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1. 发明申请

US20080299040A1 SOMATOSTATIN RECEPTOR 2 ANTAGONISTS 有权
标题翻译： SOMATOSTATIN受体2拮抗剂
公开(公告)号：US20080299040A1
公开(公告)日：2008-12-04
申请号：US12104318
申请日：2008-04-16
申请人： Jean E. F. RIVIER , Judit Erchegyi , Jean Claude Reubi , Helmut R. Maecke
发明人： Jean E. F. RIVIER , Judit Erchegyi , Jean Claude Reubi , Helmut R. Maecke
IPC分类号： A61K51/08 , C07K7/64 , A61P35/00 , A61K38/12
CPC分类号： C07K14/655 , A61K38/00 , G01N2333/655
摘要： The invention is directed to somatostatin analogs which are receptor antagonists of the somatostatin receptor, including receptor-selective antagonists, especially sst2-selective antagonists. Related compounds and compositions are included, including antagonists complexed with or conjugated to radioactive nuclides. The antagonists of the invention are useful in diagnosing and treating neoplastic and non-neoplastic mammalian diseases; such methods, and kits, are encompassed.
摘要翻译：本发明涉及作为生长抑素受体的受体拮抗剂的生长抑素类似物，包括受体选择性拮抗剂，特别是sst2选择性拮抗剂。包括相关化合物和组合物，包括与放射性核素复合或缀合的拮抗剂。本发明的拮抗剂可用于诊断和治疗肿瘤和非肿瘤性哺乳动物疾病; 包括这些方法和试剂盒。

2. 发明申请

US20050287557A1 Methods for identifying compounds for treating diabetes mellitus 审中-公开
标题翻译：鉴定化合物治疗糖尿病的方法
公开(公告)号：US20050287557A1
公开(公告)日：2005-12-29
申请号：US11123895
申请日：2005-05-06
申请人： Suad Efendic
发明人： Suad Efendic
IPC分类号： C12N5/08 , C12Q1/68 , G01N33/50
CPC分类号： G01N33/507 , G01N2333/655 , G01N2333/726 , G01N2800/042
摘要： The invention is directed to methods for identifying candidate beta cell-sensitizing compounds comprising providing a pancreatic beta islet cell population derived from a diabetic subject, contacting the beta islet cell population with one or more somatostatin receptor 5-binding compounds, and identifying those somatostatin receptor 5-binding compounds that promote insulin secretion from the pancreatic beta islet cell population at a higher rate than from a control cell population. The invention is further directed to methods for treating type II diabetes comprising administering a beta cell-sensitizing compound identified by the first method of the invention to a diabetic patient in need of treatment.
摘要翻译：本发明涉及用于鉴定候选β细胞增敏化合物的方法，其包括提供衍生自糖尿病受试者的胰岛β细胞群体，使β岛细胞群与一种或多种生长抑素受体5-结合化合物接触，并鉴定那些生长抑素受体 5种结合的化合物以比来自对照细胞群体更高的速率促进胰岛β细胞群体的胰岛素分泌。本发明还涉及用于治疗II型糖尿病的方法，包括将由本发明的第一种方法鉴定的β细胞增敏化合物给予需要治疗的糖尿病患者。

3. 发明授权

US4868107A Method for detecting antibodies against neuropeptides and drugs in human body fluid 失效
标题翻译：用于检测人体液中抗神经肽和药物的抗体的方法
公开(公告)号：US4868107A
公开(公告)日：1989-09-19
申请号：US932084
申请日：1986-11-18
申请人： Benjamin F. Roy, III
发明人： Benjamin F. Roy, III
IPC分类号： G01N33/53 , G01N33/68 , G01N33/94
CPC分类号： G01N33/6896 , G01N33/5308 , G01N33/9406 , G01N2333/48 , G01N2333/655 , G01N2333/685 , G01N2333/695 , G01N2333/70 , Y10S436/809 , Y10S436/811
摘要： An immunochemical assay, particularly an enzyme-linked immunosorbent assay has been developed to detect in a sample of human body fluid the presence of antibodies against neuropeptides or drugs. The assay makes it possible to correlate and diagnose psychobiological disorders related to the alteration in the normal level of neuropeptides or their receptors.
摘要翻译：已经开发了免疫化学测定法，特别是酶联免疫吸附测定法，以在人体液样品中检测抗神经肽或药物的抗体。该测定使得可以关联和诊断与神经肽或其受体的正常水平的改变相关的心理生物学障碍。

