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31. 发明授权

US08022088B2 Substituted bicyclic and tricyclic thrombin receptor antagonists 有权
标题翻译：取代的双环和三环凝血酶受体拮抗剂
公开(公告)号：US08022088B2
公开(公告)日：2011-09-20
申请号：US11769018
申请日：2007-06-27
申请人： Mariappan V. Chelliah , Samuel Chackalamannil , Yan Xia
发明人： Mariappan V. Chelliah , Samuel Chackalamannil , Yan Xia
IPC分类号： A01N43/40 , A61K31/44 , C07D405/00
CPC分类号： C07D405/06
摘要： Substituted bicyclic and tricyclic modified himbacine derivative of the formula: or a pharmaceutically acceptable salt or solvate of said compound wherein represents an optional double bond and wherein En, Fn, Gn, Zn, Jn, X, R3, R9, R10, R11, R32, R33, B and Het are herein defined are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other agents is also claimed.
摘要翻译：其中代表任选的双键的取代的双环和三环修饰的烟草衍生物，或其药学上可接受的盐或溶剂化物，其中En，Fn，Gn，Zn，Jn，X，R3，R9，R10，R11，R32 本文定义的R33，B和Het以及含有它们的药物组合物和通过施用所述化合物治疗与血栓形成，动脉粥样硬化，再狭窄，高血压，心绞痛，心律失常，心力衰竭和癌症相关的疾病的方法。还声称与其他药剂组合治疗。

32. 发明申请

US20110118286A1 BICYCLIC HETEROCYCLE DERIVATIVES AND THEIR USE AS GPCR MODULATORS 审中-公开
标题翻译：双相异构体衍生物及其作为GPCR调节剂的用途
公开(公告)号：US20110118286A1
公开(公告)日：2011-05-19
申请号：US13054347
申请日：2009-07-15
申请人： Santhosh Francis Neelamkavil , Craig D. Boyle , Joel M. Harris , Andre Stamford , Jinsong Hao , Bernard R. Neustadt , Samuel Chackalamannil , Yan Xia , Wiliam J. Greenlee
发明人： Santhosh Francis Neelamkavil , Craig D. Boyle , Joel M. Harris , Andre Stamford , Jinsong Hao , Bernard R. Neustadt , Samuel Chackalamannil , Yan Xia , Wiliam J. Greenlee
IPC分类号： A61K31/519 , C07D487/04 , A61P3/00
CPC分类号： C07D487/04 , C07D473/30 , C07D473/34
摘要： The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient.
摘要翻译：本发明涉及式（I）的双环杂环衍生物，包含双环杂环衍生物的组合物，以及使用双环杂环衍生物治疗或预防肥胖，糖尿病，糖尿病并发症，代谢障碍，心血管疾病或与患者G蛋白偶联受体（GPCR）的活性相关的紊乱。

33. 发明申请

US20060106050A1 Thrombin receptor antagonists 审中-公开
标题翻译：凝血酶受体拮抗剂
公开(公告)号：US20060106050A1
公开(公告)日：2006-05-18
申请号：US11311083
申请日：2005-12-19
申请人： Samuel Chakalamannil , Mariappan Chelliah , Martin Clasby , Yan Xia
发明人： Samuel Chakalamannil , Mariappan Chelliah , Martin Clasby , Yan Xia
IPC分类号： A61K31/4741 , C07D491/02
CPC分类号： C07D491/04 , C07D493/04 , C07D495/04
摘要： Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salts thereof, wherein: n1 and n2 are independently 0-2; Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group; B is alkyl or optionally substituted alkenyl; R22 is —COR23 or a carboxy, sulfinyl, sulfonyl, sulfonamide or amino acid derivative; R23 is haloalkyl; alkenyl; haloalkenyl; alkynyl; optionally substituted cycloalkyl; cycloalkyl-alkyl; aryl; arylalkyl; heteroaryl; heterocycloalkyl; or —COOH and/or —SO3H substituted alkyl; R1, R2, R3, R9, R10 and R11 are as defined in the specification; are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds.
摘要翻译：具有下式的杂环取代的三环或其药学上可接受的盐，其中：n 1和n 2个独立地为0-2; Het是任选取代的单，双或三环杂芳族基团; B是烷基或任选取代的烯基; R 22是-COR 23或羧基，亚磺酰基，磺酰基，磺酰胺或氨基酸衍生物; R 23是卤代烷基; 烯基; 卤代烯基炔基; 任选取代的环烷基环烷基 - 烷基; 芳基; 芳烷基杂芳基; 杂环烷基; 或-COOH和/或-SO 3 H取代的烷基; R 1，R 2，R 3，R 9，R 10和R 9， R 11如本说明书中所定义; 以及含有它们的药物组合物以及通过施用所述化合物治疗与血栓形成，动脉粥样硬化，再狭窄，高血压，心绞痛，心律失常，心力衰竭和癌症相关的疾病的方法。

