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1. 发明授权

US08895050B2 Flavors, flavor modifiers, tastants, taste enhancers, umami or sweet tastants, and/or enhancers and use thereof 有权
标题翻译：调味剂，调味剂，滋味剂，增味剂，鲜味或甜味剂，和/或增强剂及其用途
公开(公告)号：US08895050B2
公开(公告)日：2014-11-25
申请号：US13336272
申请日：2011-12-23
申请人： Catherine Tachdjian , Andrew P. Patron , Sara L. Adamski-Werner , Farid Bakir , Qing Chen , Vincent Darmohusodo , Stephen Terrence Hobson , Xiaodong Li , Ming Qi , Daniel H. Rogers , Marketa Rinnova , Guy Servant , Xiao-Qing Tang , Mark Zoller , David Wallace , Amy Xing , Klaus Gubernator
发明人： Catherine Tachdjian , Andrew P. Patron , Sara L. Adamski-Werner , Farid Bakir , Qing Chen , Vincent Darmohusodo , Stephen Terrence Hobson , Xiaodong Li , Ming Qi , Daniel H. Rogers , Marketa Rinnova , Guy Servant , Xiao-Qing Tang , Mark Zoller , David Wallace , Amy Xing , Klaus Gubernator
IPC分类号： A61K47/00 , G01N33/74 , C07C275/34 , G01N33/543 , C07C235/54 , C07C275/30 , G01N33/566 , C07C233/65 , A23L1/226 , C07D317/68 , C07D307/84
CPC分类号： G01N33/543 , A23L2/56 , A23L27/202 , A23L27/203 , A23L27/2054 , A23L27/88 , A23V2002/00 , A61K8/4973 , A61K8/55 , A61K47/22 , A61K47/24 , C07C233/65 , C07C235/54 , C07C275/30 , C07C275/34 , C07D307/84 , C07D317/68 , C07D405/12 , C07F9/65517 , G01N33/5041 , G01N33/566 , G01N33/74 , G01N2333/726
摘要： The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers, —savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.
摘要翻译：本发明涉及某些非天然存在的非肽酰胺化合物和酰胺衍生物，例如草酰胺，脲和丙烯酰胺，是有用的风味或调味剂，例如调味剂或调味剂和风味或味道增强剂，更特别地，用于食品，饮料和其它可食用或口服给药的药物产品或组合物的美味（味道味道）或甜味调节剂，美味或甜味调味剂和咸味或甜味增味剂。

