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1. 发明申请

US20110319352A1 Compounds That Bind Oxysterol Binding Proteins, and Methods of Use Thereof 审中-公开
标题翻译：绑定氧固醇结合蛋白的化合物及其使用方法
公开(公告)号：US20110319352A1
公开(公告)日：2011-12-29
申请号：US13139196
申请日：2009-12-11
申请人： Matthew D. Shair , Anthony Burgett , D. Ryan Anderson
发明人： Matthew D. Shair , Anthony Burgett , D. Ryan Anderson
IPC分类号： A61K31/704 , A61K31/352 , A61P35/00 , A61P9/10 , A61P25/28 , A61K31/58 , A61K31/202
CPC分类号： A61K31/498 , A61K31/56 , A61K31/569 , A61K31/7056
摘要： The invention relates in part to the discovery that certain CRAMs, such as schweinfurthin A, target OSBPs (a family of oxysterol binding proteins). Because OSBPs have been shown to be integral to atherosclerosis and Alzheimer's disease (AD), one aspect of the invention relates to the use of CRAMs, or a pharmaceutically acceptable salt, biologically active metabolite, solvate, hydrate, prodrug, enantiomer or stereoisomer thereof, in the treatment and/or prevention of atherosclerosis, Alzheimer's disease and related disorders. Another aspect of the invention relates to novel derivatives of CRAMs, or a pharmaceutically acceptable salt, biologically active metabolite, solvate, hydrate, prodrug, enantiomer or stereoisomer thereof, for the treatment and/or prevention of atherosclerosis, Alzheimer's disease and related disorders. Another aspect of the invention relates to the use of an immobilized CRAMs, such as OSW-I, to aid in screening of compounds to identify additional OSBP binders. Other aspects of the invention relate to the use of CRAMs to treat cancer, such as p21-deficient cancers.
摘要翻译：本发明部分地涉及某些CRAM，例如施赖福呋丁A，目标OSBP（氧固醇结合蛋白家族）的发现。由于OSBPs已被证明与动脉粥样硬化和阿尔茨海默氏病（AD）是不可分割的，本发明的一个方面涉及CRAM或其药学上可接受的盐，生物活性代谢物，溶剂合物，水合物，前药，对映体或立体异构体的用途，在治疗和/或预防动脉粥样硬化，阿尔茨海默病和相关疾病。本发明的另一方面涉及用于治疗和/或预防动脉粥样硬化，阿尔茨海默病和相关疾病的CRAM或其药学上可接受的盐，生物活性代谢物，溶剂化物，水合物，前药，对映体或立体异构体的新衍生物。本发明的另一方面涉及固定化CRAM（例如OSW-1）用于帮助筛选化合物以鉴定另外的OSBP结合物的用途。本发明的其它方面涉及使用CRAM来治疗癌症，例如p21缺陷型癌症。

2. 发明授权

US06448443B1 Synthesis of combinatorial libraries of compounds reminiscent of natural products 失效
标题翻译：化合物组合文库的合成使人联想到天然产物
公开(公告)号：US06448443B1
公开(公告)日：2002-09-10
申请号：US09121922
申请日：1998-07-25
申请人： Stuart L. Schreiber , Matthew D. Shair , Derek S. Tan , Michael A. Foley , Brent R. Stockwell
发明人： Stuart L. Schreiber , Matthew D. Shair , Derek S. Tan , Michael A. Foley , Brent R. Stockwell
IPC分类号： G01N3353
CPC分类号： C07D307/33 , B01J19/0046 , B01J2219/00317 , B01J2219/00364 , B01J2219/00367 , B01J2219/005 , B01J2219/00511 , B01J2219/00531 , B01J2219/00585 , B01J2219/00596 , B01J2219/00605 , B01J2219/0061 , B01J2219/00612 , B01J2219/0065 , B01J2219/00659 , B01J2219/00702 , C07C227/10 , C07C231/12 , C07C235/40 , C07C237/20 , C07C237/24 , C07C247/14 , C07C2601/14 , C07C2601/16 , C07D261/20 , C07D493/04 , C40B40/00 , C40B60/14 , C40B80/00 , G01N33/50 , Y10S435/975 , C07C229/34
摘要： The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
摘要翻译：本发明提供了使人想起天然产物及其文库的复杂化合物，以及它们生产的方法。本发明化合物和化合物文库使人联想到天然产物，因为它们含有一种或多种立体中心，并且具有高密度和多样性的功能。通常，本发明的文库由可分散的支架结构合成，其由易得的或易于合成的模板结构合成。在某些实施方案中，本发明化合物和文库是由莽草酸基环氧树脂模板合成的可分散支架产生的。在其它实施方案中，本发明的化合物和文库由从基于吡啶的模板异烟酰胺合成的可分散的支架产生。本发明还提供了一种新的邻硝基苄基光接枝剂及其合成方法。此外，本发明提供了用于确定本发明文库成员的一种或多种生物活性的方法和试剂盒。另外，本发明提供含有一个或多个文库成员的药物组合物。

3. 发明授权

US09321713B2 Hyperforin analogs, methods of synthesis, and uses thereof 有权
标题翻译： Hyperforin类似物，合成方法及其应用
公开(公告)号：US09321713B2
公开(公告)日：2016-04-26
申请号：US14123255
申请日：2012-06-01
申请人： Matthew D. Shair , Brian A. Sparling , David Moebius
发明人： Matthew D. Shair , Brian A. Sparling , David Moebius
IPC分类号： A61K31/122 , C07C49/29 , C07C49/753 , C07C49/733 , C07C49/743 , C07C45/29 , C07D493/08 , C07F7/08 , C07F7/18
CPC分类号： C07C49/753 , C07C45/29 , C07C49/733 , C07C49/743 , C07D493/08 , C07F7/081 , C07F7/0834 , C07F7/1804
摘要： The present invention provides a novel 11-step enantioselective approach to the natural product hyperforin, which enables access to a wide variety of hyperforin analogs. The present invention also provides pharmaceutical compositions comprising inventive hyperforin analogs. Hyperforin analogs synthesized using the present synthetic method are envisioned useful in the treatment of various conditions, including, but not limited to, depression and conditions characterized by depression, inflammatory skin conditions, diabetes, asthma, chronic obstructive pulmonary disease (COPD), kidney disorders, and ischemic brain damage.
摘要翻译：本发明提供了对天然产物hyperforin的新型11步对映选择性方法，其能够接近各种各样的hyperforin类似物。本发明还提供包含本发明的高福林类似物的药物组合物。使用本合成方法合成的Hyperforin类似物被设想用于治疗各种病症，包括但不限于抑郁症，特征为抑郁症，炎性皮肤病症，糖尿病，哮喘，慢性阻塞性肺病（COPD），肾脏疾病，和缺血性脑损伤。

4. 发明申请

US20140135287A1 HYPERFORIN ANALOGS, METHODS OF SYNTHESIS, AND USES THEREOF 有权
标题翻译： HYPERFORIN ANALOGS，合成方法及其用途
公开(公告)号：US20140135287A1
公开(公告)日：2014-05-15
申请号：US14123255
申请日：2012-06-01
申请人： Matthew D. Shair , Brian A. Sparling , David Moebius
发明人： Matthew D. Shair , Brian A. Sparling , David Moebius
IPC分类号： C07C49/753 , C07C45/29 , C07F7/08 , C07D493/08
CPC分类号： C07C49/753 , C07C45/29 , C07C49/733 , C07C49/743 , C07D493/08 , C07F7/081 , C07F7/0834 , C07F7/1804
摘要： The present invention provides a novel 11-step enantioselective approach to the natural product hyperforin, which enables access to a wide variety of hyperforin analogs. The present invention also provides pharmaceutical compositions comprising inventive hyperforin analogs. Hyperforin analogs synthesized using the present synthetic method are envisioned useful in the treatment of various conditions, including, but not limited to, depression and conditions characterized by depression, inflammatory skin conditions, diabetes, asthma, chronic obstructive pulmonary disease (COPD), kidney disorders, and ischemic brain damage.
摘要翻译：本发明提供了对天然产物hyperforin的新型11步对映选择性方法，其能够接近各种各样的hyperforin类似物。本发明还提供包含本发明的高福林类似物的药物组合物。使用本发明的合成方法合成的Hyperforin类似物被设想用于治疗各种病症，包括但不限于以抑郁症，炎性皮肤病症，糖尿病，哮喘，慢性阻塞性肺疾病（COPD），肾脏疾病为特征的抑郁症和病症，和缺血性脑损伤。

5. 发明申请

US20110319277A1 PRPK-TPRKB MODULATORS AND USES THEREOF 有权
标题翻译： PRPK-TPRKB调节剂及其用途
公开(公告)号：US20110319277A1
公开(公告)日：2011-12-29
申请号：US13163192
申请日：2011-06-17
申请人： Eun Sun Park , Henry E. Pelish , Astrid S. Clarke , Grace L. Williams , Maria Paola Castaldi , Alexander Arefolov , Jennifer E. Ring , Matthew D. Shair , Randall W. King
发明人： Eun Sun Park , Henry E. Pelish , Astrid S. Clarke , Grace L. Williams , Maria Paola Castaldi , Alexander Arefolov , Jennifer E. Ring , Matthew D. Shair , Randall W. King
IPC分类号： C12Q1/48 , C40B30/00 , G01N33/577
CPC分类号： C12Q1/485 , G01N2500/02
摘要： The present invention provides methods of identifying an agent that modulates PRPK, TPRKB, OSGEP, LAGE3 and its homologs, PRPK/TPRKB complex, and/or KEOPS complex. The present invention also provides compositions of such agents and methods of treating a disease, disorder, or condition associated with PRPK, TPRKB, OSGEP, LAGE3 and its homologs family (CT antigens), PRPK/TPRKB complex, and/or KEOPS complex using such an agent or composition.
摘要翻译：本发明提供鉴定调节PRPK，TPRKB，OSGEP，LAGE3及其同源物，PRPK / TPRKB复合物和/或KEOPS复合物的试剂的方法。本发明还提供了这样的药剂组合物和治疗与PRPK，TPRKB，OSGEP，LAGE3及其同系物家族（CT抗原），PRPK / TPRKB复合物和/或KEOPS复合物相关的疾病，病症或病症的方法代理或组合。

6. 发明授权

US09790253B2 OSW-1 analogs and conjugates, and uses thereof 有权
公开(公告)号：US09790253B2
公开(公告)日：2017-10-17
申请号：US14118589
申请日：2012-05-18
申请人： Matthew D. Shair , Anthony William George Burgett
发明人： Matthew D. Shair , Anthony William George Burgett
IPC分类号： C07H15/24 , C07J17/00 , C07J41/00 , C07J43/00 , C07J51/00 , A61K47/48
CPC分类号： C07J17/005 , A61K47/6803 , A61K47/6849 , A61K47/6851 , C07H15/24 , C07J41/0055 , C07J43/003 , C07J51/00
摘要： Provided are a number of compounds structurally related to OSW-1, a natural compound that binds OSBPs. Also provided are pharmaceutical compositions comprising the OSW-1 analogs, as well as methods for use of these OSW-1 analogs, or pharmaceutically acceptable salts, enantiomers, or stereoisomers thereof in the treatment of atherosclerosis. Alzheimer's disease, and cancer, including p21-deficient cancer. Conjugates of OSW-1 analogs with monoclonal antibodies, including monoclonal antibodies targeted to cancer cells, are also provided. Also provided are pharmaceutical compositions comprising the conjugates, as well as methods for use of these conjugates, in the treatment of cancer, including p21-deficient cancer.

7. 发明授权

US6020341A Enediyne quinone imines and methods of preparation and use thereof 失效
标题翻译：烯二炔醌及其制备方法及用途
公开(公告)号：US6020341A
公开(公告)日：2000-02-01
申请号：US849658
申请日：1997-10-16
申请人： Samuel J. Danishefsky , Matthew D. Shair , Taeyoung Yoon , Ting-Chao Chou , Karoline K. Mosny
发明人： Samuel J. Danishefsky , Matthew D. Shair , Taeyoung Yoon , Ting-Chao Chou , Karoline K. Mosny
IPC分类号： A61K47/48 , C07D491/044 , C07D491/08 , A61K31/47 , C07D221/18
CPC分类号： C07D491/08 , A61K47/48384 , A61K47/48407
摘要： A quinone imine enediyne possessing cytotoxic activity towards cancer cells having general structure (I) wherein R.sub.1, R.sub.2 and R.sub.3 are independently the same or different and are H, Br, Cl, F, NH.sub.2, CO.sub.2 H, OH, linear or branched alkyl, etc.; wherein R.sub.4 is H, OH or linear or branched alkoxy, linear or branched alkoxycarbonyl, etc.; wherein R.sub.5 is H, Br, Cl, F, O.dbd., OH or S--SR, or linear or branched alkyl, etc.; wherein R.sub.6 is H, Br, Cl, F, CO.sub.2 H, OH or S--SR', or linear or branched alkyl, etc.; wherein R.sub.7 is H, OH or S--SR", or linear or branched alkyl, linear or branched alkoxycarbonyl, linear or branched alkoxy or linear or branched hydroxyalkyl; and wherein R, R' and R" are independently the same or different and are linear or branched alkyl, linear or branched acyl or linear or branched alkoxyalkyl. Also provided are conjugates of the compound with cleavable peptides, enzymes, carbohydrates and monoclonal antibodies immunoreactive with cancer cells, as well as compositions comprising the analogues and conjugates, and methods of synthesis and treatment of tumors.
摘要翻译： PCT No.PCT / US95 / 15678 Sec。 371日期：1997年10月16日 102（e）日期1997年10月16日PCT 1995年12月1日PCT PCT。出版物WO96 / 16655 日期：1996年6月6日具有对具有一般结构（I）的癌细胞具有细胞毒性活性的醌亚胺烯二酮，其中R1，R2和R3独立地相同或不同，为H，Br，Cl，F，NH2，CO2H，OH，线性或支链烷基等; 其中R4是H，OH或直链或支链烷氧基，直链或支链烷氧基羰基等; 其中R 5为H，Br，Cl，F，O =，OH或S-SR，或直链或支链烷基等; 其中R6是H，Br，Cl，F，CO2H，OH或S-SR'，或直链或支链烷基等; 其中R 7为H，OH或S-SR“，或直链或支链烷基，直链或支链烷氧基羰基，直链或支链烷氧基或直链或支链羟烷基; 并且其中R，R'和R“独立地相同或不同，并且是直链或支链的烷基，直链或支链的酰基或直链或支链烷氧基烷基。还提供了化合物与可切割肽，酶，碳水化合物和与癌细胞免疫反应的单克隆抗体的缀合物，以及包含类似物和缀合物的组合物，以及合成和治疗肿瘤的方法。

8. 发明授权

US09193989B2 PRPK-TPRKB modulators and uses thereof 有权
标题翻译： PRPK-TPRKB调节剂及其用途
公开(公告)号：US09193989B2
公开(公告)日：2015-11-24
申请号：US13163192
申请日：2011-06-17
申请人： Eun Sun Park , Henry E. Pelish , Astrid S. Clarke , Grace L. Williams , Maria Paola Castaldi , Alexander Arefolov , Jennifer E. Ring , Matthew D. Shair , Randall W. King
发明人： Eun Sun Park , Henry E. Pelish , Astrid S. Clarke , Grace L. Williams , Maria Paola Castaldi , Alexander Arefolov , Jennifer E. Ring , Matthew D. Shair , Randall W. King
IPC分类号： C12Q1/48
CPC分类号： C12Q1/485 , G01N2500/02
摘要： The present invention provides methods of identifying an agent that modulates PRPK, TPRKB, OSGEP, LAGE3 and its homologs, PRPK/TPRKB complex, and/or KEOPS complex. The present invention also provides compositions of such agents and methods of treating a disease, disorder, or condition associated with PRPK, TPRKB, OSGEP, LAGE3 and its homologs family (CT antigens), PRPK/TPRKB complex, and/or KEOPS complex using such an agent or composition.
摘要翻译：本发明提供鉴定调节PRPK，TPRKB，OSGEP，LAGE3及其同源物，PRPK / TPRKB复合物和/或KEOPS复合物的试剂的方法。本发明还提供了这样的药剂组合物和治疗与PRPK，TPRKB，OSGEP，LAGE3及其同系物家族（CT抗原），PRPK / TPRKB复合物和/或KEOPS复合物相关的疾病，病症或病症的方法代理或组合。

