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1. 发明申请

WO2004093785A2 RHESUS MONKEY BOMBESIN RECEPTOR SUBTYPE-3 (BRS-3), NUCLEOTIDES ENCODING SAME, AND USES THEREOF 审中-公开
标题翻译： RHESUS MONKEY BOMBESIN受体亚型3（BRS-3），编码它们的核苷酸及其用途
公开(公告)号：WO2004093785A2
公开(公告)日：2004-11-04
申请号：PCT/US2004/011473
申请日：2004-04-14
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD. , TAN, Carina, P. , HOWARD, Andrew, D. , SANO, Hideki
发明人： TAN, Carina, P. , HOWARD, Andrew, D. , SANO, Hideki
IPC分类号： A61K
CPC分类号： C07K14/70571 , C07K14/723 , G01N2333/70571
摘要： A rhesus monkey bombesin receptor subtype-3 has been isolated, cloned and sequenced. This receptor is characteristic of the G-protein family of receptors. Isolated rhesus monkey bombesin receptor subtype-3 may be used to screen and identify novel bombesin receptor modulators that may contribute to the regulation of endocrine processes, metabolism, or the cell cycle. Such compounds may be used in the treatment of conditions that result from deregulated expression of bombesin receptor subtype-3.
摘要翻译：已经分离，克隆和测序了恒河猴铃蟾肽受体亚型3。该受体是G-蛋白家族受体的特征。分离的恒河猴铃蟾肽受体亚型-3可用于筛选和鉴定可能有助于调节内分泌过程，代谢或细胞周期的新型bombesin受体调节剂。这些化合物可用于治疗由bombesin受体亚型-3的失调表达引起的病症。

2. 发明申请

WO0009538A3 CANINE GROWTH HORMONE SECRETAGOGUE RECEPTOR 审中-公开
标题翻译： CANINE生长激素SECRETAGOGUE受体
公开(公告)号：WO0009538A3
公开(公告)日：2000-06-22
申请号：PCT/US9917915
申请日：1999-08-06
申请人： MERCK & CO INC , HOWARD ANDREW D , PALYHA OKSANA C , SMITH ROY G , TAN CARINA P
发明人： HOWARD ANDREW D , PALYHA OKSANA C , SMITH ROY G , TAN CARINA P
IPC分类号： G01N33/50 , C07K14/705 , C07K14/72 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/02 , C12N5/10 , C12N15/09 , C12P21/02 , C12Q1/02 , G01N33/15 , G01N33/566 , C07H21/04
CPC分类号： C07K14/72 , C07K14/723
摘要： A novel canine cDNA sequence that encodes the canine growth hormone secretagogue receptor (GHSR) protein is provided. Also provided is canine GHSR protein encoded by the novel cDNA sequence. Methods of expressing canine GHSR protein in recombinant systems are provided. Also provided are methods for identifying agonists and antagonists of the canine GHSR.
摘要翻译：提供了编码犬生长激素促分泌素受体（GHSR）蛋白的新型犬cDNA序列。还提供了由新的cDNA序列编码的犬GHSR蛋白。提供了在重组系统中表达犬GHSR蛋白的方法。还提供了用于鉴定犬GHSR的激动剂和拮抗剂的方法。

3. 发明申请

WO1997021730A1 GROWTH HORMONE SECRETAGOGUE RECEPTOR FAMILY 审中-公开
标题翻译：生长HORMONE SECRETAGOGUE受体家族
公开(公告)号：WO1997021730A1
公开(公告)日：1997-06-19
申请号：PCT/US1996019445
申请日：1996-12-10
申请人： MERCK & CO., INC. , ARENA, Joseph, P. , CULLY, Doris, F. , FEIGHNER, Scott, D. , HOWARD, Andrew, D. , LIBERATOR, Paul, A. , SCHAEFFER, James, M. , VAN DER PLOEG, Leonardus
发明人： MERCK & CO., INC.
IPC分类号： C07K14/705
CPC分类号： C07K14/723 , A61K38/00 , C07B59/002
摘要： Human, swine and rat growth hormone secretagogue receptors have been isolated, cloned and sequenced. Growth hormone secretagogue receptors are new members of the G-protein family of receptors. The growth hormone secretagogue receptors may be used to screen and identify compounds which bind to the growth hormone secretagogue receptor. Such compounds may be used in the treatment of conditions which occur when there is a shortage of growth hormone, such as observed in growth hormone deficient children, elderly patients with musculoskeletal impairment and recovering from hip fracture and osteoporosis.
摘要翻译：人，猪和大鼠生长激素促分泌素受体已被分离，克隆和测序。生长激素促分泌素受体是G-蛋白家族受体的新成员。生长激素促分泌素受体可用于筛选和鉴定结合生长激素促分泌素受体的化合物。这些化合物可用于治疗当生长激素短缺时发生的病症，例如在生长激素缺乏的儿童中观察到的老年肌肉骨骼损伤患者以及从髋部骨折和骨质疏松症中恢复。

