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1. 发明申请

WO0127632A3 CELLULAR RECEPTOR MUTATIONS PREDICTED BY MULTIPLE-SEQUENCE-ALLIGNMENT 审中-公开
标题翻译：细胞受体突变体由多个序列分配预测
公开(公告)号：WO0127632A3
公开(公告)日：2002-07-11
申请号：PCT/IB0001407
申请日：2000-10-02
申请人： BIOFOCUS DISCOVERY LTD , WENHAM DEAN , PACKER JEREMY CHARLES , WILLIAMS KATHLEEN M
发明人： WENHAM DEAN , PACKER JEREMY CHARLES
IPC分类号： C07K14/705 , C07K14/715 , C12N15/10 , C07K14/72 , G01N33/566
CPC分类号： C07K14/705 , C07K14/7158 , C12N15/102 , G01N2333/726
摘要： The invention relates to methods of predicting mutations that alter the activity of a receptor in a desired manner. The methods utilize multiple sequence alignment and phylogenetic profiling to identify the relatives of a given receptor that are most likely to provide useful data allowing prediction of sites to mutate in the given receptor. The methods provided are applicable to any type of receptor, and are particularly well suited for predicting sites to mutate in order to alter the activities of the so-called orphan receptors, for which no agonists are known.
摘要翻译：本发明涉及预测以所需方式改变受体活性的突变的方法。该方法利用多重序列比对和系统发育谱来鉴定给定受体的亲属，这些亲属最有可能提供有用数据，从而可以预测位点在给定受体中发生突变。所提供的方法适用于任何类型的受体，并且特别适用于预测位点突变，以便改变所谓的孤儿受体的活性，其中没有激动剂是已知的。

2. 发明申请

WO2005080390A1 IMIDAZOPYRIDINE DERIVATIVES AS BSR-3 ANTAGONISTS 审中-公开
标题翻译：咪唑吡啶衍生物作为BSR-3拮抗剂
公开(公告)号：WO2005080390A1
公开(公告)日：2005-09-01
申请号：PCT/GB2005/000547
申请日：2005-02-16
申请人： BIOFOCUS DISCOVERY LTD , WARD, Terence, James , CROSSLEY, Roger , SLATER, Martin, John
发明人： WARD, Terence, James , CROSSLEY, Roger , SLATER, Martin, John
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Compounds of the general formula (I): wherein X, Y, R and R’ are as described in the specification. Further included are pharmaceutical compositions comprising the compounds, processes for their preparation, as well as the use of the compounds for the preparation of a medicament against BRS-3 receptor-related disorders.
摘要翻译：通式（I）的化合物：其中X，Y，R和R'如说明书中所述。还包括包含该化合物的药物组合物，其制备方法，以及该化合物用于制备抗BRS-3受体相关病症的药物的用途。

3. 发明申请

WO2005103036A1 PYRIMIDIN-4-YL-1H-INDAZOL-5YL-AMINES AS CHK1 KINASES INHIBITORS 审中-公开
标题翻译：作为CHK1激酶抑制剂的吡咯烷-4-YL-1H-咪唑烷-5-胺
公开(公告)号：WO2005103036A1
公开(公告)日：2005-11-03
申请号：PCT/GB2005/001566
申请日：2005-04-22
申请人： BIOFOCUS DISCOVERY LTD , BIRAULT, Véronique , WOODLAND, Christopher, Andrew
发明人： BIRAULT, Véronique , WOODLAND, Christopher, Andrew
IPC分类号： C07D403/12
CPC分类号： C07D403/12 , C07D401/14
摘要： Compounds of Formula (I) wherein, R1 can be hydrogen, optionally substituted alkyl, optionally substituted alkoxy, OCF 3, CF 3, amino, optionally substituted aryloxy, halogen, hydroxy, CN, CO 2 H, NR 4 R 5 , CO 2 R 4 , CONR 4 R 5 , NR 4 (CO)R 5 or S(O) P R 4 ; wherein R 4 and R 5 , which can be the same or different, can be hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted heteroarylalkyl or optionally substituted arylalkyl; and wherein p is 1 or 2; R1 can be in the 3-, 4-, 6- or 7-position of the indazol ring; and R2 is optionally substituted aryl or optionally substituted heteroaryl are useful in the inhibition of protein kinases, in particular serine/threonine kinases, more particularly Chk1 kinase. The compounds can be used in medicine and particularly in the prevention and/or treatment of a wide variety of diseases including cancer, and disease states associated with angiogenesis and/or cellular proliferation.
摘要翻译：式（I）的化合物，其中R 1可以是氢，任选取代的烷基，任选取代的烷氧基，OCF 3，CF 3，氨基，任选取代的芳氧基，卤素，羟基，CN，CO 2 H，NR 4 R 5， 4，CONR 4 R 5，NR 4（CO）R 5或S（O）PR 4; 其中R 4和R 5可以相同或不同，可以是氢，任选取代的烷基，任选取代的芳基，任选取代的杂芳基烷基或任选取代的芳基烷基; 并且其中p为1或2; R1可以在吲唑环的3-，4-，6-或7-位; 并且R 2是任选取代的芳基或任选取代的杂芳基可用于抑制蛋白激酶，特别是丝氨酸/苏氨酸激酶，更特别的是Chk1激酶。所述化合物可用于医学中，特别是用于预防和/或治疗各种疾病，包括癌症，以及与血管发生和/或细胞增殖相关的疾病状态。

