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1. 发明授权

US07741479B2 Urea inhibitors of MAP kinases 失效
标题翻译： MAP激酶的尿素抑制剂
公开(公告)号：US07741479B2
公开(公告)日：2010-06-22
申请号：US11295638
申请日：2005-12-07
申请人： Enrique Luis Michelotti , Eric Bruce Springman , Duyan Nguyen , Rupa S. Shetty , Younghee Lee , Kristofer Kent Moffett , Jennifer Lee Ludington , Ted Tsutomis Fujimoto , Zenon D. Konteatis , Bin Liu , Frank Hollinger , Bruce D. Dorsey
发明人： Enrique Luis Michelotti , Eric Bruce Springman , Duyan Nguyen , Rupa S. Shetty , Younghee Lee , Kristofer Kent Moffett , Jennifer Lee Ludington , Ted Tsutomis Fujimoto , Zenon D. Konteatis , Bin Liu , Frank Hollinger , Bruce D. Dorsey
IPC分类号： C07D273/06
CPC分类号： C07D333/38 , C07D231/40 , C07D243/08 , C07D277/48 , C07D277/56 , C07D295/192 , C07D333/36 , C07D403/06 , C07D405/06 , C07D409/04 , C07D409/06 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/14 , C07D495/04
摘要： The present invention is directed to a compound having the formula wherein R1, R2, G, and Q are defined herein. The compounds of the present invention are useful as inhibitors of protein kinases such as MAP kinases, in particular p38 kinases. The present invention is also directed to compositions comprising a compound according to the above formula. The compounds and compositions described herein are useful for treating and preventing an inflammatory condition or disease. The present invention is also directed to a method of treating or preventing a protein kinase-mediated condition.
摘要翻译：本发明涉及具有下式的化合物：其中R1，R2，G和Q如本文所定义。本发明的化合物可用作蛋白激酶如MAP激酶，特别是p38激酶的抑制剂。本发明还涉及包含根据上式的化合物的组合物。本文所述的化合物和组合物可用于治疗和预防炎性疾病或疾病。本发明还涉及治疗或预防蛋白激酶介导的病症的方法。

2. 发明申请

US20060167247A1 Urea inhibitors of MAP kinases 失效
标题翻译： MAP激酶的尿素抑制剂
公开(公告)号：US20060167247A1
公开(公告)日：2006-07-27
申请号：US11295638
申请日：2005-12-07
申请人： Enrique Michelotti , Eric Springman , Duyan Nguyen , Rupa Shetty , Younghee Lee , Kristofer Moffett , Jennifer Ludington , Ted Fujimoto , Zenon Konteatis , Bin Liu , Frank Hollinger , Bruce Dorsey
发明人： Enrique Michelotti , Eric Springman , Duyan Nguyen , Rupa Shetty , Younghee Lee , Kristofer Moffett , Jennifer Ludington , Ted Fujimoto , Zenon Konteatis , Bin Liu , Frank Hollinger , Bruce Dorsey
IPC分类号： C07D417/02 , C07D413/02 , C07D409/02
CPC分类号： C07D333/38 , C07D231/40 , C07D243/08 , C07D277/48 , C07D277/56 , C07D295/192 , C07D333/36 , C07D403/06 , C07D405/06 , C07D409/04 , C07D409/06 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/14 , C07D495/04
摘要： The present invention is directed to a compound having the formula wherein R1, R2, G, and Q are defined herein. The compounds of the present invention are useful as inhibitors of protein kinases such as MAP kinases, in particular p38 kinases. The present invention is also directed to compositions comprising a compound according to the above formula. The compounds and compositions described herein are useful for treating and preventing an inflammatory condition or disease. The present invention is also directed to a method of treating or preventing a protein kinase-mediated condition.
摘要翻译：本发明涉及具有下式的化合物：其中R 1，R 2，G和Q在本文中定义。本发明的化合物可用作蛋白激酶如MAP激酶，特别是p38激酶的抑制剂。本发明还涉及包含根据上式的化合物的组合物。本文所述的化合物和组合物可用于治疗和预防炎性疾病或疾病。本发明还涉及治疗或预防蛋白激酶介导的病症的方法。

