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1. 发明专利

JP2015013877A 増殖性疾患を治療するためのサパシタビンの使用有权
标题翻译：用于治疗增殖性疾病的SAPACITABINE的应用
公开(公告)号：JP2015013877A
公开(公告)日：2015-01-22
申请号：JP2014170018
申请日：2014-08-25
申请人：サイクラセルリミテッド , Cyclacel Ltd , サイクラセルリミテッド
发明人： CHIAO JUDY
IPC分类号： A61K31/7068 , A61K9/48 , A61K47/12 , A61K47/14 , A61K47/36 , A61K47/38 , A61K47/42 , A61P35/00 , A61P35/02
CPC分类号： A61K31/7068 , A61K31/513
摘要：【課題】固形腫瘍、非小細胞肺癌(NSCLC)、などの増殖性障害を治療するための医薬の調製における下式の2’−シアノ−2’−デオキシ−N4−パルミトイル−1−&bgr;−D−アラビノフラノシルシトシン(サパシタビン或いはCYC682)又はその代謝産物の治療的適用及び改善された投薬計画の提供。【解決手段】サパシタビン又はその代謝産物は少なくとも1つの治療周期を含む投薬計画で投与され、前記治療周期は、サパシタビン又はその代謝産物の治療有効量を3週間のうち2週間、1週間につき約2〜約6日間ずつ投与する方法。【選択図】なし
摘要翻译：要解决的问题：提供：图中的式（2）的2'-氰基-2'-脱氧-N-棕榈酰-1-＆bgr-D-阿拉伯呋喃糖基胞嘧啶或其代谢物的治疗应用的用于治疗增殖性病症的药物，例如实体瘤和非小细胞肺癌（NSCLC）; 和改善的给药方案。解决方案：在包含至少一个治疗周期的给药方案中施用沙匹沙星或其代谢物。治疗周期包括在3周内给予治疗有效量的每周约2至约6天的治疗有效量的沙美他滨或其代谢物2周。

2. 发明专利

JP2013189463A Formulation 审中-公开
标题翻译：公式
公开(公告)号：JP2013189463A
公开(公告)日：2013-09-26
申请号：JP2013117637
申请日：2013-06-04
申请人： Cyclacel Ltd , サイクラセルリミテッド
发明人： WESTWOOD ROBERT , SELKIRK ALISTAIR
IPC分类号： A61K31/7068 , A61K9/48 , A61K47/14
CPC分类号： A61K9/4808 , A61K9/4866 , A61K31/513
摘要： PROBLEM TO BE SOLVED: To provide a new capsule formulation for 2'-cyano-2'-deoxy-N4-palmitoyl-1-β-D-arabinofuranosylcytosine (CYC682), which is a pyrimidine nucleoside derivative therapeutically useful in treatment and/or prevention of cancer.SOLUTION: A pharmaceutical formulation includes (i) a capsule, and (ii) a core including a crystalline CYC682 and a liquid carrier. The liquid carrier is a medium chain triglyceride oil or Gelucire 44/14. The medium chain triglyceride oil is a coconut oil or caprylic/capric triglyceride. The capsule is a gelatin capsule and is a hard capsule. The capsule includes one or more opacifying agents and/or one or more pigments. The pigments and/or the opacifying agents are each present in an amount of about 0.1 to about 10%. The opacifying agent is titanium dioxide. Titanium dioxide is present in an amount of about 2%. The capsule is sealed with a gelatin band.
摘要翻译：要解决的问题：为了提供治疗和/或治疗用途的嘧啶核苷衍生物的2'-氰基-2'-脱氧-N4-棕榈酰-1-糖基-D-阿拉伯呋喃糖基胞嘧啶（CYC682）的新型胶囊制剂，或预防癌症。解决方案：药物制剂包括（i）胶囊和（ii）包含结晶CYC682和液体载体的核心。液体载体是中链甘油三酯油或Gelucire 44/14。中链甘油三酯油是椰子油或辛酸/癸酸甘油三酸酯。胶囊是明胶胶囊，是硬胶囊。胶囊包括一种或多种不透明剂和/或一种或多种颜料。颜料和/或不透明剂各自以约0.1至约10％的量存在。不透明剂是二氧化钛。二氧化钛的含量约为2％。胶囊用明胶带密封。

