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1. 发明申请

WO2005040802A3 CYLIN BINDING PEPTIDES, AND THEIR USE IN DRUG SCREENING ASSAYS 审中-公开
标题翻译： CYLIN BINDING PEPTIDES，及其在药物筛选测定中的应用
公开(公告)号：WO2005040802A3
公开(公告)日：2005-09-15
申请号：PCT/GB2004004431
申请日：2004-10-20
申请人： CYCLACEL LTD , ZHELEVA DANIELLA I , FISCHER PETER M , MCINNES CAMPBELL , ANDREWS MARTIN J I , CHAN WENG C , ATKINSON GAIL E
发明人： ZHELEVA DANIELLA I , FISCHER PETER M , MCINNES CAMPBELL , ANDREWS MARTIN J I , CHAN WENG C , ATKINSON GAIL E
IPC分类号： A61K38/00 , A61K38/08 , C07K7/06 , G01N33/573 , G01N33/574 , A61K38/17 , C07K14/47 , G01N33/68
CPC分类号： G01N33/573 , A61K38/00 , G01N33/574
摘要： The present invention relates to p2l derived peptides capable of inhibiting CDK/cyclin complexes, particularly cyclins A or E/CDK2, by modifying the interaction with their substrates. The peptides are derived from a C-terminal region of p2l. and display selectivity for cyclin/CDK2 inhibition over cyclin/CDK4 inhibition. Variants of such peptides particularly involving certain alanine replacements are shown to be particularly potent.
摘要翻译：本发明涉及通过改变与其底物的相互作用能够抑制CDK /细胞周期蛋白复合物，特别是细胞周期蛋白A或E / CDK2的p2l衍生肽。肽衍生自p2的C末端区。并显示细胞周期蛋白/ CDK2抑制对细胞周期蛋白/ CDK4抑制的选择性。特别涉及某些丙氨酸替代物的这些肽的变体显示特别有效。

2. 发明申请

WO0140142A3 P21 DERIVED PEPTIDES CAPABLE OF INHIBITING CDK/CYCLIN COMPLEXES 审中-公开
标题翻译： P21可抑制CDK / CYCLIN复合物的衍生肽
公开(公告)号：WO0140142A3
公开(公告)日：2002-05-10
申请号：PCT/GB0004550
申请日：2000-11-29
申请人： CYCLACEL LTD , ZHELEVA DANIELLA I , FISCHER PETER M , MCINNES CAMPBELL , ANDREWS MARTIN J I , CHAN WENG C , ATKINSON GAIL E
发明人： ZHELEVA DANIELLA I , FISCHER PETER M , MCINNES CAMPBELL , ANDREWS MARTIN J I , CHAN WENG C , ATKINSON GAIL E
IPC分类号： A61K38/00 , A61P35/00 , C07K14/47 , A61K38/17 , G01N33/68
CPC分类号： C07K14/4738 , A61K38/00
摘要： The present invention relates to p21 derived peptides capable of inhibiting CDK/cyclin complexes, particularly cyclins A or E/CDK2, by modifying the interaction with their substrates. The peptides are derived from a C-terminal region of p21 and display selectivity for cyclin/CDK2 inhibition over cyclin/CDK4 inhibition. Variants of such peptides particularly involving certain alanine replacements are shown to be particularly potent.
摘要翻译：本发明涉及通过改变与其底物的相互作用能够抑制CDK /细胞周期蛋白复合物，特别是细胞周期蛋白A或E / CDK2的p21衍生肽。肽衍生自p21的C末端区域，并显示细胞周期蛋白/ CDK2抑制对细胞周期蛋白/ CDK4抑制的选择性。特别涉及某些丙氨酸替代物的这些肽的变体显示特别有效。

