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1. 发明申请

US20140045836A1 [1,2,4]TRIAZOLO[1,5-C]PYRIMIDINE DERIVATIVES AS HSP90 MODULATORS 审中-公开
标题翻译： [1,2,4]三唑并[1,5-C]嘧啶衍生物作为HSP90调节剂
公开(公告)号：US20140045836A1
公开(公告)日：2014-02-13
申请号：US14055388
申请日：2013-10-16
申请人： Elena Casale , Francesco Casuscelli , Claudio Dalvit , Paolo Polucci , Fabio Zuccotto
发明人： Elena Casale , Francesco Casuscelli , Claudio Dalvit , Paolo Polucci , Fabio Zuccotto
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to [1,2,4]triazolo[1,5-c]pyrimidine derivatives which inhibit the activity of Heat Shock Protein Hsp90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, methods of treating diseases and the pharmaceutical compositions comprising these compounds.
摘要翻译：本发明涉及抑制热休克蛋白Hsp90活性的[1,2,4]三唑并[1,5-c]嘧啶衍生物。因此，本发明的化合物可用于治疗增殖性疾病如癌症和神经变性疾病。本发明还提供了制备这些化合物的方法，治疗疾病的方法和包含这些化合物的药物组合物。

2. 发明授权

US08580783B2 [1,2,4]triazolo [1,5-c]pyrimidine derivatives as Hsp90 modulators 失效
标题翻译： [1,2,4]三唑并[1,5-c]嘧啶衍生物，为Hsp90调节剂
公开(公告)号：US08580783B2
公开(公告)日：2013-11-12
申请号：US13394255
申请日：2010-09-03
申请人： Elena Casale , Francesco Casuscelli , Claudio Dalvit , Paolo Polucci , Fabio Zuccotto
发明人： Elena Casale , Francesco Casuscelli , Claudio Dalvit , Paolo Polucci , Fabio Zuccotto
IPC分类号： A61K31/519 , A61K31/5377 , C12N9/99 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention relates to [1,2,4]triazolo[1,5-c]pyrimidine derivatives of formula (I) which inhibit the activity of Heat Shock Protein Hsp90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, methods of treating diseases and the pharmaceutical compositions comprising these compounds.
摘要翻译：本发明涉及抑制热休克蛋白Hsp90活性的式（I）的[1,2,4]三唑并[1,5-c]嘧啶衍生物。因此，本发明的化合物可用于治疗增殖性疾病如癌症和神经变性疾病。本发明还提供了制备这些化合物的方法，治疗疾病的方法和包含这些化合物的药物组合物。

3. 发明申请

US20120184546A1 [1,2,4]TRIAZOLO [1,5-C]PYRIMIDINE DERIVATIVES AS HSP90 MODULATORS 失效
标题翻译： [1,2,4]三唑并[1,5-C]嘧啶衍生物作为HSP90调节剂
公开(公告)号：US20120184546A1
公开(公告)日：2012-07-19
申请号：US13394255
申请日：2010-09-03
申请人： Elena Casale , Francesco Casuscelli , Claudio Dalvit , Paolo Polucci , Fabio Zuccotto
发明人： Elena Casale , Francesco Casuscelli , Claudio Dalvit , Paolo Polucci , Fabio Zuccotto
IPC分类号： A61K31/519 , C12N9/99 , A61P35/00 , C07D487/04 , A61K31/5377
CPC分类号： C07D487/04
摘要： The present invention relates to [1,2,4]triazolo[1,5-c]pyrimidine derivatives of formula (I) which inhibit the activity of Heat Shock Protein Hsp90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, methods of treating diseases and the pharmaceutical compositions comprising these compounds.
摘要翻译：本发明涉及抑制热休克蛋白Hsp90活性的式（I）的[1,2,4]三唑并[1,5-c]嘧啶衍生物。因此，本发明的化合物可用于治疗增殖性疾病如癌症和神经变性疾病。本发明还提供了制备这些化合物的方法，治疗疾病的方法和包含这些化合物的药物组合物。

