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Details for Patent: 8,481,581

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Details for Patent: 8,481,581

Title:S-triazolyl .alpha.-mercaptoacetanilides as inhibitors of HIV reverse transcriptase
Abstract: A series of S-triazolyl .alpha.-mercaptoacetanilides having general structure (1) are provided, where Q is CO.sub.2H, CONR.sub.2, SO.sub.3H, or SO.sub.2NR.sub.2. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections. ##STR00001##
Inventor(s): Girardet; Jean-Luc (San Diego, CA), Koh; Yung-Hyo (Irvine, CA), De La Rosa; Martha (Durham, NC), Gunic; Esmir (San Diego, CA), Hong; Zhi (Chapel Hill, NC), Lang; Stanley (Concord Twp, OH), Kim; Hong-Woo (Cambridge, MA)
Assignee: Ardea Biosciences, Inc. (San Diego, CA)
Filing Date:Jul 18, 2012
Application Number:13/552,443
Claims:1. A compound of formula ##STR00326## wherein: P is selected from the group consisting of (a): ##STR00327## R.sup.1 is selected from the group consisting of Cl, Br, I, CF.sub.3, CHF.sub.2; and CH.sub.2F; R.sup.2 and R.sup.2' are independently selected from the group consisting of H, optionally substituted C.sub.1-5acyl, 1-(C.sub.2-4acyloxy)C.sub.1-4alkoxycarbonyl, and an acyl group derived from an .alpha.-amino acid; R.sup.3 is H or CH.sub.3; R.sup.0 is selected from the group consisting of Cl, Br, CF.sub.3 and methyl; R.sup.P is C.sub.3-6cycloalkyl; and R.sup.4, R.sup.5 and R.sup.6 are independently selected from the group consisting of H, F, Br, CH.sub.3, CF.sub.3, CFH.sub.2, CF.sub.2H, isopropyl, cyclopropyl, OCH.sub.3, OH, OCF.sub.3, NH.sub.2 and NHCH.sub.3.

2. The compound of claim 1, wherein P is a substituted naphthyl and R.sup.1 is selected from the group consisting of Br, CF.sub.3, CFH.sub.2, and CF.sub.2H.

3. The compound of claim 2, wherein each of R.sup.4, R.sup.5, and R.sup.6 is H.

4. The compound of claim 2, wherein R.sup.P is cyclopropyl.

5. The compound of claim 2, wherein R.sup.1 is Br and R.sup.0 is Cl.

6. A method for inhibiting an HIV reverse transcriptase, comprising contacting the HIV reverse transcriptase with a compound of formula ##STR00328## wherein: P is selected from the group consisting of (a): ##STR00329## R.sup.1 is selected from the group consisting of Cl, Br, I, CF.sub.3, CHF.sub.2, and CH.sub.2F; R.sup.2 and R.sup.2' are independently selected from the group consisting of H, optionally substituted C.sub.1-5acyl, 1-(C.sub.2-4acyloxy)C.sub.1-4alkoxycarbonyl, and an acyl group derived from an .alpha.-amino acid; R.sup.3 is H or CH.sub.3; R.sup.0 is selected from the group consisting of Cl, Br, CF.sub.3 and methyl; R.sup.P is C.sub.3-6cycloalkyl; and R.sup.4, R.sup.5 and R.sup.6 are independently selected from the group consisting of H, F, Cl, Br, CH.sub.3, CF.sub.3, CFH.sub.2, CF.sub.2H, isopropyl, cyclopropyl, OCH.sub.3, OH, OCF.sub.3, NH.sub.2 and NHCH.sub.3.

7. The method of claim 6, wherein the HIV reverse transcriptase is a mutated reverse transcriptase.

8. The method of claim 7, wherein the mutated HIV reverse transcriptase is a K10Y, Y181C or Y188L mutant.
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