3. 发明申请

WO2005042565A3 CYCLIN GROOVE INHIBITORS 审中-公开
标题翻译： CYCLIN GROVE抑制剂
公开(公告)号：WO2005042565A3
公开(公告)日：2005-08-11
申请号：PCT/GB2004004454
申请日：2004-10-21
申请人： CYCLACEL LTD , ANDREWS MARTIN J I , MCINNES CAMPBELL , KONTOPIDIS GEORGE , FISCHER PETER M
发明人： ANDREWS MARTIN J I , MCINNES CAMPBELL , KONTOPIDIS GEORGE , FISCHER PETER M
IPC分类号： A61K38/00 , C07K14/47 , G01N33/50 , G01N33/68 , C07K5/00 , C07K5/02 , C07K7/00 , C07K7/02 , G01N33/574 , G06F19/00
CPC分类号： C07K14/4738 , A61K38/00 , G01N33/5011 , G01N33/6872 , G01N2333/4739 , G01N2333/91205 , G01N2500/02
摘要： The present invention relates to a compound of formula (I), or a variant thereof, A - (B)m - C - (D)n- E, wherein m and n are each independently 0 or 1 and A, B, C, D and E are each independently linked to the respective adjacent residue by a linker group independently selected from carboxamide, reduced carboxamide, sulfonamide, imine, semicarbazone, oxime and ethanolamine; A is (i) a natural or unnatural amino acid residue having a side chain comprising at least one H-bond acceptor moiety and at least one H-bond donor moiety, or a derivative thereof; or (ii) R(CO), wherein R is a C1-C24 hydrocarbyl group comprising at least one H-bond acceptor moiety and optionally one or more H-bond donor moieties, and where R optionally contains one or more heteroatoms selected from S, O, and N, and is optionally substituted by one or more substituents selected from halogen, OMe, CN, CF3, and NO2; each of B and D is independently an amino acid residue selected from arginine, 4-(guanidinyl)phenylalanine (4-(Gu)Phe), piperidinylglycine (PipGly), piperidinylalanine (PipAla), pyridinylalanine, histamine, N,N-(dimethyl) lysine (DMLys), citrulline, glutamine, serine, lysine, asparagine, isoleucine and alanine, or a derivative thereof; C is NH-X-CO, where X is a C1-C4 alkylene group substituted by a straight-chain or branched C1-C6 alkylene group, said C1-C6 alkylene group optionally containing a H-bond donor or H-bond acceptor moiety; E is (i) a natural or unnatural amino acid residue having an aryl or heteroaryl side chain, or a derivative thereof; or (ii) NHR', where R' is a C1-C24 hydrocarbyl group, optionally containing one or more heteroatoms selected from N, O, and S, and optionally comprising one or more H-bond acceptor or donor moieties; said hydrocarbyl group further comprising a pendent C4-C12 aryl or heteroaryl group, which itself may be optionally substituted by one or more substituents selected from a H-bond donor moiety, a H-bond acceptor moiety, a halogen, Me, Et, Pr, CF3, CN and NO2; wherein at least one of A and E is other than a natural or unnatural amino acid residue when A, B, C, D and E are each linked to the respective adjacent residue by a carboxamide group.
摘要翻译：本发明涉及式（I）化合物或其变体，A - （B）m -C-（D）n-E，其中m和n各自独立地为0或1，A，B，C D和E各自独立地通过独立地选自羧酰胺，还原羧酰胺，磺酰胺，亚胺，缩氨基脲，肟和乙醇胺的连接基团相应地相邻的相邻残基连接。 A是（i）具有侧链的天然或非天然氨基酸残基，所述侧链包含至少一个H键受体部分和至少一个H键供体部分或其衍生物; 或（ii）R（CO），其中R是包含至少一个H键受体部分和任选的一个或多个H键供体部分的C 1 -C 24烃基，并且其中R任选地含有一个或多个选自S ，O和N，并且任选地被一个或多个选自卤素，OMe，CN，CF 3和NO 2的取代基取代; B和D中的每一个独立地为选自精氨酸，4-（胍基）苯丙氨酸（4-（Gu）Phe），哌啶基甘氨酸（PipGly），哌啶基丙氨酸（PipAla），吡啶丙氨酸，组胺，N，N- ）赖氨酸（DMLys），瓜氨酸，谷氨酰胺，丝氨酸，赖氨酸，天冬酰胺，异亮氨酸和丙氨酸或其衍生物; C是NH-X-CO，其中X是被直链或支链C1-C6亚烷基取代的C1-C4亚烷基，所述C1-C6亚烷基任选地含有H-键供体或H-键受体部分 ; E是（i）具有芳基或杂芳基侧链的天然或非天然氨基酸残基或其衍生物; 或（ii）NHR'，其中R'是C 1 -C 24烃基，任选地含有一个或多个选自N，O和S的杂原子，并任选地包含一个或多个H键受体或供体部分; 所述烃基还包含悬挂的C 4 -C 12芳基或杂芳基，其本身可以任选地被一个或多个选自H键供体部分，H-键受体部分，卤素，Me，Et，Pr ，CF3，CN和NO2; 其中当A，B，C，D和E各自通过羧酰胺基团连接到相应的相邻残基时，A和E中的至少一个不是天然或非天然氨基酸残基。