2. 发明授权

US08633186B2 Modulation of chemosensory receptors and ligands associated therewith 有权
标题翻译：与其相关的化学感应受体和配体的调节
公开(公告)号：US08633186B2
公开(公告)日：2014-01-21
申请号：US12663634
申请日：2008-06-03
申请人： Catherine Tachdjian , Donald S. Karanewsky , Xiao-Qing Tang , Xiaodong Li , Feng Zhang , Guy Servant , Qing Chen , Vincent Darmohusodo , Richard Fine , Joseph R. Fotsing , Jeffrey Robert Hammaker , Xinshan Kang , Rachel D. A. Kimmich , Boris Klebansky , Haitian Liu , Goran Petrovic , Marketa Rinnova , Sara Adamski-Werner , Jeffrey Yamamoto , Hong Zhang , Albert Zlotnik , Karen Zoller
发明人： Catherine Tachdjian , Donald S. Karanewsky , Xiao-Qing Tang , Xiaodong Li , Feng Zhang , Guy Servant , Qing Chen , Vincent Darmohusodo , Richard Fine , Joseph R. Fotsing , Jeffrey Robert Hammaker , Xinshan Kang , Rachel D. A. Kimmich , Boris Klebansky , Haitian Liu , Goran Petrovic , Marketa Rinnova , Sara Adamski-Werner , Jeffrey Yamamoto , Hong Zhang , Albert Zlotnik , Mark Zoller
IPC分类号： C07D239/95 , C07D285/16 , A61K31/517 , A61K31/54
CPC分类号： A61K31/495 , A61K31/517 , A61K31/519 , C07D239/80 , C07D239/93 , C07D239/95 , C07D239/96 , C07D285/15 , C07D405/12 , C07D417/04 , C07D417/12 , C07D487/04 , C07D491/04 , C07D495/04 , C07D495/14 , C07D513/04 , C07D513/20 , C07H17/00 , G01N33/74 , G01N2333/726 , G01N2500/00 , G01N2500/04 , G06F19/16 , G06F19/18
摘要： The present invention includes methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors, and modifiers capable of modulating chemosensory receptors and their ligands. The present invention also includes modifiers of chemosensory receptors and their ligands having Formula (I), its subgenus, and specific compounds. Furthermore, the present invention includes ingestible compositions comprising the modifiers of chemosensory receptors and their ligands and methods of using the modifiers of chemosensory receptors and their ligands to enhance the sweet taste of an ingestible composition or treat a condition associated with a chemosensory receptor. In addition, the present invention include processes for preparing the modifiers of chemosensory receptors and their ligands.
摘要翻译：本发明包括用于鉴定化学感受器及其配体的调节剂的方法，例如通过确定测试实体是否适合与化学感应受体的金星蝇捕获区域内的一个或多个相互作用位点相互作用，以及能够调节化学感应受体及其配体。本发明还包括具有式（I），其亚属和特定化合物的化学感应受体及其配体的改性剂。此外，本发明包括含有化学感应受体调节剂及其配体的可摄入组合物，以及使用化学感应受体及其配体改性剂增强可摄入组合物的甜味或治疗与化学感觉受体相关的病症的方法。此外，本发明包括制备化学感受器及其配体的改性剂的方法。

3. 发明申请

US20130183252A1 COMPOUNDS THAT INHIBIT (BLOCK) BITTER TASTE IN COMPOSITION AND METHODS OF MAKING SAME 审中-公开
标题翻译：化合物组合物中的抑制（块状）双酚A的化合物及其制备方法
公开(公告)号：US20130183252A1
公开(公告)日：2013-07-18
申请号：US13370832
申请日：2012-02-10
申请人： Xiaodong LI , Andrew Patron , Catherine Tachdjian , Hong Xu , Qing Li , Alexey Pronin , Guy Servant , Lan Zhang , Thomas Brady , Vincent Darmohusodo , Melissa Arellano , Victor Selchau , Brett Weylan Ching , Donald S. Karanewsky , Paul Brust , Jing Ling , Wen Zhao , Chad Priest
发明人： Xiaodong LI , Andrew Patron , Catherine Tachdjian , Hong Xu , Qing Li , Alexey Pronin , Guy Servant , Lan Zhang , Thomas Brady , Vincent Darmohusodo , Melissa Arellano , Victor Selchau , Brett Weylan Ching , Donald S. Karanewsky , Paul Brust , Jing Ling , Wen Zhao , Chad Priest
IPC分类号： C07C311/17 , C07D223/18 , A61K8/46 , A61Q11/00 , C07D213/71 , C07D333/34 , C07D317/58 , A61K8/49 , C07C311/16 , C07C311/19 , C07C311/46 , C07C311/18 , C07C233/73 , C07D333/20 , C07D213/42 , C07D217/08 , A23L1/22 , C07D307/52
CPC分类号： C07C311/17 , A23L27/86 , A61K8/46 , A61K8/466 , A61K8/4933 , A61K8/494 , A61K8/4973 , A61K8/498 , A61K8/4986 , A61K31/135 , A61K31/4439 , A61K31/485 , A61K31/60 , A61K31/704 , A61K45/06 , A61Q11/00 , C07C233/73 , C07C311/04 , C07C311/13 , C07C311/16 , C07C311/18 , C07C311/19 , C07C311/20 , C07C311/21 , C07C311/29 , C07C311/46 , C07C323/49 , C07C335/16 , C07C335/18 , C07D213/42 , C07D213/71 , C07D217/08 , C07D223/18 , C07D307/14 , C07D307/52 , C07D317/58 , C07D333/20 , C07D333/34 , A61K2300/00
摘要： The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.
摘要翻译：本发明涉及T2R味觉受体家族中的特定人类味觉受体对存在于例如咖啡中的特定苦味化合物的反应的发现。此外，本发明涉及含有作为苦味抑制剂的特定化合物和组合物的发现，以及其作为例如咖啡和咖啡风味食品，饮料和药物中的苦味抑制剂或风味调节剂的用途。此外，本发明涉及一种拮抗多种不同人类T2R的化合物的发现及其在测定中的用途以及用于摄取人类和动物的组合物中的苦味阻滞剂。

