公开(公告)号：US20130039853A1

公开(公告)日：2013-02-14

申请号：US13562879

申请日：2012-07-31

申请人： David J. Yang ,  Dongfang Yu ,  Andrew S. Thompson ,  F. David Rollo

发明人： David J. Yang ,  Dongfang Yu ,  Andrew S. Thompson ,  F. David Rollo

IPC分类号： A61K51/08 ,  A61K38/05 ,  A61P35/00 ,  A61P35/02 ,  A61K49/22 ,  A61K49/04 ,  A61P9/00 ,  A61P9/10 ,  A61K49/00 ,  A61K49/14

摘要： Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

摘要翻译： 公开了合成螯合剂靶向配体缀合物的新方法，包含这种缀合物的组合物，以及这种缀合物的治疗和诊断应用。 组合物包括任选地螯合到一种或多种金属离子的螯合剂靶向配体缀合物。 还提出了高纯度合成这些组合物的方法。 还公开了使用这些新型组合物成像，治疗和诊断受试者疾病的方法，例如对象内的肿瘤成像方法和诊断心肌缺血的方法。

公开(公告)号：US10814013B2

公开(公告)日：2020-10-27

申请号：US13562879

申请日：2012-07-31

申请人： David J. Yang ,  Dongfang Yu ,  Andrew S. Thompson ,  F. David Rollo

发明人： David J. Yang ,  Dongfang Yu ,  Andrew S. Thompson ,  F. David Rollo

IPC分类号： A61K49/00 ,  A61K51/04 ,  A61K49/06

摘要： Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

公开(公告)号：US10925977B2

公开(公告)日：2021-02-23

申请号：US11770395

申请日：2007-06-28

申请人： David J. Yang ,  Dongfang Yu ,  Andrew S. Thompson

发明人： David J. Yang ,  Dongfang Yu ,  Andrew S. Thompson

IPC分类号： A61K49/00 ,  A61K51/04 ,  A61K49/06

摘要： Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

公开(公告)号：US20130211082A1

公开(公告)日：2013-08-15

申请号：US13810763

申请日：2011-07-15

申请人： James Alan Kerschen ,  Alexander James Bridges ,  Sean Mark Daizlel ,  Olivier Dapremont ,  Hyunjung Kim ,  Andrew S. Thompson ,  James Robert Zeller

发明人： James Alan Kerschen ,  Alexander James Bridges ,  Sean Mark Daizlel ,  Olivier Dapremont ,  Hyunjung Kim ,  Andrew S. Thompson ,  James Robert Zeller

IPC分类号： C07D239/70 ,  C07C227/20

CPC分类号： C07D455/00 ,  C07C227/20 ,  C07D239/70

摘要： A method of producing 6-amino-cyclopenta[g]quinazolines, in enantiomerically enriched form, is provided. In particular, the method may be applicable to the synthesis of N-{N-{4-[N-((6S)-2-hydroxymethyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclo-penta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino]benzoyl}-L-γ-glutamyl}-D-glutamic acid (ONX-0801).

摘要翻译： 提供以对映体富集形式生产6-氨基 - 环戊二烯并[g]喹唑啉的方法。 特别地，该方法可适用于合成N- {N- {4- [N - （（S）-2-羟甲基-4-氧代-3,4,7,8-四氢-6H-环 - 戊基[g]喹唑啉-6-基）-N-（丙-2-炔基）氨基]苯甲酰基} -L-γ-谷氨酰基} -D-谷氨酸（ONX-0801）。

公开(公告)号：US06939964B2

公开(公告)日：2005-09-06

申请号：US10891749

申请日：2004-06-24

申请人： Louis S. Crocker ,  Joseph L. Kukura, II ,  Andrew S. Thompson ,  Christine Stelmach ,  Steven D. Young

发明人： Louis S. Crocker ,  Joseph L. Kukura, II ,  Andrew S. Thompson ,  Christine Stelmach ,  Steven D. Young

IPC分类号： C07D265/18

CPC分类号： C07D265/18

摘要： The instant invention describes a method for crystallizing (−)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one from a solvent and anti-solvent solvent system and producing the crystalline product. The desired final crystal form, Form I, can be produced when using methanol or ethanol. Form II is isolated from 2-propanol and can be converted to the desired crystal form at low drying temperatures, such as between about a temperature of 40° C. and 50° C.