4. 发明申请

WO2007042786A3 4 -HETEROARYL PYRIMIDINE DERIVATIVES AND USE THEREOF AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译： 4 -HETEROARYL PYRIMIDINE衍生物及其作为蛋白激酶抑制剂的用途
公开(公告)号：WO2007042786A3
公开(公告)日：2007-06-07
申请号：PCT/GB2006003751
申请日：2006-10-09
申请人： CYCLACEL LTD , 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 , A61P29/00 , A61P31/12 , A61P35/00 , C07D401/14 , C07D403/04
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。

5. 发明申请

WO2005052147A3 METHOD OF SCREENING FOR A MODULATOR OF CDK4 审中-公开
标题翻译： CDK4调节剂筛选方法
公开(公告)号：WO2005052147A3
公开(公告)日：2005-11-24
申请号：PCT/GB2004004793
申请日：2004-11-11
申请人： CYCLACEL LTD , MCINNES CAMPBELL , THOMAS MARK , WANG SHUDONG , MCLACHLAN JANICE , MEADES CHRISTOPHER , KONTOPIDIS GEORGE , WOOD GAVIN , FISCHER PETER
发明人： MCINNES CAMPBELL , THOMAS MARK , WANG SHUDONG , MCLACHLAN JANICE , MEADES CHRISTOPHER , KONTOPIDIS GEORGE , WOOD GAVIN , FISCHER PETER
IPC分类号： C12N9/12 , C12Q1/48 , G06F19/00 , G06F19/16
CPC分类号： C12N9/1205 , C12Q1/485 , C40B30/02 , G01N2500/04 , G06F19/16 , G06F19/706 , Y02A90/24 , Y02A90/26
摘要： The present invention relates to a homology model for CDK4, and the use thereof in assays for the identification of small molecule CDK4 modulators. The invention further relates to CDK4 modulators identified by said assays, and their use in the treatment of CDK4-related disorders such as proliferative disorders.
摘要翻译：本发明涉及CDK4的同源性模型，以及其用于鉴定小分子CDK4调节剂的测定中的用途。本发明还涉及通过所述测定法鉴定的CDK4调节剂及其在治疗CDK4相关疾病如增殖性疾病中的用途。