4. 发明申请

WO1997022004A1 ASSAYS FOR GROWTH HORMONE SECRETAGOGUE RECEPTORS 审中-公开
标题翻译：生长激素分泌受体的测定
公开(公告)号：WO1997022004A1
公开(公告)日：1997-06-19
申请号：PCT/US1996019442
申请日：1996-12-10
申请人： MERCK & CO., INC. , CHAUNG, Lee-Yuh , FEIGHNER, Scott, D. , HOWARD, Andrew, D. , PONG, Sheng, S. , VAN DER PLOEG, Leonardus
发明人： MERCK & CO., INC.
IPC分类号： G01N33/566
CPC分类号： G01N33/74 , C07K14/723 , C12Q1/6897 , G01N2333/726 , G01N2500/10
摘要： An assay for the detection of growth hormone secretagogue receptors and growth hormone secretagogue related receptors is described. As these receptors are a member of the G protein coupled receptors, a subunit of the G protein must be present in order for expression to be detected. A similar assay is described where the presence of growth hormone secretagogues are detected.
摘要翻译：描述了用于检测生长激素促分泌素受体和生长激素促分泌素相关受体的测定法。由于这些受体是G蛋白偶联受体的成员，所以必须存在G蛋白的亚基以便表达被检测。描述了检测到生长激素促分泌素的存在的类似的测定。

5. 发明申请

WO1994000154A1 DNA ENCODING PRECURSOR INTERLEUKIN 1'beta' CONVERTING ENZYME 审中-公开
标题翻译： DNA编码前体蛋白1转化酶
公开(公告)号：WO1994000154A1
公开(公告)日：1994-01-06
申请号：PCT/US1993005687
申请日：1993-06-14
申请人： MERCK & CO., INC. , HOWARD, Andrew, D. , MOLINEAUX, Susan, M. , TOCCI, Michael, J. , CALAYCAY, Jimmy, R. , MILLER, Douglas, K.
发明人： MERCK & CO., INC.
IPC分类号： A61K39/395
CPC分类号： C12N9/6475 , A61K48/00
摘要： Complementary DNA (cDNA) encoding the precursor interleukin-1 beta (pre-IL-1 beta ) converting enzyme (ICE) is isolated from a cDNA library. A cDNA, encoding the full-length open reading frame (ORF) for the nascent ICE, as well as individual cDNAs encoding the 20 kDa subunit and the 10 kDa subunit of ICE are identified and sequenced. ICE is useful in the conversion of pre-IL-1 beta into mature IL-1 beta . The recombinantly produced ICE, including the individual 20 kDa and 10 kDa subunits is useful in the diagnosis of inflammatory diseases, in the production of recombinant IL-1 beta , and to identify inhibitors of ICE activity.
摘要翻译：从cDNA文库中分离编码前体白细胞介素-1β（前IL-1β）转化酶（ICE）的互补DNA（cDNA）。鉴定并测序编码新生ICE的全长开放阅读框（ORF）的cDNA以及编码20kDa亚基和10kDa亚基的单个cDNA。 ICE可以将IL-1β转化成成熟IL-1β。重组产生的ICE，包括单独的20kDa和10kDa亚基可用于诊断炎性疾病，重组IL-1β的产生和鉴定ICE活性的抑制剂。

