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1. 发明申请

WO02068600A2 ENDOGENOUS AND NON-ENDOGENOUS VERSIONS OF HUMAN G PROTEIN-COUPLED RECEPTORS 审中-公开
标题翻译：人G蛋白偶联受体的内源性和非内源性版本
公开(公告)号：WO02068600A2
公开(公告)日：2002-09-06
申请号：PCT/US0205625
申请日：2002-02-26
申请人： ARENA PHARM INC , LIAW CHEN W , CHALMERS DEREK T , BEHAN DOMINIC P , MACIEJEWSKI-LENIOR DOMINIQUE , LEONARD JAMES N , LIN I-LIN , ORTUNO DANIEL
发明人： LIAW CHEN W , CHALMERS DEREK T , BEHAN DOMINIC P , MACIEJEWSKI-LENIOR DOMINIQUE , LEONARD JAMES N , LIN I-LIN , ORTUNO DANIEL
IPC分类号： C12N15/09 , C07K14/705 , C07K14/72 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N
CPC分类号： C07K14/705
摘要： The invention disclosed in this patent docuemnt relates to transmembrane receptors, more particularly to a human G protein-coupled receptor and to mutated (non-endogenous) versions of the human GPCRs for evidence activity.
摘要翻译：本专利文献中公开的发明涉及跨膜受体，更具体地涉及人G蛋白偶联受体和用于证据活性的人GPCR的突变（非内源）版本。

2. 发明申请

WO2007047520A1 GPR22 AND METHODS RELATING THERETO 审中-公开
标题翻译： GPR22及其相关方法
公开(公告)号：WO2007047520A1
公开(公告)日：2007-04-26
申请号：PCT/US2006/040226
申请日：2006-10-12
申请人： ARENA PHARMACEUTICALS, INC. , LIAW, Chen W.
发明人： LIAW, Chen W.
IPC分类号： C12N15/09
CPC分类号： C07K14/705
摘要： Methods for generating an expression-enhanced GPR22 nucleic acid, as well as substituted GPR22 nucleic acids providing for enhanced expression of the encoded GPR22 polypeptide, are provided. In practicing the subject methods, a nucleic acid encoding a mammalian GPR22 receptor polypeptide (e.g., a wild-type nucleic acid) is expression-enhanced by identifying the various codons of the coding region for the GPR22 amino acid sequence and substituting nucleotides so as to enhance expression without changing the amino acid sequence of the encoded GPR22 polypeptide. Methods, compositions, and kits using the same for screening of modulators of GPR22 are also provided.
摘要翻译：提供了产生表达增强的GPR22核酸的方法，以及提供编码的GPR22多肽的增强表达的取代的GPR22核酸。在实施本发明方法中，通过鉴定GPR22氨基酸序列的编码区的各种密码子并用核苷酸取代编码哺乳动物GPR22受体多肽（例如野生型核酸）的核酸，可以表达增强，从而增强表达而不改变编码的GPR22多肽的氨基酸序列。还提供了用于筛选GPR22调节剂的方法，组合物和试剂盒。

3. 发明申请

WO2007027661A3 HUMAN G PROTEIN-COUPLED RECEPTOR AND MODULATORS THEREOF FOR THE TREATMENT OF ATHEROSCLEROSIS AND ATHEROSCLEROTIC DISEASE AND FOR THE TREATMENT OF CONDITIONS RELATED TO MCP-1 EXPRESSION 审中-公开
公开(公告)号：WO2007027661A3
公开(公告)日：2007-03-08
申请号：PCT/US2006/033651
申请日：2006-08-29
申请人： ARENA PHARMACEUTICALS, INC. , HAKAK, Yaron , UNETT, David J. , GATLIN, Joel , LIAW, Chen W.
发明人： HAKAK, Yaron , UNETT, David J. , GATLIN, Joel , LIAW, Chen W.
IPC分类号： G01N33/74 , C07K14/72
摘要： The present invention relates to methods of using a G protein-coupled receptor (GPCR), for example GPR84, to identify whether a candidate compound is a modulator of atherogenesis. In certain embodiments, the GPCR couples to Gi. In certain embodiments, the GPCR is human. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of atherosclerosis and atherosclerotic disease, including coronary artery disease, myocardial infarction, peripheral arterial disease, and ischemic stroke. Agonists of the invention are additionally useful as therapeutic agents for the prevention or treatment of conditions related to MCP-I expression, including but not limited to rheumatoid arthritis, Crohn's disease, and multiple sclerosis.

