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US 8,026,362 B2Granted
Non-nucleoside reverse transcriptase inhibitors
AssigneeRoche Palo Alto LLC
InventorsJoshua Kennedy-Smith, Zachary Kevin Sweeney, Jeffrey Wu
Life of this patent
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Abstract
Compounds of formula I, wherein R1, X1, X2 and A, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
Claims22
A compound according to formula I wherein:
- A is
- (a) CHR3═CHR2,
- (b) CH2R3CH2R2, or,
- (c) CHR2;
- either (i) R1 is II and R2 is hydrogen, C1-3 alkyl, C1-3 haloalkyl, C2-6 alkenyl, or CH2ORc;
- and, in addition, if A is either (a) or (b) R2 can also be halogen, NRaRb, CN, or ORc;
- or, (ii) R1 is C1-6 alkyl and R2 is II;
- X1 is O or S;
- X2 is O, or, if A is (a), X2 is O or NRd;
- R3 is hydrogen or C1-3 alkyl;
- R4 is halogen, C1-6 alkyl, C3-6 cycloalkyl C1-6 haloalkyl or C1-6 alkoxy;
- Ra and Rb are independently hydrogen, C1-3 alkyl or C1-6 acyl;
- Rc and Rd are independently hydrogen or C1-3 alkyl;
- Ar is phenyl substituted with 1 to 3 groups independently selected from halogen, cyano, C1-6 haloalkyl, C1-6 alkyl, C1-6 alkoxy or C3-6 cycloalkyl;
- n is an integer from 1 to 3;
- or,
- pharmaceutically acceptable salts thereof.
14 more elements
Dependencies are inferred from the claim text.