34. 发明授权

US5869672A Huperzine A and analogs thereof 失效
标题翻译：石杉碱甲及其类似物
公开(公告)号：US5869672A
公开(公告)日：1999-02-09
申请号：US870281
申请日：1997-06-06
申请人： Alan Paul Kozikowski , Yan Xia
发明人： Alan Paul Kozikowski , Yan Xia
IPC分类号： C07D215/48 , C07D221/22 , A01N51/00 , A61K31/655
CPC分类号： C07D221/22 , C07D215/48
摘要： The present invention relates to a method for the synthesis of certain bridged fused ring pyridines. Such bridged fused ring pyridines can be converted to huperzine A and analogs of huperzine A. The present invention also covers such bridged fused ring pyridines, compounds utilized for the preparation of the bridged fused ring pyridines and analogs of huperzine A.
摘要翻译：本发明涉及合成某些桥连稠环吡啶的方法。这种桥连稠环吡啶可以转化为石杉碱甲和石杉碱甲类似物。本发明还涵盖了这种桥连稠环吡啶，用于制备桥连稠环吡啶的化合物和石杉碱甲的类似物。

35. 发明授权

US5663344A Method for the synthesis of huperzine A and analogs thereof and compounds useful therein 失效
标题翻译：合成石杉碱甲及其类似物的方法及其中有用的化合物
公开(公告)号：US5663344A
公开(公告)日：1997-09-02
申请号：US279372
申请日：1994-07-22
申请人： Alan Paul Kozikowski , Yan Xia
发明人： Alan Paul Kozikowski , Yan Xia
IPC分类号： C07D215/48 , C07D221/22 , C07D221/06 , C07D221/16
CPC分类号： C07D221/22 , C07D215/48
摘要： The present invention relates to a method for the synthesis of certain bridged fused ring pyridines. Such bridged fused ring pyridines can be converted to huperzine A and analogs of huperzine A. The present invention also covers such bridged fused ring pyridines, compounds utilized for the preparation of the bridged fused ring pyridines and analogs of huperzine A. The compounds are capable of inhibiting cholinesterase enzymes and, therefore, are useful as pharmaceutical agents for treatment of disorders involving cholinesterase enzymes. Examples of such disorders include myasthenia gravis, Alzheimer's dementia and the improvement of senile memory loss.
摘要翻译：本发明涉及合成某些桥连稠环吡啶的方法。这样的桥连稠环吡啶可以转化为石杉碱甲和石杉碱甲的类似物。本发明还包括这种桥连稠环吡啶，用于制备桥连稠环吡啶的化合物和石杉碱甲的类似物。化合物能够抑制胆碱酯酶，因此可用作治疗涉及胆碱酯酶的疾病的药物。这种疾病的实例包括重症肌无力，阿尔茨海默氏痴呆和老年记忆丧失的改善。

36. 发明授权

US4929731A Method for the synthesis of huperzine A and analogs thereof and compounds useful therein 失效
公开(公告)号：US4929731A
公开(公告)日：1990-05-29
申请号：US313118
申请日：1989-02-21
申请人： Alan P. Kozikowski , Yan Xia
发明人： Alan P. Kozikowski , Yan Xia
IPC分类号： A61P43/00 , C07D215/48 , C07D221/04 , C07D221/22
CPC分类号： C07D221/22 , C07D215/48
摘要： The present invention relates to a method for the synthesis of certain bridged fused ring pyridines. Such bridged fused ring pyridines can be converted to huperzine A and analogs of huperzine A. The present invention also covers such bridged fused ring pyridines, compounds utilized for the preparation of the bridged fused ring pyridines and analogs of huperzine A.