4. 发明授权

US07255985B2 Fluorine NMR spectroscopy for biochemical screening 失效
标题翻译：氟化NMR光谱用于生化筛选
公开(公告)号：US07255985B2
公开(公告)日：2007-08-14
申请号：US10888378
申请日：2004-07-09
申请人： Claudio Dalvit , Elena Ardini , Maria Magdalena Flocco , Gianpaolo Fogliatto , Nicola Mongelli , Marina Veronesi
发明人： Claudio Dalvit , Elena Ardini , Maria Magdalena Flocco , Gianpaolo Fogliatto , Nicola Mongelli , Marina Veronesi
IPC分类号： C12Q1/00 , C12Q1/48
CPC分类号： C12Q1/485
摘要： High-Throughput Screening (HTS) of large compound libraries is the method of drug-lead discovery. It is now well accepted that for a functional assay, quality is more important than quantity. A biochemical NMR method originally proposed by Percival and Withers (Biochemistry, 1992, 31, 498–505) is extended to the screening of Ser/Thr kinases. The method requires the presence of a CF3 (or CF) moiety on the substrate and utilizes 19F NMR spectroscopy for the detection of the starting and enzymatically modified substrates. Experiments can be performed in real time or in an endpoint assay format using protein and substrate concentrations comparable to the ones used by other HTS techniques. Application of this technique to the phosphorylation of a substrate by the protein Ser/Thr kinase AKT1 is presented.
摘要翻译：大型化合物库的高通量筛选（HTS）是药物 - 铅发现的方法。现在人们普遍认为，对于功能测定，质量比数量更重要。最初由Percival和Withers（Biochemistry，1992,31,498-505）提出的生化NMR方法扩展到筛选Ser / Thr激酶。该方法需要在底物上存在CF 3 N（或CF）部分，并利用19 F NMR光谱法检测起始和酶修饰的底物。实验可以使用与其他HTS技术使用的蛋白质和底物浓度相当的实时或终点分析格式进行。本发明提供了蛋白质Ser / Thr激酶AKT1对底物磷酸化的应用。

5. 发明申请

US20050048594A1 Fluorine NMR spectroscopy for biochemical screening 失效
标题翻译：氟化NMR光谱用于生化筛选
公开(公告)号：US20050048594A1
公开(公告)日：2005-03-03
申请号：US10888378
申请日：2004-07-09
申请人： Claudio Dalvit , Elena Ardini , Maria Flocco , Gianpaolo Fogliato , Nicola Mongelli , Marina Veronesi
发明人： Claudio Dalvit , Elena Ardini , Maria Flocco , Gianpaolo Fogliato , Nicola Mongelli , Marina Veronesi
IPC分类号： C12Q1/00 , C12Q1/37 , C12Q1/42 , C12Q1/48 , G01N33/48
CPC分类号： C12Q1/485
摘要： High-Throughput Screening (HTS) of large compound libraries is the method of drug-lead discovery. It is now well accepted that for a functional assay, quality is more important than quantity. A biochemical NMR method originally proposed by Percival and Withers (Biochemistry, 1992, 31, 498-505) is extended to the screening of Ser/Thr kinases. The method requires the presence of a CF3 (or CF) moiety on the substrate and utilizes 19F NMR spectroscopy for the detection of the starting and enzymatically modified substrates. Experiments can be performed in real time or in an endpoint assay format using protein and substrate concentrations comparable to the ones used by other HTS techniques. Application of this technique to the phosphorylation of a substrate by the protein Ser/Thr kinase AKT1 is presented.
摘要翻译：大型化合物库的高通量筛选（HTS）是药物 - 铅发现的方法。现在人们普遍认为，对于功能测定，质量比数量更重要。最初由Percival和Withers（Biochemistry，1992,31,498-505）提出的生化NMR方法扩展到筛选Ser / Thr激酶。该方法需要在衬底上存在CF 3（或CF）部分，并利用19 F NMR光谱法检测起始和酶修饰的底物。实验可以使用与其他HTS技术使用的蛋白质和底物浓度相当的实时或终点分析形式进行。本发明提供了蛋白质Ser / Thr激酶AKT1对底物磷酸化的应用。

6. 发明授权

US06677160B1 Methods for creating a compound library and identifying lead chemical templates and ligands for target molecules 失效
标题翻译：创建化合物文库并鉴定靶分子的铅化学模板和配体的方法
公开(公告)号：US06677160B1
公开(公告)日：2004-01-13
申请号：US09677107
申请日：2000-09-29
申请人： Brian J. Stockman , Kathleen A. Farley , Claudio Dalvit
发明人： Brian J. Stockman , Kathleen A. Farley , Claudio Dalvit
IPC分类号： G01N2400
CPC分类号： C40B40/04 , G01N24/08 , G01N24/084 , G01N24/088 , G01R33/307 , G01R33/4608 , G01R33/4633 , G01R33/465 , G01R33/5605 , Y10T436/24
摘要： A method for developing a library of compounds, the compound library, a method for identifying ligands for target molecules, and a method for identifying lead chemical templates, which, for example, can be used in drug discovery and design are provided. Certain embodiments of these methods include the use of NMR spectroscopy.
摘要翻译：提供了开发化合物文库的方法，化合物文库，用于鉴定靶分子的配体的方法，以及用于鉴定铅化学模板的方法，其例如可用于药物发现和设计。这些方法的某些实施方案包括使用NMR光谱。