4. 发明授权

US08420145B2 Isosorbide derivatives and their use as flavor modifiers, tastants, and taste enhancers 有权
标题翻译：异山梨醇衍生物及其作为调味剂，促味剂和味觉增强剂的用途
公开(公告)号：US08420145B2
公开(公告)日：2013-04-16
申请号：US12396917
申请日：2009-03-03
申请人： Catherine Tachdjian , Donald S. Karanewsky , Sara L. Adamski-Werner , Jeffrey M. Yamamoto , Guy Servant
发明人： Catherine Tachdjian , Donald S. Karanewsky , Sara L. Adamski-Werner , Jeffrey M. Yamamoto , Guy Servant
IPC分类号： A23L1/22 , A23L2/56 , C07D401/02 , C07D277/20 , C07D249/04 , C07D405/02 , C07D231/10 , C07D213/02 , C07D333/10 , C07D307/04
CPC分类号： A23L1/22664 , A23L2/60 , A23L27/205 , A23L27/2052 , C07D493/04
摘要： The present invention provides isosorbide derivatives having the formula shown below and certain subgenera or species thereof, as flavor or taste modifiers, particularly, savory (“umami”) taste modifiers, savory flavoring agents and savory flavor enhancers in foods, beverages, and other comestible compositions,
摘要翻译：本发明提供了具有下列结构的异山梨醇衍生物和某些亚属或其物种，作为食品，饮料和其它可食用组合物中的风味或调味剂，特别是美味（鲜味）调味剂，咸味调味剂和咸味增味剂，

5. 发明申请

US20110224095A1 Expression of functional human olfactory cyclic nucleotide gated (CNG) channel in recombinant host cells and use thereof in cell based assays to identify smell modulators 有权
标题翻译：功能性人嗅环核苷酸门控（CNG）通道在重组宿主细胞中的表达及其在基于细胞的测定中的应用，以鉴定气味调节剂
公开(公告)号：US20110224095A1
公开(公告)日：2011-09-15
申请号：US11326441
申请日：2006-01-06
申请人： Mark Zoller , Hong Xu , Lena Staszewski , Bryan Moyer , Alexey Pronin , Jon Elliot Adler , Guy Servant , Nicholas Callamaras
发明人： Mark Zoller , Hong Xu , Lena Staszewski , Bryan Moyer , Alexey Pronin , Jon Elliot Adler , Guy Servant , Nicholas Callamaras
IPC分类号： C40B30/06 , C12Q1/02
CPC分类号： C07K14/705
摘要： The present invention relates to isolated nucleic acid sequences that encode human olfactory cyclic nucleotide gated (CNG) channel subunits, and the corresponding polypeptides. The invention further relates to the use of human CNG channels to profile, screen for, and identify compounds that modulate the human olfactory CNG channel. More specifically, the invention relates to the expression of the human olfactory CNG channel in cells, preferably mammalian cells, and the use of these cells in high throughput cell-based assays to identify compounds that enhance or block human olfactory CNG function. Compounds that activate the olfactory CNG channel will enhance smell and can be used to make foods more palatable for individuals with attenuated olfactory function. Conversely, compounds that inhibit the olfactory CNG channel will inhibit smell and can be use to block malodors. Additionally, the invention relates to the use of cell-based olfactory CNG channel assays to identify modulates of G-protein coupled receptor (GPCRs) and other proteins that regulate cyclic nucleotide levels.
摘要翻译：本发明涉及编码人嗅环核苷酸门控（CNG）通道亚基的分离的核酸序列，以及相应的多肽。本发明还涉及使用人类CNG通道来分析，筛选和鉴定调节人嗅觉CNG通道的化合物。更具体地，本发明涉及人嗅觉CNG通道在细胞，优选哺乳动物细胞中的表达，以及这些细胞在高通量细胞分析中的应用，以鉴定增强或阻断人嗅觉CNG功能的化合物。激活嗅觉CNG通道的化合物将增强气味，可用于使食物对于具有减弱的嗅觉功能的个体更可口。相反，抑制嗅觉CNG通道的化合物将抑制气味，并可用于阻止恶臭。另外，本发明涉及使用基于细胞的嗅觉CNG通道测定来鉴定调节环核苷酸水平的G蛋白偶联受体（GPCR）和其他蛋白质的调节。

