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US 2018/0002296 A1Published application
S-triazolyl alpha-mercapto acetanilides as inhibitors of hiv reverse transcriptase
AssigneeArdea Biosciences, Inc.
InventorsJean-Luc GIRARDET, Yung-Hyo KOH, Martha DE LA ROSA, Esmir GUNIC, Zhi HONG, Stanley LANG, Woo-Hong KIM
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Abstract
A series of S-triazolyl α-mercaptoacetanilides having general structure (1) are provided, where Q is CO2H, CONR2, SO3H, or SO2NR2. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.
Claims20
A compound of formula A
- wherein:
- Q is CONR′R″;
- P is selected from the group consisting of (a), (b), (c) and (d):
- R1 is selected from the group consisting of Cl, Br, I, CH3, CF3, CHF2, and CH2F;
- R3 is H or CH3;
- R′ and R″ are independently selected from the group consisting of H, lower alkyl, and lower alkyl substituted with one or more OR, CO2R, NHR, NR2, or CF3 groups wherein R is H or lower alkyl, or R′ and R″ together with the nitrogen atom to which they are attached form a 4-, 5-, or 6-membered heterocyclic ring;
- R0 is selected from the group consisting of Cl, Br, CF3 and methyl;
- RP is selected from the group consisting of halogen, methyl, ethyl, propyl, isopropyl, cyclopropylmethyl, and C3-C6 cycloalkyl;
- R4, R5 and R6 are independently selected from the group consisting of H, F, Cl, Br, CH3, CF3, CFH2, CF2H, isopropyl, cyclopropyl, OCH3, OH, OCF3, NH2 and NHCH3;
- U and U′ are independently selected from N and CH;
- R7 is selected from the group consisting of Cl, Br, I, CH3, CF3, OCH3, isopropyl, cyclopropyl, tert-butyl, and cyclobutyl;
- and
- R8, R9, R10 and R11 are independently H or CH3.
10 more elements
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A compound of Formula A
- wherein:
- R1 is C1-3 alkyl, —CF3, —CHF2, —CH2F, —Cl, —Br, —NH2, or hydrogen;
- R2 is an aryl or heteroaryl moiety containing a cycloalkyl or heterocyclic group which can be further substituted with alkyl, cycloalkyl, aryl or heteroaryl moieties;
- Q is a C3-5 cycloalkyl;
- W is S, O, or an optionally substituted amine;
- R3 is C1-3 alkyl, —CF3, —CHF2, —CH2F, —Cl, —Br;
- and
- R4 is —COR′, wherein R′ is —NH2 or —NH(alkyl).
5 more elements
A compound of Formula
- wherein:
- R1 is C1-3 alkyl, —CF3, —CHF2, —CH2F, —Cl, —Br, —NH2, or hydrogen;
- R2 is an 4-Q-naphth-1-yl or 4-Q-phen-1-yl-;
- Q is C2-5 alkyl;
- W is S, O or an optionally substituted amine;
- R3 is C1-3 alkyl, —CF3, —CHF2, —CH2F, —Cl, —Br;
- and
- R4 is —COR′, wherein R′ is —NH2 or —NH(alkyl).
5 more elements
Dependencies are inferred from the claim text.