3. 发明申请

WO2005116025A3 2-SUBSTITUTED-4-HETEROARYL-PYRIMIDINES USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISORDERS 审中-公开
标题翻译：用于治疗增殖性疾病的2-取代-4-异氟尿嘧啶
公开(公告)号：WO2005116025A3
公开(公告)日：2006-02-23
申请号：PCT/GB2005002134
申请日：2005-05-26
申请人： CYCLACEL LTD , WANG SHUDONG , WOOD GAVIN , DUNCAN KENNETH , MEADES CHRISTOPHER , GIBSON DARRON , MCLACHLAN JANICE , FISCHER PETER
发明人： WANG SHUDONG , WOOD GAVIN , DUNCAN KENNETH , MEADES CHRISTOPHER , GIBSON DARRON , MCLACHLAN JANICE , FISCHER PETER
IPC分类号： C07D417/00 , C07D417/04 , C07D417/14 , A61K31/505
CPC分类号： C07D417/04 , C07D417/14
摘要： The present invention relates to selected substituted pyrimidines their preparation, pharmaceutical compositions containing them and their use as inhibitors of one or more protein kinases, and hence their use in the treatment of proliferative disorders, viral disorders and/or other disorders.
摘要翻译：本发明涉及其制备的选择性取代的嘧啶，含有它们的药物组合物及其作为一种或多种蛋白激酶的抑制剂的用途，因此涉及其用于治疗增殖性病症，病毒性疾病和/或其它疾病。

4. 发明申请

WO2004087954A3 CELL CYCLE RELATED MARKERS 审中-公开
标题翻译：细胞周期相关标记
公开(公告)号：WO2004087954A3
公开(公告)日：2005-01-27
申请号：PCT/GB2004001334
申请日：2004-03-26
申请人： CYCLACEL LTD , GREEN SIMON R , FRAME SHEELAGH , BLAKE DAVID
发明人： GREEN SIMON R , FRAME SHEELAGH , BLAKE DAVID
IPC分类号： C12Q1/68
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。

5. 发明申请

WO2004063362A3 CELL CYCLE PROGRESSION PROTEINS 审中-公开
标题翻译：细胞周期蛋白进展
公开(公告)号：WO2004063362A3
公开(公告)日：2004-12-02
申请号：PCT/GB0305635
申请日：2003-12-31
申请人： CYCLACEL LTD , GLOVER DAVID , BELL GRAHAM , FRENZ LISA , MIDGLEY CAROL
发明人： GLOVER DAVID , BELL GRAHAM , FRENZ LISA , MIDGLEY CAROL
IPC分类号： C07K14/435 , C07K14/47 , G01N33/50 , G01N33/574 , C12N5/06 , A61K38/16 , A61K39/395 , C07H21/02 , C07K14/00 , C07K16/18 , C07K16/44 , C12Q1/68
CPC分类号： G01N33/5008 , C07K14/43581 , C07K14/4702 , G01N33/5011 , G01N33/5091
摘要： The invention describes human genes involved in cell cycle progression, including mitosis and meiosis. The invention also relates to the used of these "cell cycle progression" genes and proteins in the modulation of cell cycle progression in cells and methods for identifying modulators of these genes or proteins and hence modulators of mitosis and meiosis.
摘要翻译：本发明描述涉及细胞周期进程的人类基因，包括有丝分裂和减数分裂。本发明还涉及在细胞中细胞周期进程调节中使用这些“细胞周期进程”基因和蛋白质以及用于鉴定这些基因或蛋白质以及因此有丝分裂和减数分裂的调节剂的调节剂的方法。

