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1. 发明申请

WO2016075477A9 PROCESS FOR THE PURIFICATION OF THE AXL TYROSINE RECEPTOR KINASE INHIBITOR "R428" 审中-公开
标题翻译：用于纯化AXL酪氨酸受体激酶抑制剂“R428”的方法
公开(公告)号：WO2016075477A9
公开(公告)日：2017-07-06
申请号：PCT/GB2015053442
申请日：2015-11-13
申请人： BERGENBIO AS , JONES NICHOLAS ANDREW
发明人： PETERSEN LENE RAUNKJAER
IPC分类号： C07D403/04
CPC分类号： C07D403/14 , C07D403/04
摘要： A process for purifying 1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazine-3-yl)-N 3- (7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulene-2-yl)-1H-1,2,4-triazole-3,5- diamine free base is described, the process comprising a) dissolving a quantity of crude 1-(6,7-dihydro-5H- benzo[6,7]cyclohepta[1,2-c]pyridazine-3-yl)-N 3-(7-(pyrrolidin-1-yl)-6,7,8,9- tetrahydro-5H-benzo[7]annulene-2-yl)-1H-1,2,4-triazole-3,5-diamine in a mixed solvent of C1-5alcohol and water, together with an acid, and b) increasing the pH of the solution resulting from (a) until 1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazine-3-yl)-N 3-(7-(pyrrolidin-1-yl)-6,7,8,9- tetrahydro-5H-benzo[7]annulene-2-yl)-1H-1,2,4-triazole-3,5-diamine free base is precipitated from the alcohol-water mixed solvent.
摘要翻译：纯化1-（6,7-二氢-5H-苯并[6,7]环庚并[1,2-c]哒嗪-3-基）-N 3-（7-（吡咯烷-1-基） - 6,7,8,9-四氢-5H-苯并[7]轮烯-2-基）-1H-1,2,4-三唑-3,5-二胺游离碱的方法，该方法包括a）将（6,7-二氢-5H-苯并[6,7]环庚并[1,2-c]哒嗪-3-基）-N 3-（7-（吡咯烷-1-基）-6 ，7,8,9-四氢-5H-苯并[7]轮烯-2-基）-1H-1,2,4-三唑-3,5-二胺在C1-5醇和水的混合溶剂中与（a）得到的溶液的pH值提高至1-（6,7-二氢-5H-苯并[6,7]环庚并[1,2-c]哒嗪-3-基） - N 3-（7-（吡咯烷-1-基）-6,7,8,9-四氢-5H-苯并[7]轮烯-2-基）-1H-1,2,4-三唑-3,5 - 二胺游离碱从醇 - 水混合溶剂中沉淀出来。

2. 发明申请

WO2015082887A2 USE OF KINASE INHIBITORS 审中-公开
标题翻译：激酶抑制剂的使用
公开(公告)号：WO2015082887A2
公开(公告)日：2015-06-11
申请号：PCT/GB2014/053548
申请日：2014-11-28
申请人： BERGENBIO AS , JONES, Nicholas, Andrew
发明人： MICKLEM, David, Robert
IPC分类号： A61K31/4196
CPC分类号： A61K31/502 , A61K31/4196
摘要： The invention provides a compound for use for treating, preventing or managing a condition associated with the activation, mutation and/or over -expression of one or more kinases, wherein if the condition is associated with Axl over -expression, it is also associated with the activation, mutation and/or over-expression of one or more other kinases, and wherein the compound has a structure according to formula (I) : wherein the symbols used in formula (I) are as defined herein.
摘要翻译：本发明提供用于治疗，预防或控制与一种或多种激酶的活化，突变和/或过度表达相关的病症的化合物，其中如果所述病症与Axl结合 - 表达，其还与一种或多种其他激酶的激活，突变和/或过度表达有关，并且其中所述化合物具有根据式（I）的结构：其中式（I）中使用的符号为在此定义。

3. 发明申请

WO2010106331A8 MASS-SENSITIVE SENSOR COMPRISING IMMOBILISED CELLS ON ITS SURFACE AND METHOD OF DETECTING LIGAND BINDING MAKING USE OF THE SENSOR 审中-公开
标题翻译：在其表面上包含固定化细胞的质感传感器和检测配体结合的方法制造传感器的使用
公开(公告)号：WO2010106331A8
公开(公告)日：2011-10-13
申请号：PCT/GB2010000496
申请日：2010-03-19
申请人： ATTANA AB , KAECK CAMILLA , SAINT-GUIRONS JULIEN , INGEMARSSON BJOERN , LUNDELL KERSTIN , JONES NICHOLAS ANDREW
发明人： KAECK CAMILLA , SAINT-GUIRONS JULIEN , INGEMARSSON BJOERN , LUNDELL KERSTIN
IPC分类号： G01N33/543 , G01N21/55
CPC分类号： G01N33/54373 , C12N11/06 , G01N29/022 , G01N29/036 , G01N2291/0255 , G01N2291/0256 , G01N2291/0426
摘要： A mass-sensitive chemical sensor, the chemical sensor having inactivated cells adhered to a sensing surface thereof and being suitable for detection of an interaction between an analyte ligand and the adhered, inactive cells by means of the change in mass at the sensor surface due to binding of analyte ligand to the cells, wherein the sensor is provided with, or forms part of, a flow cell.
摘要翻译：一种质量敏感的化学传感器，其化学传感器具有粘附到其感测表面上的失活的细胞，并且适于通过传感器表面上的质量变化来检测分析物配体和被粘附的非活性细胞之间的相互作用，因为分析物配体与细胞的结合，其中传感器被提供有或形成流动池的一部分。

