TREATMENT OF PROLIFERATIVE DISEASES WITH PYRIMIDODIAZEPINONES

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United States of America Patent

APP PUB NO 20150320762A1
SERIAL NO

14387963

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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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 heterocycloalkyl group selected from piperidinyl, piperazinyl, morpholinyl and tetrahydropyranyl, wherein said heterocycloalkyl group is optionally further substituted by one or more (CH2)—R19 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 μM to about 1 μM 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 μM to about 1 μM within about 6 hours. Further claims relate to a method of treatment based on this dosing regimen, and kits relating to the same.

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Patent Owner(s)

Patent OwnerAddress
CYCLACEL LIMITEDLONDON EC2Y 5AU

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
DAVIS, Susan Angus, GB 14 45
ZHELEVA, Daniella I Fife, GB 12 102

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