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    METHODS FOR PRODUCING OLFACTORY GPCRS
    1.
    发明申请
    METHODS FOR PRODUCING OLFACTORY GPCRS 审中-公开
    生产OLFACTORY GPCRS的方法

    公开(公告)号：WO2005051984A2

    公开(公告)日：2005-06-09

    申请号：PCT/US2004038339

    申请日：2004-11-15

    Applicant: ARENA PHARM INC ,  HUNG GENE ,  ORTUNO DANIEL ,  UNETT DAVID ,  GATLIN JOEL

    Inventor： HUNG GENE ,  ORTUNO DANIEL ,  UNETT DAVID ,  GATLIN JOEL

    IPC: C07K14/705 ,  C07K14/72 ,  C07K14/00

    CPC classification number: C07K14/723

    Abstract: The subject invention provides a method for producing an olfactory GPCR in a cell. In general, the methods involve introducing an expression cassette containing a promoter operably linked to a nucleic acid encoding an olfactory PCR into a macroglial cell, e.g., a Schwann or oligodendritic cell, and maintaining the cell under conditions suitable for production of the olfactory GPCR. Also provided is a macroglial cell containing a recombinant nucleic acid encoding an olfactory GPCR, methods of screening for modulators of olfactory GPCR activity, and a kit for producing an olfactory GPCR in a macroglial cell. The invention finds most use in research on flavors and fragrances, and, consequently, has a variety of research and industrial applications.

    Abstract translation: 本发明提供了一种在细胞中产生嗅觉GPCR的方法。 一般而言，所述方法涉及将包含与编码嗅觉PCR的核酸可操作连接的启动子的表达盒导入大神经胶质细胞例如雪旺氏或少突胶质细胞，并将细胞维持在适于产生嗅觉GPCR的条件下。 还提供了含有编码嗅觉GPCR的重组核酸的大胶质细胞，筛选嗅觉GPCR活性调节剂的方法以及用于在大胶质细胞中产生嗅觉GPCR的试剂盒。 本发明最广泛地用于香料和香料的研究，因此具有多种研究和工业应用。

    GPR35 AND MODULATORS THEREOF FOR THE TREATMENT OF METABOLIC-RELATED DISORDERS
    3.
    发明申请
    GPR35 AND MODULATORS THEREOF FOR THE TREATMENT OF METABOLIC-RELATED DISORDERS 审中-公开
    GPR35的调节剂用于治疗与代谢相关的疾病

    公开(公告)号：WO2005119252A2

    公开(公告)日：2005-12-15

    申请号：PCT/US2005/018082

    申请日：2005-05-23

    Applicant: ARENA PHARMACEUTICALS, INC. ,  LEONARD, James N. ,  CHU, Zhi Liang ,  UNETT, David J. ,  GATLIN, Joel E. ,  GAIDAROV, Ibragim ,  QIU, Jun ,  SKINNER, Philip J. ,  BOATMAN, P. Douglas

    Inventor： LEONARD, James N. ,  CHU, Zhi Liang ,  UNETT, David J. ,  GATLIN, Joel E. ,  GAIDAROV, Ibragim ,  QIU, Jun ,  SKINNER, Philip J. ,  BOATMAN, P. Douglas

    IPC: G01N33/50

    CPC classification number: G01N33/6893 ,  A61K31/425 ,  G01N2333/726 ,  G01N2500/00

    Abstract: The present invention relates to a method for identifying a metabolic stabilizing compound, comprising: a) contacting a candidate compound with GPR35, and b) determining whether GPR35 functionality is increased, wherein an increase in GPR35 functionality is indicative of the candidate compound being a metabolic stabilizing compound. The invention further relates to use of a GPR35 modulator for the manufacture of a medicament for use as a metabolic stabilizing agent. In addition, the invention relates to a method for increasing GPR35 function, comprising contacting GPR35 with an effective amount of a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein X is O or S; and R1, R2, R3, R4, and R5 are each independently selected from the group consisting of H, C1-4 alkoxy, C1-4 alkyl, halogen, hydroxyl, and nitro; wherein said C1-4 alkoxy is optionally substituted with carbo-C1-4-alkoxy or carboxy.

