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1. 发明申请

US20150320762A1 TREATMENT OF PROLIFERATIVE DISEASES WITH PYRIMIDODIAZEPINONES 审中-公开
标题翻译：用吡咯烷酮治疗增殖性疾病
公开(公告)号：US20150320762A1
公开(公告)日：2015-11-12
申请号：US14387963
申请日：2013-03-28
申请人： Cyclacel limited
发明人： Susan DAVIS , Daniella I. ZHELEVA
IPC分类号： A61K31/551 , A61K9/00
CPC分类号： A61K9/0019 , A61K31/551
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 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.
摘要翻译：本发明的第一方面涉及用于治疗增殖性疾病的式（I）化合物或其药学上可接受的盐，其中：X为NR7; R1和R2各自独立地为H，烷基或环烷基; R3是选自哌啶基，哌嗪基，吗啉基和四氢吡喃基的6元杂环烷基，其中所述杂环烷基任选进一步被一个或多个（CH 2）R 19基团取代; R4和R4'各自独立地为H或烷基; 或R 4和R 4'一起形成螺环烷基; Q是CH或N; R6为OR8或卤素; n为1,2或3; R19是H，烷基，芳基或环烷基; R 7和R 8各自独立地为H或烷基; 并且其中所述化合物根据给药方案给药，所述给药方案：（i）维持约50至约500nM的血浆浓度达约16小时; 或（ii）维持约0.5μM至约1μM的血浆浓度达约6小时; 或（iii）在约6小时内达到不超过约500nM的最大血浆浓度（C max）; 或（iv）在约16小时内达到不大于约200nM的最大血浆浓度（C max）; 或（v）在约6小时内达到约0.5μM至约1μM的最大血浆浓度（C max）。进一步的权利要求涉及基于该给药方案的治疗方法和与其相关的试剂盒。

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