- SUBSTITUTED PYRAZOLE COMPOUNDS AS TOLL RECEPTOR INHIBITORS
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Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein G, A, R1, and R5 are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
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- DUAL KINASE-BROMODOMAIN INHIBITORS
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Provided herein are compounds of Formula (I) that are dual inhibitors of kinases and bromo-domain proteins. The disclosure also relates to pharmaceutical compositions containing such compounds, methods for using such compounds in the treatment of cancers, particularly, the treatment of multiple myeloma cancers, and to related uses.
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- PHARMACEUTICALLY ACTIVE COMPOUNDS
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The invention is directed to compounds of general formula (I), and pharmaceutical compositions containing such compounds. The compounds and compositions have valuable pharmaceutical properties. In particular, they may be used for the treatment of cancer. Novel intermediates and novel methods of preparation are also disclosed.
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- Substituted Benzo-Imidazo-Pyrido-Diazepine Compounds
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The present invention relates to substituted benzo-imidazo-pyrido-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-imidazo-pyrido-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
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Page/Page column 112
(2012/05/07)
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- Protective Agent for Retinal Neuronal Cell Comprising Indazole Derivative as Active Ingredient
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As a result of intensive studies for the purpose of finding a new medicinal use of an indazole derivative, it was found that an indazole derivative inhibits glutamate-induced retinal neuronal cell death in rat fetal retinal neuronal cells, in other words, the indazole derivative acts directly on the retinal neuronal cells and exhibits an effect of protecting retinal neuronal cells. Accordingly, the indazole derivative is useful for the prevention or treatment of an eye disease associated with retinal neuronal cell damage or retinal damage.
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Page/Page column 7
(2009/01/23)
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- PROTECTIVE AGENT FOR RETINAL NEURONAL CELL COMPRISING INDAZOLE DERIVATIVE AS ACTIVE INGREDIENT
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As a result of intensive studies for the purpose of finding a new medicinal use of an indazole derivative, it was found that an indazole derivative inhibits glutamate-induced retinal neuronal cell death in rat fetal retinal neuronal cells, in other words, the indazole derivative acts directly on the retinal neuronal cells and exhibits an effect of protecting retinal neuronal cells. Accordingly, the indazole derivative is useful for the prevention or treatment of an eye disease associated with retinal neuronal cell damage or retinal damage.
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Page/Page column 10
(2010/11/29)
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- Synthesis and biological study of 2-amino-4-aryl-5-chloropyrimidine analogues as inhibitors of VEGFR-2 and cyclin dependent kinase 1 (CDK1)
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The series of 2-amino-4-aryl-5-chloropyrimidines was discovered to be potent for both VEGFR-2 and CDK1. Described here are the chemistry for analogue synthesis, SAR study, and its kinase selectivity prolifing. The full rat PK data and in vivo efficacy stu
- Huang, Shenlin,Li, Ronghua,Connolly, Peter J.,Emanuel, Stuart,Fuentes-Pesquera, Angel,Adams, Mary,Gruninger, Robert H.,Seraj, Jabed,Middleton, Steven A.,Davis, Jeremy M.,Moffat, David F.C.
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p. 2179 - 2183
(2008/02/01)
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- NOVEL INDAZOLE DERIVATIVE
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An object of the present invention is to create a novel indazole derivative useful as a drug and to find a novel pharmacological action of the derivative. The compound of the present invention is represented by the formula [I] and has an excellent Rho kinase inhibiting action. In the formula, a ring X is a benzene ring or a pyridine ring; R1 and R2 are H or alkyl; R3 and R4 are halogen, H, OH, alkoxy, alkenyloxy, alkynyloxy, cycloalkyloxy, cycloalkenyloxy, aryloxy, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, carboxy, hydrocarbonyl, alkylcarbonyl, etc.; and R5 is halogen atom, H, OH, alkoxy, aryloxy, alkyl or aryl. Each group can be substituted.
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Page/Page column 33
(2008/06/13)
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- 4,5-disubstituted-2-aminopyrimidines
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Pyrimidines of formla (1) are described: wherein R1is a —XR6group; R2and R3which may be the same or different is each a hydrogen or halogen atom or a group selected from an optionally substituted aliphatic, cycl
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