3. 发明申请

US20050123995A1 Methods and systems for analyzing and determining ligand-residue interaction 失效
标题翻译：用于分析和测定配体 - 残基相互作用的方法和系统
公开(公告)号：US20050123995A1
公开(公告)日：2005-06-09
申请号：US10920234
申请日：2004-08-18
申请人： Stephan Brunner , David Mosenkis , Frank Hollinger , William Chiang
发明人： Stephan Brunner , David Mosenkis , Frank Hollinger , William Chiang
IPC分类号： C12Q20060101 , G01N33/48 , G01N33/50 , G01N33/53 , G01N33/569 , G06F17/00 , G06F17/30 , G06F19/00 , G06F19/16
CPC分类号： G01N33/5695 , G06F19/16 , G06F19/701 , G06F19/706
摘要： A method implemented in the form of a computer simulation code for evaluating the free energy of binding between polypeptide amino acid residues and one or more molecular fragment types is presented. The basis of the method is a novel weighted Metropolis Monte Carlo approach for sampling the grand canonical ensemble. By making use of the properties of the grand canonical ensemble, the affinity of fragments for binding in the vicinity of each protein residue can be efficiently computed. The binding volume associated to each fragment-residue pair is estimated on the basis of a simple proximity criteria, and a useful affinity mapping of the protein surface can be obtained in this way. The analysis of such data for various fragment types provides valuable information to help identify protein binding sites, as well as to identify key fragments used for building potential drug leads.
摘要翻译：提出了一种用于评估多肽氨基酸残基与一种或多种分子片段类型之间的结合自由能的计算机模拟代码形式的方法。该方法的基础是一种新颖的加权大都会蒙特卡罗方法，用于抽样大规模集合。通过利用大规模集合的性质，可以有效地计算片段在每个蛋白质残基附近的结合亲和力。基于简单的接近标准估计与每个片段 - 残基对相关联的结合体积，并且可以以这种方式获得蛋白质表面的有用亲和力图谱。对于各种片段类型的这种数据的分析提供了有价值的信息，以帮助鉴定蛋白质结合位点，以及鉴定用于构建潜在药物引线的关键片段。

4. 发明申请

US20130303516A1 NOVEL TRIAZINE COMPOUNDS 有权
标题翻译：新颖的化合物
公开(公告)号：US20130303516A1
公开(公告)日：2013-11-14
申请号：US13981579
申请日：2012-01-25
申请人： Sundeep Dugar , Dinesh Mahajan , Chandraban Rhushikesh Deokar , Peter Frank Hollinger , Kamal Kishore Kapoor
发明人： Sundeep Dugar , Dinesh Mahajan , Chandraban Rhushikesh Deokar , Peter Frank Hollinger , Kamal Kishore Kapoor
IPC分类号： C07D413/14 , C07D417/14 , C07D471/04 , C07D403/14 , C07D491/107 , C07D498/08 , C07D401/14
CPC分类号： C07D413/14 , C07D401/14 , C07D403/14 , C07D413/04 , C07D417/14 , C07D471/04 , C07D491/107 , C07D498/08
摘要： The present invention relates to novel triazine compounds of formula (1), methods of their preparation, pharmaceutical compositions containing these compounds and the use of these compounds to treat proliferative disorders such as tumors and cancers and also other conditions and disorders related to or associated with dysregulation of PI3 Kinases, PI3 Kinase pathway, mTOR and/or the mTOR pathway.
摘要翻译：本发明涉及式（1）的新型三嗪化合物，其制备方法，含有这些化合物的药物组合物以及这些化合物用于治疗增殖性疾病如肿瘤和癌症的用途，以及与其相关或与之相关的其他病症和病症 PI3激酶，PI3激酶途径，mTOR和/或mTOR途径的调节异常。