4. 发明申请

WO2010020799A3 COMPOSITIONS FOR THE TREATMENT OF NEOPLASTIC DISEASES 审中-公开
标题翻译：用于治疗神经疾病的组合物
公开(公告)号：WO2010020799A3
公开(公告)日：2010-10-14
申请号：PCT/GB2009002068
申请日：2009-08-24
申请人： SLOTERVAART PARTICIPATIES BV , STICHTING HET NL KANKER I , BEIJNEN JACOB HENDRIK , SCHELLENS JOHANNES HENRICUS MATTHIAS , MOES JOHANNES , NUIJEN BASTIAAN , JONES NICHOLAS ANDREW
发明人： BEIJNEN JACOB HENDRIK , SCHELLENS JOHANNES HENRICUS MATTHIAS , MOES JOHANNES , NUIJEN BASTIAAN
IPC分类号： A61K9/14 , A61K9/19 , A61K9/48 , A61K31/337 , A61K31/426 , A61K45/06 , A61P35/00
CPC分类号： A61K9/19 , A61K9/141 , A61K9/145 , A61K9/146 , A61K9/1617 , A61K9/1635 , A61K9/1652 , A61K9/1694 , A61K9/4858 , A61K9/4866
摘要： Solid pharmaceutical taxane compositions for oral administration comprising a substantially amorphous taxane, a carrier and a surfactant, wherein the substantially amorphous taxane is prepared by a solvent evaporation method and, in particular, spray drying. Methods of preparation of the composition and uses of the composition are also included.
摘要翻译：用于口服给药的固体药物紫杉烷组合物，其包含基本上无定形的紫杉烷，载体和表面活性剂，其中基本上无定形的紫杉烷通过溶剂蒸发法，特别是喷雾干燥制备。还包括组合物的制备方法和组合物的用途。

5. 发明申请

WO2009112823A3 METAL COMPLEXES 审中-公开
公开(公告)号：WO2009112823A3
公开(公告)日：2009-09-17
申请号：PCT/GB2009/000650
申请日：2009-03-10
申请人： UNIVERSITÄT ZÜRICH , ALBERTO, Roger , BRABAND, Henrik , JONES, Nicholas, Andrew
发明人： ALBERTO, Roger , BRABAND, Henrik , JONES, Nicholas, Andrew
IPC分类号： C07F13/00 , A61K51/00
摘要： A method for synthesizing a complex having the formula: [L3MO3]" wherein L 3 represents a tridentate ligand, M represents a metal selected from Tc an Re, and n is a charge from -2 to +1, the method comprising: a) reaction of pertechnetate or perrhenate with a reducing agent and L 3 , or b) reaction of pertechnetate or perrhenate with a Lewis acid and L 3 , wherein the synthesis (a) or (b) is carried out in an aqueous medium.

6. 发明申请

WO2008068516A1 CHELATING AGENT 审中-公开
标题翻译：电话代理
公开(公告)号：WO2008068516A1
公开(公告)日：2008-06-12
申请号：PCT/GB2007/004733
申请日：2007-12-10
申请人： TECHNISCHE UNIVERSITÄT MÜNCHEN , JONES, Nicholas, Andrew , KNÖR, Sebastian , MODLINGER, Armin , WESTER, Hans-Jürgen , KESSLER, Horst
发明人： KNÖR, Sebastian , MODLINGER, Armin , WESTER, Hans-Jürgen , KESSLER, Horst
IPC分类号： C07D257/02 , A61K31/395 , A61P35/00
CPC分类号： C07D257/02 , Y02P20/55
摘要： A compound of the formula: wherein R 1 is selected from H, methyl, ethyl, carboxyl protecting groups and hydrophilic moieties, R 2 and R 3 are independently selected from H, methyl, ethyl and carboxyl protecting groups, R 4 is selected from H, methyl, ethyl, hydrophilic moieties and carboxyl protecting groups, and R 5 is an aryl, heteroaryl, alkyl or a combination of these groups and is substituted with a carbonyl group, an aminooxy group or a functional group suitable for participating in a cycloaddition reaction. The compounds of the invention maybe useful as bifunctional chelating agents which allow chemoselective attachment to targeting molecules.
摘要翻译：下式的化合物：其中R 1选自H，甲基，乙基，羧基保护基和亲水部分，R 2和R 3 >独立地选自H，甲基，乙基和羧基保护基，R 4选自H，甲基，乙基，亲水部分和羧基保护基，R 5，是芳基，杂芳基，烷基或这些基团的组合，并被羰基，氨基氧基或适于参与环加成反应的官能团取代。本发明的化合物可用作双功能螯合剂，其允许化学选择性连接靶向分子。

