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    Novel exendin agonist compounds
    6.
    发明申请
    Novel exendin agonist compounds 有权
    新型毒蜥外泌激素化合物

    公开(公告)号：US20070010656A1

    公开(公告)日：2007-01-11

    申请号：US11511738

    申请日：2006-08-28

    申请人： Nigel Beeley ,  Kathryn Prickett

    发明人： Nigel Beeley ,  Kathryn Prickett

    IPC分类号： A61K38/10 ,  C07K7/08

    CPC分类号： C07K14/57563 ,  A61K38/00

    摘要： Novel exendin agonist compounds are provided. These compounds are useful in treating Type I and II diabetes and conditions which would be benefited by lower plasma glucose and delaying and/or slowing gastric emptying

    摘要翻译： 提供了新的毒蜥外泌激素化合物。 这些化合物可用于治疗I型和II型糖尿病，并且可通过降低血浆葡萄糖和延迟和/或减缓胃排空而受益的病症

    Carbamate or urea derivatives, their preparation and pharmaceutical compositions comprising them
    7.
    发明授权
    Carbamate or urea derivatives, their preparation and pharmaceutical compositions comprising them 失效
    氨基甲酸酯或脲衍生物，其制备方法和包含它们的药物组合物

    公开(公告)号：US4840967A

    公开(公告)日：1989-06-20

    申请号：US70580

    申请日：1987-07-07

    申请人： Nigel Beeley ,  Gerard Cremer

    发明人： Nigel Beeley ,  Gerard Cremer

    IPC分类号： A61K31/36 ,  A61K31/17 ,  A61K31/235 ,  A61K31/27 ,  A61K31/275 ,  A61K31/357 ,  A61P3/00 ,  A61P3/14 ,  A61P9/00 ,  A61P9/06 ,  A61P9/12 ,  C07C67/00 ,  C07C313/00 ,  C07C319/20 ,  C07C323/41 ,  C07D317/58

    CPC分类号： C07C323/41

    摘要： A compound which is a carbamate or urea derivative of general formula (I) ##STR1## wherein X is hydrogen, halogen or methylthio,Y is oxygen or ##STR2## R is C.sub.1 -C.sub.4 alkyl, R.sub.1 is hydrogen, one or two halogen atoms or trifluoromethyl groups, a methyl group, a methyl group, a cyano group, a nitro group, a methoxycarbonyl group, a methylenedioxy group linked to two adjacent carbon atoms of the benzene ring to which it is attached, or a fused benzo group forming an .alpha.-naphthyl or .beta.-naphthyl group with the benzene ring to which it is attached,R.sub.2 is a linear or branched C.sub.1 -C.sub.8 alkyl or alkenyl group optionally substituted with halogen atoms or a methoxy group, a cyclopropylmethyl group, or a phenyl group optionally substituted with one or two halogen atoms or methyl groups,n is 1 or 2, andm is 2 or 3, or an addition salt thereof with a pharmacologically acceptable acid is pharmacologically active as a calcium antagonist.

    摘要翻译： 作为通式（I）的氨基甲酸酯或脲衍生物的化合物其中X是氢，卤素或甲硫基，Y是氧或R 1是C 1 -C 4烷基，R 1是氢，一个或 两个卤素原子或三氟甲基，甲基，甲基，氰基，硝基，甲氧基羰基，与其所连接的苯环的两个相邻碳原子连接的亚甲二氧基或稠合苯并 基团与其所连接的苯环形成α-萘基或β-萘基，R2是任选被卤素原子或甲氧基取代的直链或支链C 1 -C 8烷基或链烯基，环丙基甲基或 任选被一个或两个卤素原子或甲基取代的苯基，n为1或2，m为2或3，或其与药理学可接受的酸的加成盐作为钙拮抗剂具有药理活性。

    Inotropic and diuretic effects of GLP-1 and GLP-1 agonists
    8.
    发明申请
    Inotropic and diuretic effects of GLP-1 and GLP-1 agonists 失效
    GLP-1和GLP-1激动剂的变力和利尿作用

    公开(公告)号：US20050037958A1

    公开(公告)日：2005-02-17

    申请号：US10656093

    申请日：2003-09-05

    申请人： Andrew Young ,  Will Vine ,  Nigel Beeley ,  Kathryn Prickett

    发明人： Andrew Young ,  Will Vine ,  Nigel Beeley ,  Kathryn Prickett

    IPC分类号： A61K31/00 ,  A61K38/22 ,  A61K38/26

    CPC分类号： A61K38/26 ,  A61K31/00 ,  A61K38/2278 ,  Y10S514/866

    摘要： Methods for increasing urine flow are disclosed, comprising administration of an effective amount of GLP-1, an exendin, or an exendin or GLP-1 agonist. Methods for increasing urinary sodium excretion and decreasing urinary potassium concentration are also disclosed. The methods are useful for treating conditions or disorders associated with toxic hypervolemia, such as renal failure, congestive heart failure, nephrotic syndrome, cirrhosis, pulmonary edema, and hypertension. The present invention also relates to methods for inducing an inotropic response comprising administration of an effective amount of GLP-1, an exendin, or an exendin or GLP-1 agonist. These methods are useful for treating conditions or disorders that can be alleviated by an increase in cardiac contractility such as congestive heart failure. Pharmaceutical compositions for use in the methods of the invention are also disclosed.

    摘要翻译： 公开了增加尿流量的方法，包括施用有效量的GLP-1，毒蜥外泌肽或毒蜥外泌肽或GLP-1激动剂。 还公开了增加尿钠排泄量和降低尿钾浓度的方法。 该方法可用于治疗与毒性高血容量相关的病症或病症，例如肾衰竭，充血性心力衰竭，肾病综合征，肝硬化，肺水肿和高血压。 本发明还涉及诱导肌力反应的方法，包括施用有效量的GLP-1，毒蜥外泌肽或毒蜥外泌肽或GLP-1激动剂。 这些方法可用于治疗可通过增加心脏收缩力如充血性心力衰竭而减轻的病症或障碍。 还公开了用于本发明方法的药物组合物。