公开(公告)号：US10093718B2

公开(公告)日：2018-10-09

申请号：US15483353

申请日：2017-04-10

Applicant: Senomyx, Inc.

Inventor： Jon Elliot Adler ,  Sergey Zozulya ,  Xiaodong Li ,  Shawn O'Connell ,  Lena Luukkonen

IPC: G01N33/566 ,  C07K14/705 ,  C07K14/72

Abstract: Methods are provided for identifying human and non-human primate cells which respond to sweet tastants. These methods screen for human or non-human primate cells which express a polypeptide which binds to or responds to sweet tastants. These cells may be used in binding and functional assays to screen for compounds which modulate sweet taste.

公开(公告)号：US09790265B2

公开(公告)日：2017-10-17

申请号：US14715168

申请日：2015-05-18

Applicant: SENOMYX, INC.

Inventor： Jon Elliot Adler ,  Xiaodong Li ,  Lena Luukkonen ,  Shawn O'Connell ,  Sergey Zozulya

IPC: C07K16/00 ,  C07K14/72 ,  G01N33/74 ,  G06F19/12 ,  C07K14/705 ,  C12Q1/68 ,  G01N33/50 ,  G01N33/68

CPC classification number: C07K14/723 ,  C07K14/705 ,  C07K2319/00 ,  C12Q1/6883 ,  G01N33/5041 ,  G01N33/6872 ,  G01N33/74 ,  G01N2333/726 ,  G06F19/12

Abstract: Newly identified mammalian taste-cell-specific G protein-coupled receptors, and the genes and cDNA encoding said receptors are described. Specifically, T1R G protein-coupled receptors active in taste signaling, and the genes and cDNA encoding the same, are described, along with methods for isolating such genes and for isolating and expressing such receptors. Methods for representing taste perception of a particular taste stimulus in a mammal are also described, as are methods for generating novel molecules or combinations of molecules that elicit a predetermined taste perception in a mammal, and methods for simulating one or more tastes. Further, methods for stimulating or blocking taste perception in a mammal are also disclosed.

公开(公告)号：US20170219567A1

公开(公告)日：2017-08-03

申请号：US15264785

申请日：2016-09-14

Applicant: SENOMYX, INC.

Inventor： Jon E. ADLER ,  Xiaodong Li ,  Lena Luukkonen ,  Hong Xu ,  Fernando Echeverri

IPC: G01N33/50 ,  G01N33/74 ,  C07K14/72

CPC classification number: G01N33/5041 ,  C07K14/723 ,  G01N33/5008 ,  G01N33/5023 ,  G01N33/74 ,  G01N2333/705 ,  G01N2333/726 ,  G01N2500/00

Abstract: Newly identified mammalian taste-cell-specific G protein-coupled receptors which function as hetero-oligomeric complexes in the sweet taste transduction pathway, and the genes and cDNA encoding said receptors are described. Specifically, T1R G protein-coupled receptors active in sweet taste signaling as hetero-oligomeric complexes, and the genes and cDNA encoding the same, are described, along with methods for isolating such genes and for isolating and expressing such receptors. Methods for identifying putative taste modulating compounds using such hetero-oligomeric complexes also described, as is a novel surface expression facilitating peptide useful for targeting integral plasma membrane proteins to the surface of a cell.

公开(公告)号：US09637536B2

公开(公告)日：2017-05-02

申请号：US14696896

申请日：2015-04-27

Applicant: Senomyx, Inc.

Inventor： Jon Elliot Adler ,  Sergey Zozulya ,  Xiaodong Li ,  Shawn O'Connell ,  Lena Luukkonen

IPC: C12N15/12 ,  C07K14/705 ,  C07K14/72

CPC classification number: C07K14/723 ,  C07K14/705 ,  C07K2319/00

Abstract: Newly identified mammalian taste-cell-specific G protein-coupled receptors, and the genes and cDNA encoding said receptors are provided. Specifically, T1R G protein-coupled receptors active in taste signaling, and the genes and cDNA encoding the same, are provided, along with methods for isolating such genes and for isolating and expressing such receptors.