    Abstract translation: 本发明涉及用于鉴定代谢稳定化合物的方法，包括：a）使候选化合物与GPR35接触，和b）确定GPR35的功能是否增加，其中GPR35功能的增加指示候选化合物是代谢 稳定化合物。 本发明还涉及GPR35调节剂在制备用作代谢稳定剂的药物中的用途。 另外，本发明涉及增加GPR35功能的方法，包括使GPR35与有效量的式（I）化合物或其可药用盐接触，其中X为O或S; R 1，R 2，R 3，R 4和R 5各自独立地选自H，C 1-4烷氧基，C 1-4烷基，卤素，羟基和硝基; 其中所述C 1-4烷氧基任选被C 1-4 - 烷氧基或羧基取代。

    MODULATORS OF HUMAN G PROTEIN-COUPLED RECEPTORS FOR THE TREATMENT OF HYPERGLYCEMIA AND RELATED DISORDERS
    4.
    发明申请
    MODULATORS OF HUMAN G PROTEIN-COUPLED RECEPTORS FOR THE TREATMENT OF HYPERGLYCEMIA AND RELATED DISORDERS 审中-公开
    人G蛋白相关受体调节剂治疗高血压和相关疾病

    公开(公告)号：WO2005116653A3

    公开(公告)日：2006-05-18

    申请号：PCT/US2005012447

    申请日：2005-04-12

    Applicant: ARENA PHARM INC ,  QIU JUN ,  WEBB ROBERT R ,  UNETT DAVID J ,  GATLIN JOEL E ,  CONNOLLY DANIEL T

    Inventor： QIU JUN ,  WEBB ROBERT R ,  UNETT DAVID J ,  GATLIN JOEL E ,  CONNOLLY DANIEL T

    IPC: G01N33/566 ,  A61K31/427 ,  A61K31/4439 ,  A61K45/06 ,  C07D417/04 ,  G01N33/68 ,  G01N33/76

    CPC classification number: C07D417/04 ,  A61K31/427 ,  A61K31/4439 ,  G01N33/76 ,  G01N2333/726

    Abstract: The present invention relates to methods of identifying whether one or more candidate compounds is a modulator of a G protein-coupled receptor (GPCR) or a modulator of blood glucose concentration. In certain embodiments, the GPCR is human. The present invention also relates to methods of using a modulator of the GPCR. A preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for lowering blood glucose concentration, for preventing or treating certain metabolic disorders, such as insulin resistance, impaired glucose tolerance, and diabetes, and for preventing or treating a complication of an elevated blood glucose concentration, such as atherosclerosis, heart disease, stroke, hypertension and peripheral vascular disease.

    Abstract translation: 本发明涉及鉴定一种或多种候选化合物是G蛋白偶联受体（GPCR）或血糖浓度调节剂的调节剂的方法。 在某些实施方案中，GPCR是人。 本发明还涉及使用GPCR的调制器的方法。 优选的调节剂是激动剂。 本发明的激动剂可用作降低血糖浓度的治疗剂，用于预防或治疗某些代谢紊乱，例如胰岛素抵抗，葡萄糖耐量异常和糖尿病，以及用于预防或治疗血糖浓度升高的并发症， 作为动脉粥样硬化，心脏病，中风，高血压和外周血管疾病。

    MODULATORS OF GPR35 FOR THE TREATMENT OF METABOLIC-RELATED DISORDERS
    5.
    发明申请
    MODULATORS OF GPR35 FOR THE TREATMENT OF METABOLIC-RELATED DISORDERS 审中-公开
    GPR35的调节剂用于治疗与代谢相关的疾病

