100256-33-5Relevant academic research and scientific papers
PROCESS FOR PREPARING 2,6-DIALKYLPHENYLACETIC ACIDS
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, (2022/01/04)
The invention relates to a multi-stage process for preparing 2,6-dialkylphenylacetic acids of the general formula (I) by reacting 2,6-dialkylbromobenzenes with (1) magnesium, (2) a formamide, (3) an acid, (4) hydrogenation of the benzaldehyde obtained, (5
Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides
Laufer, Radoslaw,Ng, Grace,Liu, Yong,Patel, Narendra Kumar B.,Edwards, Louise G.,Lang, Yunhui,Li, Sze-Wan,Feher, Miklos,Awrey, Don E.,Leung, Genie,Beletskaya, Irina,Plotnikova, Olga,Mason, Jacqueline M.,Hodgson, Richard,Wei, Xin,Mao, Guodong,Luo, Xunyi,Huang, Ping,Green, Erin,Kiarash, Reza,Lin, Dan Chi-Chia,Harris-Brandts, Marees,Ban, Fuqiang,Nadeem, Vincent,Mak, Tak W.,Pan, Guohua J.,Qiu, Wei,Chirgadze, Nickolay Y.,Pauls, Henry W.
, p. 4968 - 4997 (2014/10/16)
TTK kinase was identified by in-house siRNA screen and pursued as a tractable, novel target for cancer treatment. A screening campaign and systematic optimization, supported by computer modeling led to an indazole core with key sulfamoylphenyl and acetamido moieties at positions 3 and 5, respectively, establishing a novel chemical class culminating in identification of 72 (CFI-400936). This potent inhibitor of TTK (IC50 = 3.6 nM) demonstrated good activity in cell based assay and selectivity against a panel of human kinases. A co-complex TTK X-ray crystal structure and results of a xenograft study with TTK inhibitors from this class are described.
KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME
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Page/Page column 80, (2011/10/31)
The present teachings provide a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Also described are a pharmaceutical composition and method of use thereof.
Aryldiones incorporating a [1,4,5]oxadiazepane ring. Part I: Discovery of the novel cereal herbicide pinoxaden
Muehlebach, Michel,Boeger, Manfred,Cederbaum, Fredrik,Cornes, Derek,Friedmann, Adrian A.,Glock, Jutta,Niderman, Thierry,Stoller, Andre,Wagner, Trixie
experimental part, p. 4241 - 4256 (2009/10/02)
Derivatives of the new class of 3-hydroxy-4-phenyl-5-oxo-pyrazolines were optimized towards both herbicidal activity on key annual grass weed species and selectivity in small grain cereal crops. The generic structure can be separated into three parts for the analysis of the structure-activity relationships, namely the aryl, the dione with its prodrug forms and the hydrazine moiety. Each area appears to play distinct and different roles in overall expression of biological performance which is further beneficially influenced by adjuvant response and safener action. Pinoxaden 6, a novel graminicide for use in wheat and barley incorporating a [1,4,5]oxadiazepane ring, eventually emerged as a development candidate from the discovery and optimization process.
C2-phenyl-substituted cyclic keto-enols used as pesticides and herbicides
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Page/Page column 65, (2010/11/30)
The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y, Z and CKE are as defined in the description, to processes for their preparation and to their use as pesticides and herbicides.
