发明名称 TREATMENT OF PROLIFERATIVE DISEASES WITH PYRIMIDODIAZEPINONES
摘要 A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, for use in treating a proliferative disorder, wherein: X is NR7; R1 and R2 are each independently H, alkyl or cycloalkyl; R3 is a 6-membered heterocycloalkyi group selected from piperidinyl, piperazinyl, morpholinyl and tetrahydropyranyl, wherein said heterocycloalkyi group is optionally further substituted by one or more (CH2)nR19 groups; R4 and R4' are each independently H or alkyl; or R4 and R4' together form a spiro cycloalkyl group; Q is CH or N; R6 is OR8 or halogen; n is 1, 2 or 3; R19 is H, alkyl, aryl or a cycloalkyl group; R7 and R8 are each independently H or alkyl; and wherein said compound is administered in accordance with a dosing regimen which: (i) maintains a plasma concentration of from about 50 to about 500 nM for a period of up to about 16 hours; or (ii) maintains a plasma concentration of from about 0.5 muMu to about 1 muMu for a period of up to about 6 hours; or (iii) achieves a maximum plasma concentration (Cmax) of no more than about 500 nM within a period of about 6 hours; or (iv) achieves a maximum plasma concentration (Cmax) of no more than about 200 nM within a period of about 16 hours; or (v) achieves a maximum plasma concentration (Cmax) of about 0.5 muMu to about 1 muMu within about 6 hours. Further claims relate to a method of treatment based on this dosing regimen, and kits relating to the same.
申请公布号 WO2013144632(A1) 申请公布日期 2013.10.03
申请号 WO2013GB50816 申请日期 2013.03.28
申请人 CYCLACEL LIMITED 发明人 DAVIS, SUSAN;ZHELEVA, DANIELLA
分类号 A61K9/00;A61K31/551;A61K31/5513 主分类号 A61K9/00
代理机构 代理人
主权项
地址