    公开(公告)号：WO2005119252A3

    公开(公告)日：2006-01-12

    申请号：PCT/US2005018082

    申请日：2005-05-23

    Applicant: ARENA PHARM INC ,  LEONARD JAMES N ,  CHU ZHI LIANG ,  UNETT DAVID J ,  GATLIN JOEL E ,  GAIDAROV IBRAGIM ,  QIU JUN ,  SKINNER PHILIP J ,  BOATMAN P DOUGLAS

    Inventor： LEONARD JAMES N ,  CHU ZHI LIANG ,  UNETT DAVID J ,  GATLIN JOEL E ,  GAIDAROV IBRAGIM ,  QIU JUN ,  SKINNER PHILIP J ,  BOATMAN P DOUGLAS

    IPC: A61K31/425 ,  G01N33/50 ,  A61P3/06 ,  A61P3/10

    CPC classification number: G01N33/6893 ,  A61K31/425 ,  G01N2333/726 ,  G01N2500/00

    Abstract: The present invention relates to a method for identifying a metabolic stabilizing compound, comprising: a) contacting a candidate compound with GPR35, and b) determining whether GPR35 functionality is increased, wherein an increase in GPR35 functionality is indicative of the candidate compound being a metabolic stabilizing compound. The invention further relates to use of a GPR35 modulator for the manufacture of a medicament for use as a metabolic stabilizing agent. In addition, the invention relates to a method for increasing GPR35 function, comprising contacting GPR35 with an effective amount of a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein X is O or S; and R1, R2, R3, R4, and R5 are each independently selected from the group consisting of H, C1-4 alkoxy, C1-4 alkyl, halogen, hydroxyl, and nitro; wherein said C1-4 alkoxy is optionally substituted with carbo-C1-4-alkoxy or carboxy.

    Abstract translation: 本发明涉及用于鉴定代谢稳定化合物的方法，包括：a）使候选化合物与GPR35接触，和b）确定GPR35的功能是否增加，其中GPR35功能的增加指示候选化合物是代谢 稳定化合物。 本发明还涉及GPR35调节剂在制备用作代谢稳定剂的药物中的用途。 另外，本发明涉及增加GPR35功能的方法，其包括使GPR35与有效量的式（I）化合物或其药学上可接受的盐接触，其中X为O或S; 并且R 1，R 2，R 3，R 4和R 5各自独立地选自H，C 1-4烷氧基，C 1-4烷基，卤素，羟基和硝基; 其中所述C 1-4烷氧基任选被碳-C 1-4 - 烷氧基或羧基取代。

    HUMAN G PROTEIN-COUPLED RECEPTOR AND MODULATORS THEREOF FOR THE TREATMENT OF HYPERGLYCEMIA AND RELATED DISORDERS
    8.
    发明申请
    HUMAN G PROTEIN-COUPLED RECEPTOR AND MODULATORS THEREOF FOR THE TREATMENT OF HYPERGLYCEMIA AND RELATED DISORDERS 审中-公开
    人G蛋白偶联受体及其调节剂治疗高血压和相关疾病

    公开(公告)号：WO2005116653A2

    公开(公告)日：2005-12-08

    申请号：PCT/US2005/012447

    申请日：2005-04-12

    Applicant: ARENA PHARMACEUTICALS, INC. ,  QIU, Jun ,  WEBB, Robert R. ,  UNETT, David J. ,  GATLIN, Joel E. ,  CONNOLLY, Daniel T.

    Inventor： QIU, Jun ,  WEBB, Robert R. ,  UNETT, David J. ,  GATLIN, Joel E. ,  CONNOLLY, Daniel T.

    IPC: G01N33/566

    CPC classification number: C07D417/04 ,  A61K31/427 ,  A61K31/4439 ,  G01N33/76 ,  G01N2333/726

    Abstract: The present invention relates to methods of identifying whether one or more candidate compounds is a modulator of a G protein-coupled receptor (GPCR) or a modulator of blood glucose concentration. In certain embodiments, the GPCR is human. The present invention also relates to methods of using a modulator of the GPCR. A preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for lowering blood glucose concentration, for preventing or treating certain metabolic disorders, such as insulin resistance, impaired glucose tolerance, and diabetes, and for preventing or treating a complication of an elevated blood glucose concentration, such as atherosclerosis, heart disease, stroke, hypertension and peripheral vascular disease.

