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公开(公告)号：US06774109B2
公开(公告)日：2004-08-10
申请号：US08961968
申请日：1997-10-31
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。
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公开(公告)号：US5763200A
公开(公告)日：1998-06-09
申请号：US440061
申请日：1995-05-12
IPC分类号： G01N33/566 , A61K38/04 , A61K38/31 , A61K45/00 , A61P5/00 , A61P5/02 , G01N33/15 , G01N33/74 , G01N33/58 , C07K14/655 , G01N33/554
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 hyper-amylinemia 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选择性配体治疗高胰岛淀粉样变性血症的方法。
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公开(公告)号：US6004928A
公开(公告)日：1999-12-21
申请号：US78111
申请日：1998-05-13
IPC分类号： A61K38/31
CPC分类号： A61K38/31
摘要： The present invention relates to a method of decreasing body weight in a patient. The method includes the step of administering a therapeutically effective amount of a type-5 selective somatostatin agonist to the patient.
摘要翻译： 本发明涉及减轻患者体重的方法。 该方法包括向患者施用治疗有效量的5型选择性生长抑素激动剂的步骤。
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4.发明授权Extracts, compounds and pharmaceutical compositions having anti-diabetic activity and their use 失效具有抗糖尿病活性的提取物，化合物和药物组合物及其用途公开(公告)号：US07416744B2
公开(公告)日：2008-08-26
申请号：US11248614
申请日：2005-10-13
摘要： The invention relates inter alia to pharmaceutical compositions containing an extract obtainable from a plant of the genus Trichocaulon or Hoodia having anti-diabetic activity; and to the use of such extracts and to compound (1) as herein defined and its analogues for the manufacture of medicaments having anti-diabetic activity.
摘要翻译： 本发明特别涉及含有可从具有抗糖尿病活性的Trichocaulon或Hoodia植物获得的提取物的药物组合物; 以及这些提取物的使用以及如本文定义的化合物（1）及其类似物用于制备具有抗糖尿病活性的药物。
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5.发明授权Somatostatin and somatostatin agonists for treating insulin insensitivity and Syndrome X 失效生长抑素和生长抑素激动剂用于治疗胰岛素不敏感症和X综合症公开(公告)号：US07256174B2
公开(公告)日：2007-08-14
申请号：US10369143
申请日：2003-02-18
摘要： The present invention relates to a method of treating insulin resistance or Syndrome X by administering a therapeutically effective amount of a somatostatin agonist or a pharmaceutical composition comprised of a somatostatin agonist to a patient suffering from insulin resistance or Syndrome X.
摘要翻译： 本发明涉及一种治疗胰岛素抵抗或综合征X的方法，其通过将治疗有效量的生长抑素激动剂或包含生长抑素激动剂的药物组合物施用于患有胰岛素抵抗或X综合征的患者。
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公开(公告)号：US20130165446A1
公开(公告)日：2013-06-27
申请号：US13696978
申请日：2011-05-11
IPC分类号： A61K31/5025 , A61K31/427 , C07D471/04 , A61K45/06 , C07D403/14 , A61K31/4184 , C07D487/04 , A61K31/4439 , C07D417/14 , A61K31/437
CPC分类号： C07D417/14 , C07D403/14 , C07D471/04
摘要： The present invention addresses the problem of finding a compound having both PPAR activation activity and angiotensin receptor antagonistic activity. The present invention is a benzo- or pyrido-imidazole derivative represented by general formula (I), a pharmaceutically acceptable salt thereof, or a ester or amide thereof (where A is biphenyl methyl-imidazolyl, biphenyl methyl-benzimidazolyl, or the like, B is divalent benzimidazolyl or the like, C is carboxyl or the like, E is divalent phenyl, naphthyl, or the like, G is a dangling bond, oxygen, or the like, Q is oxygen or sulfur, n is an integer from 1 to 6, p is an integer from 1 to 6, V is a dangling bond, oxygen, or the like, and R is hydrogen, alkyl, or the like).
