Back to results
US 7,683,087 B2Granted
N[S(4-aryl-triazol-3-yl)α-mercaptoacetyl] -p-amino benzoic acids as HIV reverse transcriptase inhibitors
AssigneeArdea Biosciences, Inc.
InventorsJean-Luc Girardet, Martha de la Rosa, Zhi Hong, Stanley Lang
Life of this patent
Estimating the term…
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.
Claims36
A compound of formula
- wherein:
- Ar is
- 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;
- R6 is H, F, Cl, Br, CH3, CF3, CFH2, CF2H, ethyl, isopropyl, cyclopropyl, OCH3, OH, OCF3, NH2 or NHCH3;
- and
- R7 is selected from the group consisting of Cl, Br, I, CH3, CF3;
- OCH3, isopropyl, cyclopropyl, tert-butyl, cyclobutyl, and methyl.
11 more elements
Dependencies are inferred from the claim text.