- Discovery of triazolinone non-nucleoside inhibitors of HIV reverse transcriptase
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Novel non-nucleoside inhibitors of HIV-RT that contain pyridazinone isosteres were prepared, and a series of triazolinones were found to be potent inhibitors of HIV replication. These compounds were active against several NNRTI-resistant virus strains. Ph
- Sweeney, Zachary K.,Acharya, Sahaja,Briggs, Andrew,Dunn, James P.,Elworthy, Todd R.,Fretland, Jennifer,Giannetti, Anthony M.,Heilek, Gabrielle,Li, Yu,Kaiser, Ann C.,Martin, Michael,Saito, Y. David,Smith, Mark,Suh, Judy M.,Swallow, Steven,Wu, Jeffrey,Hang, Julie Q.,Zhou, Amy S.,Klumpp, Klaus
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- HETEROCYCLIC ANTIVIRAL COMPOUNDS
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Compounds of formula I, wherein R1, R2, R3, X1, X2 and Ar, 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.
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Page/Page column 20
(2009/07/17)
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- CHEMICAL COMPOUNDS
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The present invention relates to compounds that are a non-nucleoside reverse transcriptase inhibitors, and to processes for the preparation and use of the same. Specifically, the present invention includes methods of using such compounds in the treatment of human immunodeficiency virus infection.
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- CHEMICAL COMPOUNDS
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The present invention relates to compounds that are a non-nucleoside reverse transcriptase inhibitors, and to processes for the preparation and use of the same. Specifically, the present invention includes methods of using such compounds in the treatment of human immunodeficiency virus infection.
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- Non-nucleoside reverse transcriptase inhibitors
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The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A1, A2, A3 or A4 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
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Page/Page column 17-18
(2008/06/13)
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- Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase
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Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are recommended components of preferred combination antiretroviral therapies used for the treatment of HIV. These regimens are extremely effective in suppressing virus replication. Structure-based o
- Sweeney, Zachary K.,Harris, Seth F.,Arora, Nidhi,Javanbakht, Hassan,Li, Yu,Fretland, Jennifer,Davidson, James P.,Billedeau, J. Roland,Gleason, Shelley K.,Hirschfeld, Donald,Kennedy-Smith, Joshua J.,Mirzadegan, Taraneh,Roetz, Ralf,Smith, Mark,Sperry, Sarah,Suh, Judy M.,Wu, Jeffrey,Tsing, Stan,Villase?or, Armando G.,Paul, Amber,Su, Guoping,Heilek, Gabrielle,Hang, Julie Q.,Zhou, Amy S.,Jernelius, Jesper A.,Zang, Fang-Jie,Klumpp, Klaus
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experimental part
p. 7449 - 7458
(2010/01/21)
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- Non-nucleoside reverse transcriptase inhibitors
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The present invention provides for compounds useful for treating an HIV-1 infection, or preventing an HIV-1 infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, R5 and X are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds. [image]
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Page/Page column 22
(2008/06/13)
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- Non-nucleoside reverse transcriptase inhibitors
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The present invention provides compounds for treating or preventing an HIV infection, or treating AIDS or ARC comprising administering a compound according to formula I where Ar, R1-R5, R7a, R7b, R7c, R8-R10, X1, X2 m, n, o and p are as defined herein.
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Page/Page column 42
(2008/06/13)
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- Process for preparing pyridazinone compounds
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The present invention provides a process for the preparation 6-[3-(hetero)aryloxy-2-fluoro-benzyl]-2H-pyridazin-3-one compounds 1 where R2 is an optionally substituted aryl or an optionally substituted heteroaryl, R6 is NO2, NH2, alkyl, halogen, or a function group readily derived therefrom and R4c is hydrogen or alkyl. There also is provided a process for the preparation of phenylacetic acid compounds 2, wherein R2 and R6 are as defined previously and R5a is hydrogen or alkyl, which are useful for the preparation of pyridazinone compounds.
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Page/Page column 17
(2008/06/13)
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- Non-nucleoside reverse transcriptase inhibitors
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This invention relates to novel pyridazinone derivatives of formula I wherein R1-R4, R7, R8 and X1 are as defined in the summary and pharmaceutically acceptable salts and solvates thereof, methods to inhibit or modulate Human Immunodeficiency Virus (HIV) reverse transcriptase with compounds of formula I, pharmaceutical compositions containing of formula I admixed with at least one solvent, carrier or excipient and processes to prepare compounds of formula I. The compounds are useful for treating disorders in which HIV and genetically related viruses are implicated
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Page/Page column 85
(2010/02/08)
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