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1. 发明申请

WO2004005278A1 BISARYLSULFONAMIDE COMPOUNDS AND THEIR USE IN CANCER THERAPY 审中-公开
标题翻译： BISARYLSULFONAMIDE化合物及其在癌症治疗中的应用
公开(公告)号：WO2004005278A1
公开(公告)日：2004-01-15
申请号：PCT/GB2003/002923
申请日：2003-07-07
申请人： CYCLACEL LIMITED , WANG, Shudong , GIBSON, Darren , DUNCAN, Kenneth , BAILEY, Kevin , THOMAS, Mark , MacCALLUM, David , ZHELEVA, Daniella , TURNER, Nicholas, John , FISCHER, Peter, Martin
发明人： WANG, Shudong , GIBSON, Darren , DUNCAN, Kenneth , BAILEY, Kevin , THOMAS, Mark , MacCALLUM, David , ZHELEVA, Daniella , TURNER, Nicholas, John , FISCHER, Peter, Martin
IPC分类号： C07D333/42
CPC分类号： C07D213/70 , A61K31/43 , A61K31/4439 , A61K31/454 , A61K31/5377 , C07C311/21 , C07C311/29 , C07C311/44 , C07D207/34 , C07D207/36 , C07D209/14 , C07D209/16 , C07D213/71 , C07D231/12 , C07D235/30 , C07D263/32 , C07D277/36 , C07D277/56 , C07D285/06 , C07D285/10 , C07D295/185 , C07D319/18 , C07D333/34 , C07D333/42 , C07D333/62 , C07D409/04 , C07D409/12 , C07D413/04 , C07D513/04
摘要： The present invention relates to the use of bisarylsulfonamide compounds of formula (I) wherein W is a C I-5 branched or unbranched alkyl group or a C 2-5 alkenyl group; nis0or1; R 1 is H, a C, 1-8 branched or unbranched alkyl group, a C 2-8 alkenyl group, or an aryl or aralkyl group; Ar 1 is a substituted thienyl, furyl, pyrrolyl, imidazothiazolyl, thiazolyl, pyridyl or phenyl group; and Ar 2 is a substituted phenyl, indolyl or benzoimidazolyl group; in the preparation of a medicament for treating proliferative disorders. Further aspects of the invention relate to compounds of formula (I), pharmaceutical compositions thereof, and an assay for determining binding to HDM2.
摘要翻译：本发明涉及式（I）的双芳基磺酰胺化合物，其中W是C1-5支链或非支链烷基或C2-5烯基; nis0or1; R 1是H，C 1-8支链或非支链烷基，C 2-8烯基或芳基或芳烷基; Ar 1是取代的噻吩基，呋喃基，吡咯基，咪唑并噻唑基，噻唑基，吡啶基或苯基; Ar 2是取代的苯基，吲哚基或苯并咪唑基; 在制备用于治疗增殖性疾病的药物中。本发明的其它方面涉及式（I）化合物，其药物组合物和用于测定与HDM2结合的测定法。

2. 发明申请

WO2005075468A2 COMPOUNDS 审中-公开
标题翻译：含有蛋白激酶抑制活性的吡啶并 - 吡啶二酮
公开(公告)号：WO2005075468A2
公开(公告)日：2005-08-18
申请号：PCT/GB2005/000405
申请日：2005-02-07
申请人： CYCLACEL LIMITED , DUNCAN, Kenneth , GIBSON, Darren , WANG, Shudong , ZHELEVA, Daniella , FISCHER, Peter
发明人： DUNCAN, Kenneth , GIBSON, Darren , WANG, Shudong , ZHELEVA, Daniella , FISCHER, Peter
IPC分类号： C07D417/00
CPC分类号： C07D417/04 , C07D417/14
摘要： The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salts thereof, wherein: Z 1 :1 is N or CH; ;Z 2 and Z 3 are each independently N or CR 7 ; :R l , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 are each independently H, R 8 , or R 9 ; each R 8 is independently a hydrocarbyl group; and each R 9 is independently halo, NO 2 , alkoxy, CN, CF 3 , S0 3 H, SO 2 NR 10 R 11 , S0 2 R 12 , NR 13 R 14 (CH 2 ) a COOR 15 , (CH 2 ) b CONR 16 R 17 , (CH 2 ) C COR 18 or (CH 2 ) d OH; a, b, c and d are each independently 0, 1 2 3 or 4; R10-18 are each independently H or alkyl; provided that when R l and R 2 are both H, Z l is CH; or Z 2 is N; or Z l is CH and Z 2 is N; and wherein the compound is other than 4-(4,5-dimethylthiazol-2-yl)-N-(3,4,5trimethoxyphenyl)-2-pyrimidineamine or 4-(5-(2-hydroxyethyl)-4-methylthiazol-2-yl)N-(3,4,5-trimethoxyphenyl)-2-pyrimidineamine. Further aspects relate to the use of compounds of formula (I) in the preparation of a medicament for treating one or more disorders selected from a proliferative disorder, a viral disorder, a CNS disorder, diabetes, stroke or alopecia.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中：Z 1：1是N或CH; Z 2和Z 3各自独立地为N或CR 7; R 1，R 2，R 3，R 4，R 5，R 6和R 7各自独立地为H，R 8或R 9 >; 每个R 8独立地是烃基; 并且每个R 9独立地是卤素，NO 2，烷氧基，CN，CF 3，SO 3 H，SO 2 NR 10 R 11，SO 2 R 12，NR 13 R 14（CH 2）a COOR 15，（CH 2）b CONR 16 R 17，（CH 2）C COR 18或（CH 2）d OH; a，b，c和d各自独立地为0，1 2 3或4; R 10-18各自独立地为H或烷基; 条件是当R 1和R 2都是H时，Z 1是CH; 或Z 2为N; 或Z 1为CH且Z 2为N; 并且其中所述化合物不是4-（4,5-二甲基噻唑-2-基）-N-（3,4,5-三甲氧基苯基）-2-嘧啶胺或4-（5-（2-羟乙基）-4-甲基噻唑吡啶-2-基）-N-（3,4,5-三甲氧基苯基）-2-嘧啶胺。其它方面涉及式（I）化合物在制备用于治疗选自增殖性病症，病毒病症，CNS病症，糖尿病，中风或脱发的一种或多种病症的药物中的用途。

3. 发明申请

WO2007042786A2 COMPOUND 审中-公开
标题翻译：复合
公开(公告)号：WO2007042786A2
公开(公告)日：2007-04-19
申请号：PCT/GB2006/003751
申请日：2006-10-09
申请人： CYCLACEL LIMITED , WOOD, Gavin , MEADES, Christopher, Keith , FISCHER, Peter , WANG, Shudong , DUNCAN, Kenneth , ZHELEVA, Daniella , MCINNES, Campbell , THOMAS, Mark
发明人： WOOD, Gavin , MEADES, Christopher, Keith , FISCHER, Peter , WANG, Shudong , DUNCAN, Kenneth , ZHELEVA, Daniella , MCINNES, Campbell , THOMAS, Mark
IPC分类号： A61K31/506 , C07D401/14 , C07D403/04 , A61P29/00 , A61P31/12 , A61P35/00
CPC分类号： C07D401/14 , C07D403/04
摘要： The present invention relates to compounds of formula (I) or formula (II), or pharmaceutically acceptable salts thereof. Further aspects relate to pharmaceutical compositions comprising compounds according to the invention, and the use of said compounds in the preparation of a medicament for treating a variety of disorders, including proliferative disorders, viral disorders, stroke, etc.
摘要翻译：本发明涉及式（I）或式（II）化合物或其药学上可接受的盐。其它方面涉及包含根据本发明的化合物的药物组合物，以及所述化合物在制备用于治疗各种疾病（包括增殖性病症，病毒性疾病，中风等）的药物中的用途。

4. 发明申请

WO2007042784A2 COMPOUND 审中-公开
标题翻译：复合
公开(公告)号：WO2007042784A2
公开(公告)日：2007-04-19
申请号：PCT/GB2006/003748
申请日：2006-10-09
申请人： CYCLACEL LIMITED , JONES, Stuart , WESTWOOD, Bob , THOMAS, Mark , MCLACHLAN, Janice , DUNCAN, Kenneth , SCAEROU, Fred , ZHELEVA, Daniella
发明人： JONES, Stuart , WESTWOOD, Bob , THOMAS, Mark , MCLACHLAN, Janice , DUNCAN, Kenneth , SCAEROU, Fred , ZHELEVA, Daniella
IPC分类号： C07D487/04 , A61K31/437
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts thereof, wherein Z is NR 11 , NHCO, NHSO 2 , NHCH 2 , CH 2 , CH 2 CH 2 , or CH=CH; X is a hydrocarbyl group optionally substituted by one or more R 12 groups; R 10 and R 11 are each independently H or alkyl; R 1 -R 4 are each independently H or (CH 2 ) m R 12 , where m is O, 1, 2, or 3; each R 12 is independently (CH 2 ) a R 16 , where each R 16 is independently selected from O(CH 2 ) b R 13 , R 13 , COR 13 , COOR 13 , CN, CONR 13 R 14 , NR 13 R 14 , NR 13 COR 14 , SR 13 , SOR 13 , SO 2 R 13 , NR 13 SO 2 R 14 , SO 2 OR 13 , SO 2 NR 13 R 14 , halogen, CF 3 , and NO 2 , and wherein each a is 0, 1, 2, or 3 and b is 0, 1, 2, or 3; R 13 and R 14 are each independently H or (CH 2 ) n R 15 , where n is 0, 1, 2, or 3; and each R 15 is independently selected from alkyl, cycloalkyl, heteroaryl, aralkyl, aryl and heterocycloalkyl, each of which may be optionally substituted by one or more substituents selected from halogen, OH, CN, COO-alkyl, aralkyl, SO 2 -alkyl, SO 2 -aryl, COOH, CO- alkyl, CO-aryl, NH 2 , NH-alkyl, N(alkyl) 2 , CF 3 , alkyl and alkoxy, wherein said alkyl and alkoxy groups may be further substituted by one or more OH groups. Further aspects of the invention relate to pharmaceutical compositions comprising compounds of formula I, and the use of compounds of formula (I) in the preparation of a medicament for treating a variety of disorders, including proliferative disorders, viral disorders, stroke, etc.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中Z为NR 11，NHCO，NHSO 2，NHCH 2， CH 2 CH 2，CH 2 CH 2或CH = CH; X是任选被一个或多个R 12基团取代的烃基; R 10和R 11各自独立地为H或烷基; R 1〜R 4各自独立地为H或（CH 2 CH 2）m R 12， SUP>，其中m是O，1,2或3; 每个R 12独立地是（CH 2）2，其中每个R 16独立地是（CH 2） SUP>独立地选自O（CH 2）2 R 13，R 13，COR 12， 13，COOR 13，CN，CONR 13，R 14，NR 13，R 12， 14，13号，14号，13号，13号，13号，14号 13，13，13，13，14，14，14，14，14， SO 2，SO 2，R 13，R 14，R 14，R 14，R 14，和NO 2 2，并且其中每个a是0,1,2或3，b是0,1,2或3; R 13和R 14各自独立地为H或（CH 2 CH 2）n R 15， SUP>，其中n为0,1,2或3; 并且每个R 15独立地选自烷基，环烷基，杂芳基，芳烷基，芳基和杂环烷基，其各自可以任选地被一个或多个选自卤素，OH，CN，COO-烷基的取代基取代，芳烷基，SO 2 - 烷基，SO 2 - 芳基，COOH，CO-烷基，CO-芳基，NH 2 - ， - NH-烷基，N（烷基）亚烷基，CF 3，烷基和烷氧基，其中所述烷基和烷氧基可进一步被一个或多个OH基取代。本发明的其它方面涉及包含式I化合物的药物组合物，以及式（I）化合物在制备用于治疗各种病症（包括增殖性病症，病毒性疾病，中风等）的药物中的用途。

5. 发明申请

WO2005108421A1 CRYSTAL STRUCTURE OF HUMAN PROLIFERATING CELL NUCLEAR ANTIGEN (PCNA) AND USES THEREOF 审中-公开
标题翻译：人类增殖细胞核抗原（PCNA）的晶体结构及其用途
公开(公告)号：WO2005108421A1
公开(公告)日：2005-11-17
申请号：PCT/GB2005/001764
申请日：2005-05-10
申请人： CYCLACEL LIMITED , KONTOPIDIS, George , ZHELEVA, Daniella , McINNES, Campbell , FISCHER, Peter , WALKINSHAW, Malcolm
发明人： KONTOPIDIS, George , ZHELEVA, Daniella , McINNES, Campbell , FISCHER, Peter , WALKINSHAW, Malcolm
IPC分类号： C07K14/47
CPC分类号： C07K14/4738 , C07K2299/00
摘要： The present invention relates to crystals comprising human PCNA, and methods and assays for designing and identifying small molecule PCNA inhibitors using said crystals.
摘要翻译：本发明涉及包含人PCNA的晶体，以及使用所述晶体设计和鉴定小分子PCNA抑制剂的方法和测定法。

