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|Title:||Fitness assay and associated methods|
|Abstract:||The present invention provides an assay for determining the biochemical fitness of a biochemical species in a mutant replicating biological entity relative to its predecessor. The present invention further provides a continuous fluorogenic assay for measuring the anti-HIV protease activity of protease inhibitor. The present invention also provides a method of administering a therapeutic compound that reduces the chances of the emergence of drug resistance in therapy. The present invention also provides a compound of formula (I) or a pharmaceutically acceptable salt, a prodrug, a composition, or an ester thereof, wherein A is a group of formulas (A), (B), (C) or (D); R.sup.1, R.sup.2, R.sup.3, R.sup.5 or R.sup.6 is H, or an optionally substituted and/or heteroatom-bearing alkyl, alkenyl, alkynyl, or cyclic group; Y and/or Z are CH.sub.2, O, S, SO, SO.sub.2, amino, amides, carbamates, ureas, or thiocarbonyl derivatives thereof, optionally substituted with an alkyl, alkenyl, or alkynyl group; n is from 1 to 5; X is a bond, an optionally substituted methylene or ethylene, an amino, O or S; Q is C(O), C(S), or SO.sub.2; m is from 0 to 6; R.sup.4 is OH, .dbd.O (keto), NH.sub.2, or alkylamino, including esters, amides, and salts thereof; and W is C(O), C(S), S(O), or SO.sub.2. Optionally, R.sup.5 and R.sup.6, together with the N--W bond of formula (I), comprises a macrocyclic ring.|
|Inventor(s):||Erickson; John W. (Frederick, MD), Gulnik; Sergei V. (Frederick, MD), Mitsuya; Hiroaki (Chevy Chase, MD), Ghosh; Arun K. (River Forest, IL)|
|Assignee:||The United States of America as represented by the Department of Health and Human Services (Washington, DC) N/A (Urbana, IL) Board of Trustees of the University of Illinois (|
Patent Claim Types:|
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Back Citations: 39th percentile
Forward Citations: 1st percentile
|Applicant||Tradename||Generic Name||Dosage||NDA||Approval Date||Type||RLD||Patent No.||Patent Expiration||Product||Substance||Delist Req.||Patented / Exclusive Use|
|TABLET;ORAL||021976-004||Dec 18, 2008||RX||No||7,470,506*PED||► subscribe||Y|
|TABLET;ORAL||021976-005||Dec 18, 2008||RX||No||7,470,506*PED||► subscribe||Y|
|TABLET;ORAL||021976-001||Jun 23, 2006||DISCN||No||7,470,506*PED||► subscribe||Y|
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|PCT Filed||June 23, 1999||PCT Application Number:||PCT/US99/14119|
|PCT Publication Date:||December 29, 1999||PCT Publication Number:||WO99/67417|
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