摘要翻译： 本发明解决了找到具有PPAR活化活性和血管紧张素受体拮抗作用的化合物的问题。 本发明是由通式（I）表示的苯并或吡啶并咪唑衍生物，其药学上可接受的盐或其酯或酰胺（其中A为联苯甲基 - 咪唑基，联苯甲基 - 苯并咪唑基等， B是二价苯并咪唑基等，C是羧基等，E是二价苯基，萘基等，G是悬挂键，氧等，Q是氧或硫，n是1的整数 至6，p为1至6的整数，V为悬挂键，氧等，R为氢，烷基等）。
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公开(公告)号：US20110082195A1
公开(公告)日：2011-04-07
申请号：US12863842
申请日：2009-01-21
IPC分类号： A61K31/352 , A61K31/045 , A61P3/04 , A61P3/10 , A61P3/00 , A61P9/00
CPC分类号： A61K31/352 , A61K31/05
摘要： The present invention relates to the use of CBD alone or in combination with another cannabinoid, in the manufacture of a pharmaceutical or neutraceutical formulation for use in controlling cholesterol levels in a subject. It also relates to the use of THCV alone or in combination with another cannabinoid, in the manufacture of a pharmaceutical or neutraceutical formulation for use in increasing energy expenditure in a subject. Furthermore the CBD alone or in combination with another cannabinoid or the THCV alone or in combination with another cannabinoid are used as part of a regime to manage or treat type I or II diabetes, obesity, dyslipidaemia, related metabolic disorders and cardiovascular disease.
摘要翻译： 本发明涉及在制造用于控制受试者中的胆固醇水平的药物或中性制剂中单独使用或与另一种大麻素组合使用。 它还涉及在制造用于增加受试者的能量消耗的药物或中性制剂中单独或与另一种大麻素组合使用THCV。 此外，单独使用CBD或与另一种大麻素或单独使用THCV或与另一种大麻素组合的CBD被用作管理或治疗I型或II型糖尿病，肥胖，血脂异常，相关代谢紊乱和心血管疾病的制度的一部分。
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8.发明授权公开(公告)号：US07662784B2
公开(公告)日：2010-02-16
申请号：US11289800
申请日：2005-11-29
IPC分类号： A61K38/08
CPC分类号： A61Q19/06 , A61K8/64 , A61K38/31 , A61K2800/70
摘要： The present invention relates to a method of decreasing body weight in a patient. The method includes the step of administering a therapeutically effective amount of a somatostatin or a somatostatin agonist to said patient. A pharmaceutical/cosmetic composition comprises the somatostatin or somatostatin agonist. Such products are used to prepare such compositions for the reduction or body weight in a human or mammalian animal.
摘要翻译： 本发明涉及减轻患者体重的方法。 该方法包括向所述患者施用治疗有效量的生长抑素或生长抑素激动剂的步骤。 药物/化妆品组合物包含生长抑素或生长抑素激动剂。 这样的产品用于制备用于人或哺乳动物中的还原或体重的这种组合物。
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9.发明授权公开(公告)号：US07033616B2
公开(公告)日：2006-04-25
申请号：US09891615
申请日：2001-06-27
摘要： The invention relates inter alia to pharmaceutical compositions containing an extract obtainable from a plant of the genus Trichocaulon or Hoodia having anti-diabetic activity; and to the use of such extracts and to compound (1) as herein defined and its analogues for the manufacture of medicaments having anti-diabetic activity.
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公开(公告)号：US07034003B1
公开(公告)日：2006-04-25
申请号：US09423684
申请日：1998-05-13
IPC分类号： A61K38/00
CPC分类号： A61Q19/06 , A61K8/64 , A61K38/31 , A61K2800/70
摘要： The present invention relates to a method of decreasing body weight in a patient. The method includes the step of administering a therapeutically effective amount of a somatostatin or a somatostatin agonist to said patient. A pharmaceutical/cosmetic composition comprises the somatostatin or somatostatin agonist. Such products are used to prepare such compositions for the reduction of body weight in a human or mammalian animal.
摘要翻译： 本发明涉及减轻患者体重的方法。 该方法包括向所述患者施用治疗有效量的生长抑素或生长抑素激动剂的步骤。 药物/化妆品组合物包含生长抑素或生长抑素激动剂。 这样的产品用于制备用于减少人或哺乳动物体重的这样的组合物。
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