- NOVEL IMIDAZO-PYRAZINE DERIVATIVES
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The invention provides novel imidazo-pyrazine derivatives having the general formula (I), and pharmaceutically acceptable salts thereof, wherein X, m, n, and R1to R3 are as described herein: formula (I). Further provided are pharmace
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- 3. 4 - diphenyl - 4H - 1, 2, 4 - triazole derivative and its preparation method and application (by machine translation)
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The invention discloses 3, 4 - diphenyl - 4H - 1, 2, 4 - triazole derivative and its preparation method and application. In particular, the invention relates to the formula (I) structure of 3, 4 - diphenyl - 4H - 1, 2, 4 - triazole derivatives, its stereoisomers or its pharmaceutically acceptable salt, formula (I) in the definition of each substituent is as defined in the specification. These structure of novel compound with heat shock protein HSP90 inhibitory activity, can be used for treating cancer, neurodegenerative diseases, inflammatory diseases, autoimmune diseases, ischemic brain injury and the like, it has broad application prospects. (by machine translation)
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- Triazole derivative having HSP90 (Heat Shock Protein) inhibiting activity, as well as preparation method and application of triazole derivative
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The invention discloses a triazole derivative having an HSP90 (Heat Shock Protein) inhibiting activity, as well as a preparation method and an application of the triazole derivative. Specifically, the invention relates to the triazole derivative having a structure as shown in a formula (I), a stereisomer of the triazole derivative and a pharmaceutically acceptable salt, wherein the definition of each substituent group in the formula (I) and the definition in a description are the same. The compound with a novel structure has the HSP90 inhibiting activity, can be used to cure cancers, neurodegenerative disorders, inflammation diseases, autoimmune diseases, ischemic brain injuries and the like, and has a broad application prospect.
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- Fused bicyclic derivatives of 2,4-diaminopyrimidine as c-Met inhibitors
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The HGF-c-Met signaling axis is an important paracrine mediator of epithelial-mesenchymal cell interactions involving the regulation of multiple cellular activities including cell motility, mitogenesis, morphogenesis, and angiogenesis. Dysregulation of c-Met signaling (e.g., overexpression or increased activation) is associated with the development of a wide range of tumor types; thus, inhibiting the HGF-c-Met pathway is predicted to lead to anti-tumor effects in many cancers. Elaboration of a 2-arylaminopyrimidine scaffold led to a series of potent c-Met inhibitors bearing a C4-2-amino-N-methylbenzamide group. Specifically, a series of C2-benzazepinone analogs demonstrated potent inhibition of c-Met in enzymatic and cellular assays. Kinase selectivity could be tuned by varying the nature of the alkyl group on the benzazepinone nitrogen.
- Weinberg, Linda R.,Albom, Mark S.,Angeles, Thelma S.,Husten, Jean,Lisko, Joseph G.,McHugh, Robert J.,Milkiewicz, Karen L.,Murthy, Seetha,Ott, Gregory R.,Theroff, Jay P.,Tripathy, Rabindranath,Underiner, Ted L.,Zificsak, Craig A.,Dorsey, Bruce D.
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p. 164 - 167
(2011/03/17)
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- 1-Benzazepine-3-Sulfonylamino-2-Pyrroridones as Factor Xa Inhibitors
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The invention relates to chemical entities of formula (I): and/or pharmaceutically acceptable derivative(s) thereof. The invention also relates to processes for the preparation of compounds of formula (I), pharmaceutical compositions containing compounds
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Page/Page column 13
(2009/01/20)
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- OXAZOLIDINONE DERIVATES N-SUBSTITUTED BY A TRICYCLIC RING, FOR USE AS ANTIBACTERIAL AGENTS
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Compounds of formula (I) and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula (I) as well as pharmaceutically acceptable compositions comprising compounds of formula (I). Compounds of formula (I) as disclosed herein can be used in a variety of applications including use as antibacterial P is a tricyclic ring system as defined in claiml.
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Page/Page column 95-96
(2010/02/08)
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- Synthesis of 7-mercapto-2,3,4,5-tetrahydro-1H-1-benzazepin-2-one
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The synthesis of 7-mercapto-2,3,4,5-tetrahydro-1H-1-benzazepin-2-one - a potential monomer for preparing network polymers - is reported.
- Osadchii, S. A.,Kochubei, N. V.
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p. 1674 - 1676
(2007/10/03)
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- Lipoxygenase Inhibitors, III: Synthesis of Tetrahydrobenzazepinone Phenylhydrazones
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Tetrahydro-2H-benzazepin-2-ones as starting substances are synthesized by Beckmann rearrangement or Schmidt reaction.The tetrahydrobenzazepinones are transformed into the thiones, thiolactim ethers and phenylhydrazones.The compounds are tested as inhibitors of soja lipoxygenase.
- Buege, Axel,Locke, Christian,Koehler, Thomas,Nuhn, Peter
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