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1. 发明申请

WO2008154286A2 MODULATION OF CHEMOSENSORY RECEPTORS AND LIGANDS ASSOCIATED THEREWITH 审中-公开
标题翻译：化学感受器的调节和与之相关的配体
公开(公告)号：WO2008154286A2
公开(公告)日：2008-12-18
申请号：PCT/US2008/065907
申请日：2008-06-05
申请人： SENOMYX, INC. , LI, Xiaodong , ZHANG, Feng , XU, Hong , TACHDJIAN, Catherine , ADAMSKI-WERNER, Sara , PATRON, Andrew , ZLOTNIK, Albert , ZOLLER, Mark , KLEBANSKY, Boris , FINE, Richard , KANG, Xinshan
发明人： LI, Xiaodong , ZHANG, Feng , XU, Hong , TACHDJIAN, Catherine , ADAMSKI-WERNER, Sara , PATRON, Andrew , ZLOTNIK, Albert , ZOLLER, Mark , KLEBANSKY, Boris , FINE, Richard , KANG, Xinshan
IPC分类号： A61K31/495 , A61P27/00 , C07D487/00 , C12N5/06 , G01N33/53 , G06G7/48
CPC分类号： A61K31/495 , C07F9/65586 , C07F9/65616 , G01N33/566 , G01N2333/726 , G01N2500/04 , G06F19/16 , G06F19/18
摘要： The present invention 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：本发明提供了用于鉴定化学感受器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。

2. 发明申请

WO2008154221A2 MODULATION OF CHEMOSENSORY RECEPTORS AND LIGANDS ASSOCIATED THEREWITH 审中-公开
标题翻译：化学感受器的调节和与之相关的配体
公开(公告)号：WO2008154221A2
公开(公告)日：2008-12-18
申请号：PCT/US2008/065650
申请日：2008-06-03
申请人： SENOMYX, INC. , TACHDJIAN, Catherine , KARANEWSKY, Donald S. , TANG, Xiao-qing , LI, Xiaodong , ZHANG, Feng , SERVANT, Guy , CHEN, Qing , DARMOHUSODO, Vincent , FINE, Richard , FOTSING, Joseph R. , HAMMAKER, Jeffrey Robert , KANG, Xinshan , KIMMICH, Rachel, D.A. , KLEBANSKY, Boris , LIU, Haitian , PETROVIC, Goran , RINNOVA, Marketa , ADAMSKI-WERNER, Sara , YAMAMOTO, Jeffrey , ZHANG, Hong , ZLOTNIK, Albert , ZOLLER, Mark
发明人： TACHDJIAN, Catherine , KARANEWSKY, Donald S. , TANG, Xiao-qing , LI, Xiaodong , ZHANG, Feng , SERVANT, Guy , CHEN, Qing , DARMOHUSODO, Vincent , FINE, Richard , FOTSING, Joseph R. , HAMMAKER, Jeffrey Robert , KANG, Xinshan , KIMMICH, Rachel, D.A. , KLEBANSKY, Boris , LIU, Haitian , PETROVIC, Goran , RINNOVA, Marketa , ADAMSKI-WERNER, Sara , YAMAMOTO, Jeffrey , ZHANG, Hong , ZLOTNIK, Albert , ZOLLER, Mark
IPC分类号： A61K31/495 , A61K31/517 , A61K31/519 , A61P27/00 , C07D487/00 , C12N5/06 , G01N33/53
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 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

WO2009025793A2 IDENTIFICATION OF HUMAN T2R RECEPTORS THAT RESPOND TO BITTER COMPOUNDS THAT ELICIT THE BITTER TASTE IN COMPOSITIONS, AND THE USE THEREOF IN ASSAYS TO IDENTIFY COMPOUNDS THAT INHIBIT (BLOCK) BITTER TASTE IN COMPOSITIONS AND USE THEREOF 审中-公开
标题翻译：识别符合组合物中双歧杆菌组合物的双特异度化合物的人类T2R受体，以及其在测定中的用途，以鉴定组合物中的禁止（块状）双歧杆菌组合物及其用途的化合物
公开(公告)号：WO2009025793A2
公开(公告)日：2009-02-26
申请号：PCT/US2008/009864
申请日：2008-08-19
申请人： SENOMYX, INC. , LI, Xiaodong , PATRON, Andrew , TACHDJIAN, Catherine , XU, Hong , LI, Qing , PRONIN, Alexey , SERVANT, Guy , ZHANG, Lan , BRADY, Thomas , DARMOHUSODO, Vincent , ARELLANO, Melissa , SELCHAU, Victor , CHING, Brett Weylan , KARANEWSKY, Donald S. , BRUST, Paul , LING, Jing , ZHAO, Wen , PRIEST, Chad
发明人： LI, Xiaodong , PATRON, Andrew , TACHDJIAN, Catherine , XU, Hong , LI, Qing , PRONIN, Alexey , SERVANT, Guy , ZHANG, Lan , BRADY, Thomas , DARMOHUSODO, Vincent , ARELLANO, Melissa , SELCHAU, Victor , CHING, Brett Weylan , KARANEWSKY, Donald S. , BRUST, Paul , LING, Jing , ZHAO, Wen , PRIEST, Chad
IPC分类号： C12Q1/68
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味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. 发明申请

