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1. 发明授权

US10927113B2 Process for preparing purine derivatives 有权
公开(公告)号：US10927113B2
公开(公告)日：2021-02-23
申请号：US16480858
申请日：2018-01-25
申请人： Cyclacel Limited
发明人： Benjamin Mark Skead , Robert Westwood , Derek Londesbrough , Julian Scott Northen , Jonathan Charles Christian Atherton
IPC分类号： C07D473/16 , C07D473/40
摘要： The present invention relates to a process for preparing a compound of formula [I], said process comprising the steps of: formula [II]+formula [III]→formula [I] (i) forming a reaction mixture comprising (a) a compound of formula [II], (b) a compound of formula [III] and (c) 1,2-propanediol or polyethylene glycol, or a mixture thereof, and optionally (d) a base; (ii) heating said reaction mixture to a temperature of at least about 150° C. to form a compound of formula [I]; (iii) isolating said compound of formula [I]; and (iv) optionally converting said compound of formula [I] into salt form; wherein: R1 and R2 are each independently H, alkyl or haloalkyl; R3 and R4 are each independently H, alkyl, haloalkyl or aryl; R5 is alkyl, alkenyl, cycloalkyl or cycloalkyl-alkyl, each of which may be optionally substituted with one or more OH groups; R6 is selected from cyclopropylamino, cyclopropylmethylamino, cyclobutylamino, cyclobutylmethylamino and formula (A) where one of X, Y and Z is N and the remainder are CR9; R7, R8 and each R9 are independently H, alkyl or haloalkyl, wherein at least one of R7, R8 and R9 is other than H. Further aspects of the invention relate to a highly diastereoselective process for the preparation of compounds of formula [III], a process for preparing intermediates of formula [II], and other intermediates useful in the synthesis of compounds of formula [I], and to a process for preparing the crystalline tartrate salt and free base of compounds of formula [I].

2. 发明授权

US09573951B2 Crystalline forms of a purine derivative 有权
标题翻译：嘌呤衍生物的结晶形式
公开(公告)号：US09573951B2
公开(公告)日：2017-02-21
申请号：US14524686
申请日：2014-10-27
申请人： Cyclacel Limited
发明人： Benjamin Mark Skead , Christopher Peter Worrall , Jonathan Charles Christian Atherton , Julian Scott Northen , Philippe Fernandes
IPC分类号： C07D473/00 , C07D473/16 , G01F1/115 , G01P3/48 , G01P5/07 , A61K31/52 , C07C51/41 , C07C57/145 , C07C57/15 , C07C59/245 , C07C59/255 , C07C59/265 , C07C65/05 , C07C303/32 , C07C309/04 , C07C309/29
CPC分类号： C07D473/16 , A61K31/52 , C07B2200/13 , C07C51/412 , C07C57/145 , C07C57/15 , C07C59/245 , C07C59/255 , C07C59/265 , C07C65/05 , C07C303/32 , C07C309/04 , C07C309/29 , G01F1/115 , G01P3/4802 , G01P5/07
摘要： The present invention relates to new crystalline forms of a purine derivative which exhibits excellent anti-tumor activity. The invention also relates to a pharmaceutical composition containing said crystalline forms as an active ingredient, and use thereof in the prevention or treatment of disease. The invention further relates to a process for preparing the crystalline forms.
摘要翻译：本发明涉及嘌呤衍生物的新结晶形式，其具有优异的抗肿瘤活性。本发明还涉及含有所述结晶形式作为活性成分的药物组合物及其在预防或治疗疾病中的用途。本发明还涉及制备结晶形式的方法。

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