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公开(公告)号：US10117948B2
公开(公告)日：2018-11-06
申请号：US15187169
申请日：2016-06-20
IPC分类号： A61K38/14 , A61K47/64 , C07K1/113 , C07K9/00 , A61K47/48 , C07K1/107 , C07K1/13 , C07K14/47 , A61K47/68
摘要： Disclosed are chemical transformations for the conjugation of unprotected peptide biomolecules. The disclosed chemical transformations relate to methods of selective cysteine and selenocysteine functionalization of unprotected peptide and protein molecules. The processes feature several significant advantages over existing methods of peptide modification, including specificity towards selenocysteine over other nucleophiles (e.g., amines, hydroxyls), excellent functional group tolerance, and mild reaction conditions. Also disclosed are syntheses of arylated cysteine and arylated selenocysteine peptide compounds.
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公开(公告)号：US20160367693A1
公开(公告)日：2016-12-22
申请号：US15187169
申请日：2016-06-20
CPC分类号： C07K1/1075 , A61K38/14 , A61K47/64 , A61K47/6851 , C07K1/1077 , C07K1/13 , C07K9/008 , C07K14/47
摘要： Disclosed are chemical transformations for the conjugation of unprotected peptide biomolecules. The processes feature several significant advantages over existing methods of peptide modification, including specificity towards selenocysteine over other nucleophiles (e.g., amines, hydroxyls), excellent functional group tolerance, and mild reaction conditions.
摘要翻译： 公开了用于未保护肽生物分子缀合的化学转化。 该方法具有优于现有的肽修饰方法的几个显着优点，包括对于其它亲核试剂（例如胺，羟基）的硒代半胱氨酸的特异性，优异的官能团耐受性和温和的反应条件。
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公开(公告)号：US20160031824A1
公开(公告)日：2016-02-04
申请号：US14776184
申请日：2014-03-17
IPC分类号： C07D235/16 , C07D405/04 , C07D403/04 , C07D401/12 , C07D409/12
CPC分类号： C07D235/16 , A61K31/4184 , A61K31/4439 , A61K45/06 , C07D235/08 , C07D401/12 , C07D403/04 , C07D405/04 , C07D409/12 , A61K2300/00
摘要： The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and pharmaceutical compositions thereof. The present invention also provides methods and kits using the inventive compounds and pharmaceutical compositions for treating and/or preventing diseases associated with protein aggregation, such as amyloidoses (e.g., Parkinson's disease and Alzheimer's disease), treating and/or preventing neurodegenerative diseases, treating and/or preventing diseases associated with Tar DNA binding protein 43 kDa, reducing or preventing protein aggregation, and/or modulating E3 ubiquitin ligase in a subject in need thereof.
摘要翻译： 本发明提供新的式（I）化合物及其药学上可接受的盐，溶剂合物，水合物，多晶型物，共晶体，互变异构体，立体异构体，同位素标记的衍生物，前药及其药物组合物。 本发明还提供使用本发明化合物和药物组合物治疗和/或预防与蛋白质聚集相关的疾病的方法和试剂盒，例如淀粉样变性（例如帕金森病和阿尔茨海默病），治疗和/或预防神经变性疾病，治疗和/ /或预防与Tar DNA结合蛋白43kDa相关的疾病，在有需要的受试者中减少或预防蛋白质聚集和/或调节E3泛素连接酶。
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![[2.2]paracyclophane-derived donor/acceptor-type molecules for OLED applications](/abs-image/US/2018/05/15/US09972791B2/abs.jpg.150x150.jpg)
公开(公告)号：US09972791B2
公开(公告)日：2018-05-15
申请号：US15172623
申请日：2016-06-03
IPC分类号： H01L51/00 , C07D487/08 , C09K11/06 , C07D209/94 , C07D403/10 , C08G61/02 , C08G61/12 , C08G73/06 , H01L51/52 , H01L51/50 , H01L51/05
CPC分类号： H01L51/0072 , C07D209/94 , C07D403/10 , C07D487/08 , C08G61/02 , C08G61/124 , C08G73/0672 , C08G2261/143 , C08G2261/146 , C08G2261/148 , C08G2261/149 , C08G2261/5222 , C08G2261/95 , C09K11/06 , C09K2211/1007 , C09K2211/1029 , C09K2211/1033 , C09K2211/1037 , C09K2211/1051 , C09K2211/1059 , C09K2211/1466 , H01L51/0035 , H01L51/0067 , H01L51/0558 , H01L51/5012 , H01L51/5024 , H01L51/5206 , H01L51/5221
摘要： Disclosed are [2.2]paracyclophane-derivative compounds and related polymers that are useful as stable, efficient, blue-light emitting compounds for OLED applications.