WO2011159781A2 BITTER TASTE MODULATORS 审中-公开
标题翻译： BITTER TASTE调制器
公开(公告)号：WO2011159781A2
公开(公告)日：2011-12-22
申请号：PCT/US2011/040491
申请日：2011-06-15
申请人： SENOMYX, INC. , TACHDJIAN, Catherine , LI, Xiaodong , KARANEWSKY, Donald S. , FOTSING, Joseph , PATRON, Andrew , DARMOHUSODO, Vincent , SELCHAU, Victor , CHING, Brett
发明人： TACHDJIAN, Catherine , LI, Xiaodong , KARANEWSKY, Donald S. , FOTSING, Joseph , PATRON, Andrew , DARMOHUSODO, Vincent , SELCHAU, Victor , CHING, Brett
IPC分类号： C07D307/46 , C07D307/54 , C07C233/81 , A61K31/341 , A61K31/195 , A23L1/015 , A23L1/29 , A61P43/00
CPC分类号： C07C235/40 , A23K20/121 , A23L27/86 , C07C233/63
摘要： The present invention includes antagonists of human type 2 taste receptors (hT2Rs) having structural Formula (I). The present invention also provides compositions containing these antagonists, the use of these antagonists for modulating taste perception, particularly bitter taste, and the method of preparing these antagonists (I).
摘要翻译：本发明包括具有结构式（I）的人2型味觉受体（hT2Rs）的拮抗剂。本发明还提供含有这些拮抗剂的组合物，这些拮抗剂用于调节味觉，特别是苦味的用途以及制备这些拮抗剂的方法（I）。

5. 发明申请

WO2011123693A1 SWEET FLAVOR MODIFIER 审中-公开
标题翻译：甜味调味剂
公开(公告)号：WO2011123693A1
公开(公告)日：2011-10-06
申请号：PCT/US2011/030802
申请日：2011-03-31
申请人： SENOMYX, INC. , TACHDJIAN, Catherine , TANG, Xiao-Qing , KARANEWSKY, Donald, S. , SERVANT, Guy , LI, Xiaodong , ZHANG, Feng , CHEN, Qing , ZHANG, Hong , DAVIS, Timothy , DARMOHUSODO, Vincent , WONG, Melissa , SELCHAU, Victor
发明人： TACHDJIAN, Catherine , TANG, Xiao-Qing , KARANEWSKY, Donald, S. , SERVANT, Guy , LI, Xiaodong , ZHANG, Feng , CHEN, Qing , ZHANG, Hong , DAVIS, Timothy , DARMOHUSODO, Vincent , WONG, Melissa , SELCHAU, Victor
IPC分类号： A01N43/42 , A61K31/47
CPC分类号： C07D495/04 , A23L2/56 , A23L27/2054 , A23L27/88 , A23V2002/00 , A61K47/22 , C07D215/54 , C07D215/60 , C07D401/12 , C07D405/12 , C07D471/04 , C07D491/048
摘要： The present invention includes compounds having structural formula (I), or pharmaceutically acceptable salts, solvate, and/or ester thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of ingestible compositions. Furthermore, the present invention provides methods for preparing the compounds.
摘要翻译：本发明包括具有结构式（I）的化合物或其药学上可接受的盐，溶剂化物和/或酯。这些化合物可用作甜味调味剂。本发明还包括包含本发明化合物的组合物和增强可摄入组合物的甜味的方法。此外，本发明提供了制备化合物的方法。

