- INHIBITORS OF NOTCH SIGNALLING PATHWAY AND USE THEREOF IN TREATMENT OF CANCERS
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The present invention relates to new inhibitors of Notch signalling pathway and its use in the treatment and/or prevention of cancers.
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Page/Page column 152
(2020/10/21)
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- COMPOUNDS FOR THE TREATMENT OF ONCOVIRUS INDUCED CANCER AND METHODS OF USE THEREOF
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The pesent invention relates to compounds of formula (I) pharmaceutically-acceptable salts, hydrates, solvates, or stereoisomers thereof and their use for the prevention and treatment of oncovirus induced cancer in a subject.
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Page/Page column 129-130
(2020/10/21)
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- MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE
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Provided are IDO inhibitor compounds of Formula I and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases. Formula (I):
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Page/Page column 86
(2019/01/17)
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- 1,4-THIAZINE DIOXIDE AND 1,2,4-THIADIAZINE DIOXIDE DERIVATIVES AS BETA-SECRETASE INHIBITORS AND METHODS OF USE
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The present disclosure provides a class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A, X, R2, R2', R3, R4, R5, R6, and R7 of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Aβ plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, and other central nervous system conditions.
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Page/Page column 280
(2018/07/05)
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- Substituted pyridine and pyrimidine derivatives and their use in treating viral infections
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The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.
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Page/Page column 148; 149; 150
(2016/09/26)
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- SUBSTITUTED PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE IN TREATING VIRAL INFECTIONS
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The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.
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Page/Page column 174-175
(2010/04/03)
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- SUBSTITUTED HYDROXYETHYL AMINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE
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The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1a, R1b, R1c, B, W, R3, R4 and R5 are defined herein. In another embodiment, the invention provides compounds of general Formula II wherein A1, A2, A3, A4, R1a, R1b, R1c, R2, R4, R5, W, X and Z are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formula II, intermediates and processes useful for the preparation of compounds of Formulas I and II.
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Page/Page column 124
(2009/01/20)
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- SUBSTITUTED HYDROXYETHYL AMINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE
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The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I or Formula II wherein RIa, RIb, RIc, B, R3, R4, R5 and W of Formula I, and RIa, RIb, RIc, R2, R2a, R3, R4, R5, R6, Al, A2, A3, A4, W, X, Z, m and n of Formula II are defined herein.
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Page/Page column 212-213
(2009/01/20)
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- HETEROCYCLE-SUBSTITUTED BENZIMIDAZOLE DERIVATIVE
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Compounds having glucokinase activating effects and being useful as treatments for diabetes, which are represented by the following formula (I): (wherein X1 to X4 represent a carbon atom, etc., ring A represents a 5- or 6-membered heteroaryl having from 1 to 4 hetero atoms selected from the group consisting of a nitrogen atom, a sulfur atom and an oxygen atom, X5 represent an oxygen atom, etc., X represent a carbon atom, etc., Het represents a 5- or 6-membered aliphatic hetero ring, R1 represents aryl, etc., R2 represents formyl, etc., R3 represents -C1-6 alkyl, etc.), as well as their pharmaceutically acceptable salts.
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Page/Page column 58
(2010/11/30)
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- BETA-SECRETASE MODULATORS AND METHODS OF USE
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The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula (I), methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula (I), or compositions including them, to a subject. The invention also comprises further embodiments of Formulas (II) and (III), intermediates and processes useful for the preparation of compounds of the invention.
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Page/Page column 121-122
(2010/11/27)
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