- Structure-based Design of Pyridone-Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition
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Dysregulated translation of mRNA plays a major role in tumorigenesis. Mitogen-activated protein kinase interacting kinases (MNK)1/2 are key regulators of mRNA translation integrating signals from oncogenic and immune signaling pathways through phosphoryla
- Reich, Siegfried H.,Sprengeler, Paul A.,Chiang, Gary G.,Appleman, James R.,Chen, Joan,Clarine, Jeff,Eam, Boreth,Ernst, Justin T.,Han, Qing,Goel, Vikas K.,Han, Edward Z. R.,Huang, Vera,Hung, Ivy N. J.,Jemison, Adrianna,Jessen, Katti A.,Molter, Jolene,Murphy, Douglas,Neal, Melissa,Parker, Gregory S.,Shaghafi, Michael,Sperry, Samuel,Staunton, Jocelyn,Stumpf, Craig R.,Thompson, Peggy A.,Tran, Chinh,Webber, Stephen E.,Wegerski, Christopher J.,Zheng, Hong,Webster, Kevin R.
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p. 3516 - 3540
(2018/05/01)
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- Isoindoline, azaisoindoline, dihydroindenone and dihydroazaindenone inhibitors of Mnk1 and Mnk2
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The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. For Formula I compounds A1, A2
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Page/Page column 44
(2018/11/21)
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- ANTI-ANGIOGENESIS COMPOUND, INTERMEDIATE AND USE THEREOF
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Disclosed are an anti-abnormal proliferation of angiogenesis compound represented by formula I, use and intermediate thereof. The compound has good effect against abnormal proliferation of angiogenesis, and the activity of the compound is produced by inhibiting VEGFR2. The compound can be used for treating diseases, such as wet macular degeneration, inflammation, malignant tumor and the like, caused by abnormity of angiogenesis and protein kinases such as VEGFR2, FGFR2 and the like.
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Paragraph 0076; 0077
(2016/04/10)
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- ANTI-ANGIOGENESIS COMPOUND, INTERMEDIATE AND USE THEREOF
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Disclosed are an anti-abnormal proliferation of angiogenesis compound represented by formula I, use and intermediate thereof. The compound has good effect against abnormal proliferation of angiogenesis, and the activity of the compound is produced by inhibiting VEGFR2. The compound can be used for treating diseases, such as wet macular degeneration, inflammation, malignant tumor and the like, caused by abnormity of angiogenesis and protein kinases such as VEGFR2, FGFR2 and the like.
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Paragraph 0093; 0096-0098
(2016/11/02)
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- Α 7 as intranuclear hydroxynicotinic acetylcholine receptor quinuclidines compd.
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PROBLEM TO BE SOLVED: To provide ligands for the nicotinic α-7 receptor used for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.SOLUTION: The disclosure provides compounds of the specified formula I, including their salts, and compositions and methods using the compounds.
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Paragraph 0653; 0654
(2018/10/03)
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- HETEROCYCLIC COMPOUND
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The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
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Paragraph 0673
(2015/01/18)
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- PYRAZOLOPYRIDINES AND PYRAZOLOPYRIDINES AND THEIR USE AS TYK2 INHIBITORS
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The invention provides compounds of Formula (I), stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula (I) and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy, as TYK2 Kinase inhibitors.
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Page/Page column 174
(2012/06/01)
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- Two-level self-organisation of arrays of [2x2] grid-type tetranuclear metal complexes by hydrogen bonding
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Here we report on the synthesis and characterisation of four new complexes of the [2x2] M4II grid-type (M = Co, Fe, Zn) with oligopyridine-derived ligands. The presence of aminopyrazine and aminopyrimidine moieties at the edge of the ligands potentially enables the formation of infinite hydrogen-bonded multi-grid networks. The ligands were synthesised by subsequent stannylations and Stille-type coupling reactions. The complexes were obtained by self-assembly of the ligand with the metal salt. The single-crystal X-ray structure was determined for the Co complex 7 containing aminopyrimidine as the hydrogen-bonding moiety [P1; a = 15.4976(4), b = 18.2114(6), c = 31.9538(10) A, α = 86.9809(13), β = 83.4137(18), γ = 67.2828(16)°]. The crystal structure reveals hydrogen bonding in one direction, thus forming infinite chains of grids, whereas in the second direction of a layer, only weak attractive interactions are found. Anions and solvent molecules are situated between the layers, thus inhibiting any direct interaction between them. Cocrystallisation of the complementary complexes should enable the recognition-controlled alternating arrangement of grids incorporating different metal ions in a chessboard-like manner. Wiley-VCH Verlag GmbH, 2001.
- Breuning, Esther,Ziener, Ulrich,Lehn, Jean-Marie,Wegelius, Elina,Rissanen, Kari
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p. 1515 - 1521
(2007/10/03)
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