6. 发明申请

WO2013025560A1 SWEET FLAVOR MODIFIER 审中-公开
标题翻译：甜味调味剂
公开(公告)号：WO2013025560A1
公开(公告)日：2013-02-21
申请号：PCT/US2012/050461
申请日：2012-08-10
申请人： SENOMYX, INC. , TACHDJIAN, Catherine , TANG, Xiao Qing , KARANEWSKY, Donald S. , SERVANT, Guy , LI, Xiaodong , ZHANG, Feng , CHEN, Qing , ZHANG, Hong , DAVIS, Timothy , DARMOHUSODO, Vincent , WONG, Melissa , SELCHAU, Victor
发明人： TACHDJIAN, Catherine , TANG, Xiao Qing , KARANEWSKY, Donald S. , SERVANT, Guy , LI, Xiaodong , ZHANG, Feng , CHEN, Qing , ZHANG, Hong , DAVIS, Timothy , DARMOHUSODO, Vincent , WONG, Melissa , SELCHAU, Victor
IPC分类号： C07D215/42 , C07D403/12 , C07D405/12 , C07D413/12 , A61K31/4725 , A61P1/00
CPC分类号： C07D405/12 , A23L2/60 , A23L27/88 , A23V2002/00 , A61K47/22 , C07D215/42 , C07D215/54 , C07D401/12 , C07D451/06
摘要： The present invention includes compounds having structural formula (I), or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of compositions.
摘要翻译：本发明包括具有结构式（I）的化合物或其盐或溶剂化物。这些化合物可用作甜味调味剂。本发明还包括包含本发明化合物的组合物和增强组合物甜味的方法。

7. 发明申请

WO2003001876A3 T1R HETERO-OLIGOMERIC TASTE RECEPTORS AND CELL LINES THAT EXPRESS SAID RECEPTORS AND USE THEREOF FOR IDENTIFICATION OF TASTE COMPOUNDS 审中-公开
公开(公告)号：WO2003001876A3
公开(公告)日：2003-01-09
申请号：PCT/US2002/019970
申请日：2002-06-26
申请人： SENOMYX, INC. , ZOLLER, Mark, T. , LI, Xiaodong , STASZEWSKI, Lena , O'CONNELL, Shawn , ZOZULYA, Sergey , ADLER, Jon, Elliott , XU, Hong , ECHEVERRI, Fernando
发明人： ZOLLER, Mark, T. , LI, Xiaodong , STASZEWSKI, Lena , O'CONNELL, Shawn , ZOZULYA, Sergey , ADLER, Jon, Elliott , XU, Hong , ECHEVERRI, Fernando
IPC分类号： G01N33/53
摘要： The present invention relates to the discovery that the T1R receptors assemble to form functional taste receptors. Particularly, it has been discovered that co-expression of T1R1 and T1R3 results in a taste receptor that responds to umami taste stimuli, including monosodium glutamate. Also, it has been discovered that co-expression of the T1R2 and T1R3 receptors results in a taste receptor that responds to sweet taste stimuli including naturally occurring and artificial sweeteners. Also the present invention relates to the use of hetero-oligomeric taste receptors comprising T1R1/T1R3 and T1R2/T1R3 in assays to identify compounds that respectively respond to umami taste stimuli and sweet taste stimuli. Further, the invention relates to the constitutive of cell lines that stably or transiently co-express a combination of T1R1 and T1R3; or T1R2 and T1R3; under constitutive or inducible conditions. The use of these cells lines in cell-based assays to identify umami and sweet taste modulatory compounds is also provided, particularly high throughput screening assays that detect receptor activity by use of fluorometric imaging. Finally, the invention relates to the discovery that some compounds, e.g., lactisole, inhibit both the activities of human T1R2/T1R3 and T1R1/T1R3 receptors, and accordingly the sweet and umami taste, suggesting that these receptors may be the only sweet and umami receptors.