4. 发明授权

US07879859B2 Diagnosis and treatment of type 2 diabetes and other disorders 失效
标题翻译：诊断和治疗2型糖尿病等疾病
公开(公告)号：US07879859B2
公开(公告)日：2011-02-01
申请号：US11664381
申请日：2006-11-17
申请人： Yun-Ping Zhou , Jing Li , Weizhen Wu , Jin Shang , John R. Thompson , Nancy A. Thornberry
发明人： Yun-Ping Zhou , Jing Li , Weizhen Wu , Jin Shang , John R. Thompson , Nancy A. Thornberry
IPC分类号： A61K31/50 , A61K31/496 , A61K31/44 , A61K31/415 , A61K31/40
CPC分类号： G01N33/74 , A61K31/437 , A61K31/496 , G01N33/6893 , G01N2333/655 , G01N2500/04 , G01N2800/042 , Y10S514/866
摘要： The present application features the use of the somatostatin subtype 3 receptor (SST3) as a target for affecting insulin secretion and for diagnosing diabetes related disorders. Glucose stimulated insulin secretion was found to be stimulated by knocking down expression of SST3 and through the use of a SST3 selective antagonist.
摘要翻译：本申请的特征在于使用生长抑素亚型3受体（SST3）作为影响胰岛素分泌和诊断糖尿病相关疾病的靶标。发现葡萄糖刺激的胰岛素分泌是通过敲低SST3的表达和通过使用SST3选择性拮抗剂来刺激的。

5. 发明申请

US20050118099A1 Thiol-mediated drug attachment to targeting peptides 审中-公开
标题翻译：硫醇介导的药物与靶向肽的连接
公开(公告)号：US20050118099A1
公开(公告)日：2005-06-02
申请号：US10796158
申请日：2004-03-10
申请人： Gary Braslawsky , Paul Chinn
发明人： Gary Braslawsky , Paul Chinn
IPC分类号： A61K38/00 , A61K47/48 , A61K49/00 , A61K51/00 , A61K51/08 , C07K20060101 , C07K14/655
CPC分类号： C07K14/6555 , A61K47/64 , A61K51/083 , A61K51/088 , G01N2333/655
摘要： Compositions and methods for thiol-specific attachment of therapeutic and diagnostic agents to somatostatin and other targeting peptides.
摘要翻译：治疗和诊断试剂对生长抑素和其他靶向肽的硫醇特异性连接的组合物和方法。

6. 发明授权

US06613572B2 Agent for expression of long-term potentiation of synaptic transmission comprising compound having brain somatostatin activation property 失效
标题翻译：用于表达包含具有脑生长抑素激活性的化合物的突触传递的长期增强的药剂
公开(公告)号：US06613572B2
公开(公告)日：2003-09-02
申请号：US10041592
申请日：2002-01-10
申请人： Nobuya Matsuoka , Masamichi Satoh
发明人： Nobuya Matsuoka , Masamichi Satoh
IPC分类号： G01N3348
CPC分类号： G01N33/5058 , A61K31/00 , A61K31/445 , A61K31/4468 , A61K31/4545 , A61K31/495 , A61K31/496 , C07D211/58 , C07D211/96 , C07D213/81 , C07D295/185 , C07D295/192 , C07D295/205 , C07D295/26 , C07D401/12 , G01N33/5008 , G01N33/502 , G01N33/5088 , G01N2333/655
摘要： The present invention relates to an agent for the expression of long-term potentiation of synaptic transmission, which contains a compound having a brain somatostatin activation property as an active ingredient and to a screening method of an agent for the expression of long-term potentiation of synaptic transmission, which uses a somatostatin releasing property as an index. The present invention is useful for the prophylaxis and/or treatment of cerebral diseases of dementia, amnesia, manic-depressive psychosis, schizophrenia, Parkinson's disease, psychosomatic disease and the like.
摘要翻译：本发明涉及用于表达突变传播的长期增强作用的试剂，其包含具有作为活性成分的脑生长抑素活化性的化合物和用于表达长期增强作用的试剂的筛选方法突触传递，其使用生长抑素释放特性作为指标。本发明可用于预防和/或治疗痴呆，遗忘症，躁狂抑郁精神病，精神分裂症，帕金森病，心身疾病等脑疾病。