4. 发明申请

WO2005003101A2 COMPOUNDS WHICH BIND TO THE ACTIVE SITE OF PROTEIN KINASE ENZYMES 审中-公开
标题翻译：与蛋白激酶酶活性位点结合的化合物
公开(公告)号：WO2005003101A2
公开(公告)日：2005-01-13
申请号：PCT/GB2004002849
申请日：2004-07-01
申请人： BIOFOCUS DISCOVERY LTD , BIRAULT VERONIQUE , HARRIS JOHN C
发明人： BIRAULT VERONIQUE , HARRIS JOHN C
IPC分类号： C07D213/74 , C07D241/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/14 , C07D241/00
CPC分类号： C07D213/74 , C07D241/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/14
摘要： The present invention relates to a compound and a group of compounds which are inhibitors of Rho kinase (ROK, ROCK). In addition, the invention relates to methods of treatment and use of the compounds in the manufacture of a medicament for application to a number of therapeutic indications including cardiovascular disease (coronary vasospasm, hypertensive disease, arteriosclerosis), stroke, cancer, erectile dysfunction, asthma, osteoporosis, glaucoma and AIDS. The compounds can be used in screening programmes against protein kinases. The invention also provides methods for making compounds and libraries that include these compounds.
摘要翻译：本发明涉及作为Rho激酶（ROK，ROCK）抑制剂的化合物和一组化合物。此外，本发明涉及治疗和使用化合物在制备用于多种治疗适应症的药物中的应用的方法，包括心血管疾病（冠状动脉血管痉挛，高血压疾病，动脉硬化），中风，癌症，勃起功能障碍，哮喘，骨质疏松症，青光眼和艾滋病。该化合物可用于抗蛋白激酶的筛选方案。本发明还提供了制备包含这些化合物的化合物和文库的方法。

5. 发明申请

WO02095400A3 METHODS FOR IDENTIFYING RECEPTOR UP- AND DOWNMODULATORS 审中-公开
标题翻译：识别受体上和下载体的方法
公开(公告)号：WO02095400A3
公开(公告)日：2003-09-18
申请号：PCT/IB0202990
申请日：2002-05-16
申请人： BIOFOCUS DISCOVERY LTD , CHADWICK MARK P , COSSET FRANCOIS-LOIS , LAVILLETTE DIMITRI
发明人： CHADWICK MARK P , COSSET FRANCOIS-LOIS , LAVILLETTE DIMITRI
IPC分类号： G01N33/50 , G01N33/566 , G01N33/58
CPC分类号： G01N33/5091 , G01N33/5008 , G01N33/5011 , G01N33/566 , G01N33/58 , G01N33/582 , G01N2333/05 , G01N2333/705 , G01N2333/70578 , G01N2333/71 , G01N2333/726
摘要： The invention provides assays for identifying a receptor modulator wherein a transferable label is contacted with a candidate receptor modulator, a fusion protein comprising a viral receptor binding moiety and a ligand, and a target cell that expresses a cell surface-ligand-receptor. Alternatively, a virus particle comprising a mutant envelope protein, wherein the virus particle can bind to a viral receptor but demonstrates impaired entry into a cell, and further comprising a transferable label is contacted with a fusion protein comprising a viral receptor binding moiety and a ligand, and a target cell that expresses a cell surface receptor capable of binding to the ligand of the fusion protein. Binding of the fusion protein to a virus receptor on the target cell inhibits or activates transfer of the transferable label from the virus particle to the cell.
摘要翻译：本发明提供用于鉴定受体调节剂的测定法，其中可转移标记物与候选受体调节剂，包含病毒受体结合部分和配体的融合蛋白以及表达细胞表面 - 配体 - 受体的靶细胞接触。或者，包含突变包膜蛋白的病毒颗粒，其中所述病毒颗粒可以结合病毒受体，但是表现出进入细胞受损，并且进一步包含可转移标记物与包含病毒受体结合部分和配体的融合蛋白接触，以及表达能够结合融合蛋白的配体的细胞表面受体的靶细胞。融合蛋白与靶细胞上的病毒受体的结合抑制或激活可转移标记从病毒颗粒转移到细胞。