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公开(公告)号：US20210206791A1
公开(公告)日：2021-07-08
申请号：US16081370
申请日：2017-03-02
摘要： Disclosed are methods of selective cysteine and selenocysteine modification on peptide/protein molecules under physiologically relevant conditions. The methods feature several advantages over existing methods of peptide modification, such as specificity towards thiols and selenols over other nucleophiles (e.g., amines, hydroxyls), excellent functional group tolerance, and mild reaction conditions, including completely aqueous reaction conditions. Also disclosed are methods of preparing palladium complexes in the presence of oxygen.
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公开(公告)号：US09790188B2
公开(公告)日：2017-10-17
申请号：US14776184
申请日：2014-03-17
IPC分类号： C07D235/04 , A61K31/4184 , C07D235/16 , A61K45/06 , A61K31/4439 , C07D235/08 , C07D401/12 , C07D403/04 , C07D405/04 , C07D409/12
CPC分类号： C07D235/16 , A61K31/4184 , A61K31/4439 , A61K45/06 , C07D235/08 , C07D401/12 , C07D403/04 , C07D405/04 , C07D409/12 , A61K2300/00
摘要： The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and pharmaceutical compositions thereof. The present invention also provides methods and kits using the inventive compounds and pharmaceutical compositions for treating and/or preventing diseases associated with protein aggregation, such as amyloidoses (e.g., Parkinson's disease and Alzheimer's disease), treating and/or preventing neurodegenerative diseases, treating and/or preventing diseases associated with Tar DNA binding protein 43 kDa, reducing or preventing protein aggregation, and/or modulating E3 ubiquitin ligase in a subject in need thereof.
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![[2.2]Paracyclophane-Derived Donor/Acceptor-Type Molecules for OLED Applications](/abs-image/US/2016/12/08/US20160359118A1/abs.jpg.150x150.jpg)
7.发明申请[2.2]Paracyclophane-Derived Donor/Acceptor-Type Molecules for OLED Applications 有权[2.2]用于OLED应用的对环磷烷衍生的供体/受体型分子公开(公告)号：US20160359118A1
公开(公告)日：2016-12-08
申请号：US15172623
申请日：2016-06-03
IPC分类号： H01L51/00 , C08G73/06 , C07D209/94 , C07D403/10 , C07D487/08 , C09K11/06
CPC分类号： H01L51/0072 , C07D209/94 , C07D403/10 , C07D487/08 , C08G61/02 , C08G61/124 , C08G73/0672 , C08G2261/143 , C08G2261/146 , C08G2261/148 , C08G2261/149 , C08G2261/5222 , C08G2261/95 , C09K11/06 , C09K2211/1007 , C09K2211/1029 , C09K2211/1033 , C09K2211/1037 , C09K2211/1051 , C09K2211/1059 , C09K2211/1466 , H01L51/0035 , H01L51/0067 , H01L51/0558 , H01L51/5012 , H01L51/5024 , H01L51/5206 , H01L51/5221
摘要： Disclosed are [2.2]paracyclophane-derivative compounds and related polymers that are useful as stable, efficient, blue-light emitting compounds for OLED applications.
