is O, S or NH, and Y is --O-- or --N(R.sub.6)-- wherein R.sub.6 is hydrogen, loweralkyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl; and L.sub.1 is selected from the group consisting of: a) --O--, b) --S--, c) --N(R.sub.7)-- wherein R.sub.7 is hydrogen loweralkyl, cycloalkyl or cycloalkylalkyl, d) --O-alkylenyl-, e) --S-alkylenyl-, f) --S(O)-alkylenyl-, g) --S(O).sub.2-alkylenyl-, h) --N(R.sub.7)-akylenyl- wherein R.sub.7 is defined as above, i) -alkylenyl-O--, j) -alkylenyl-S--, k) -alkylenyl-N(R.sub.7)-- wherein R.sub.7 is defined as above, l) -alkylenyl-, and m) -alkenylenyl-.

2. The process of claim 1, wherein R.sub.1 and R.sub.2 are arylalkyl, R.sub.3 is loweralkyl, R.sub.4 is aryl, and L.sub.1 is --O-alkylenyl-.

3. The process of claim 1, wherein 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, R.sub.4 is 2,6-dimethylphenyl which is optionally substituted with a substituent selected from the group consisting of loweratkyl and halo, L.sub.1 is --O--CH.sub.2--, n is 1 or 2, X is O or S, and Y is --CH.sub.2-- or --NH--.

4. The process of claim 1, wherein R.sub.1 and R.sub.2 are benzyl, R.sub.3 is loweralkyl, R.sub.4 is 2,6-dimethylphenyl, L.sub.1 is --O--CH.sub.2--, n is 1 or 2, X is O or S, and Y is --NH--.

5. A process for the preparation of a compound of formula I or a pharmaceutically acceptable salt, ester or prodrug thereof, ##STR00092## said process comprising reacting compound of the formula: ##STR00093## with a compound of the formula: ##STR00094## or an activated ester derivative thereof, wherein: R.sub.1 and R.sub.2 are independently selected from the group consisting of loweralkyl, cycloalkylalkyl and arylalkyl; R.sub.3 is loweralkyl, hydroxyalkyl or cycloalkylalkyl; R.sub.4 is aryl; R.sub.5 is ##STR00095## wherein n is 1, 2 or 3, X is O, S or NH, and Y is --O-- or --N(R.sub.6)-- wherein R.sub.6 is hydrogen, loweralkyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl; and L.sub.1 is selected from the group consisting of: a) --O--, b) --S--, c) --N(R.sub.7)-- wherein R.sub.7 is hydrogen, loweralkyl, cycloalkyl or cyoloalkylalkyl, d) --O-alkylenyl-, e) --S-alkylenyl-, f) --S(O)-alkylenyl-, g) --S(O).sub.2-alkylenyl-, h) --N(R.sub.7)-alkylenyl- wherein R.sub.7 is defined as above, i) -alkylenyl-O--, j) -alkylenyl-S--, k) -alkylenyl-N(R.sub.7)-- wherein R.sub.7 is defined as above, l) -alkylenyl-, and m) -alkenylenyl-.

6. The process of claim 5, wherein R.sub.1 and R.sub.2 are arylalkyl, R.sub.3 is loweralkyl, R.sub.4 is aryl, and L.sub.1 is --O-alkylenyl-.

7. The process of claim 5, wherein 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, R.sub.4 is 2,6-dimethylphenyl which is optionally substituted with a substituent selected from the group consisting of loweralkyl and halo, L.sub.1 is --O--CH.sub.2--, n is 1 or 2, X is O or S, and Y is --CH.sub.2-- or --NH--.

8. The process of claim 5, wherein R.sub.1 and R.sub.2 are benzyl, R.sub.3 is loweralkyl, R.sub.4 is 2,6-dimethylphenyl, L.sub.1 is --O--CH.sub.2--, n is 1 or 2, X is O or S, and Y --NH--.

9. A process for the preparation of a compound of Formula I according to claim 4, wherein said compound is (2S,3S,5S)-2-(2,6-dimethylphenoxyacetyl)amino-3-hydroxy-5-[2S-(1-tetrahyd- ro-pyrimid-2-onyl)-3-methyl butanoyl]amino-1,6-diphenylhexane, and said process further comprises: dissolving said compound in ethanol, isopropanol, or acetonitrile to provide a solution, and adding water to said solution to produce an amorphous solid.

10. A process for the preparation of a compound of Formula I according to claim 8, wherein said compound is (2S,3S,5S)-2-(2,6-dimethylphenoxyacetyl)amino-3-hydroxy-5-[2S-(1-tetrahyd- ro-pyrimid-2-onyl)-3-methyl butanoyl]amino-1,6-diphenylhexane, and said process further comprises: dissolving said compound in ethanol, isopropanol, or acetonitrile to provide a solution, and adding water to said solution to produce an amorphous solid.

11. A process for the preparation of a compound of Formula I according to claim 4, wherein X is O.

12. A process for the preparation of a compound of Formula I according to claim 8, wherein X is O.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc