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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

WO2006075152A1 4- (1H-INDOL-3-YL) -PYRIMIDIN-2-YLAMINE DERIVATES AND THEIR USE IN THERAPY 审中-公开
标题翻译： 4-（1H-吲哚-3-基） - 嘧啶-2-基]胺衍生物及其在治疗中的用途
公开(公告)号：WO2006075152A1
公开(公告)日：2006-07-20
申请号：PCT/GB2006/000087
申请日：2006-01-11
申请人： CYCLACEL LIMITED , FISCHER, Peter, Martin , WANG, Shudong , MEADES, Christopher, Keith , ANDREWS, Martin, James, Inglis , GIBSON, Darren , DUNCAN, Kenneth
发明人： FISCHER, Peter, Martin , WANG, Shudong , MEADES, Christopher, Keith , ANDREWS, Martin, James, Inglis , GIBSON, Darren , DUNCAN, Kenneth
IPC分类号： C07D401/14 , C07D403/04 , C07D405/14 , A61K31/506 , A61K31/5377 , A61P5/48 , A61P9/00 , A61P9/04 , A61P17/14 , A61P25/00 , A61P29/00 , A61P31/00 , A61P33/00 , A61P35/00
CPC分类号： C07D401/14 , C07D403/04 , C07D405/14
摘要： The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts thereof. The present invention seeks to provide further substituted heteroaryl-substituted pyrimidine derivatives. More specifically, the invention relates to compounds that have broad therapeutic applications in the treatment of a number of different diseases and/or that are capable of inhibiting one or more protein kinases.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐。本发明寻求提供进一步取代的杂芳基取代的嘧啶衍生物。更具体地，本发明涉及在治疗许多不同疾病和/或能够抑制一种或多种蛋白激酶方面具有广泛治疗应用的化合物。

5. 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。

6. 发明申请

WO2005116025A2 COMPOUNDS 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：WO2005116025A2
公开(公告)日：2005-12-08
申请号：PCT/GB2005/002134
申请日：2005-05-26
申请人： CYCLACEL LIMITED , 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
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。

7. 发明申请

WO2004056368A1 THERAPEUTIC APPLICATIONS OF 2-SUBSTITUTED 4-HETEROARYLRYRIMIDINES 审中-公开
标题翻译： 2-取代的四异丙基嘧啶的治疗应用
公开(公告)号：WO2004056368A1
公开(公告)日：2004-07-08
申请号：PCT/GB2003/005558
申请日：2003-12-18
申请人： CYCLACEL LIMITED , WANG, Shudong , MEADES, Christopher , WOOD, Gavin , DUNCAN, Kenneth , ZHEVELA, Daniella , FISCHER, Peter
发明人： WANG, Shudong , MEADES, Christopher , WOOD, Gavin , DUNCAN, Kenneth , ZHEVELA, Daniella , FISCHER, Peter
IPC分类号： A61K31/506
CPC分类号： A61K31/506
摘要： The present invention relates to the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein (A) one of X and Y is S, and the other is N; or one of X and Y is NH or N-R 5 , and the other is C-R 6 ; "a" is a single bond; "b", "c", "d", "e" and "f' are single or double bonds so as to form a heteroaryl ring; R 1 is is R 7 with the proviso that R 1 is other than H or Me; or (B) one of X and Y is S, and the other is NH or N-R 5 ; "a" and "d" are each double bonds; "b", "c", "e" and "f' are each single bonds; R 1 is oxo; and R 2 , R 3 , R 4 , R 5 , and R 6 are each independently H or R 7 ; R 7 is a group (CH 2 ) n -R 8 , wherein n is 0, 1, 2, 3 or 4 and wherein R 8 is selected from alkyl, aryl, heteroaryl, heterocycloalkyl, F, Cl, Br, I, CF 3 , NO 2 , CN, OH, O-alkyl, O-aryl, 0- heteroaryl, 0-heterocycloalkyl, CO-alkyl, CO-aryl, CO-heteroaryl, CO-heterocycloalkyl, COO-alkyl, NH 2 , NH-alkyl, NH-aryl, N(alkyl) 2 , NH-heteroaryl, NH-heterocycloalkyl, COOH, CONH 2 , CONH-alkyl, CON(alkyl) 2 , CONH-aryl, CONH-heteroaryl, CONHheterocycloalkyl, SO 3 H, S0 2 -alkyl, SO 2 -aryl, S0 2 -heteroaryl, SO 2 -heterocycloalkyl, SO 2 NH 2 , SO 2 NH-alkyl, SO 2 N(alkyl) 2 , SO 2 NH-aryl, SO 2 NH-heteroaryl, or SO 2 NHheterocycloalkyl, wherein said alkyl, aryl, heteroaryl, and heterocycloalkyl groups are optionally substituted with one or more groups selected from halogeno, NO 2 , OH, 0methyl, NH 2 , COOH, CONH 2 and CF 3 ; in the preparation of a medicament for treating diabetes. The compounds of the invention also have applications in the treatment of CNS disorders, alopecia, cardiovascular disorders and stroke.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐的用途，其中（A）X和Y之一是S，另一个是N; 或X和Y之一是NH或N-R 5，另一个是C-R 6; “a”是单一债券; “b”，“c”，“d”，“e”和“f”是单键或双键，以形成杂芳基环; R 1为R 7，条件是R 1，不是H或Me;或（B）X和Y之一是S，另一个是NH或NR 5;“a”和“d”分别是双键;“b”，“c” “e”和“f”均为单一债券; R 1是氧代; R 2，R 3，R 4，R 5和R 6各自独立地为H或R 7; R 7是基团（CH 2）n R 8，其中n是0,1,2,3或4，并且其中R 8选自烷基，芳基，杂芳基，杂环烷基，F，Cl，Br， I，CF 3，NO 2，CN，OH，O-烷基，O-芳基，O-杂芳基，O-杂环烷基，CO-烷基，CO-芳基，CO-杂芳基，CO-杂环烷基，COO-烷基，NH 2，NH- 烷基，NH-芳基，N（烷基）2，NH-杂芳基，NH-杂环烷基，COOH，CONH 2，CONH-烷基，CON（烷基）2，CONH-芳基，CONH-杂芳基，CONHheterocycloalkyl，SO3H， SO 2 - 芳基，SO 2 - 杂芳基，SO 2 - 杂环烷基，SO 2 NH 2，SO 2 NH-烷基，SO 2 N（烷基）2，SO 2 NH-芳基，SO 2 NH-杂芳基或SO 2 NH-杂环烷基，其中所述烷基，芳基，杂芳基和杂环烷基任选被一个或多个选自卤代，NO 2，OH，O甲基，NH 2，COOH，CONH 2和CF 3的基团; 在制备用于治疗糖尿病的药物中。本发明的化合物还可用于治疗CNS疾病，脱发，心血管疾病和中风。