8. 发明申请

WO2007047988A2 CHIMERIC HUMAN SWEET-UMAMI AND UMAMI-SWEET TASTE RECEPTORS 审中-公开
标题翻译： CHIMERIC人类SWEET-UMAMI和UMAMI-SWEET TASTE RECEPTORS
公开(公告)号：WO2007047988A2
公开(公告)日：2007-04-26
申请号：PCT/US2006/041158
申请日：2006-10-19
申请人： SENOMYX, INC. , LI, Xiaodong , ZHANG, Feng , XU, Hong , LI, Qing
发明人： LI, Xiaodong , ZHANG, Feng , XU, Hong , LI, Qing
IPC分类号： C07K14/705
CPC分类号： C07K14/705 , C12N2503/00 , C12N2510/00
摘要： This invention relates to chimeric taste receptors comprising the extracellular portion of one TlR or a variant or fragment thereof, either TlRl or T1R2, and the transmembrane portion of another TlR or a variant or fragment thereof, either TlRl or T1R2, preferably associated with a T1R3 polypeptide and a suitable G protein. These chimeric taste receptors and cells which express such chimeric taste receptors are useful in assays for identifying sweet and umami ligands as well in assays for identifying sweet and umami enhancers. Additionally, these chimeric taste receptors and cells which express same can be used to map and determine where specific sweet and umami ligands interact with their respective receptors and to elucidate the mechanism of receptor activation.
摘要翻译：本发明涉及包含一种TlR的细胞外部分或其变体或片段，即T1R1或T1R2的嵌合味觉感受器，以及T1R1或其变体或片段的跨膜部分，T1R1或T1R2，优选与T1R3相关多肽和合适的G蛋白。这些嵌合味觉受体和表达这种嵌合味觉受体的细胞可用于鉴定甜味和鲜味配体的测定以及用于鉴定甜味和鲜味增强剂的测定中。此外，这些嵌合味觉受体和表达相同的细胞可以用于绘制和确定特定甜味和鲜味配体与其各自受体相互作用的位置，并阐明受体活化的机制。

9. 发明申请

WO2008030429A2 NOVEL HAPLOTYPE OF HUMAN T2R RECEPTOR HT2R50 AND ITS USE IN ASSAYS FOR IDENTIFYING HUMAN BITTER TASTE MODULATORS 审中-公开
标题翻译：人类T2R受体HT2R50的新型HAPLOTYPE及其在鉴定人类口干调节剂中的应用
公开(公告)号：WO2008030429A2
公开(公告)日：2008-03-13
申请号：PCT/US2007/019300
申请日：2007-09-05
申请人： SENOMYX, INC. , LI, Xiaodong , PRONIN, Alexey , XU, Hong
发明人： LI, Xiaodong , PRONIN, Alexey , XU, Hong
IPC分类号： C07K14/705
CPC分类号： C07K14/705
摘要： The present invention relates to the discovery of a novel haplotype of the human taste receptor hT2R50 in the T2R taste receptor family that responds to particular bitter ligands, i.e. , 2-acetylpyrazine and ethylpyrazine. The present invention also relates to the use of this novel haplotype in assays for identifying ligands that modulate the activation of the hT2R50 taste receptor. These compounds potentially may be used as additives in foods, beverages and medicinals for modifying (blocking) hT2R50-associated bitter taste.
摘要翻译：本发明涉及T2R味觉受体家族中人味觉受体hT2R50的新型单倍型的发现，其对特定的苦味配体即2-乙酰基吡嗪和乙基吡嗪。本发明还涉及这种新型单元型在用于鉴定调节hT2R50味觉受体活化的配体的测定中的用途。这些化合物可能在食品，饮料和药物中用作修饰（阻断）hT2R50相关苦味的添加剂。

10. 发明申请

WO2005015158A3 T1R HETERO-OLIGOMERIC TASTE RECEPTORS, CELL LINES THAT EXPRESS SAID RECEPTORS, AND TASTE COMPOUNDS 审中-公开
公开(公告)号：WO2005015158A3
公开(公告)日：2005-02-17
申请号：PCT/US2004/025459
申请日：2004-08-06
申请人： SENOMYX INC. , LI, Xiaodong , STASZEWSKI, Lena , XU, Hong
发明人： LI, Xiaodong , STASZEWSKI, Lena , XU, Hong
IPC分类号： C12P21/06
摘要： The invention relates to compounds that specifically bind a T1R1/T1R3 or T1R2/T1R3 receptor or fragments or subunits thereof. The present invention also relates to the use of hetero-oligomeric and chimeric taste receptors comprising T1R1/T1R3 and T1R2/T1R3 in assays to identify compounds that respectively respond to umami taste stimuli and sweet taste stimuli. Further, the invention relates to the constitutive of cell lines that stably or transiently co-express a combination of T1R1 and T1R3; or T1R2 and T1R3; under constitutive or inducible conditions. The use of these cells lines in cell-based assays to identify umami and sweet taste modulatory compounds is also provided, particularly high throughput screening assays that detect receptor activity by use of fluorometric imaging.

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