6. 发明授权

US07928111B2 Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors 有权
标题翻译：包括取代的噻吩并嘧啶酮衍生物作为调节化学感应受体的配体的化合物
公开(公告)号：US07928111B2
公开(公告)日：2011-04-19
申请号：US11836074
申请日：2007-08-08
申请人： Catherine Tachdjian , Xiao-Qing Tang , Sara Werner , Marketa Rinnova , Qing Chen , Guy Servant , Xiaodong Li , Feng Zhang , Haitian Liu , Albert Zlotnik , Mark Zoller , Boris Klebansky , Richard Fine , Xinshan Kang
发明人： Catherine Tachdjian , Xiao-Qing Tang , Sara Werner , Marketa Rinnova , Qing Chen , Guy Servant , Xiaodong Li , Feng Zhang , Haitian Liu , Albert Zlotnik , Mark Zoller , Boris Klebansky , Richard Fine , Xinshan Kang
IPC分类号： A61K31/519
CPC分类号： C07D513/04 , A23L2/39 , A23L2/60 , A23L27/30 , A23L27/31 , A23L27/33 , A23L27/34 , A23L27/88 , C07D215/42 , C07D215/54 , C07D215/56 , C07D239/70 , C07D239/84 , C07D239/94 , C07D239/95 , C07D285/16 , C07D417/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/056 , C07D493/04 , C07D495/04 , C07D495/14 , C07D513/20 , G01N33/566
摘要： The present invention provides compounds including substituted thienopyrimidinone derivatives of Formula (IIc) as ligands for modulating chemosensory receptors: These compounds are useful as sweet taste enhancers in comestible or medicinal compositions. The present invention also provides screening methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors as well as modifiers capable of modulating chemosensory receptors and their ligands.
摘要翻译：本发明提供了包含式（IIc）的取代的噻吩并嘧啶酮衍生物作为调节化学感应受体的配体的化合物：这些化合物可用作食用或药用组合物中的甜味增强剂。本发明还提供了用于鉴定化学感应受体及其配体的调节剂的筛选方法，例如通过确定测试实体是否适合与化学感应受体的金星蝇捕获结构域内的一个或多个相互作用位点相互作用，以及能够调节化学感受器及其配体。