摘要翻译： 本发明描述了从溶剂和反溶剂溶剂体系中结晶（ - ） - 6-氯-4-环丙基乙炔基-4-三氟甲基-1,4-二氢-2H-3,1-苯并恶嗪-2-酮的方法 并产生结晶产物。 当使用甲醇或乙醇时，可以制备所需的最终结晶形式I。 形式II从2-丙醇中分离出来，并且可以在低的干燥温度例如在约40℃和50℃的温度之间转化为所需的晶形。

公开(公告)号：US5698741A

公开(公告)日：1997-12-16

申请号：US680940

申请日：1996-07-15

申请人： Andrew S. Thompson ,  Edward G. Corley ,  Edward J. J. Grabowski ,  Nobuyoshi Yasuda

发明人： Andrew S. Thompson ,  Edward G. Corley ,  Edward J. J. Grabowski ,  Nobuyoshi Yasuda

IPC分类号： C07B53/00 ,  C07C213/00 ,  C07C215/68 ,  C07C215/70 ,  C07C217/58 ,  C07D265/18 ,  C07C211/00 ,  C07C51/16

CPC分类号： C07D265/18 ,  C07C213/00 ,  C07C215/70 ,  C07C217/58 ,  Y02P20/55

摘要： An improved synthesis of a highly potent HIV reverse transcription inhibitor is disclosed, involving an acetylide and a trifluoromethyl ketone which produces a chiral product in the presence of a chiral amino alcohol.

摘要翻译： 公开了改进的高效HIV逆转录抑制剂的合成，涉及在手性氨基醇存在下产生手性产物的乙酰化物和三氟甲基酮。

公开(公告)号：US10370403B2

公开(公告)日：2019-08-06

申请号：US15135969

申请日：2016-04-22

申请人： Paul B. Savage ,  Thomas E. Jacks ,  Ross A. Miller ,  Andrew S. Thompson ,  Jared Lynn Randall

发明人： Paul B. Savage ,  Thomas E. Jacks ,  Ross A. Miller ,  Andrew S. Thompson ,  Jared Lynn Randall

IPC分类号： C07J41/00 ,  C07J9/00

摘要： Disclosed herein are methods of making ceragnenin compounds for treating, preventing, or diagnosing diseases, disorders, or conditions associated with bacterial or viral infections, cancer, inflammation, and osteogenesis. Ceragenin compounds display broad-spectrum antibacterial activity utilizing a mode of action similar to antimicrobial peptides, but without the high synthesis costs and susceptibility to proteolytic degradation. Ceragenin compounds reproduce the amphiphilic morphology found in many antimicrobial peptides and display potent and diverse biological activities, including anti-bacterial, anti-cancer, anti-inflammatory, bone growth promotion, and wound healing promotion.

公开(公告)号：US08173703B2

公开(公告)日：2012-05-08

申请号：US12574135

申请日：2009-10-06

申请人： Falko Diedrich ,  Birgit Neudecker ,  Eberhard Wieland ,  Joseph A. Lewis, II ,  Joseph C. DiNardo ,  Andrew S. Thompson ,  James Alan Kerschen ,  Peter C. Wade

发明人： Falko Diedrich ,  Birgit Neudecker ,  Eberhard Wieland ,  Joseph A. Lewis, II ,  Joseph C. DiNardo ,  Andrew S. Thompson ,  James Alan Kerschen ,  Peter C. Wade