    Abstract translation: 本发明涉及鉴定一种或多种候选化合物是G蛋白偶联受体（GPCR）或血糖浓度调节剂的调节剂的方法。 在某些实施方案中，GPCR是人。 本发明还涉及使用GPCR调制器的方法。 优选的调节剂是激动剂。 本发明的激动剂可用作降低血糖浓度的治疗剂，用于预防或治疗某些代谢紊乱，例如胰岛素抵抗，葡萄糖耐量异常和糖尿病，以及用于预防或治疗血糖浓度升高的并发症， 作为动脉粥样硬化，心脏病，中风，高血压和外周血管疾病。

    METHODS FOR PRODUCING OLFACTORY GPCRS
    9.
    发明申请
    METHODS FOR PRODUCING OLFACTORY GPCRS 审中-公开

    公开(公告)号：WO2005051984A3

    公开(公告)日：2005-06-09

    申请号：PCT/US2004/038339

    申请日：2004-11-15

    Applicant: ARENA PHARMACEUTICALS, INC. ,  HUNG, Gene ,  ORTUNO, Daniel ,  UNETT, David ,  GATLIN, Joel

    Inventor： HUNG, Gene ,  ORTUNO, Daniel ,  UNETT, David ,  GATLIN, Joel

    IPC: C12N15/12

    Abstract: The subject invention provides a method for producing an olfactory GPCR in a cell. In general, the methods involve introducing an expression cassette containing a promoter operably linked to a nucleic acid encoding an olfactory PCR into a macroglial cell, e.g., a Schwann or oligodendritic cell, and maintaining the cell under conditions suitable for production of the olfactory GPCR. Also provided is a macroglial cell containing a recombinant nucleic acid encoding an olfactory GPCR, methods of screening for modulators of olfactory GPCR activity, and a kit for producing an olfactory GPCR in a macroglial cell. The invention finds most use in research on flavors and fragrances, and, consequently, has a variety of research and industrial applications.

    MODULATORS OF G PROTEIN-COUPLED FORMYL PEPTIDE RECEPTOR-LIKE 2 AND THEIR THERAPEUTIC USE AGAINST CELL DEATH-RELATED DISORDERS
    10.
    发明申请
    MODULATORS OF G PROTEIN-COUPLED FORMYL PEPTIDE RECEPTOR-LIKE 2 AND THEIR THERAPEUTIC USE AGAINST CELL DEATH-RELATED DISORDERS 审中-公开

    公开(公告)号：WO2004083867A3

    公开(公告)日：2004-09-30

    申请号：PCT/US2004/008191

    申请日：2004-03-15

    Applicant: ARENA PHARMACEUTICALS INC. ,  VILLEGAS, Sonia ,  KELNER, Gregory ,  UNETT, David ,  GATLIN, Joel

    Inventor： VILLEGAS, Sonia ,  KELNER, Gregory ,  UNETT, David ,  GATLIN, Joel

    IPC: G01N33/74

    Abstract: The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In certain embodiments, the GPCR is human. In certain embodiments, the GPCR is expressed endogenously by neuronal cells or muscle cells. In certain embodiments, the GPCR is neuroprotective or myoprotective. In certain embodiments, the GPCR is a Humanin receptor. The present invention also relates to methods of using a modulator of said GPCR. A preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of neurodegenerative diseases in general, including Alzheimer's disease, Parkinson's disease, prion-associated disease, stroke and motor-neuron disease in particular, peripheral neuropathy, cerebral amyloid beta-protein angiopathy, and ischemic heart disease, including myocardial infarction and congestive heart failure. Podocarpa-8, 11, 13-trien-16-amide derivatives carrying at least a substituent on the aromatic ring are the identified modulators.

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