6. 发明申请

WO2004085409A3 COMPOUNDS AND LIBRARIES OF PYRIDINES, PYRAZINES, IMIDAZO[1,2-A]PYRAZINES AND 1H-IMIDAZO[4,5-B]PYRAZIN-2-ONES AND FIRST AND SECOND MEDICAL USES THEREOF 审中-公开
标题翻译：吡啶，吡嗪，咪唑并[1,2-A]吡啶和1H-咪唑并[4,5-B]吡嗪-2-酮的化合物和文库及其第一和第二医疗用途
公开(公告)号：WO2004085409A3
公开(公告)日：2004-12-23
申请号：PCT/GB2004001399
申请日：2004-03-26
申请人： BIOFOCUS DISCOVERY LTD , HARRIS JOHN , CHURCH NICOLA , PROUD ANDREW , KLING MARCEL , VICKERY BENJAMIN D
发明人： HARRIS JOHN , CHURCH NICOLA , PROUD ANDREW , KLING MARCEL , VICKERY BENJAMIN D
IPC分类号： A61P3/10 , A61P29/00 , A61P35/00 , A61P35/04 , C07D213/74 , C07D241/18 , C07D241/20 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/14 , C07D487/04
CPC分类号： C07D213/74 , C07D241/18 , C07D241/20 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/14 , C07D487/04
摘要： The present invention relates to pyridine,pyrazine,imidoz[1,2a]pyrazine and 1H-imidoz[4,5-b]pyrazin-2-one compounds capable of binding to the active site of protein kinase enzymes. The invention further relates to libraries of these compounds and a family of libraries of these compounds for use in screening programmes against protein kinases as well as the individual compounds for use in hit to lead and lead optimisation projects, and similar stages in the drug discovery process. The invention also provides methods for making compounds and libraries, thereof.
摘要翻译：本发明涉及能够结合蛋白激酶的活性位点的吡啶，吡嗪，亚氨基[1,2a]吡嗪和1H-亚氨基[4,5-b]吡嗪-2-酮化合物。本发明还涉及这些化合物的文库以及用于筛选针对蛋白激酶的程序的这些化合物的文库族，以及用于命中铅和优化项目的单个化合物，以及药物发现过程中的类似阶段。本发明还提供了制备其化合物和文库的方法。

7. 发明申请

WO2004085409A2 COMPOUND LIBRARIES 审中-公开
标题翻译：复合图书馆
公开(公告)号：WO2004085409A2
公开(公告)日：2004-10-07
申请号：PCT/GB2004/001399
申请日：2004-03-26
申请人： BIOFOCUS DISCOVERY LTD , HARRIS, John , CHURCH, Nicola , PROUD, Andrew , KLING, Marcel , VICKERY, Benjamin, D.
发明人： HARRIS, John , CHURCH, Nicola , PROUD, Andrew , KLING, Marcel , VICKERY, Benjamin, D.
IPC分类号： C07D241/00
CPC分类号： C07D213/74 , C07D241/18 , C07D241/20 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/14 , C07D487/04
摘要： The present invention relates to compounds capable of binding to the active site of protein kinase enzymes. The invention further relates to libraries of compounds and a family of libraries of compounds for use in screening programmes against protein kinases as well as the individual compounds for use in hit to lead and lead optimisation projects, and similar stages in the drug discovery process. The invention also provides methods for making compounds and libraries.
摘要翻译：本发明涉及能够结合蛋白激酶的活性位点的化合物。本发明还涉及化合物文库和用于筛选针对蛋白激酶的程序的化合物文库族，以及用于引导和引导优化项目的命中的个体化合物，以及药物发现过程中的类似阶段。本发明还提供了制备化合物和文库的方法。

