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filingDate 2013-03-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2015-05-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber JP-2015514703-A
titleOfInvention Treatment of proliferative diseases with pyrimidodiazepinone
abstract A first aspect of the invention is a compound of formula (I) or a pharmaceutically acceptable salt thereof for use in the treatment of a proliferative disorder, wherein X is NR 7 ; R 1 and R 2 are each independently H, alkyl, or cycloalkyl; R 3 is a 6-membered heterocycloalkyl group selected from piperidinyl, piperazinyl, morpholinyl, and tetrahydropyranyl, and the heterocycloalkyl The group may be further substituted with one or more (CH 2 ) n R 19 groups; R 4 and R 4 ′ are each independently H or alkyl; or R 4 and R 4 ′ Together form a spirocycloalkyl group; Q is CH or N; R 6 is OR 8 or halogen; n is 1, 2, or 3; R 19 is H, alkyl, a Lumpur, or cycloalkyl group; the R 7 and R 8 are each independently H or alkyl; wherein the compound is administered in accordance with the following dosing regimen, compound, or a pharmaceutically tolerated for the use (I) maintaining a plasma concentration of about 50 to about 500 nM for a period of up to about 16 hours; or (ii) maintaining a plasma concentration of about 0.5 μM to about 1 μM for a period of up to about 6 hours. Or (iii) achieving a maximum plasma concentration (Cmax) of about 500 nM or less in a period of about 6 hours; or (iv) a maximum plasma concentration (Cmax) of about 200 nM or less of a period of about 16 hours or less. Or (v) achieve a maximum plasma concentration (Cmax) of about 0.5 μM to about 1 μM within about 6 hours. Further claims relate to methods of treatment based on this dosing regimen and kits related thereto. [Chemical 1] (I)
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priorityDate 2012-03-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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