IPC分类号： A61K31/225 ,  A61K8/00

CPC分类号： A61K8/37 ,  A61K8/375 ,  A61K8/67 ,  A61K8/671 ,  A61K8/673 ,  A61K8/676 ,  A61K8/678 ,  A61K8/97 ,  A61Q17/04 ,  A61Q19/004 ,  A61Q19/007 ,  A61Q19/02 ,  A61Q19/06 ,  A61Q19/08 ,  A61Q19/10 ,  A61Q90/00 ,  C07C67/08 ,  C07C67/14 ,  C07C67/28 ,  C07C67/31 ,  C07C69/67 ,  C07C69/95 ,  C07C2601/16 ,  C07C69/28 ,  C07C69/675

摘要： The present invention relates to novel carboxylic acid-substituted idebenone derivatives, skin treatment compositions containing these carboxylic acid-substituted idebenone derivatives, methods of treating skin changes by topical application of these carboxylic acid-substituted idebenone derivatives, and their methods of synthesis. The carboxylic acid-substituted idebenone derivatives of the present invention are unexpectedly effective in treating skin, particularly with respect to skin tolerance. When included in a topical composition, the carboxylic acid-substituted idebenone derivatives of the present invention have an antioxidant effect that is useful in treating a skin change.

摘要翻译： 本发明涉及新的羧酸取代的艾地苯醌衍生物，含有这些羧酸取代的艾地苯醌衍生物的皮肤处理组合物，通过局部施用这些羧酸取代的艾地苯醌衍生物来治疗皮肤变化的方法及其合成方法。 本发明的羧酸取代的艾地苯醌衍生物在治疗皮肤方面是意想不到的，特别是在皮肤耐受性方面。 当包含在局部组合物中时，本发明的羧酸取代的艾地苯醌衍生物具有可用于治疗皮肤变化的抗氧化作用。

公开(公告)号：US20100113781A1

公开(公告)日：2010-05-06

申请号：US12531016

申请日：2008-03-12

申请人： John Charles Tomesch ,  Peng Li ,  Wei Yao ,  Qiang Zhang ,  James David Beard ,  Andrew S. Thompson ,  Hua Cheng

发明人： John Charles Tomesch ,  Peng Li ,  Wei Yao ,  Qiang Zhang ,  James David Beard ,  Andrew S. Thompson ,  Hua Cheng

IPC分类号： C07D241/36 ,  C07D471/04

CPC分类号： C07D471/16 ,  C07D471/04

摘要： The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines.

摘要翻译： 本发明提供了制备取代的杂环稠合的γ-咔啉的方法，可用于制备它们的中间体和制备这种中间体的方法和这种杂环稠合的γ-咔啉。

公开(公告)号：US06639071B2

公开(公告)日：2003-10-28

申请号：US10000537

申请日：2001-10-19

申请人： Louis S. Crocker ,  Joseph L. Kukura, II ,  Andrew S. Thompson ,  Christine Stelmach ,  Steven D. Young

发明人： Louis S. Crocker ,  Joseph L. Kukura, II ,  Andrew S. Thompson ,  Christine Stelmach ,  Steven D. Young

IPC分类号： C07D26518

CPC分类号： C07D265/18

摘要： The instant invention describes a method for crystallizing (−)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one from a solvent and anti-solvent system and producing the crystalline product. The desired final crystal form, Form I, can be produced when using methanol or ethanol. Form II is isolated from 2-propanol and can be converted to the desired crystal form at low drying temperatures, such as between about a temperature of 40° C. and 50° C.

摘要翻译： 本发明描述了从溶剂和反溶剂体系中结晶（ - ） - 6-氯-4-环丙基乙炔基-4-三氟甲基-1,4-二氢-2H-3,1-苯并恶嗪-2-酮的方法， 产生结晶产物。 当使用甲醇或乙醇时，可以生产所需的最终晶型I。 形式II从2-丙醇中分离出来，并且可以在低的干燥温度例如在约40℃和50℃的温度之间转化为所需的晶形。