- Novel(1,2,4)triazolo(1,5-a)pyridylphosphine oxide and use thereof
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The present invention relates to novel(1,2,4)triazolo(1,5-a)pyridinyl phosphorus oxides and uses thereof. Wherein the compound is a compound represented by a formula I, or a pharmaceutically acceptable salt thereof, or a hydrate thereof, or a solvate thereof, or a metabolite thereof, or a stereoisomer thereof, or a tautomer thereof, or a prodrug thereof, and R1 to R5 are as defined in the specification. The compound disclosed by the invention can be used for preparing a medicine for treating and/or preventing cancers.
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Paragraph 0055; 0058; 0061-0062
(2020/07/24)
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- Tyrosine Kinase Inhibitor And Uses Thereof
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Disclosed is a compound of Formula (I) or a pharmaceutically acceptable salt, ester, or solvate thereof, or their stereoisomers, which can be used as tyrosine kinase inhibitor. Also disclosed is a method for preparing the compound, a pharmaceutical composition and a kit comprising the compound, and uses of the compound. The compound can be used as tyrosine kinase inhibitor, or can be used to reduce or inhibit activity of EGFR or mutant thereof, such as EGFR mutant comprising T790M mutation, in a cell, or to treat and/or prevent a disease associated with overactivity of EGFR, such as cancer.
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Paragraph 0663-0664
(2017/05/15)
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- CHEMICAL COMPOUNDS
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The present invention relates to compounds of Formula (I) and/or Formula (Ia): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit ALK kinase activity, and thus may be used for the tr
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Page/Page column 25
(2012/02/06)
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- THIAZOLE SULFONAMIDE AND OXAZOLE SULFONAMIDE KINASE INHIBITORS
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The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents
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Page/Page column 108
(2010/10/03)
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- 2- [ (2-{PHENYLAMINO}-1H-PYRROLO [2, 3-D] PYRIMIDIN-4-YL) AMINO] BENZAMIDE DERIVATIVES AS IGF-1R INHIBITORS FOR THE TREATMENT OF CANCER
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Novel pyrrolopyrimidines as shown in formula (I) and pharmaceutically acceptable derivatives thereof. The compounds are useful in the inhibition of IGF-1R.
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Page/Page column 142-143
(2009/04/25)
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- Imidazopyridine Kinase Inhibitors
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The present invention provides imidazopyridine compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
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Page/Page column 122
(2009/01/20)
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- Design and synthesis of highly potent and selective (2-arylcarbamoyl- phenoxy)-acetic acid inhibitors of aldose reductase for treatment of chronic diabetic complications
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Recent efforts to identify treatments for chronic diabetic complications have resulted in the discovery of a novel series of highly potent and selective (2-arylcarbamoyl-phenoxy)-acetic acid aldose reductase inhibitors. The compound class features a core template that utilizes an intramolecular hydrogen bond to position the key structural elements of the pharmacophore in a conformation, which promotes a high binding affinity. The lead candidate, example 40, 5-fluoro-2-(4-bromo-2-fluoro-benzylthiocarbamoyl)-phenoxyacetic acid, inhibits aldose reductase with an IC50 of 30 nM, while being 1100 times less active against aldehyde reductase, a related enzyme involved in the detoxification of reactive aldehydes. In addition, example 40 lowers nerve sorbitol levels with an ED50 of 31 mg/kg/d po in the 4-day STZ-induced diabetic rat model.
- Van Zandt, Michael C.,Sibley, Evelyn O.,McCann, Erin E.,Combs, Kerry J.,Flam, Brenda,Sawicki, Diane R.,Sabetta, Al,Carrington, Anne,Sredy, Janet,Howard, Eduardo,Mitschler, Andre,Podjarny, Alberto D.
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p. 5661 - 5675
(2007/10/03)
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- Substituted phenoxyacetic acids
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Disclosed are substituted phenoxyacetic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds, alone or in combination with other therapeutic agents, and methods of treatment employing the compounds and pharmaceutical compositions, as well as methods for their synthesis.
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