7. 发明申请

US20090220662A1 ISOSORBIDE DERIVATIVES AND THEIR USE AS FLAVOR MODIFIERS, TASTANTS, AND TASTE ENHANCERS 有权
标题翻译：异烟肼衍生物及其作为改性剂，TASTANTS和增强剂的用途
公开(公告)号：US20090220662A1
公开(公告)日：2009-09-03
申请号：US12396917
申请日：2009-03-03
申请人： Catherine TACHDJIAN , Donald S. Karanewsky , Sara L. Adamski-Werner , Jeffrey M. Yamamoto , Guy Servant
发明人： Catherine TACHDJIAN , Donald S. Karanewsky , Sara L. Adamski-Werner , Jeffrey M. Yamamoto , Guy Servant
IPC分类号： A23L1/226 , C07D249/04 , C07D401/02 , C07D261/06 , C07D493/02 , C07D409/14 , C07D277/20 , C07D405/14
CPC分类号： A23L1/22664 , A23L2/60 , A23L27/205 , A23L27/2052 , C07D493/04
摘要： The present invention provides isosorbide derivatives having the formula shown below and certain subgenera or species thereof, as flavor or taste modifiers, particularly, savory (“umami”) taste modifiers, savory flavoring agents and savory flavor enhancers in foods, beverages, and other comestible compositions,
摘要翻译：本发明提供具有下列结构的异山梨醇衍生物和某些亚属或其种类作为调味剂或调味剂，特别是食品，饮料和其他食物中的美味（“鲜味”）调味剂，咸味调味剂和咸味增味剂组合物，

8. 发明申请

US20080268471A1 USE OF SPECIFIC T2R RECEPTORS TO IDENTIFY COMPOUNDS THAT BLOCK BITTER TASTE 有权
标题翻译：使用特异性T2R受体鉴别化合物
公开(公告)号：US20080268471A1
公开(公告)日：2008-10-30
申请号：US12041956
申请日：2008-03-04
申请人： Alexey Pronin , Judy Connor , Huixian Tang , Walter Keung , Guy Servant , Jon Elliot Adler , Shawn O'Connell , Paul Brust
发明人： Alexey Pronin , Judy Connor , Huixian Tang , Walter Keung , Guy Servant , Jon Elliot Adler , Shawn O'Connell , Paul Brust
IPC分类号： G01N33/53 , G01N33/566
CPC分类号： G01N33/566 , G01N2333/726 , G01N2500/02 , G01N2500/04 , G01N2500/10
摘要： Assays for identifying compounds that modulate, preferably inhibit bitter taste associated with the activation of hT2R4, hT2R44 and/or hT2R61 are provided. The compounds identified according to these assays should modulate, e.g., inhibit bitter taste associated with bitter tasting compounds including quinine, 6-nitrosaccharin, saccharin and/or denatonium. These compounds are useful additives for foods, beverages or medicinal preparationshaving a bitter taste.
摘要翻译：提供了用于鉴定调节，优选抑制与激活hT2R4，hT2R44和/或hT2R61相关的苦味的化合物的分析。根据这些测定法鉴定的化合物应调节，例如抑制与苦味化合物（包括奎宁，6-亚硝基糖精，糖精和/或丹参）相关的苦味。这些化合物是具有苦味的食品，饮料或药用制剂的有用添加剂。