7. 发明授权

US07470543B2 Methods for identifying ligands using competitive binding 1H NMR experiments 失效
标题翻译：使用竞争性结合的1 H NMR实验鉴定配体的方法
公开(公告)号：US07470543B2
公开(公告)日：2008-12-30
申请号：US10454996
申请日：2003-06-05
申请人： Claudio Dalvit , Brian J Stockman
发明人： Claudio Dalvit , Brian J Stockman
IPC分类号： G01N24/00
CPC分类号： G01R33/46 , G01N24/08 , G01R33/4625 , G01R33/465 , Y10T436/24
摘要： A method of identifying a ligand to a target molecule that includes: providing a reference compound that interacts with the target molecule; collecting a 1D 1H nuclear magnetic resonance spectrum of the reference compound in the presence of the target molecule; providing a plurality of test samples, each test sample including at least one test compound; collecting a 1D 1H nuclear magnetic resonance spectrum of the reference compound in the presence of each test sample and the target molecule; comparing the spectrum of the reference compound in the presence of the target molecule to the spectrum of the reference compound in the presence of each test sample and the target molecule to determine a change in one or more of the reference compound resonances; and identifying at least one test compound that interacts with the target molecule, wherein the test compound displaces the reference compound.
摘要翻译：鉴定靶分子的配体的方法，其包括：提供与靶分子相互作用的参考化合物; 在靶分子存在下收集参考化合物的1D 1H核磁共振谱; 提供多个测试样品，每个测试样品包括至少一种测试化合物; 在每个测试样品和靶分子的存在下收集参考化合物的1D 1H核磁共振谱; 在每个测试样品和靶分子的存在下，将目标分子存在下的参考化合物的光谱与参考化合物的光谱进行比较，以确定一种或多种参考化合物共振的变化; 以及鉴定与所述靶分子相互作用的至少一种测试化合物，其中所述测试化合物置换所述参考化合物。

8. 发明申请

US20080233603A1 Fluorine NMR spectroscopy for biochemical screening 审中-公开
标题翻译：氟化NMR光谱用于生化筛选
公开(公告)号：US20080233603A1
公开(公告)日：2008-09-25
申请号：US11825779
申请日：2007-07-09
申请人： Claudio Dalvit , Elena Ardini , Maria Magdalena Flocco , Gianpaolo Fogliatto , Nicola Mongelli , Marina Veronesi
发明人： Claudio Dalvit , Elena Ardini , Maria Magdalena Flocco , Gianpaolo Fogliatto , Nicola Mongelli , Marina Veronesi
IPC分类号： C12Q1/48 , C12Q1/00 , C12Q1/42 , C12Q1/37
CPC分类号： C12Q1/485
摘要： High-Throughput Screening (HTS) of large compound libraries is the method of drug-lead discovery. It is now well accepted that for a functional assay, quality is more important than quantity. A biochemical NMR method originally proposed by Percival and Withers (Biochemistry, 1992, 31, 498-505) is extended to the screening of Ser/Thr kinases. The method requires the presence of a CF3 (or CF) moiety on the substrate and utilizes 19F NMR spectroscopy for the detection of the starting and enzymatically modified substrates. Experiments can be performed in real time or in an endpoint assay format using protein and substrate concentrations comparable to the ones used by other HTS techniques. Application of this technique to the phosphorylation of a substrate by the protein Ser/Thr kinase AKT1 is presented.
摘要翻译：大型化合物库的高通量筛选（HTS）是药物 - 铅发现的方法。现在人们普遍认为，对于功能测定，质量比数量更重要。最初由Percival和Withers（Biochemistry，1992,31,498-505）提出的生化NMR方法扩展到筛选Ser / Thr激酶。该方法需要在底物上存在CF 3 N（或CF）部分，并利用19 F NMR光谱法检测起始和酶修饰的底物。实验可以使用与其他HTS技术使用的蛋白质和底物浓度相当的实时或终点分析格式进行。本发明提供了蛋白质Ser / Thr激酶AKT1对底物磷酸化的应用。

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