6. 发明申请

WO2013171473A1 DOSAGE REGIMEN FOR SAPACITABINE AND SELICICLIB 审中-公开
标题翻译：用于SAPACITABINE和SELICICLIB的剂量计
公开(公告)号：WO2013171473A1
公开(公告)日：2013-11-21
申请号：PCT/GB2013/051236
申请日：2013-05-14
申请人： CYCLACEL LIMITED
发明人： CHIAO, Judy , BLAKE, David , ZHELEVA, Daniella , DAVIS, Susan , GREEN, Simon , SHAPIRO, Geoffrey
IPC分类号： A61K31/52 , A61K31/706 , A61K31/505 , A61P35/00
CPC分类号： A61K31/7068 , A61K9/0053 , A61K31/52 , A61P35/00 , A61P35/02 , A61K2300/00
摘要： A first aspect of the invention relates to a method of treating a proliferative disorder in a subject, said method comprising administering to the subject a therapeutically effective amount of (i) sapacitabine, or a metabolite thereof; and (ii) seliciclib; in accordance with a dosing regimen comprising at least one first treatment cycle and at least one second treatment cycle, wherein said first treatment cycle comprises: (a) administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, for 3 to 5 consecutive days for 2 weeks, starting on day d, where d is the first day of treatment with sapacitabine, or the metabolite thereof, in said first treatment cycle; and (b) optionally administering a therapeutically effective amount of seliciclib for 3 to 5 consecutive days for 2 weeks, starting on day (d-1) relative to the administration of sapacitabine or the metabolite thereof, in said first treatment cycle; followed by a rest period of at least 2 weeks, or until treatment-related toxicities are resolved, whichever is longer; and wherein said second treatment cycle comprises: (a) administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, for 3 to 5 consecutive days for 2 weeks, starting on day d, where d is the first day of treatment with sapacitabine, or the metabolite thereof, in said second treatment cycle; and (b) administering a therapeutically effective amount of seliciclib for 3 to 5 consecutive days for 2 weeks, starting on day (d-1) relative to the administration of sapacitabine or the metabolite thereof, in said second treatment cycle; followed by a rest period of at least 2 weeks, or until treatment-related toxicities are resolved, whichever is longer. Further aspects of the invention relate to a kit of parts, and corresponding uses.
摘要翻译：本发明的第一方面涉及治疗受试者中增殖性疾病的方法，所述方法包括给予受试者治疗有效量的（i）西他滨或其代谢物; 和（ii）seliciclib; 根据包含至少一个第一治疗周期和至少一个第二治疗周期的给药方案，其中所述第一治疗周期包括：（a）连续施用治疗有效量的沙美沙胺或其代谢物3至5天持续2周，从d天开始，其中d是在所述第一治疗周期中用西他滨或其代谢物治疗的第一天; 和（b）在所述第一个治疗周期中相对于施用西来昔布或其代谢物，在第（d-1）天开始，任选地施用治疗有效量的西拉替尼连续3至5天，持续2周; 之后休息至少2周，或直到治疗相关毒性得到解决，以较长者为准; 并且其中所述第二治疗周期包括：（a）从第d天开始，给予治疗有效量的沙美他滨或其代谢物连续3至5个星期，其中d是用西他滨的第一天治疗，或其代谢物，在所述第二处理循环中; 和（b）在所述第二治疗周期中相对于施用西他滨或其代谢物，在第（d-1）天开始，施用治疗有效量的联用西拉霉3至5个连续2周。其次是至少2周的休息期，或直到治疗相关的毒性被解决为止，以较长者为准。本发明的其它方面涉及一组零件和相应的用途。

7. 发明申请

WO2013144632A1 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：WO2013144632A1
公开(公告)日：2013-10-03
申请号：PCT/GB2013/050816
申请日：2013-03-28
申请人： CYCLACEL LIMITED
发明人： DAVIS, Susan , ZHELEVA, Daniella
IPC分类号： A61K9/00 , A61K31/5513 , A61K31/551
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 NR 7 ; R 1 and R 2 are each independently H, alkyl or cycloalkyl; R 3 is a 6-membered heterocycloalkyi group selected from piperidinyl, piperazinyl, morpholinyl and tetrahydropyranyl, wherein said heterocycloalkyi group is optionally further substituted by one or more (CH 2 ) n R 19 groups; R 4 and R 4' are each independently H or alkyl; or R 4 and R 4' together form a spiro cycloalkyl group; Q is CH or N; R 6 is OR 8 or halogen; n is 1, 2 or 3; R 19 is H, alkyl, aryl or a cycloalkyl group; R 7 and R 8 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 μΜ to about 1 μΜ 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 μΜ to about 1 μΜ 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地进一步被一个或多个（CH 2）n 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）维持血浆浓度为约0.5μM至约1μM至多约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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