6. 发明申请

WO2005047526A2 METHOD 审中-公开
标题翻译：方法
公开(公告)号：WO2005047526A2
公开(公告)日：2005-05-26
申请号：PCT/GB2004004762
申请日：2004-11-12
申请人： CYCLACEL LTD , MCINNES CAMPBELL , MCLACHLAN JANICE , MEZNA MOKDAD , FISCHER PETER
发明人： MCINNES CAMPBELL , MCLACHLAN JANICE , MEZNA MOKDAD , FISCHER PETER
IPC分类号： C07D311/22 , C07D417/04 , C07D473/16 , C07D491/16 , C07D493/06 , C07K14/47 , C12N9/12 , C12Q1/48 , G06F17/50 , C12Q1/00
CPC分类号： C07D493/06 , C07D311/22 , C07D417/04 , C07D473/16 , C07K2299/00 , C12N9/1205 , G01N2333/9121 , G01N2500/02 , Y02A90/24 , Y02A90/26
摘要： The present invention relates to a homology model for PLK, and the use thereof in assays for the indentification of small molecule PLK modulators. The invention further relates to PLK modulators identified by said assays, and their use in the treatment of PLK-related disorders such as proliferative disorders.
摘要翻译：本发明涉及PLK的同源性模型，以及其在小分子PLK调节剂识别测定中的应用。本发明还涉及通过所述测定鉴定的PLK调节剂及其在治疗PLK相关疾病如增殖性疾病中的用途。

7. 发明专利

SI1567522T1 Pirimidinske spojine 未知
公开(公告)号：SI1567522T1
公开(公告)日：2008-02-29
申请号：SI200331044
申请日：2003-11-14
申请人： CYCLACEL LTD
发明人： WANG SHUDONG , MEADES CHRISTOPHER , WOOD GAVIN , O'BOYLE JANICE , MCINNES CAMPBELL , FISCHER PETER
IPC分类号： C07D417/00 , A61K31/00 , A61K31/506 , A61K31/513 , A61P35/00 , C07D417/04

8. 发明专利

DE60316468D1 未知
公开(公告)号：DE60316468D1
公开(公告)日：2007-10-31
申请号：DE60316468
申请日：2003-11-14
申请人： CYCLACEL LTD
发明人： WANG SHUDONG , MEADES CHRISTOPHER , WOOD GAVIN , O'BOYLE JANICE , MCINNES CAMPBELL , FISCHER PETER
IPC分类号： C07D417/04 , A61K31/506 , A61K31/513 , A61P35/00

9. 发明专利

GB2358864B Peptides 未知
公开(公告)号：GB2358864B
公开(公告)日：2002-11-13
申请号：GB0029151
申请日：2000-11-29
申请人： CYCLACEL LTD
发明人： ZHELEVA DANIELLA I , FISCHER PETER MARTIN , MCINNES CAMPBELL , ANDREWS MARTIN J I , CHAN WENG C , ATKINSON GAIL E
IPC分类号： A61K38/00 , A61P35/00 , C07K14/47 , C07K7/06 , A61K38/08 , A61K38/12 , C07K5/04 , C07K7/52 , G01N33/68

10. 发明专利

GB2358864A Peptide inhibitors of Cdk/cyclin complexes derived from p21waf1 未知
公开(公告)号：GB2358864A
公开(公告)日：2001-08-08
申请号：GB0029151
申请日：2000-11-29
申请人： CYCLACEL LTD
发明人： ZHELEVA DANIELLA I , FISCHER PETER MARTIN , MCINNES CAMPBELL , ANDREWS MARTIN J I , CHAN WENG C , ATKINSON GAIL E
IPC分类号： A61K38/00 , A61P35/00 , C07K14/47 , C07K7/06 , A61K38/08 , A61K38/12 , C07K5/04 , C07K7/52 , G01N33/68
摘要： Peptides which have the sequence of SEQ ID NOS: 1, 2 or 3 or variants of these peptides are claimed. These are derived from p21 WAF1 corresponding to p21 C terminal amino acids 149-159 and typically contain the conserved region XLXF or variants upon this region. Such peptides are preferential inhibitors of the CDK2/cyclin complex rather than the CDK4/cyclin complex. In alternative embodiments of the invention many different amino acid substitutions are claimed, especially specific alanine replacements, as are cyclic forms of these peptides. The use of these compounds in medicaments is claimed. Assays for substances that bind or interact with cyclin/CDK complexes are alternatively claimed. Also claimed are drug screening assays for substances that bind in the cyclin groove or to specific cyclin A amino acids.

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