6. 发明申请

WO0050563A9 G PROTEIN-COUPLED RECEPTOR RESEMBLING GALANIN RECEPTORS 审中-公开
标题翻译： G蛋白偶联受体阻断GALANIN受体
公开(公告)号：WO0050563A9
公开(公告)日：2001-08-30
申请号：PCT/US0004416
申请日：2000-02-22
申请人： MERCK & CO INC , MERCK FROSST CANADA INC , UNIV TORONTO , HOWARD ANDREW D , NEILL GARY P O , DOWD BRIAN O , GEORGE SUSAN
发明人： HOWARD ANDREW D , O'NEILL GARY P , O'DOWD BRIAN , GEORGE SUSAN
IPC分类号： C07K14/72 , C12N5/10 , C12N15/00 , C12N15/09 , C12N15/11 , C12N15/12 , C12N15/63
CPC分类号： C07K14/723
摘要： Human and rat DNAs encoding a novel G-protein coupled receptor, GPR54, as well as proteins encoded by the DNAs, are provided. Methods of identifying agonists and antagonists of GPR54 are also provided.
摘要翻译：提供了编码新型G蛋白偶联受体GPR54的人和大鼠DNA，以及由DNA编码的蛋白质。还提供了鉴定GPR54的激动剂和拮抗剂的方法。

7. 发明申请

WO0050563A3 G PROTEIN-COUPLED RECEPTOR RESEMBLING GALANIN RECEPTORS 审中-公开
标题翻译： G蛋白偶联受体阻断GALANIN受体
公开(公告)号：WO0050563A3
公开(公告)日：2000-12-21
申请号：PCT/US0004416
申请日：2000-02-22
申请人： MERCK & CO INC , MERCK FROSST CANADA INC , UNIV TORONTO , HOWARD ANDREW D , NEILL GARY P O , DOWD BRIAN O , GEORGE SUSAN
发明人： HOWARD ANDREW D , O'NEILL GARY P , O'DOWD BRIAN , GEORGE SUSAN
IPC分类号： C07K14/72
CPC分类号： C07K14/723
摘要： Human and rat DNAs encoding a novel G-protein coupled receptor, GPR54, as well as proteins encoded by the DNAs, are provided. Methods of identifying agonists and antagonists of GPR54 are also provided.
摘要翻译：提供了编码新型G蛋白偶联受体GPR54的人和大鼠DNA，以及由DNA编码的蛋白质。还提供了鉴定GPR54的激动剂和拮抗剂的方法。

8. 发明申请

WO2010120578A1 MICRORNA AS A BIOMARKER OF PANCREATIC ISLET BETA-CELL ENGAGEMENT 审中-公开
标题翻译： MICRORNA作为PANCREATIC ISLET BETA-CELL参与的生物标记
公开(公告)号：WO2010120578A1
公开(公告)日：2010-10-21
申请号：PCT/US2010/029887
申请日：2010-04-05
申请人： MERCK SHARP & DOHME CORP. , ZHOU, Yun-Ping , HOWARD, Andrew, D. , SHANG, Jin
发明人： ZHOU, Yun-Ping , HOWARD, Andrew, D. , SHANG, Jin
IPC分类号： C12Q1/68
CPC分类号： C12Q1/686 , C12Q1/6883 , C12Q2600/106 , C12Q2600/136 , C12Q2525/207 , C12Q2521/107
摘要： MicroRNAs (miRNAs) are short non-coding RNAs that regulate gene expression and which play important roles in many cell types, including as described herein, the pancreatic β-cell. Glucagon like peptide-1 (GLP-1), a hormone released from intestinal L-cells following meal intake, exerts pleiotropic effects on β-cell function including raising intracellular cAMP levels and now represents an important therapy for type 2 diabetes. Expression of miR-132 and miR212 is upregulated by CREB protein in response increased cAMP levels in the cell; therefore, methods for detecting and evaluating β-cell engagement by GLP-1 receptor agonists by monitoring miR-132 and miR-212 expression in a subject is described. The methods herein are particularly useful in the context of longitudinal clinical trials, such as those designed for testing the durability of any single or combination therapy in type 2 diabetes populations. Because the expression of these miRNAs is not affected by glucose, fatty acid, insulin, or β-cell function, monitoring miR-132 and miR-212 expression can be used to monitor the efficacy of any agent that effects an increase cAMP in β-cells. Such agents include for example, GLP-1, glucagon, GPR-119, and GIP receptor agonists; dipeptidyl peptidase IV (DPP IV) inhibitors; and phosphodiesterase inhibitors.
摘要翻译：微小RNA（miRNA）是调节基因表达的短非编码RNA，其在许多细胞类型中起重要作用，包括本文所述的胰腺β细胞。胰高血糖素样肽-1（GLP-1）是膳食摄入后从肠道L细胞释放的激素，对β细胞功能具有多效性，包括提高细胞内cAMP水平，现在代表了2型糖尿病的重要疗法。 miR-132和miR212的表达由CREB蛋白上调，响应细胞中cAMP水平升高; 因此，描述了通过监测受试者中的miR-132和miR-212表达来检测和评估GLP-1受体激动剂的β细胞接合的方法。本文的方法在纵向临床试验的背景下特别有用，例如设计用于测试2型糖尿病人群中任何单一或联合疗法的耐久性的那些。由于这些miRNA的表达不受葡萄糖，脂肪酸，胰岛素或β细胞功能的影响，监测miR-132和miR-212的表达可用于监测影响ß- 细胞。这些药剂包括例如GLP-1，胰高血糖素，GPR-119和GIP受体激动剂; 二肽基肽酶IV（DPP IV）抑制剂; 和磷酸二酯酶抑制剂。