37. 发明授权

US10074196B2 Reconstructing a three-dimensional image dataset from two-dimensional projection images, X-ray device and computer program 有权
公开(公告)号：US10074196B2
公开(公告)日：2018-09-11
申请号：US15356587
申请日：2016-11-19
申请人： Sebastian Bauer , Andreas Maier , Yan Xia
发明人： Sebastian Bauer , Andreas Maier , Yan Xia
IPC分类号： G06K9/00 , G06T11/00 , G06T7/00
CPC分类号： G06T11/003 , A61B6/032 , A61B6/06 , A61B6/4441 , G06T7/0012 , G06T11/006 , G06T2207/10116 , G06T2211/421 , G06T2211/432
摘要： A method for reconstructing a three-dimensional image dataset from two-dimensional projection images includes recording the projection images using a collimator downstream of an X-ray source. A local Laplace filter is initially applied to the projection data of the projection images during the reconstruction using filtered back-projection. After this, high-frequency spikes arising in the Laplace-filtered projection data at boundaries to the image region are removed by a spike filter, and a global residual filter is applied. A fit parameter describing a fit function approximating the projection data characteristic in the uncorrected projection images inside the image region is determined based on at least marginal values of the projection data present at the boundaries. Next, following on from the use of the residual filter, an additive correction of the residual-filtered projection data in the image region is performed with the fit function scaled by a scaling factor.

38. 发明申请

US20170148192A1 RECONSTRUCTING A THREE-DIMENSIONAL IMAGE DATASET FROM TWO-DIMENSIONAL PROJECTION IMAGES, X-RAY DEVICE AND COMPUTER PROGRAM 审中-公开
公开(公告)号：US20170148192A1
公开(公告)日：2017-05-25
申请号：US15356587
申请日：2016-11-19
申请人： Sebastian Bauer , Andreas Maier , Yan Xia
发明人： Sebastian Bauer , Andreas Maier , Yan Xia
IPC分类号： G06T11/00 , G06T7/00
CPC分类号： G06T11/003 , A61B6/032 , A61B6/06 , A61B6/4441 , G06T7/0012 , G06T11/006 , G06T2207/10116 , G06T2211/421 , G06T2211/432
摘要： A method for reconstructing a three-dimensional image dataset from two-dimensional projection images includes recording the projection images using a collimator downstream of an X-ray source. A local Laplace filter is initially applied to the projection data of the projection images during the reconstruction using filtered back-projection. After this, high-frequency spikes arising in the Laplace-filtered projection data at boundaries to the image region are removed by a spike filter, and a global residual filter is applied. A fit parameter describing a fit function approximating the projection data characteristic in the uncorrected projection images inside the image region is determined based on at least marginal values of the projection data present at the boundaries. Next, following on from the use of the residual filter, an additive correction of the residual-filtered projection data in the image region is performed with the fit function scaled by a scaling factor.