6. 发明申请

WO03045971A3 SOLVATES OF 3.BETA., 28-DIACETOXY-18-OXO-19, 20, 21, 29, 30-PENTANORLUPAN-22-OIC ACID, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS THEREOF 审中-公开
标题翻译： 3.BETA。，28-二羧酸-18-OXO-19,20,21,29,30-泛醇 - 22-酸的溶液，其制备方法及其药物组合物
公开(公告)号：WO03045971A3
公开(公告)日：2003-07-31
申请号：PCT/GB0205231
申请日：2002-11-21
申请人： CYCLACEL LTD , UNIV KARLOVA , UNIV PALACKEHO , FISCHER PETER M , SAREK JAN , BLANEY PAUL M , COLLIER PIERS , FERGUSON JOHN R , HULL JONATHAN D
发明人： FISCHER PETER M , SAREK JAN , BLANEY PAUL M , COLLIER PIERS , FERGUSON JOHN R , HULL JONATHAN D , HAJDUCH MARIAN
IPC分类号： A61P35/00 , C07J63/00 , C07J71/00 , A61K31/565
CPC分类号： C07J63/008 , C07J71/0005
摘要： The present invention relates to 3beta,28-diacetoxy-18-oxo-19,20,21,29,30-pentanorlupan-22-oic acid methanol solvate, its use in medicine and processes for its preparation.
摘要翻译：本发明涉及3β，28-二乙酰氧基-18-氧代-19,20,21,29,30-戊酰氧基-22-酸甲醇溶剂化物，其用于医药及其制备方法。

7. 发明申请

WO0248178A3 CYCLOPHILIN-BINDING LIGANDS 审中-公开
标题翻译：环磷酰胺结合配体
公开(公告)号：WO0248178A3
公开(公告)日：2002-11-14
申请号：PCT/GB0105540
申请日：2001-12-13
申请人： CYCLACEL LTD , WALKINSHAW MALCOLM DOUGLAS , TAYLOR PAUL , TURNER NICHOLAS JOHN , FLITSCH SABINE LAHJA
发明人： WALKINSHAW MALCOLM DOUGLAS , TAYLOR PAUL , TURNER NICHOLAS JOHN , FLITSCH SABINE LAHJA
IPC分类号： C07C271/18 , C07C271/20 , C07C271/22 , A61K31/325
CPC分类号： C07C271/18 , C07B2200/07 , C07C271/20 , C07C271/22 , C07C2601/14 , C07C2601/16
摘要： The present invention relates to a compound of formula (I) wherein (i) when a and c are double bonds, R is absent, b is a single bond, R is formula (II) or (ii) when a and c are single bonds, b is a double bond, and R is H, R is formula (III) wherein X is straight or branched chain C1-6 alkyl, -(CH2)nAr, C1-6 cycloalkyl, or (CH2)nR", where R" is a cyclic hydrocarbyl group; Y is a natural or unnatural amino acid side chain; W is OH or NHR , wherein R is CH(Y')CO2X', where X' and Y' are defined as for X and Y respectively, and may be the same or different to X and Y respectively; and Z1 and Z2 are each independently H, straight or branched chain C1-6 alkyl, straight or branched chain C1-6 alkenyl, -(CH2)nAr, -(CH2)n-CO2R', -(CH2)p-CH=CH-(CH2)qAr where p and q are each independently O to 5, R' is C1-6 alkyl; and each n may be the same or different and is from 1 to 5.
摘要翻译：本发明涉及式（I）化合物，其中（i）当a和c为双键时，R 2不存在，b为单键，R 1为式（II）或（ii）当a和c为单键时，b为双键，R 1为H，R 2为式（III），其中X为直链或支链C1-6烷基， - （CH2）nAr，C1 -6环烷基或（CH 2）n R“，其中R”为环状烃基; Y是天然或非天然氨基酸侧链; W是OH或NHR 3，其中R 3是CH（Y'）CO 2 X'，其中X'和Y'分别定义为X和Y，并且可以分别与X和Y相同或不同 ; 和Z 1和Z 2各自独立地为H，直链或支链C 1-6烷基，直链或支链C 1-6烯基， - （CH 2）n Ar， - （CH 2）n -CO 2 R'， - （CH 2）p -CH- CH-（CH 2）q Ar，其中p和q各自独立地为O至5，R'为C 1-6烷基; 并且每个n可以相同或不同，为1至5。