公开(公告)号：US20160251372A1

公开(公告)日：2016-09-01

申请号：US15059142

申请日：2016-03-02

Applicant: SENOMYX, INC.

Inventor： Catherine Tachdjian ,  Xiao Qing Tang ,  Donald S. Karanewsky ,  Guy Servant ,  Xiaodong Li ,  Feng Zhang ,  Qing Chen ,  Hong Zhang ,  Timothy Davis ,  Vincent Darmohusodo ,  Melissa Wong ,  Victor Selchau

IPC: C07D495/04 ,  A61K47/22 ,  A23L2/56 ,  C07D401/12 ,  C07D405/12 ,  C07D215/54 ,  C07D471/04

CPC classification number: C07D495/04 ,  A23L2/56 ,  A23L27/2054 ,  A23L27/88 ,  A23V2002/00 ,  A61K47/22 ,  C07D215/54 ,  C07D215/60 ,  C07D401/12 ,  C07D405/12 ,  C07D471/04 ,  C07D491/048

Abstract: 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.

公开(公告)号：US20150265711A1

公开(公告)日：2015-09-24

申请号：US14731224

申请日：2015-06-04

Applicant: SENOMYX, INC.

Inventor： Catherine Tachdjian ,  Xiao Qing Tang ,  Donald S. Karanewsky ,  Guy Servant ,  Xiaodong Li ,  Feng Zhang ,  Qing Chen ,  Hong Zhang ,  Timothy Davis ,  Vincent Darmohusodo ,  Melissa Wong ,  Victor Selchau

IPC: A61K47/22 ,  A23L2/56 ,  A23L1/226

CPC classification number: C07D495/04 ,  A23L2/56 ,  A23L27/2054 ,  A23L27/88 ,  A23V2002/00 ,  A61K47/22 ,  C07D215/54 ,  C07D215/60 ,  C07D401/12 ,  C07D405/12 ,  C07D471/04 ,  C07D491/048

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US09834544B2

公开(公告)日：2017-12-05

申请号：US14337764

申请日：2014-07-22

Applicant: SENOMYX, INC.

Inventor： Catherine Tachdjian ,  Xiao Qing Tang ,  Donald S. Karanewsky ,  Guy Servant ,  Xiaodong Li ,  Feng Zhang ,  Qing Chen ,  Hong Zhang ,  Timothy James Davis ,  Vincent Darmohusodo ,  Melissa S. Wong ,  Victor Selchau

IPC: C07D405/12 ,  A23L2/60 ,  C07D401/12 ,  C07D215/54 ,  C07D451/06 ,  A61K47/22 ,  C07D215/42 ,  A23L27/00

CPC classification number: C07D405/12 ,  A23L2/60 ,  A23L27/88 ,  A23V2002/00 ,  A61K47/22 ,  C07D215/42 ,  C07D215/54 ,  C07D401/12 ,  C07D451/06

Abstract: 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.

公开(公告)号：US09459250B2

公开(公告)日：2016-10-04

申请号：US14477027

申请日：2014-09-04

Applicant: SENOMYX, INC.

Inventor： Xiaodong Li ,  Lena Staszewski ,  Hong Xu

IPC: G01N33/543 ,  A23L1/226 ,  C07C233/65 ,  C07C235/54 ,  C07C275/30 ,  C07C275/34 ,  C07D307/84 ,  C07D317/68 ,  G01N33/566 ,  G01N33/74 ,  G01N33/50 ,  A23L1/22 ,  A23L2/56 ,  A61K8/49 ,  A61K8/55 ,  A61K47/22 ,  A61K47/24 ,  C07D405/12 ,  C07F9/655 ,  C07K14/705

CPC classification number: 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

Abstract: The invention relates to compounds that specifically bind a T1R1/T1R3 or T1R2/T1R3 receptor or fragments or sub-units 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.

