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1. 发明授权

US08592581B2 Trisubstituted purine derivatives 有权
标题翻译：三取代嘌呤衍生物
公开(公告)号：US08592581B2
公开(公告)日：2013-11-26
申请号：US12573337
申请日：2009-10-05
申请人： Peter William Sheldrake , Butrus Atrash , Simon Green , Edward McDonald , Sheelagh Frame
发明人： Peter William Sheldrake , Butrus Atrash , Simon Green , Edward McDonald , Sheelagh Frame
IPC分类号： A61K31/52 , C07D473/16
CPC分类号： C07D473/16
摘要： The present invention relates to compounds of formula (I) 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 or 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 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 each R9 is other than H. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula (I), and the use of said compounds in treating proliferative disorders, viral disorders, stroke, alopecia, CNS disorders, neurodegenerative disorders, or diabetes.
摘要翻译：本发明涉及式（I）化合物，其中：R 1和R 2各自独立地为H，烷基或卤代烷基; R 3和R 4各自独立地为H，烷基，卤代烷基或芳基; R5是烷基或环烷基或环烷基 - 烷基，其各自可以任选地被一个或多个OH基团取代; R 6选自环丙基氨基，环丙基甲基氨基，环丁基氨基，环丁基甲基氨基，其中X，Y和Z中的一个为N，其余为CR 9; R 7，R 8和R 9各自独立地为H，烷基或卤代烷基，其中R 7，R 8和R 9中的至少一个不是H.本发明的另一方面涉及包含式（I）化合物的药物组合物，使用所述化合物治疗增殖性疾病，病毒性疾病，中风，脱发，中枢神经系统疾病，神经变性疾病或糖尿病。

2. 发明申请

US20090306098A1 COMBINATION OF ROSCOVITINE AND A HDCA INHIBITOR TO TREAT PROLIFERATIVE DISEASES 审中-公开
标题翻译：罗素维生素和HDCA抑制剂联合治疗增殖性疾病
公开(公告)号：US20090306098A1
公开(公告)日：2009-12-10
申请号：US12093418
申请日：2006-11-13
申请人： Simon Green , Sheelagh Frame , Ian Fleming
发明人： Simon Green , Sheelagh Frame , Ian Fleming
IPC分类号： A61K31/52 , A61P35/00
CPC分类号： A61K45/06 , A61K31/52 , A61K2300/00
摘要： A first aspect of the invention relates to a combination comprising roscovitine, or a pharmaceutically acceptable salt thereof, and a HDAC inhibitor selected from sodium butyrate, or a prodrug thereof, suberoylanilide hydroxamic acid (SAHA), sodium valproate and trichostatin A (TSA). A second aspect of the invention relates to a pharmaceutical product comprising roscovitine, or a pharmaceutically acceptable salt thereof, and a HDAC inhibitor selected from sodium butyrate, or a prodrug thereof, suberoylanilide hydroxamic acid (SAHA), sodium valproate and trichostatin A (TSA) as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method for treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering roscovitine, or a pharmaceutically acceptable salt thereof, and a HDAC inhibitor selected from sodium butyrate, or a prodrug thereof, suberoylanilide hydroxamic acid (SAHA), sodium valproate and trichostatin A (TSA) to a subject.
摘要翻译：本发明的第一方面涉及包含roscovitine或其药学上可接受的盐和选自丁酸钠或其前药，辛二酰苯胺异羟肟酸（SAHA），丙戊酸钠和曲古抑菌素A（TSA）的HDAC抑制剂的组合。本发明的第二方面涉及包含roscovitine或其药学上可接受的盐和选自丁酸钠或其前药，辛二酰苯胺异羟肟酸（SAHA），丙戊酸钠和曲古抑菌素A（TSA）的HDAC抑制剂的药物产品，作为在治疗中同时，连续或分开使用的组合制剂。本发明的第三方面涉及一种治疗增殖性疾病的方法，所述方法包括同时，依次或分别施用roscovitine或其药学上可接受的盐，以及选自丁酸钠或其前药的辛卡酰苯胺异羟肟酸的HDAC抑制剂酸（SAHA），丙戊酸钠和曲古抑菌素A（TSA）。

3. 发明申请

US20060204975A1 Markers for cyclin dependent kinase inhibitors 审中-公开
标题翻译：细胞周期蛋白依赖性激酶抑制剂的标记
公开(公告)号：US20060204975A1
公开(公告)日：2006-09-14
申请号：US11242244
申请日：2005-10-03
申请人： Simon Green , Sheelagh Frame , David Blake
发明人： Simon Green , Sheelagh Frame , David Blake
IPC分类号： C12Q1/68 , A61K31/522
CPC分类号： C12Q1/6886 , C12Q2600/136
摘要： The present invention relates to pharmacodynamic markers for CDKIs including the candidate 2,6,9-tri-substituted purine known as roscovitine. The identity of these markers facilitates the convenient identification of roscovitine-like activity both in vitro and in vivo.
摘要翻译：本发明涉及CDKI的药效学标志物，其包括称为roscovitine的候选2,6,9-三取代嘌呤。这些标记的身份有助于在体外和体内方便地鉴定类似罗素维生素的活性。

4. 发明授权

US09173938B2 Combination of a purine-based CDK inhibitor with a tyrosine kinase inhibitor and use thereof in the treatment of proliferative disorders 有权
标题翻译：基于嘌呤的CDK抑制剂与酪氨酸激酶抑制剂的组合以及其在治疗增殖性疾病中的用途
公开(公告)号：US09173938B2
公开(公告)日：2015-11-03
申请号：US12573358
申请日：2009-10-05
申请人： Simon Green , Sheelagh Frame , Ian Fleming
发明人： Simon Green , Sheelagh Frame , Ian Fleming
IPC分类号： C07D473/34 , A61K31/52 , A61K45/06 , A61K31/517
CPC分类号： A61K45/06 , A61K31/517 , A61K31/52 , Y02A50/411 , A61K2300/00
摘要： The present invention relates to combination comprising (i) an ErbB inhibitor; and (ii) a CDK inhibitor, or a pharmaceutically acceptable salt thereof, selected from: (a) roscovitine; (b) 3-{9-isopropyl-6-[(pyridin-3-ylmethyl)-amino]-9H-purin-2-ylamino}-2-methyl-pentan-2-ol; (c) 3-{9-isopropyl-6-[(pyridin-3-ylmethyl)-amino]-9H-purin-2-ylamino}-pentan-2-ol; and (d) (2R,3S-3-(6-((4,6-dimethylpyridin-3-ylmethylamino)-9-isopropyl-9H-purin-2-ylamino)pentan-2-ol.Further aspects of the invention relate to pharmaceutical products and pharmaceutical compositions comprising combinations according to the invention, and methods of treatment using the same.
摘要翻译：本发明涉及组合，其包含（i）ErbB抑制剂; 和（ii）选自以下的CDK抑制剂或其药学上可接受的盐：（a）roscovitine; （b）3- {9-异丙基-6 - [（吡啶-3-基甲基） - 氨基] -9H-嘌呤-2-基氨基} -2-甲基 - 戊-2-醇; （c）3- {9-异丙基-6 - [（吡啶-3-基甲基） - 氨基] -9H-嘌呤-2-基氨基} - 戊-2-醇; 和（d）（2R，3S-3-（6 - （（4,6-二甲基吡啶-3-基甲基氨基）-9-异丙基-9H-嘌呤-2-基氨基）戊-2-醇本发明的其它方面涉及包含根据本发明的组合的药物产品和药物组合物，以及使用其的治疗方法。

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