9. 发明申请

WO2004093785A3 RHESUS MONKEY BOMBESIN RECEPTOR SUBTYPE-3 (BRS-3), NUCLEOTIDES ENCODING SAME, AND USES THEREOF 审中-公开
标题翻译： RHESUS MONKEY BOMBESIN受体亚型3（BRS-3），编码它们的核苷酸及其用途
公开(公告)号：WO2004093785A3
公开(公告)日：2005-05-06
申请号：PCT/US2004011473
申请日：2004-04-14
申请人： MERCK & CO INC , BANYU PHARMA CO LTD , TAN CARINA P , HOWARD ANDREW D , SANO HIDEKI
发明人： TAN CARINA P , HOWARD ANDREW D , SANO HIDEKI
IPC分类号： A61K20060101 , C07H21/04 , C07K14/47 , C07K14/705 , C12N15/12 , C12N15/63 , G01N33/566 , G01N33/567
CPC分类号： C07K14/70571 , C07K14/723 , G01N2333/70571
摘要： A rhesus monkey bombesin receptor subtype-3 has been isolated, cloned and sequenced. This receptor is characteristic of the G-protein family of receptors. Isolated rhesus monkey bombesin receptor subtype-3 may be used to screen and identify novel bombesin receptor modulators that may contribute to the regulation of endocrine processes, metabolism, or the cell cycle. Such compounds may be used in the treatment of conditions that result from deregulated expression of bombesin receptor subtype-3.
摘要翻译：已经分离，克隆和测序了恒河猴铃蟾肽受体亚型3。该受体是G-蛋白家族受体的特征。分离的恒河猴铃蟾肽受体亚型-3可用于筛选和鉴定可能有助于调节内分泌过程，代谢或细胞周期的新型bombesin受体调节剂。这些化合物可用于治疗由bombesin受体亚型-3的失调表达引起的病症。

10. 发明申请

WO2003027239A3 MELANIN-CONCENTRATING HORMONE RECEPTOR ANTAGONIST BINDING PROTEIN 审中-公开
公开(公告)号：WO2003027239A3
公开(公告)日：2003-04-03
申请号：PCT/US2002/029931
申请日：2002-09-20
申请人： MERCK & CO., INC. , HOWARD, Andrew, D. , PAN, Jie , FONG, Tung, M. , MARSH, Donald, J. , SAILER, Andreas, W.
发明人： HOWARD, Andrew, D. , PAN, Jie , FONG, Tung, M. , MARSH, Donald, J. , SAILER, Andreas, W.
IPC分类号： C07K1/00
摘要： The present invention features MCH-1R antagonist binding proteins. MCH-1R antagonist binding proteins described herein are based on an MCH-1R having one or more alterations to the second intracellular loop or carboxy terminus that render the receptor substantially inactive to MCH binding. An MCH-1R antagonist binding protein can bind MCH-1R antagonists, but does not exhibit high affinity MCH binding and is not activated by the MCH.

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