9. 发明申请

US20050059094A1 Electrophysiological assay using oocytes that express human ENaC and the use phenamil to improve the effect of ENaC enhancers in assays using membrane potential reporting dyes 有权
标题翻译：使用表达人类ENaC的卵母细胞进行电生理测定，并使用苯胺胺改善ENaC增强子在使用膜电位报告染料的测定中的作用
公开(公告)号：US20050059094A1
公开(公告)日：2005-03-17
申请号：US10887233
申请日：2004-07-09
申请人： Guy Servant , Hong Chang , Cyril Redcrow , Sumita Ray , Imran Clark
发明人： Guy Servant , Hong Chang , Cyril Redcrow , Sumita Ray , Imran Clark
IPC分类号： C07H21/04 , C07K1/00 , C12N1/20 , C12P21/06 , C12Q20060101 , G01N33/50 , G01N33/53 , G01N33/566 , G01N33/567 , G01N33/68
CPC分类号： G01N33/6872 , C12N15/85 , C12N2320/10 , C12N2503/02 , C12Q1/025 , G01N33/5044 , G01N2500/10
摘要： In one aspect, the present invention relates to a mammalian cell-based high-throughput assay for the profiling and screening of human epithelial sodium channel (hENaC) cloned from a human kidney c-DNA library and is also expressed in other tissues including human taste tissue. The present invention further relates to amphibian oocyte-based medium-throughput electrophysiological assays for identifying human ENaC modulators, preferably ENaC enhancers. Compounds that modulate ENaC function in a cell-based ENaC assay are expected to affect salty taste in humans. The assays described herein have advantages over existing cellular expression systems. In the case of mammalian cells, such assays can be run in standard 96 or 384 well culture plates in high-throughput mode with enhanced assay results being achieved by the use of a compound that inhibits ENaC function, preferably an amiloride derivative such as Phenamil. In the case of the inventive oocyte electrophysiological assays (two-electrode voltage-clamp technique), these assays facilitate the identification of compounds which specifically modulate human ENaC. The assays of the invention provide a robust screen useful to detect compounds that facilitate (enhance) or inhibit hENaC function. Compounds that enhance or block human ENaC channel activity should thereby modulate salty taste in humans.
摘要翻译：一方面，本发明涉及从人肾C-DNA文库克隆的人上皮钠通道（hENaC）的分析和筛选的基于哺乳动物细胞的高通量测定，并且还在包括人类味道的其它组织中表达组织。本发明还涉及用于鉴定人类ENaC调节剂，优选ENaC增强子的两栖动物基于卵母细胞的中等通量电生理测定法。在基于细胞的ENaC测定中调节ENaC功能的化合物预期会影响人类的咸味。本文所述的测定法优于现有的细胞表达系统。在哺乳动物细胞的情况下，这种测定可以在高通量模式的标准96或384孔培养板中进行，通过使用抑制ENaC功能的化合物，优选阿米洛利衍生物，如苯胺，可以实现增强的测定结果。在本发明的卵母细胞电生理测定（双电极电压钳技术）的情况下，这些测定有助于鉴定特异性调节人类ENaC的化合物。本发明的测定提供了可用于检测促进（增强）或抑制hENaC功能的化合物的强壮屏幕。增强或阻断人类ENaC通道活性的化合物应该调节人体的咸味。

10. 发明授权

US09459259B2 Electrophysiological assays using oocytes that express human enac and the use of phenamil to improve the effect of enac enhancers in assays using membrane potential reporting dyes 有权
公开(公告)号：US09459259B2
公开(公告)日：2016-10-04
申请号：US10563758
申请日：2004-07-09
申请人： Guy Servant , Hong Chang , Cyril Redcrow , Sumita Ray , Imran Clark , Bryan Moyer
发明人： Guy Servant , Hong Chang , Cyril Redcrow , Sumita Ray , Imran Clark , Bryan Moyer
IPC分类号： G01N33/68 , G01N33/50
CPC分类号： G01N33/6872 , C12N15/85 , C12N2320/10 , C12N2503/02 , C12Q1/025 , G01N33/5044 , G01N2500/10
摘要： In one aspect, the present invention relates to a mammalian cell-based high-throughput assay for the profiling and screening of human epithelial sodium channel (hENaC) cloned from a human kidney c-DNA library and is also expressed in other tissues including human taste tissue. The present invention further relates to amphibian oocyte-based medium-throughput electrophysiological assays for identifying human ENaC modulators, preferably ENaC enhancers. Compounds that modulate ENaC function in a cell-based ENaC assay are expected to affect salty taste in humans. The assays described herein have advantages over existing cellular expression systems. In the case of mammalian cells, such assays can be run in standard 96 or 384 well culture plates in high-throughput mode with enhanced assay results being achieved by the use of a compound that inhibits ENaC function, preferably an amiloride derivative such as Phenamil. In the case of the inventive oocyte electrophysiological assays (two-electrode voltage-clamp technique), these assays facilitate the identification of compounds which specifically modulate human ENaC. The assays of the invention provide a robust screen useful to detect compounds that facilitate (enhance) or inhibit hENaC function. Compounds that enhance or block human ENaC channel activity should thereby modulate salty taste in humans.

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