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US 2007/0179157 A1Published application
Nonnucleoside reverse transcriptase inhibitors
AssigneeRoche Palo Alto LLC
InventorsJames Dunn, Steven Swallow, Zachary Sweeney
Life of this patent
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Abstract
This invention relates to methods of treating an HIV infection with novel heterocyclic compounds of formula I wherein R1—R4, X1 and X2 are as defined in the summary and pharmaceutically acceptable salts, and methods to inhibit or modulate Human Immunodeficiency Virus (HIV) reverse transcriptase with compounds of formula I.
Claims9
1-23. (canceled)
A method for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC, comprising administering to a host in need thereof a therapeutically effective amount of a compound of formula I
- wherein:
- X1 is selected from the group consisting of R5O, R5S(O)n, R5CH2, R5CH2O, R5CH2S(O)n, R5OCH2, R5S(O)n, CH2 and NR5R6;
- X2 is selected from the group consisting of O, S, and NR7;
- R1 and R2 are
- (i) each independently selected from the group consisting of hydrogen, C1-6 alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, C1-6 haloalkoxy, C1-6 haloalkylthio, halogen, amino, alkylamino, dialkylamino, aminoacyl, nitro and cyano;
- or,
- (ii) taken together are —CH═CH—CH═CH—, or
- (iii) taken together along with the carbons to which they are attached to form a five- or six-membered heteroaromatic or heterocyclic ring with a one or two heteroatoms independently selected from the group consisting of O, S and NH;
- R3 and R4 are each independently selected from the group consisting of hydrogen, C1-6 alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkoxy, C1-6 haloalkyl halogen, amino, alkylamino, dialkylamino, aminoacyl, nitro and cyano;
- R5 is selected from the group consisting of phenyl, naphthyl, pyrdinyl, pyridinyl N-oxide, indolyl, indolyl N-oxide, quinolinyl, quinolinyl N-oxide,, pyrimidinyl, pyrazinyl and pyrrolyl;
- wherein, said phenyl, said naphthyl, said pyrdinyl, said pyridinyl N-oxide, said indolyl, said indolyl N-oxide, said quinolinyl, said quinolinyl N-oxide,, said pyrimidinyl, said pyrazinyl and said pyrrolyl groups are optionally substituted with one to three substituents independently selected from the group consisting of hydrogen, C1-6 alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, C1-6 haloalkoxy, C1-6 haloalkylthio, halogen, amino, alkylamino, dialkylamino, aminoacyl, acyl, alkoxycarbonyl, carbamoyl, N-alkylcarbamoyl, N,N-dialkylcarbamoyl, nitro and cyano;
- R6 is hydrogen, C1-6 alkyl, or acyl;
- R7 is hydrogen or C1-6 alkyl optionally substituted with one or two substituents independently selected from the group consisting of hydroxy, alkoxy, thiol, alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, halogen, amino, alkylamino, dialkylamino, aminoalkyl, alkylaminoalkyl, and dialkylamino;
- n is an integer from 0 to 2;
- or, acid addition salts thereof.
12 more elements
31-41. (canceled)
Dependencies are inferred from the claim text.