摘要翻译： 公开了可用作OLED应用的稳定，有效的蓝光发光化合物的[2.2]对环芳烃衍生物化合物和相关聚合物。
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公开(公告)号：US20150045570A1
公开(公告)日：2015-02-12
申请号：US14521727
申请日：2014-10-23
IPC分类号： C07F15/00
CPC分类号： C07F15/006 , C07B37/04 , C07F9/28 , C07F15/0086
摘要： Described are palladium precatalysts, and methods of making and using them. The palladium precatalysts show improved stability and improved reactivity in comparison to previously-described palladium precatalysts.
摘要翻译： 描述的是钯催化剂，以及制备和使用它们的方法。 与之前描述的钯催化剂相比，钯预催化剂显示改进的稳定性和改善的反应性。
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公开(公告)号：US09944607B2
公开(公告)日：2018-04-17
申请号：US14435790
申请日：2013-10-16
申请人： Whitehead Institute for Biomedical Research , Massachusetts Institute of Technology , The Broad Institute, Inc.
发明人： Benjamin Vincent , Luke Whitesell , Susan L. Lindquist , Willmen Youngsaye , Stephen L. Buchwald , Jean-Baptiste Langlois , Jun Pu , Benito Munoz , Sivaraman Dandapani
IPC分类号： C07D235/02 , C07D233/86 , C07D491/052 , A01N43/52 , A01N43/653 , A01N43/90 , A01N47/20 , A61K31/4184 , A61K31/4188 , A61K31/4196 , C07D491/107 , C12Q1/18
CPC分类号： C07D235/02 , A01N43/52 , A01N43/653 , A01N43/90 , A01N47/20 , A61K31/4184 , A61K31/4188 , A61K31/4196 , C07D233/86 , C07D491/052 , C07D491/107 , C12Q1/18 , G01N2333/395 , G01N2333/40
摘要： The present invention provides novel compounds (e.g., compounds of Formula (I)), and pharmaceutically acceptable salts, solvates, hydrate, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits comprising the inventive Compounds, or compositions thereof, for treating and/or preventing a fungal or protozoan infection, inhibiting the activity of a fungal or protozoan enzyme, killing a fungus or protozoan, or inhibiting the growth of a fungus or protozoan. The fungus may be a Candida species, Sacchawmyces species, or other pathogenic fungal species. The compounds of the invention may inhibit the activity of fungal or protozoan mitochondrial phosphate carrier protein.
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公开(公告)号：US09738610B2
公开(公告)日：2017-08-22
申请号：US14430308
申请日：2013-09-24
申请人： Whitehead Institute for Biomedical Research , The Broad Institute, Inc. , Massachusetts Institute of Technology
发明人： Benjamin Vincent , Luke Whitesell , Susan L. Lindquist , Willmen Youngsaye , Stephen L. Buchwald , Jean-Baptiste Langlois , Partha P. Nag , Amal Ting , Barbara J. Morgan , Benito Munoz , Sivaraman Dandapani , Bruce Tidor , Raja R. Srinivas
IPC分类号： C07D231/56 , C07D403/06 , C07D413/06 , A61K31/416 , A61K31/422 , A61P31/10 , C07D409/04 , C07D401/04 , C07D401/06 , C07D405/04 , C07D417/06
CPC分类号： C07D231/56 , C07D401/04 , C07D401/06 , C07D403/06 , C07D405/04 , C07D409/04 , C07D413/06 , C07D417/06
摘要： The present invention provides novel compounds (e.g., compounds of Formula (I)), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits comprising the inventive compounds, or compositions thereof, for treating and/or preventing a fungal or protozoan infection, inhibiting the activity of a fungal or protozoan enzyme, killing a fungus or protozoon, or inhibiting the growth of a fungus or protozoon. The fungus may be a Candida species, Aspergillus species, or other pathogenic fungal species. The compounds of the invention may inhibit the activity of fungal or protozoan cytochrome b and/or fungal or protozoan Hsp90. The present invention also provides synthetic methods of the inventive compounds.
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