4. 发明申请

WO2002068600A3 ENDOGENOUS AND NON-ENDOGENOUS VERSIONS OF HUMAN G PROTEIN-COUPLED RECEPTORS 审中-公开
公开(公告)号：WO2002068600A3
公开(公告)日：2002-09-06
申请号：PCT/US2002/005625
申请日：2002-02-26
申请人： ARENA PHARMACEUTICALS, INC. , LIAW, Chen, W. , CHALMERS, Derek, T. , BEHAN, Dominic, P. , MACIEJEWSKI-LENIOR, Dominique , LEONARD, James, N. , LIN, I-Lin , ORTUNO, Daniel
发明人： LIAW, Chen, W. , CHALMERS, Derek, T. , BEHAN, Dominic, P. , MACIEJEWSKI-LENIOR, Dominique , LEONARD, James, N. , LIN, I-Lin , ORTUNO, Daniel
IPC分类号： C07H21/04
摘要： The invention disclosed in this patent docuemnt relates to transmembrane receptors, more particularly to a human G protein-coupled receptor and to mutated (non-endogenous) versions of the human GPCRs for evidence activity.

5. 发明申请

WO2004083394A3 HUMAN G PROTEIN-COUPLED RECEPTORS AND MODULATORS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS 审中-公开
标题翻译：人类G蛋白偶联受体及其调节剂用于治疗炎症性疾病
公开(公告)号：WO2004083394A3
公开(公告)日：2005-08-11
申请号：PCT/US2004007930
申请日：2004-03-15
申请人： ARENA PHARM INC , VILLEGAS SONIA , LIAW CHEN
发明人： VILLEGAS SONIA , LIAW CHEN
IPC分类号： C07H21/04 , C07K14/72 , C12N20060101 , C12N5/02 , C12N15/74 , C12P21/06 , G01N33/53
CPC分类号： C07K14/723 , A61K38/00 , C07K14/705 , G01N33/6863 , G01N2333/726 , G01N2500/00
摘要： The invention disclosed in this patent document relates to transmembrane receptors, particularly to a human G protein-coupled receptor, more particularly to a CXC chemokine receptor subtype 3 (CXCR3), and most particularly to mutated (non-endogenous) version of the human CXCR3 for evidence of constitutive activity and uses thereof. In some embodiments the altered versions of CXCR3 are used, inter alia, for the direct identification of candidate compounds such as receptor agonists, inverse agonists, partial agonist or antagonist for use in, for example and not limitation, graft rejection; inflammatory skin disease; inflammatory bowel disease; allergic inflammation, allergic pulmonary inflammation, inflammatory demyelinating neuropathy, CNS inflammation; rheumatoid arthritis, bronchiolitis obliterans syndrome, periodontal disease and neurodegenerative disease.
摘要翻译：本专利文献中公开的发明涉及跨膜受体，特别是涉及人G蛋白偶联受体，更具体地涉及CXC趋化因子受体亚型3（CXCR3），最特别地涉及人CXCR3的突变（非内源）版本作为组成性活动的证据及其用途。在一些实施方案中，CXCR3的改变形式尤其用于直接鉴定候选化合物，例如受体激动剂，反向激动剂，部分激动剂或拮抗剂，用于例如但不限于移植排斥反应; 炎性皮肤病; 炎症性肠病; 过敏性炎症，过敏性肺部炎症，炎性脱髓鞘神经病，CNS炎症; 类风湿关节炎，闭塞性细支气管炎综合征，牙周病和神经变性疾病。

6. 发明申请

WO2007027661A2 HUMAN G PROTEIN-COUPLED RECEPTOR AND MODULATORS THEREOF FOR THE TREATMENT OF ATHEROSCLEROSIS AND ATHEROSCLEROTIC DISEASE AND FOR THE TREATMENT OF CONDITIONS RELATED TO MCP-1 EXPRESSION 审中-公开
标题翻译：人G蛋白偶联受体及其治疗ATHEROSCLOSOSIS和ATHEROSCLEROTIC DISEASE治疗与MCP-1表达相关的条件的调节剂
公开(公告)号：WO2007027661A2
公开(公告)日：2007-03-08
申请号：PCT/US2006033651
申请日：2006-08-29
申请人： ARENA PHARM INC , HAKAK YARON , UNETT DAVID J , GATLIN JOEL , LIAW CHEN W
发明人： HAKAK YARON , UNETT DAVID J , GATLIN JOEL , LIAW CHEN W
IPC分类号： G01N33/74 , C07K14/72
CPC分类号： G01N33/5041 , A61K38/1709 , A61K49/0008 , C07K14/47 , C07K14/723 , G01N33/6893 , G01N33/74 , G01N2333/726 , G01N2500/00 , G01N2800/32 , G01N2800/323
摘要： The present invention relates to methods of using a G protein-coupled receptor (GPCR) to identify whether a candidate compound is a modulator of atherogenesis. In certain embodiments, the GPCR couples to Gi. In certain embodiments, the GPCR is human. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of atherosclerosis and atherosclerotic disease, including coronary artery disease, myocardial infarction, peripheral arterial disease, and ischemic stroke. Agonists of the invention are additionally useful as therapeutic agents for the prevention or treatment of conditions related to MCP-1 expression, including but not limited to rheumatoid arthritis, Crohn's disease, and multiple sclerosis.
摘要翻译：本发明涉及使用G蛋白偶联受体（GPCR）鉴定候选化合物是否是动脉粥样硬化形成的调节剂的方法。在某些实施方案中，GPCR与Gi连接。在某些实施方案中，GPCR是人。本发明的激动剂可用作预防或治疗动脉粥样硬化和动脉粥样硬化疾病（包括冠状动脉疾病，心肌梗死，外周动脉疾病和缺血性中风）的治疗剂。本发明的激动剂另外可用作预防或治疗与MCP-1表达相关的病症的治疗剂，包括但不限于类风湿性关节炎，克罗恩氏病和多发性硬化症。