8. 发明申请

WO0159446A3 ASSAY FOR DETECTING CHANGE IN MEMBRANE POTENTIAL 审中-公开
标题翻译：用于检测膜电位变化的测定
公开(公告)号：WO0159446A3
公开(公告)日：2002-03-14
申请号：PCT/GB0100516
申请日：2001-02-09
申请人： BIOFOCUS DISCOVERY LTD , CASTLE NEIL
发明人： CASTLE NEIL
IPC分类号： G01N33/50 , G01N33/68
CPC分类号： G01N33/5076
摘要： Improved methods for detecting changes in ion channel activity are described. A membrane with first and second ion channels is provided. The transmembrane potential of the membrane is predominantly set by the first or second ion channel, which are in dominant/recessive relationship and have opposite effects on the transmembrane potential. When the first ion channel is dominant, inhibition of that ion channel allows the second ion channel to predominantly set the transmembrane potential. Because the ion channels have opposite effects on the transmembrane potential, the magnitude of the change in transmembrane potential when the first ion channel is inhibited is greater than the magnitude of the change when the first ion channel is inhibited in the absence of the second ion channel. Such enhanced changes in transmembrane potential are more readily detectable. The methods can be used as screening assays to identify inhibitors of ion channel activity. Corresponding methods allowing identification of activators and enhancers of ion channel activity are also described.
摘要翻译：描述了用于检测离子通道活性变化的改进方法。提供具有第一和第二离子通道的膜。膜的跨膜电位主要由第一或第二离子通道设定，其处于显性/隐性关系，并且对跨膜电位具有相反的作用。当第一离子通道占优势时，该离子通道的抑制允许第二离子通道主要设定跨膜电位。因为离子通道对跨膜电位具有相反的作用，所以当第一离子通道被抑制时，跨膜电位变化的大小大于当不存在第二离子通道时第一离子通道被抑制时的变化幅度。跨膜电位的这种增强的变化更易于检测。该方法可用作筛选测定以鉴定离子通道活性的抑制剂。还描述了允许鉴定离子通道活性的活化剂和增强剂的相应方法。

9. 发明申请

WO0125477A3 KINASE AND PHOSPHATASE ASSAYS 审中-公开
标题翻译：激酶和磷酸酶测定
公开(公告)号：WO0125477A3
公开(公告)日：2002-01-31
申请号：PCT/GB0003736
申请日：2000-09-29
申请人： BIOFOCUS DISCOVERY LTD , FREARSON JULIE ANN
发明人： FREARSON JULIE ANN
IPC分类号： C12Q1/42 , C12Q1/48 , G01N33/573
CPC分类号： C12Q1/485 , C12Q1/42 , G01N2500/00
摘要： Methods for screening for modulators of kinase or phosphatase activity are described. The methods comprise: a) providing a serine or threonine kinase and a substrate which can be phosphorylated by the kinase; b) contacting the kinase with its substrate in the presence and absence of a candidate modulator of the activity of the kinase under conditions which permit phosphorylation of the substrate by the kinase; c) contacting the substrates treated according to step (b) with a reporter, excluding a natural antibody, which binds phosphorylated substrate with higher affinity than unphosphorylated substrate; and d) comparing binding of the reporter to the substrate treated according to step (b) in the presence of the candidate modulator with binding of the reporter to the substrate treated according to step (b) in the absence of the candidate modulator. Examples of reporters for use in such assays include 14-3-3 proteins and WW domain containing proteins.
摘要翻译：描述了筛选激酶或磷酸酶活性调节剂的方法。所述方法包括：a）提供可由激酶磷酸化的丝氨酸或苏氨酸激酶和底物; b）在允许由激酶磷酸化底物的条件下，在存在和不存在激酶活性的候选调节剂的情况下，使激酶与其底物接触; c）使根据步骤（b）处理的底物与不含天然抗体的报告基团接触，所述报告物以比非磷酸化底物更高的亲和力结合磷酸化底物; 以及d）比较在候选调节剂存在下报告基团与根据步骤（b）处理的底物的结合，所述候选调节剂在不存在候选调节剂的情况下结合报道基因与根据步骤（b）处理的底物结合。用于此类测定的记者的实例包括14-3-3蛋白质和含有WW结构域的蛋白质。

10. 发明专利

GB0510880D0 Compound library 未知
公开(公告)号：GB0510880D0
公开(公告)日：2005-07-06
申请号：GB0510880
申请日：2005-05-27
申请人： BIOFOCUS DISCOVERY LTD

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