7. 发明申请

WO2016075477A1 PROCESS FOR THE PURIFICATION OF THE AXL TYROSINE RECEPTOR KINASE INHIBITOR "R428" 审中-公开
标题翻译： AXL酪氨酸受体激酶抑制剂“R428”的纯化方法
公开(公告)号：WO2016075477A1
公开(公告)日：2016-05-19
申请号：PCT/GB2015/053442
申请日：2015-11-13
申请人： BERGENBIO AS , JONES, Nicholas Andrew
发明人： PETERSEN, Lene Raunkjaer
IPC分类号： C07D403/04
CPC分类号： C07D403/14 , C07D403/04
摘要： A process for purifying 1-(6,7-dihydro-5 H -benzo[6,7]cyclohepta[1,2-c]pyridazine-3-yl)- N 3 - (7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5 H -benzo[7]annulene-2-yl)-1 H -1,2,4-triazole-3,5- diamine free base is described, the process comprising a) dissolving a quantity of crude 1-(6,7-dihydro-5 H - benzo[6,7]cyclohepta[1,2-c]pyridazine-3-yl)- N 3 -(7-(pyrrolidin-1-yl)-6,7,8,9- tetrahydro-5 H -benzo[7]annulene-2-yl)-1 H -1,2,4-triazole-3,5-diamine in a mixed solvent of C 1-5 alcohol and water, together with an acid, and b) increasing the pH of the solution resulting from (a) until 1-(6,7-dihydro-5 H -benzo[6,7]cyclohepta[1,2-c]pyridazine-3-yl)- N 3 -(7-(pyrrolidin-1-yl)-6,7,8,9- tetrahydro-5 H -benzo[7]annulene-2-yl)-1 H -1,2,4-triazole-3,5-diamine free base is precipitated from the alcohol-water mixed solvent.
摘要翻译：纯化1-（6,7-二氢-5H-苯并[6,7]环庚并[1,2-c]哒嗪-3-基）-N 3 - （7-（吡咯烷-1-基） - 6,7,8,9-四氢-5H-苯并[7]环烯-2-基）-1H-1,2,4-三唑-3,5-二胺游离碱的方法，该方法包括：a）将粗品1-（6,7-二氢-5H-苯并[6,7]环庚并[1,2-c]哒嗪-3-基）-N 3 - （7-（吡咯烷-1-基）-6 ，7,8,9-四氢-5H-苯并[7]环烯-2-基）-1H-1,2,4-三唑-3,5-二胺在C1-5醇和水的混合溶剂中连同一种酸，和b）增加由（a）直到1-（6,7-二氢-5H-苯并[6,7]环庚并[1,2-c]哒嗪-3-基） - N 3-（7-（吡咯烷-1-基）-6,7,8,9-四氢-5H-苯并[7]环烯-2-基）-1H-1,2,4-三唑-3,5- - 二胺游离碱从醇 - 水混合溶剂中沉淀。

8. 发明申请

WO2012156676A1 MONOCLINIC CRYSTALLINE FORM OF ASENAPINE MALEATE WITH A SPECIFIC PARTICLE SIZE DISTRIBUTION 审中-公开
标题翻译：具有特定粒度分布的ASENAPINE MALEATE的单克隆晶体形式
公开(公告)号：WO2012156676A1
公开(公告)日：2012-11-22
申请号：PCT/GB2012/000449
申请日：2012-05-18
申请人： LABORATORIOS LESVI S.L. , FREIXAS PASCUAL, Glòria , SOLÀ CARANDELL, Lluis , CERÓN BERTRAN, Jordi , JONES, Nicholas Andrew
发明人： FREIXAS PASCUAL, Glòria , SOLÀ CARANDELL, Lluis , CERÓN BERTRAN, Jordi
IPC分类号： A61K31/407 , C07D491/04 , A61P25/18
CPC分类号： C07D491/044 , A61K31/407 , C07B2200/13 , C07D491/04 , Y10T428/2982
摘要： A monoclinic crystalline form of asenapine maleate is described, which is characterized in that it is not micronised and has a particle size distribution characterized by a d90 of 40 μm or less. A process for the preparation of a monoclinic crystalline form of asenapine maleate is also described, the process comprising the following steps: a) providing a mixture of monoclinic asenapine maleate and an organic solvent which, under the conditions of the process, acts as an antisolvent; b) stirring the mixture at a temperature between 15 and 60°C; and c) collecting the crystals, wherein the organic solvent is selected from alcohols, ketones, ethers, esters, hydrocarbons or mixtures thereof.
摘要翻译：描述了马来酸asenapine的单斜晶体形式，其特征在于其不是微粉化的，并且具有由d90为40μm或更小的特征的粒度分布。还描述了制备马来酸阿替平的单斜晶体形式的方法，所述方法包括以下步骤：a）提供马来酸单斜铁酸阿替平与有机溶剂的混合物，其在该方法的条件下作为反溶剂 ; b）在15至60℃的温度下搅拌该混合物; 和c）收集晶体，其中有机溶剂选自醇，酮，醚，酯，烃或其混合物。

