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US 2010/0137590 A1Published application
N[S(4-ARYL-TRIAZOL-3-YL)alpha-MERCAPTOACETYL] -P-AMINO BENZOIC ACIDS AS HIV REVERSE TRANSCRIPTASE INHIBITORS
AssigneeArdea Biosciences, Inc.
InventorsJean-Luc Girardet, Yung-hyo Koh, Martha De La Rosa, Zhi Hong, Stanley Lang
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Abstract
A series of S-triazolyl α-mercaptoacetanilides having N-(α-mercaptoacetyl) p amino benzoic acid derivatives. are provided, where Q is CO2H, 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.
Claims10
A compound of formula
- wherein:
- R1 is selected from the group consisting of Cl, Br, I, CH3, CF3, CHF2, and CH2F;
- X is O or NH;
- R2 is H, a pharmaceutically acceptable cation or C1-3 alkyl, when X is O;
- or
- XR2 is NHCH2CH2COOR13 or NHCH(R12)COOR13 where R12 is C1-4 alkyl or aryl-C1-4 alkyl and R13 a pharmaceutically acceptable cation or C1-3 alkyl;
- R3 is H or CH3;
- R0 is selected from the group consisting of Cl, Br, CF3 and methyl;
- RP is selected from the group consisting of methyl, ethyl, propyl, isopropyl, cyclopropylmethyl, and C3-6 cycloalkyl;
- R4, R5 and R6 are independently selected from the group consisting of H, F, Cl, Br, CH3, CF3, CFH2, CF2H, ethyl, isopropyl, cyclopropyl, OCH3, OH, OCF3, NH2 and NHCH3;
- and
- Q and Q′ are independently selected from N and CH.
9 more elements
-22. (canceled)
A compound selected from the group consisting of:
- wherein Q1 is CO2H or SO2H;
- and Q2 is C3-5 cycloalkyl or C2-5 alkyl.
Dependencies are inferred from the claim text.