5. 发明申请

US20100029628A1 2,4,5-Substituted Piperidines as Renin Inhibitors 审中-公开
标题翻译： 2,4,5-取代哌啶酮作为肾素抑制剂
公开(公告)号：US20100029628A1
公开(公告)日：2010-02-04
申请号：US11887227
申请日：2006-03-30
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Christiane Marti , Stefan Stutz , Stjepan Jelakovic , Zenon D. Konteatis , Jennifer L. Ludington , Michael Quirmbach , Aleksandar Stojanovic , Dirk Behnke , Frank Hollinger
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Christiane Marti , Stefan Stutz , Stjepan Jelakovic , Zenon D. Konteatis , Jennifer L. Ludington , Michael Quirmbach , Aleksandar Stojanovic , Dirk Behnke , Frank Hollinger
IPC分类号： A61K31/538 , C07D413/02 , A61P9/00 , A61P13/00
CPC分类号： C07D413/12 , C07D413/14
摘要： SP-P2140 ATE-132—Abstract Novel substituted piperidines of the general formula (I) and (II) with the substituent definitions as explained in detail in the description are described. The compounds are suitable in particular as renin inhibitors and are highly potent.
摘要翻译： SP-P2140ATE-132-摘要描述了通式（I）和（II）的具有取代基定义的新颖取代的哌啶，如在说明书中详细说明的。该化合物特别适合作为肾素抑制剂，并且是非常有效的。

6. 发明授权

US07687495B2 Substituted piperidines 失效
标题翻译：取代的哌啶
公开(公告)号：US07687495B2
公开(公告)日：2010-03-30
申请号：US12076221
申请日：2008-03-14
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Christiane Marti , Stefan Stutz , Stjepan Jelakovic , Zenon D. Konteatis , Jennifer L. Ludington , Michael Quirmbach , Aleksandar Stojanovic , Dirk Behnke , Frank Hollinger
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Christiane Marti , Stefan Stutz , Stjepan Jelakovic , Zenon D. Konteatis , Jennifer L. Ludington , Michael Quirmbach , Aleksandar Stojanovic , Dirk Behnke , Frank Hollinger
IPC分类号： C07D401/02 , A61K31/50 , A61K31/4965
CPC分类号： C07D413/12 , C07D413/14
摘要： Substituted piperidines of formulae (I) and (II) with the substituent definitions as explained in the specification. The compounds are suitable in particular as renin inhibitors and are highly potent.
摘要翻译：式（I）和（II）的取代的哌啶与说明书中所述的取代基定义相同。该化合物特别适合作为肾素抑制剂，并且是非常有效的。

7. 发明申请

US20070005258A1 Identification of ligands for macromolecules 审中-公开
标题翻译：鉴定大分子配体
公开(公告)号：US20070005258A1
公开(公告)日：2007-01-04
申请号：US11146417
申请日：2005-06-07
申请人： Frank Guarnieri , Frank Hollinger , Stephan Brunner , William Chiang , Matthew Clark , George Talbot , Jason Ferrara
发明人： Frank Guarnieri , Frank Hollinger , Stephan Brunner , William Chiang , Matthew Clark , George Talbot , Jason Ferrara
IPC分类号： G06F19/00
CPC分类号： G16B15/00 , G16B45/00
摘要： Methods and systems of analyzing positions and orientations of molecular fragments to generate macromolecular binding ligands, including analyzing the positions and orientations of molecular fragments in relation to other molecular fragments to bond the molecular fragments to form ligands.
摘要翻译：分析分子片段的位置和取向以产生大分子结合配体的方法和系统，包括分析与其它分子片段相关的分子片段的位置和取向以键合分子片段以形成配体。

