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Generated: February 20, 2018

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Title:N[S(4-aryl-triazol-3-yl).alpha.-mercaptoacetyl]-p-amino benozioc acids as HIV reverse transcriptase inhibitors
Abstract: A series of S-triazolyl .alpha.-mercaptoacetanilides having N-(.alpha.-mercaptoacetyl) p amino benzoic acid derivatives. ##STR00001## are provided, where Q is CO.sub.2H, or a salt or ester thereof, or a C(O)N-linked amino acid. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.
Inventor(s): Girardet; Jean-Luc (Aliso Viejo, CA), Koh; Yung-hyo (Irvine, CA), de la Rosa; Martha (Fountain Valley, CA), Hong; Zhi (Irvine, CA), Lang; Stanley (Laguna Niguel, CA)
Assignee: Ardea Biosciences, Inc. (San Diego, CA)
Filing Date:Nov 30, 2005
Application Number:11/291,653
Claims:1. A compound of formula ##STR00108## wherein: ##STR00109## R.sup.1 is selected from the group consisting of Cl, Br, I, CH.sub.3, CF.sub.3, CHF.sub.2, and CH.sub.2F; X is O or NH; R.sup.2 is H, a pharmaceutically acceptable cation or C.sub.1-3 alkyl, when X is O; or XR.sup.2 is NHCH.sub.2CH.sub.2COOR.sup.13 or NHCH(R.sup.12)COOR.sup.13 where R.sup.12 is C.sub.1-4 alkyl or aryl-C.sub.1-4 alkyl and R.sup.13 a pharmaceutically acceptable cation or C.sub.1-3 alkyl; 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 selected from the group consisting of methyl, ethyl, propyl, isopropyl, cyclopropylmethyl, and C.sub.3-6 cycloalkyl; 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, ethyl, isopropyl, cyclopropyl, OCH.sub.3, OH, OCF.sub.3, NH.sub.2 and NHCH.sub.3.

2. The compound of claim 1, wherein X is O.

3. The compound of claim 2, wherein none of R.sup.4, R.sup.5, and R.sup.6 is OH, NH.sub.2 or NHCH.sub.3.

4. The compound of claim 2, wherein at least one of R.sup.4, R.sup.5, and R.sup.6 is other than H or CH.sub.3.

5. The compound of claim 3 wherein at least one of R.sup.4, R.sup.5, and R.sup.6 is other than H or CH.sub.3.

6. The compound of claim 3, wherein R.sub.1 is selected from the group consisting of Br, CF.sub.3, CFH.sub.2, and CF.sub.2H.

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

8. The compound of claim 7, wherein R.sup.P is cyclopropyl.

9. The compound of claim 7, which is 4-[2-(5-bromo-4-[4-cyclopropylnaphthalen-1-yl]-4H-1,2,4-triazol-3-ylthio)- acetamido]-3-chlorobenzoic acid or an ester or a pharmaceutically acceptable salt thereof.

10. The compound of claim 9, wherein R.sup.2 is H.

11. The compound of claim 6, wherein R.sup.1 is Br and R.sup.0 is Cl.

12. The compound of claim 6, wherein Ar is 7-substituted naphthyl.

13. The compound of claim 12, wherein R.sup.4 is 7-ethyl, 7-OCH.sub.3, or 7-cyclopropyl, and each of R.sup.5 and R.sup.6 are H.

14. The compound of claim 13, which is 4-[2-(5-bromo-4-[7-methoxy-4-methylnaphthalen-1-yl]-4H-1,2,4-triazol-3-yl- thio)acetamido]-3-chlorobenzoic acid or an ester or a pharmaceutically acceptable salt thereof.

15. The compound of claim 14, wherein R.sup.2 is H.

16. The compound of claim 6, where R.sup.0 is Cl.

17. The compound of claim 16, wherein R.sup.P is cyclopropyl.

18. The compound of claim 17, which is 4-[2-(5-bromo-4-[4-cyclopropyl-7-methoxynaphthalen-1-yl]-4H-1,2,4-triazol- -3-ylthio)acetamido]-3-chlorobenzoic acid or an ester or a pharmaceutically acceptable salt thereof.

19. The compound of claim 18, wherein R.sup.2 is H.
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