39. 发明授权

US09045579B2 Periodic nanostructures from self assembled wedge-type block-copolymers 有权
标题翻译：来自自组装楔形嵌段共聚物的定期纳米结构
公开(公告)号：US09045579B2
公开(公告)日：2015-06-02
申请号：US13801710
申请日：2013-03-13
申请人： Yan Xia , Benjamin R Sveinbjornsson , Robert H Grubbs , Raymond Weitekamp , Garret M Miyake , Victoria Piunova , Christopher Scot Daeffler
发明人： Yan Xia , Benjamin R Sveinbjornsson , Robert H Grubbs , Raymond Weitekamp , Garret M Miyake , Victoria Piunova , Christopher Scot Daeffler
IPC分类号： C08F26/06 , C08F2/00 , C08F10/00 , C08F299/00 , C08G81/00 , C08F222/04 , C08F222/40 , C08F293/00 , C08F232/08 , B82Y40/00 , C08G61/08
CPC分类号： C08G61/124 , B81C2201/0149 , B82Y40/00 , C08F222/04 , C08F222/40 , C08F232/08 , C08F293/00 , C08F299/00 , C08G61/08 , C08G81/00 , C08G2261/126 , C08G2261/128 , C08G2261/1426 , C08G2261/146 , C08G2261/148 , C08G2261/149 , C08G2261/3241 , C08G2261/3324 , C08G2261/418 , C08G2261/74
摘要： The invention provides a class of wedge-type block copolymers having a plurality of chemically different blocks, at least a portion of which incorporates a wedge group-containing block providing useful properties. For example, use of one or more wedge group-containing blocks in some block copolymers of the invention significantly inhibits chain entanglement and, thus, the present block copolymers materials provide a class of polymer materials capable of efficient molecular self-assembly to generate a range of structures, such as periodic nanostructures and microstructures. Materials of the present invention include copolymers having one or more wedge group-containing blocks, and optionally for some applications copolymers also incorporating one or more polymer side group-containing blocks. The present invention also provides useful methods of making and using wedge-type block copolymers.
摘要翻译：本发明提供了一类具有多个化学上不同的嵌段的楔形嵌段共聚物，其至少一部分包含提供有用特性的含楔基团的嵌段。例如，在本发明的一些嵌段共聚物中使用一个或多个含楔基团的嵌段显着抑制链缠结，因此本发明的嵌段共聚物材料提供了能够有效分子自组装以产生范围的一类聚合物材料的结构，如周期性纳米结构和微结构。本发明的材料包括具有一个或多个含楔基团的嵌段的共聚物，并且任选地用于某些应用也包含一个或多个含聚合物侧基的嵌段的共聚物。本发明还提供制备和使用楔形嵌段共聚物的有用方法。

40. 发明申请

US20140057836A1 HCV NS3 PROTEASE INHIBITORS 有权
标题翻译： HCV NS3蛋白酶抑制剂
公开(公告)号：US20140057836A1
公开(公告)日：2014-02-27
申请号：US13960343
申请日：2013-08-06
申请人： Thomas BARA , Sathesh Bhat , Dipshika Biswas , Linda Brockunier , Duane Burnette , Samuel Chackalamannil , Mariappan Vasu Cheliah , Austin Chen , Martin Clasby , Vince J. Colandrea , Zhuyan Guo , Yongxin Han , Charles Jayne , Hubert Josien , Karen Marcantonio , Shouwu Miao , Santhosh Neelamkavil , Patrick Pinto , Murali Rajogopalan , Unmesh Shah , Francisco Velazquez , Srikanth Venkatraman , Yan Xia
发明人： Thomas BARA , Sathesh Bhat , Dipshika Biswas , Linda Brockunier , Duane Burnette , Samuel Chackalamannil , Mariappan Vasu Cheliah , Austin Chen , Martin Clasby , Vince J. Colandrea , Zhuyan Guo , Yongxin Han , Charles Jayne , Hubert Josien , Karen Marcantonio , Shouwu Miao , Santhosh Neelamkavil , Patrick Pinto , Murali Rajogopalan , Unmesh Shah , Francisco Velazquez , Srikanth Venkatraman , Yan Xia
IPC分类号： C07K5/08 , A61K45/06 , A61K38/06
CPC分类号： C07K5/08 , A61K38/06 , A61K45/06 , C07D419/00 , C07D491/22
摘要： The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.
摘要翻译：本发明涉及含有螺环状的丙型肝炎病毒（HCV）NS3蛋白酶抑制剂，这些化合物的用途，以及这些化合物的合成。

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