8. 发明申请

US20050222776A1 Method for fragment preparation 审中-公开
标题翻译：片段制备方法
公开(公告)号：US20050222776A1
公开(公告)日：2005-10-06
申请号：US10813553
申请日：2004-03-31
申请人： Jennifer Ludington , Ted Fujimoto , Frank Hollinger
发明人： Jennifer Ludington , Ted Fujimoto , Frank Hollinger
IPC分类号： G01N33/48 , G01N33/50 , G01N33/68 , G06F19/00
CPC分类号： G01N33/6803 , G16B15/00
摘要： A method for characterizing a molecular fragment to collect data related to the fragment that allows its evaluation for drug discovery purposes. Starting with a two-dimensional model of the fragment, an initial three-dimensional model of the fragment is derived. Conformers of the fragment are identified. The conformers are then clustered, and a representative conformer is selected from each cluster. An ab initio or semi-empirical calculation and analysis is performed on one or more of the selected conformers. Each atom in the selected conformer is then assigned a type. The selected conformer is analyzed to determine if it is structurally symmetric. If so, the three-dimensional model of the fragment is adjusted to reflect the symmetry. The size of the fragment is calculated to allow geometric analysis of how the fragment physically fits with the protein and/or other fragments. The solvation energy of the fragment is calculated. The free energy curve for the fragment is calculated. Derivatization points for the fragment are then determined; a score is then assigned to each derivatization point, reflecting the ease or difficulty in bonding at the derivatization points. The fragment is then assigned a name and categorized. The fragment and its data derived in the above process can then be stored in a database.
摘要翻译：用于表征分子片段以收集与该片段相关的数据的方法，其允许其评估药物发现目的。从片段的二维模型开始，导出片段的初始三维模型。确定片段的构象。然后将构象异构体聚集，并从每个聚类中选择代表性构象。对一个或多个所选构象进行从头或半经验的计算和分析。然后将所选构象异构体中的每个原子分配一个类型。分析所选择的构象异构体以确定其是否在结构上对称。如果是这样，则调整片段的三维模型以反映对称性。计算片段的大小以允许对片段与蛋白质和/或其他片段物理匹配的几何分析。计算片段的溶剂化能。计算片段的自由能曲线。然后确定片段的衍生点; 然后将分数分配给每个衍生化点，反映在衍生化点处的粘合的容易性或难度。然后将该片段分配一个名称并进行分类。然后将上述过程中导出的片段及其数据存储在数据库中。

9. 发明申请

US20050123993A1 Methods of determining ligand residue binding affinity 审中-公开
标题翻译：确定配体残基结合亲和力的方法
公开(公告)号：US20050123993A1
公开(公告)日：2005-06-09
申请号：US10730267
申请日：2003-12-09
申请人： Stephan Brunner , David Mosenkis , Frank Hollinger , William Chiang
发明人： Stephan Brunner , David Mosenkis , Frank Hollinger , William Chiang
IPC分类号： G01N33/48 , G01N33/50 , G01N33/53 , G01N33/569 , G06F19/00
CPC分类号： G01N33/5695 , G16B15/00
摘要： Methods and systems for determining the affinity between polypeptide amino acid residues and one or more molecular fragments, and for using the affinity values to aid in drug design including a computer simulation which calculates the interaction energy between a polypeptide and at least one molecular fragment. An affinity value is then assigned to at least one fragment and residue pair if the fragment is in the vicinity of the residue. Affinity values are used to rank fragments, build ligands and determine binding sites.
摘要翻译：用于确定多肽氨基酸残基与一个或多个分子片段之间的亲和力的方法和系统，以及用于使用亲和力值来辅助药物设计，包括计算多肽与至少一个分子片段之间的相互作用能的计算机模拟。如果片段在残基附近，则将亲和力值分配给至少一个片段和残基对。亲和力值用于对片段进行排序，构建配体并确定结合位点。

10. 发明申请

US20080171748A1 Substituted piperidines 失效
标题翻译：取代的哌啶
公开(公告)号：US20080171748A1
公开(公告)日：2008-07-17
申请号：US12076221
申请日：2008-03-14
申请人： Peter Herold , Robert Mah , Vincenzo Tschinke , Christiane Marti , Stefan Stutz , Stjepan Jelakovic , Zenon D. Konteatis , Jennifer L. Ludington , Michael Quirmbach , Aleksandar Stojanovic , Dirk Behnke , Frank Hollinger
发明人： Peter Herold , Robert Mah , Vincenzo Tschinke , Christiane Marti , Stefan Stutz , Stjepan Jelakovic , Zenon D. Konteatis , Jennifer L. Ludington , Michael Quirmbach , Aleksandar Stojanovic , Dirk Behnke , Frank Hollinger
IPC分类号： A61K31/50 , A61K31/4965
CPC分类号： C07D413/12 , C07D413/14
摘要： Substituted piperidines of formulae (I) and (II) with the substituent definitions as explained in the specification. The compounds are suitable in particular as renin inhibitors and are highly potent.
摘要翻译：式（I）和（II）的取代的哌啶与说明书中所述的取代基定义相同。该化合物特别适合作为肾素抑制剂，并且是非常有效的。

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