9. 发明申请

US20140135279A1 OSW-1 ANALOGS AND CONJUGATES, AND USES THEREOF 有权
标题翻译： OSW-1模拟和结合及其用途
公开(公告)号：US20140135279A1
公开(公告)日：2014-05-15
申请号：US14118589
申请日：2012-05-18
申请人： Matthew D. Shair
发明人： Matthew D. Shair
IPC分类号： C07J17/00
CPC分类号： C07J17/005 , A61K47/6803 , A61K47/6849 , A61K47/6851 , C07H15/24 , C07J41/0055 , C07J43/003 , C07J51/00
摘要： Provided are a number of compounds structurally related to OSW-1, a natural compound that binds OSBPs. Also provided are pharmaceutical compositions comprising the OSW-1 analogs, as well as methods for use of these OSW-1 analogs, or pharmaceutically acceptable salts, enantiomers, or stereoisomers thereof in the treatment of atherosclerosis. Alzheimer's disease, and cancer, including p21-deficient cancer. Conjugates of OSW-1 analogs with monoclonal antibodies, including monoclonal antibodies targeted to cancer cells, are also provided. Also provided are pharmaceutical compositions comprising the conjugates, as well as methods for use of these conjugates, in the treatment of cancer, including p21-deficient cancer.
摘要翻译：提供了许多与OSW-1结合相关的化合物，OSW-1是结合OSBPs的天然化合物。还提供了包含OSW-1类似物的药物组合物，以及用于治疗动脉粥样硬化的这些OSW-1类似物或其药学上可接受的盐，对映异构体或立体异构体的方法。阿尔茨海默病和癌症，包括p21缺陷型癌症。还提供了OSW-1类似物与单克隆抗体的缀合物，包括靶向癌细胞的单克隆抗体。还提供了包含缀合物的药物组合物以及用于这些缀合物的方法用于治疗癌症，包括p21缺陷型癌症。

10. 发明授权

US07109377B2 Synthesis of combinatorial libraries of compounds reminiscent of natural products 有权
公开(公告)号：US07109377B2
公开(公告)日：2006-09-19
申请号：US10185364
申请日：2002-06-27
申请人： Stuart L. Schreiber , Matthew D. Shair , Derek S. Tan , Michael A. Foley , Brent R. Stockwell
发明人： Stuart L. Schreiber , Matthew D. Shair , Derek S. Tan , Michael A. Foley , Brent R. Stockwell
IPC分类号： C07C233/00
CPC分类号： C07D307/33 , B01J19/0046 , B01J2219/00317 , B01J2219/00364 , B01J2219/00367 , B01J2219/005 , B01J2219/00511 , B01J2219/00531 , B01J2219/00585 , B01J2219/00596 , B01J2219/00605 , B01J2219/0061 , B01J2219/00612 , B01J2219/0065 , B01J2219/00659 , B01J2219/00702 , C07C227/10 , C07C231/12 , C07C235/40 , C07C237/20 , C07C237/24 , C07C247/14 , C07C2601/14 , C07C2601/16 , C07D261/20 , C07D493/04 , C40B40/00 , C40B60/14 , C40B80/00 , G01N33/50 , Y10S435/975 , C07C229/34
摘要： The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.

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