8. 发明申请

WO2009017795A1 INDAZOLE COMPOUNDS FOR TREATING INFLAMMATORY DISORDERS, DEMYELINATING DISORDERS AND CANCERS 审中-公开
标题翻译：用于治疗炎性疾病，脱发性疾病和癌症的INDAZOLE化合物
公开(公告)号：WO2009017795A1
公开(公告)日：2009-02-05
申请号：PCT/US2008/009263
申请日：2008-07-30
申请人： XANTHUS PHARMACEUTICALS, INC. , AJAMI, Alfred, M. , DUNCAN, Kenneth
发明人： AJAMI, Alfred, M. , DUNCAN, Kenneth
IPC分类号： C07D471/16 , A61P31/00 , A61P29/00 , A61P35/00 , A61K31/4745
CPC分类号： C07D471/16
摘要： Compounds of formula (I) or formula (Ia) and a method of treating a patient suffering from certain inflammatory disorders, demyelinating disorders, FLT3- mediated disorders, CSF-lR-mediated disorders, cancers and leukemias, comprising administering to said patient a therapeutically effective amount of a compound of formula (I) or formula (Ia) or a pharmaceutically acceptable salt thereof. (Ia). Definitions for the variables are provided herein.
摘要翻译：式（I）或式（Ia）的化合物和治疗患有某些炎性疾病，脱髓鞘疾病，FLT3介导的病症，CSF-1R介导的病症，癌症和白血病的患者的方法，包括向所述患者施用治疗有效量的式（I）或式（Ia）化合物或其药学上可接受的盐。（IA）。变量的定义在这里提供。

9. 发明申请

WO2004001070A1 SURROGATE MARKERS FOR THE DETERMINATION OF THE DISEASE STATUS OF AN INDIVIDUAL INFECTED BY MYCOBACTERIUM TUBERCULOSIS 审中-公开
标题翻译：用于确定由MYCOBACTERIUM TUBCCOSOS感染的个体疾病状况的标记
公开(公告)号：WO2004001070A1
公开(公告)日：2003-12-31
申请号：PCT/GB2003/002630
申请日：2003-06-18
申请人： GLAXO GROUP LIMITED , DUNCAN, Kenneth , LUKEY, Pauline, Teresa , MISTRY, Rohitbhai
发明人： DUNCAN, Kenneth , LUKEY, Pauline, Teresa , MISTRY, Rohitbhai
IPC分类号： C12Q1/68
CPC分类号： C12Q1/6883 , C12Q2600/158
摘要： The invention relates to a method of determining the disease status of an individual that has been or is infected with M. tuberculosis comprising: (a) obtaining a sample from an individual that has been or is infected with M. tuberculosis ; (b) analysing the expression of at least one polynucleotide sequence selected from the group consisting of: (i) a polynucleotide sequence comprising of any of SEQ ID No:1 to SEQ ID No:11; and(ii) any other wild type polynucleotide sequence encoding the same protein or peptide as that encoded by the polynucleotide sequences defined in (i) to generate a test expression pattern; and (c) comparing the test expression pattern with an expression pattern of an uninfected individual or an expression pattern of an individual that has been or is infected with M. tuberculosis and having a known disease status, and classifying the disease status of said individual on the basis of said comparison.
摘要翻译：本发明涉及确定已经或已被感染结核分枝杆菌的个体的疾病状态的方法，其包括：（a）获得已经或已被感染结核分枝杆菌的个体的样品; （b）分析至少一种选自以下的多核苷酸序列的表达：（i）包含SEQ ID No：1至SEQ ID No：11中任一个的多核苷酸序列; 和（ii）编码与（i）中定义的多核苷酸序列编码的相同蛋白质或肽相同的其它野生型多核苷酸序列以产生测试表达模式; 和（c）将测试表达模式与未感染个体的表达模式或已经或已被感染结核分枝杆菌并具有已知疾病状态的个体的表达模式进行比较，并将所述个体的疾病状态分类到比较的基础。

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