9. 发明申请

WO2010106331A3 MASS-SENSITIVE SENSOR COMPRISING IMMOBILISED CELLS ON ITS SURFACE AND METHOD OF DETECTING LIGAND BINDING MAKING USE OF THE SENSOR 审中-公开
标题翻译：在其表面上包含固定化细胞的质感传感器和检测配体结合的方法制造传感器的使用
公开(公告)号：WO2010106331A3
公开(公告)日：2010-11-11
申请号：PCT/GB2010000496
申请日：2010-03-19
申请人： ATTANA AB , KAECK CAMILLA , SAINT-GUIRONS JULIEN , INGEMARSSON BJOERN , LUNDELL KERSTIN , JONES NICHOLAS ANDREW
发明人： KAECK CAMILLA , SAINT-GUIRONS JULIEN , INGEMARSSON BJOERN , LUNDELL KERSTIN
IPC分类号： G01N33/543 , G01N21/55
CPC分类号： G01N33/54373 , C12N11/06 , G01N29/022 , G01N29/036 , G01N2291/0255 , G01N2291/0256 , G01N2291/0426
摘要： A mass-sensitive chemical sensor, the chemical sensor having inactivated cells adhered to a sensing surface thereof and being suitable for detection of an interaction between an analyte ligand and the adhered, inactive cells by means of the change in mass at the sensor surface due to binding of analyte ligand to the cells, wherein the sensor is provided with, or forms part of, a flow cell.
摘要翻译：一种质量敏感的化学传感器，其化学传感器具有粘附到其感测表面上的失活的细胞，并且适于通过传感器表面上的质量变化来检测分析物配体和被粘附的非活性细胞之间的相互作用，因为分析物配体与细胞的结合，其中传感器被提供有或形成流动池的一部分。

10. 发明申请

WO2009027644A3 COMPOSITIONS FOR THE TREATMENT OF NEOPLASTIC DISEASES 审中-公开
标题翻译：用于治疗神经疾病的组合物
公开(公告)号：WO2009027644A3
公开(公告)日：2009-12-17
申请号：PCT/GB2008002854
申请日：2008-08-22
申请人： STICHTING HET NL KANKER I , SLOTERVAART PARTICIPATIES BV , BEIJNEN JACOB HENDRIK , SCHELLENS JOHANNES HENRICUS MATTHIAS , MOES JOHANNES , NUIJEN BASTIAAN , JONES NICHOLAS ANDREW
发明人： BEIJNEN JACOB HENDRIK , SCHELLENS JOHANNES HENRICUS MATTHIAS , MOES JOHANNES , NUIJEN BASTIAAN
IPC分类号： A61K9/14 , A61K9/19 , A61K9/48 , A61K31/337 , A61K31/426 , A61K45/06 , A61P35/00
CPC分类号： A61K9/146 , A61K9/19 , A61K9/4858 , A61K31/337 , A61K31/426 , A61K45/06 , A61K2300/00
摘要： Pharmaceutical compositions and methods for the treatment of neoplastic disease and comprising the combination of a taxane, such as docetaxel, with a CYP3A4 inhibitor, such as ritonavir. Methods of treatment of neoplastic disease incorporating the administration of a taxane and the administration of a CYP3A4 inhibitor, either simultaneously or separately, are also included. Further, kits for carrying out the methods are included. Solid pharmaceutical taxane compositions for oral administration comprising a substantially amorphous taxane, a carrier and a surfactant are also included.
摘要翻译：用于治疗肿瘤疾病并包含紫杉烷如多西紫杉醇与CYP3A4抑制剂如利托那韦的组合的药物组合物和方法。还包括同时或分别施用紫杉烷和施用CYP3A4抑制剂的肿瘤疾病的治疗方法。此外，还包括用于执行方法的套件。还包括用于口服给药的固体药物紫杉烷组合物，其包含基本上无定形的紫杉烷，载体和表面活性剂。

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