Abstract translation: 本发明涉及特异性结合T1R1 / T1R3或T1R2 / T1R3受体或其片段或亚单位的化合物。 本发明还涉及包含T1R1 / T1R3和T1R2 / T1R3的异低聚和嵌合味觉感受器在测定中用于鉴定分别响应于鲜味刺激和甜味刺激的化合物的用途。 此外，本发明涉及稳定或瞬时共表达T1R1和T1R3的组合的细胞系的组成; 或T1R2和T1R3; 在组成型或诱导性条件下。 还提供了在基于细胞的测定中使用这些细胞系以鉴定鲜味和甜味调节化合物，特别是通过使用荧光成像检测受体活性的高通量筛选测定。

公开(公告)号：US09170254B2

公开(公告)日：2015-10-27

申请号：US14243380

申请日：2014-04-02

Applicant: SENOMYX, INC.

Inventor： Xiaodong Li ,  Hong Xu ,  Qing Li ,  Huixian Tang ,  Alexey Pronin

IPC: G01N33/50 ,  G01N33/566

CPC classification number: G01N33/566 ,  G01N33/5008 ,  G01N33/5023 ,  G01N2500/00 ,  G01N2500/10

Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds. Also, the invention relates to the discovery of specific hT2R9 alleles and their disparate activity in functional assays with the same biter ligands. The invention further relates to the use of these T2R receptors in assays for identifying ligands that modulate the activation of these taste receptors by specific bitter ligands and related compounds. These compounds may be used as additives and/or removed from foods, beverages, cosmetics and medicinals in order to modify (block) T2R-associated bitter taste. Also T2R ligands may be used as therapeutics to treat and modulate T2R associated gastrointestinal and metabolic functions as well as treat gastrointestinal and metabolic diseases such as eating disorders, food sensing, food absorption, obesity, diabetes, Crohn's disease, celiac disease, et al.

Abstract translation: 本发明涉及T2R味觉受体家族中的特定人味受体对特定苦味化合物的反应的发现。 此外，本发明涉及特异性hT2R9等位基因的发现及其在具有相同配体配体的功能测定中的不同活性。 本发明还涉及这些T2R受体在用于鉴定通过特定的苦配体和相关化合物调节这些味觉受体的活化的配体的测定中的用途。 这些化合物可以用作添加剂和/或从食品，饮料，化妆品和药物中去除，以便改变（阻断）T2R相关的苦味。 也可以使用T2R配体作为治疗和调节T2R相关胃肠道和代谢功能以及治疗胃肠道和代谢疾病如饮食失调，食物感觉，食物吸收，肥胖，糖尿病，克罗恩病，乳糜泻等的治疗剂。

公开(公告)号：US09091686B2

公开(公告)日：2015-07-28

申请号：US13770251

申请日：2013-02-19

Applicant: Senomyx, Inc.

Inventor： Xiaodong Li ,  Lena Staszewski ,  Hong Xu

IPC: G01N33/543 ,  A23L1/226 ,  C07C233/65 ,  C07C235/54 ,  C07C275/30 ,  C07C275/34 ,  C07D307/84 ,  C07D317/68 ,  G01N33/566 ,  G01N33/74 ,  C07K14/705

CPC classification number: 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

Abstract: The invention relates to compounds that specifically bind a T1R1/T1R3 or T1R2/T1R3 receptor or fragments or sub-units 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.

Abstract translation: 本发明涉及特异性结合T1R1 / T1R3或T1R2 / T1R3受体或其片段或亚单位的化合物。 本发明还涉及包含T1R1 / T1R3和T1R2 / T1R3的异低聚和嵌合味觉感受器在测定中用于鉴定分别响应于鲜味刺激和甜味刺激的化合物的用途。 此外，本发明涉及稳定或瞬时共表达T1R1和T1R3的组合的细胞系的组成; 或T1R2和T1R3; 在组成型或诱导性条件下。 还提供了在基于细胞的测定中使用这些细胞系以鉴定鲜味和甜味调节化合物，特别是通过使用荧光成像检测受体活性的高通量筛选测定。