7. 发明申请

WO2004083394A2 HUMAN G PROTEIN-COUPLED RECEPTORS AND MODULATORS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS 审中-公开
标题翻译：人类G蛋白偶联受体及其调节剂用于治疗炎症性疾病
公开(公告)号：WO2004083394A2
公开(公告)日：2004-09-30
申请号：PCT/US2004/007930
申请日：2004-03-15
申请人： ARENA PHARMACEUTICALS INC. , VILLEGAS, Sonia , LIAW, Chen
发明人： VILLEGAS, Sonia , LIAW, Chen
IPC分类号： C12N
CPC分类号： C07K14/723 , A61K38/00 , C07K14/705 , G01N33/6863 , G01N2333/726 , G01N2500/00
摘要： The invention disclosed in this patent document relates to transmembrane receptors, particularly to a human G protein-coupled receptor, more particularly to a CXC chemokine receptor subtype 3 (CXCR3), and most particularly to mutated (non-endogenous) version of the human CXCR3 for evidence of constitutive activity and uses thereof. In some embodiments the altered versions of CXCR3 are used, inter alia, for the direct identification of candidate compounds such as receptor agonists, inverse agonists, partial agonist or antagonist for use in, for example and not limitation, graft rejection; inflammatory skin disease; inflammatory bowel disease; allergic inflammation, allergic pulmonary inflammation, inflammatory demyelinating neuropathy, CNS inflammation; rheumatoid arthritis, bronchiolitis obliterans syndrome, periodontal disease and neurodegenerative disease.
摘要翻译：本专利文献中公开的发明涉及跨膜受体，特别是涉及人G蛋白偶联受体，更具体地涉及CXC趋化因子受体亚型3（CXCR3），最特别地涉及人CXCR3的突变（非内源）版本作为组成性活动的证据及其用途。在一些实施方案中，CXCR3的改变形式尤其用于直接鉴定候选化合物，例如受体激动剂，反向激动剂，部分激动剂或拮抗剂，用于例如但不限于移植排斥反应; 炎性皮肤病; 炎症性肠病; 过敏性炎症，过敏性肺部炎症，炎性脱髓鞘神经病，CNS炎症; 类风湿关节炎，闭塞性细支气管炎综合征，牙周病和神经变性疾病。

8. 发明申请

WO2003062396A9 NON-ENDOGENOUS VERSIONS OF HUMAN G PROTEIN-COUPLED RECEPTOR: FSHR 审中-公开
公开(公告)号：WO2003062396A9
公开(公告)日：2003-07-31
申请号：PCT/US2003/002136
申请日：2003-01-22
申请人： ARENA PHARMACEUTICALS, INC. , LIAW, Chen
发明人： LIAW, Chen
IPC分类号： C07K14/72

