- HETEROCYCLIC DERIVATIVES AND USE THEREOF
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A heterocyclic derivative represented by formula (I), or a pharmaceutically acceptable salt or a stereoisomer thereof, which has an inhibitory effect on the activation of STAT3 protein, and is useful for the prevention or treatment of diseases associated with the activation of STAT3 protein.
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Page/Page column 130
(2015/01/06)
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- New Pharmaceutical Compounds
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Compounds of formula I, wherein A and R1-R7, are as defined in the claims, exhibit TRPA1 activity and are thus useful as TRPA1 modulators.
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Page/Page column 17
(2012/12/13)
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- PHENYL- SULFONYL DERIVATIVES AS MEDIATORS OF TRPA1 RECEPTOR ACTIVITY FOR THE TREATMENT OF PAIN
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Compounds of formula I, wherein A and R1-R7, are as defined in the claims, exhibit TRPA1 activity and useful as TRPA1 modulators.
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Page/Page column 32-33
(2012/12/13)
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- NUCLEAR TRANSPORT MODULATIORS AND USES THEREOF
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The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g
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Page/Page column 115-116
(2011/10/03)
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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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Page/Page column 39
(2009/01/23)
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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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Page/Page column 37
(2009/01/23)
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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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Page/Page column 57
(2009/01/24)
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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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- Non-nucleoside reverse transcriptase inhibitors
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Compounds of formula I, wherein R1, R2, R3, R4, Ra, X, X1, and Y 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 15
(2009/01/20)
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- Non-nucleoside reverse transcriptase inhibitors
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Compounds of formula I, wherein R1, R2, R3, R4, R5, X, Y, 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
(2008/12/08)
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- NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
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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.
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Page/Page column 29-30
(2009/01/20)
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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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- 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 16
(2008/06/13)
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- PYRAZOLE AMIDES FOR TREATING HIV INFECTIONS
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This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereof, wherein R' to R4, n W, X and Y are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful ín the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
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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 84; 85
(2010/02/08)
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- PYRAZOLE DERIVATIVES
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This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereof, wherein R1 to R4, n W, X and Y are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
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- Pyrazole derivatives
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This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivatives thereof, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such, the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
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