7. 发明申请

US20030118586A1 G protein coupled receptor protein, production and use thereof 审中-公开
标题翻译： G蛋白偶联受体蛋白，其生产和使用
公开(公告)号：US20030118586A1
公开(公告)日：2003-06-26
申请号：US10184426
申请日：2002-06-28
发明人： Shuji Hinuma , Ryo Fujii , Yuji Kawamata
IPC分类号： A61K039/395 , G01N033/53 , C07H021/04 , C12P021/02 , C12N005/06
CPC分类号： C07K14/705 , A01K2217/05 , A01K2217/075 , G01N2333/5757 , G01N2333/595 , G01N2333/63 , G01N2333/645 , G01N2333/655 , G01N2333/726 , G01N2500/02 , G01N2500/04
摘要： Rabbit gastropyrolic part smooth muscle-derived G protein coupled receptor proteins, partial peptides thereof; and DNAs containing said protein or partial peptide-encoding DNA are provided. The receptor protein and the DNA coding for said protein can be used for {circle over (1)} determination of ligands; {circle over (2)} acquisition of antibody and antiserum; {circle over (3)} construction of expression system for of a recombinant type receptor protein; {circle over (4)} development of the receptor binding assay system using said expression system and screening of the candidate compounds for pharmaceuticals; {circle over (5)} conducting a drug design based upon a comparison with structurally analogous ligands and receptors; {circle over (6)} preparation of probes and PCR primers for a gene diagnosis; {circle over (7)} preparation of transgenic animals; and {circle over (8)} preparation of model patient animals deficient in the receptor protein DNA. Elucidation of the structure and property of the G protein coupled receptor is particularly related to the development of unique pharmaceuticals which act on such a system.
摘要翻译：兔子胃部分平滑肌衍生的G蛋白偶联受体蛋白，其部分肽; 并提供含有所述蛋白质或部分肽编码DNA的DNA。受体蛋白和编码所述蛋白质的DNA可以用于（循环（1个配体的测定; {循环（2次获得抗体和抗血清; {circle over（3构建重组型受体蛋白质的表达系统 ;（循环（使用所述表达系统的受体结合测定系统的4个开发和用于药物的候选化合物的筛选）;循环（5个基于与结构上类似的配体和受体的比较进行药物设计; 6制备用于基因诊断的探针和PCR引物;（循环（7个转基因动物的制备）和{循环（8个缺陷受体蛋白DNA的模型患者动物的制备），阐明G蛋白的结构和性质偶联受体与作用于这种系统的独特药物的开发特别相关。

8. 发明授权

US08691761B2 Somatostatin receptor 2 antagonists 有权
标题翻译：生长抑素受体2拮抗剂
公开(公告)号：US08691761B2
公开(公告)日：2014-04-08
申请号：US12104318
申请日：2008-04-16
申请人： Jean E. F. Rivier , Judit Erchegyi , Jean Claude Reubi , Helmut R. Maecke
发明人： Jean E. F. Rivier , Judit Erchegyi , Jean Claude Reubi , Helmut R. Maecke
IPC分类号： A61K38/31 , A61P3/10
CPC分类号： C07K14/655 , A61K38/00 , G01N2333/655
摘要： The invention is directed to somatostatin analogs which are receptor antagonists of the somatostatin receptor, including receptor-selective antagonists, especially sst2-selective antagonists. Related compounds and compositions are included, including antagonists complexed with or conjugated to radioactive nuclides. The antagonists of the invention are useful in diagnosing and treating neoplastic and non-neoplastic mammalian diseases; such methods, and kits, are encompassed.
摘要翻译：本发明涉及作为生长抑素受体的受体拮抗剂的生长抑素类似物，包括受体选择性拮抗剂，特别是sst2选择性拮抗剂。包括相关化合物和组合物，包括与放射性核素复合或缀合的拮抗剂。本发明的拮抗剂可用于诊断和治疗肿瘤和非肿瘤性哺乳动物疾病; 包括这些方法和试剂盒。

