4377-58-6Relevant articles and documents
INHIBITOR OF CASEIN KINASE 1DELTA AND CASEIN KINASE 1E
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, (2013/06/05)
There is provided a novel oxazolone derivative having inhibitory activity against casein kinase 1δ and casein kinase 1ε. In addition, the present inhibitor inhibits casein kinase 1δ and casein kinase 1ε, and thus there is also provided a pharmaceutical agent useful for the treatment and/or prevention of diseases, with the pathological conditions of which the activation mechanism of casein kinase 1δ or casein kinase 1ε is associated. There is further provided a pharmaceutical agent useful for the treatment of particularly, circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer. An inhibitor of casein kinase 1δ and casein kinase 1ε comprising, as an act ingredient, an oxazolone derivative represented by the following general formula (1), a salt thereof, a solvate thereof, or a hydrate thereof: wherein X represents a halogen atom (which may be any one of a fluorine atom, a chlorine atom, a bromine atom, and an iodine atom).
Processes and intermediates for preparing 2-fluorothiophene derivatives
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, (2008/06/13)
A process for the preparation of the compound of the formula: wherein R1 is OH, which comprises the steps of a) treating the compound of the formula: with an inorganic fluoride, of the formula M2F wherein M2 is an alkali metal cation, at an elevated temperature in the presence of a compound of the formula R4P+Z- and a compound of the formula R5vic (COW)2 wherein R4 and R5 are each selected from optionally substituted (C6-C10) aryl and optionally substituted (C1-C6) alkyl, and W is halo; to form the compound of the formula: and b) I) treating the compound of the formula IV with an aqueous solution of a base, of the formula MOH, wherein M is an alkali metal cation, and ii) treating the product of step i) with a mineral acid. A compound of the formula: wherein R1 is selected from the group consisting of, halo, R7O, R7COO and N(R8)2 wherein R7 is (C1-C6)alkyl or (C6-C10)aryl and each R8 is selected from hydrogen and R7 with the proviso that R7 is not methyl when R1 is R7O.