9. 发明申请

WO0177172A3 NON-ENDOGENOUS, CONSTITUTIVELY ACTIVATED KNOWN G PROTEIN-COUPLED RECEPTORS 审中-公开
标题翻译：非特异性，一般激活的已知的G蛋白偶联受体
公开(公告)号：WO0177172A3
公开(公告)日：2003-01-30
申请号：PCT/US0111098
申请日：2001-04-05
申请人： ARENA PHARM INC , LEHMANN-BRUINSMA KARIN , LIAW CHEN W , LIN I-LIN
发明人： LEHMANN-BRUINSMA KARIN , LIAW CHEN W , LIN I-LIN
IPC分类号： G01N33/50 , A61K38/00 , C07K14/705 , C07K14/72 , C12N15/12 , C12Q1/02 , G01N33/15 , G01N33/68
CPC分类号： G01N33/74 , A61K38/00 , C07K14/705 , C07K14/723 , C07K2319/00 , G01N2333/726 , G01N2500/10
摘要： The invention disclosed in this patent document relates to transmembrane receptors, more particularly to a human G protein-coupled receptor for which the endogenous ligand is known ("known GPCRs"), and most particularly to mutated (non-endogenous) versions of the knowns GPCRs for use, most preferably in screening assays for the direct identification of candidate compounds as inverse agonists, agonists and partial agonists.
摘要翻译：本专利文献中公开的发明涉及跨膜受体，更具体地涉及内源性配体已知的人G蛋白偶联受体（“已知GPCR”），最特别地涉及已知的突变（非内源）版本 GPCRs，最优选用于直接鉴定作为反向激动剂，激动剂和部分激动剂的候选化合物的筛选试验。

10. 发明申请

WO0022129A9 NON-ENDOGENOUS, CONSTITUTIVELY ACTIVATED HUMAN G PROTEIN-COUPLED RECEPTORS 审中-公开
标题翻译：非内源性，一般激活的人G蛋白偶联受体
公开(公告)号：WO0022129A9
公开(公告)日：2000-09-14
申请号：PCT/US9923938
申请日：1999-10-12
申请人： ARENA PHARM INC , BEHAN DOMINIC P , CHALMERS DEREK T , LIAW CHEN W
发明人： BEHAN DOMINIC P , CHALMERS DEREK T , LIAW CHEN W
IPC分类号： G01N33/50 , A61K38/00 , A61K45/00 , A61P43/00 , C07D231/12 , C07D231/16 , C07D409/12 , C07K5/08 , C07K7/06 , C07K14/705 , C07K14/72 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N15/09 , C12N15/12 , C12N15/16 , C12Q1/02 , G01N33/15 , G01N33/566
CPC分类号： C07D231/12 , A61K38/00 , C07D231/16 , C07D409/12 , C07K14/705 , C07K14/70571 , C07K14/723 , G01N33/566 , G01N2333/726 , G01N2500/00
摘要： Disclosed herein are constitutively activated, non-endogenous versions of endogenous human G protein-coupled receptors comprising (a) the following amino acid sequence region (C-terminus to N-terminus orientation) and/or (b) the following nucleic acid sequence region (3' to 5' orientation) transversing the transmembrane-6 (TM6) and intracellular loop-3 (IC3) regions of the GPCR: (a) P AA15 X and/or (b) P (AA-codon)15 Xcodon, respectively. In a most preferred embodiment, P and P are endogenous proline and an endogenous nucleic acid encoding region encoding proline, respectively, located within TM6 of the non-endogenous GPCR; AA15 and (AA-codon)15 are 15 endogenous amino acid residues and 15 codons encoding endogenous amino acid residues, respectively; and X and Xcodon are non-endogenous lysine and a non-endogenous nucleic acid encoding region encoding lysine, respectively, located within IC3 of the non-endogenous GPCR. Because it is most preferred that the non-endogenous human GPCRs which incorporate these mutations are incorporated into mammalian cells and utilized for the screening of the candidate compounds, the non-endogenous human GPCR incorporating the mutation need not be purified and isolated per se (i.e., these are incorporated within the cellular membrane of a mammalian cell), although such purified and isolated non-endogenous human GPCRs are well within the purview of this disclosure.
摘要翻译：本文公开了内源性人G蛋白偶联受体的组成型激活的非内源型，其包含（a）以下氨基酸序列区（C末端至N末端取向）和/或（b）以下核酸序列区（3'至5'方向）横切GPCR的跨膜-6（TM6）和细胞内环3（IC3）区域：（a）P 1 AA15 X和/或（b）P < -codon）15 Xcodon。在最优选的实施方案中，P 1和P <密码子是分别位于非内源性GPCR TM6内的内源性脯氨酸和编码脯氨酸的内源核酸编码区; AA15和（AA-密码子）15分别是15个内源氨基酸残基和15个编码内源氨基酸残基的密码子; X和Xcodon是分别位于非内源GPCR的IC3内的非内源性赖氨酸和编码赖氨酸的非内源核酸编码区。因为最优选的是将含有这些突变的非内源性人GPCR并入哺乳动物细胞中并用于筛选候选化合物，所以引入突变的非内源性人GPCR不需要被纯化和分离（即，，这些被并入哺乳动物细胞的细胞膜），尽管这种纯化和分离的非内源性人GPCR完全在本公开的范围内。

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