9. 发明授权

US06774109B2 Inhibition of amylin release 失效
标题翻译：抑制胰岛淀粉样多肽释放
公开(公告)号：US06774109B2
公开(公告)日：2004-08-10
申请号：US08961968
申请日：1997-10-31
申请人： Simon Jon Dunmore , Michelle Davenport , Michael Anthony Cawthorne
发明人： Simon Jon Dunmore , Michelle Davenport , Michael Anthony Cawthorne
IPC分类号： A61K3808
CPC分类号： G01N33/74 , A61K38/31 , G01N2333/655 , G01N2333/72 , G01N2500/00
摘要： A method of determining the ability of a compound to both bind to somatostatin type-5 receptor (“SSTR-5”) and inhibit amylin release. The method includes obtaining a preparation, either a cell preparation or a membrane preparation, which contains SSTR-5; incubating the preparation, the compound, and a SSTR-5 ligand, at least one of the ligand and the compound being detectably labeled; determining the ability of the compound to compete against the ligand for binding to SSTR-5; if and only if the compound is determined to be able to bind to SSTR-5, obtaining pancreatic cells; incubating the compound, the pancreatic cells, and an amylin release stimulator under conditions in which the amylin release stimulator would induce release of amylin from the pancreatic cells; and determining the ability of the compound to inhibit amylin release. Also disclosed is a method of treating hyperamylinemia with a ligand selective for SSTR-5.
摘要翻译：测定化合物结合生长抑素5型受体（“SSTR-5”）并抑制胰岛淀粉样多肽释放的能力的方法。该方法包括获得含有SSTR-5的制剂，细胞制剂或膜制剂; 孵育制剂，化合物和SSTR-5配体，至少一种配体和化合物被可检测地标记; 确定化合物与配体竞争结合SSTR-5的能力; 当且仅当该化合物被确定为能够结合SSTR-5时，获得胰腺细胞; 在胰岛淀粉样多肽释放刺激剂将诱导胰岛淀粉样多肽从胰腺细胞释放的条件下孵育化合物，胰腺细胞和胰岛淀粉样多肽释放刺激物; 并确定该化合物抑制胰岛淀粉样多肽释放的能力。还公开了一种用SSTR-5选择性配体治疗高蛋白血症的方法。

10. 发明申请

US20040146951A1 Inhibition of amylin release 审中-公开
公开(公告)号：US20040146951A1
公开(公告)日：2004-07-29
申请号：US10753717
申请日：2004-01-08
发明人： Simon Jon Dunmore , Michelle Davenport , Michael Anthony Cawthorne
IPC分类号： G01N033/53 , G01N033/567 , C12N005/06
CPC分类号： G01N33/74 , A61K38/31 , G01N2333/655 , G01N2333/72 , G01N2500/00
摘要： A method of determining the ability of a compound to both bind to somatostatin type-5 receptor (nullSSTR-5null) and inhibit amylin release. The method includes obtaining a preparation, either a cell preparation or a membrane preparation, which contains SSTR-5; incubating the preparation, the compound, and a SSTR-5 ligand, at least one of the ligand and the compound being detectably labeled; determining the ability of the compound to compete against the ligand for binding to SSTR-5; if and only if the compound is determined to be able to bind to SSTR-5, obtaining pancreatic cells; incubating the compound, the pancreatic cells, and an amylin release stimulator under conditions in which the amylin release stimulator would induce release of amylin from the pancreatic cells; and determining the ability of the compound to inhibit amylin release. Also disclosed is a method of treating hyperamylinemia with a ligand selective for SSTR-5.

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