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Summary for Patent: 8,148,374
|Title:||Modulators of pharmacokinetic properties of therapeutics|
|Abstract:||The present application provides for a compound of Formula IV, ##STR00001## or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.|
|Inventor(s):||Desai; Manoj C. (Pleasant Hill, CA), Liu; Hongtao (Cupertino, CA), Xu; Lianhong (Palo Alto, CA)|
|Assignee:||Gilead Sciences, Inc. (Foster City, CA)|
1. A compound which is ##STR00294## or a pharmaceutically acceptable salt thereof.
2. A pharmaceutical composition comprising the compound or salt of claim 1, and a pharmaceutically acceptable carrier or excipient.
3. The pharmaceutical composition of claim 2, further comprising at least one therapeutic agent which is metabolized by cytochrome P450.
4. The pharmaceutical composition of claim 3, wherein the at least one therapeutic agent is selected from the group consisting of HIV protease inhibitors, HIV non-nucleoside inhibitors of reverse transcriptase, HIV nucleoside inhibitors of reverse transcriptase, HIV nucleotide inhibitors of reverse transcriptase, HIV integrase inhibitors, gp41 inhibitors, CXCR4 inhibitors, gp120 inhibitors, G6PD inhibitors, NADH-oxidase inhibitors, CCR5 inhibitors, capsid polymerization inhibitors, other drugs for treating HIV, interferons, ribavirin, NS3 protease inhibitors, alpha-glucosidase 1 inhibitors, hepatoprotectants, non-nucleoside inhibitors of HCV, NS5a inhibitors, NS5b polymerase inhibitors, other drugs for treating HCV, and combinations thereof.
5. A compound which is: ##STR00295## or a pharmaceutically acceptable salt thereof.
6. A method for inhibiting cytochrome P450 monooxygenase in a patient in need thereof, comprising administering to the patient an amount of the compound ##STR00296## or a pharmaceutically acceptable salt thereof, which is effective to inhibit cytochrome P450 monooxygenase in the patient.
7. The method of claim 6, wherein the cytochrome P450 monooxygenase enzyme that is inhibited is 3A isoenzyme.
8. The method of claim 7, wherein the cytochrome P450 monooxygenase enzyme that is inhibited is 3A4 isoenzyme.
9. The method of claim 8, wherein cytochrome P450 monooxygenase isoenzyme 2C9 is not inhibited or is inhibited substantially less than the 3A4 isoenzyme.
10. The method of claim 7, wherein the compound ##STR00297## or the pharmaceutically acceptable salt thereof does not inhibit or weakly inhibits one or more protease enzymes.
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