8. 发明申请

WO0190096A3 TRITERPENOID DERIVATIVES AND THEIR USE AS ANTIPROLIFERATIVE AGENTS 审中-公开
标题翻译：三磷酸酯衍生物及其用作抗增生剂
公开(公告)号：WO0190096A3
公开(公告)日：2002-03-07
申请号：PCT/GB0102341
申请日：2001-05-23
申请人： UNIVERZITA PALACKEHO V OLOMOUC , UNIV KARLOVA , CYCLACEL LTD , HAJDUCH MARIAN , SAREK JAN
发明人： HAJDUCH MARIAN , SAREK JAN
IPC分类号： A61K31/343 , A61P35/00 , C07D307/00
CPC分类号： C07D307/00 , A61K31/343
摘要： The present invention relates to the use of a compound of formula (I), or a pharmaceutically acceptable salt, crystal form, complex, hydrate, or hydrolysable ester thereof, in the preparation of a medicament for treating a patient suffering from leukaemia, cancer or other proliferative disorder. A further embodiment relates to the use of a compound of formula (I) in an assay for detecting the phosphorylation state of cellular substrates. The present invention also relates to novel compounds of formula (Ia), and the chemical synthesis thereof.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，晶体形式，复合物，水合物或可水解的酯在制备用于治疗患有白血病，癌症或其他增殖性疾病。另一实施方案涉及式（I）化合物在用于检测细胞底物的磷酸化状态的测定中的用途。本发明还涉及新的式（Ia）化合物及其化学合成。

9. 发明专利

JP2014076994A Pyrimidine derivatives as protein kinase inhibitors 有权
标题翻译：吡啶衍生物作为蛋白激酶抑制剂
公开(公告)号：JP2014076994A
公开(公告)日：2014-05-01
申请号：JP2013230231
申请日：2013-11-06
申请人： Cyclacel Ltd , サイクラセルリミテッド
发明人： HOLLICK JONATHAN JAMES , STUART DONALD JONES , FLYNN CLAIRE JUNE , MICHAEL GEORGE THOMAS
IPC分类号： C07D487/04 , A61K31/551 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07D519/00 , C12N9/99
CPC分类号： C07D487/04 , A61K31/551 , C07D453/02 , C07D487/10 , C07D519/00
摘要： PROBLEM TO BE SOLVED: To provide substituted pyrimidine derivatives and their use in therapy; and more specifically, compounds capable of inhibiting one or more protein kinases, particularly polo-like kinases, pharmaceutical compositions containing the compounds and their use in treating proliferative diseases and the like.SOLUTION: The present invention relates to a compound of the formula VIII, or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：待解决的问题：提供取代的嘧啶衍生物及其在治疗中的应用; 更具体地，能够抑制一种或多种蛋白激酶，特别是polo样激酶的化合物，含有该化合物的药物组合物及其在治疗增殖性疾病中的用途。本发明涉及式VIII化合物，或其药学上可接受的盐或酯。

10. 发明专利

JPH11322610A CYCLIN-DEPENDENT KINASE INHIBITOR 失效
公开(公告)号：JPH11322610A
公开(公告)日：1999-11-24
申请号：JP12328198
申请日：1998-05-06
申请人： CYCLACEL LTD
发明人： RIBOR HAVRICHEK , MIROSLAV SUTORNADO , MARIAN HAIDOUF
IPC分类号： C07D473/16 , A61K31/52 , A61P35/00 , A61P35/02 , A61P43/00
摘要： PROBLEM TO BE SOLVED: To prepare a drug composition inhibiting cdk(cyclin-dependent kinase) 4 and/or cdk 7 when treating a cancerous or a leukemic proliferating disease, by including a specific compound as an active principle. SOLUTION: This drug composition is prepared by including 2-[(3- hydroxypropyl)amino]-6-benzylamino-9-isopropylpurine (or its salt) or 2-[(1- ethyl-2-hydroxyethyl)amino]-6-benzylamino-9-isopropylpurine (or its salt). The composition causes the death of cells in proliferating in the case of cancer, leukemia, etc. Cyclin-dependent kinases participating in the cell cycle control contain at least one catalytic subunit and at least one control subunit, and are controlled through fugitive bond with cyclin D1-D3 (cdk2-cdk4-cdk5-cdk6), cyclin H (cdk7) or the like.

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