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    Mixed amylin activity compounds
    4.
    发明授权
    Mixed amylin activity compounds 失效
    混合胰淀素活性化合物

    公开(公告)号：US06936584B1

    公开(公告)日：2005-08-30

    申请号：US09622104

    申请日：1999-02-05

    申请人： Nigel R. A. Beeley ,  Kathryn Prickett ,  Kevin Beaumont

    发明人： Nigel R. A. Beeley ,  Kathryn Prickett ,  Kevin Beaumont

    IPC分类号： A61K38/00 ,  C07K14/575 ,  A61K37/02 ,  C07K7/10

    CPC分类号： C07K14/575 ,  A61K38/00 ,  Y10S514/866

    摘要： Compounds which inhibit certain activities of amylin but which also act as amylin agonists with respect to other amylin activities are disclosed. Such compounds are useful in treating disturbances in fuel metabolism in mammals, including but not limited to, diabetes, mellitus, including Type I diabetes and Type II diabetes, impaired glucose tolerance, insulin resistance and Syndrome X. The present invention also relates to methods of treating Type I diabetes, beneficially regulating gastrointestinal motility, treating impaired glucose tolerance, treating postprandial hyperglycemia, treating obesity and treating Syndromne X, comprising administration of a therapeutically effective amount of certain compounds, as described herein.

    摘要翻译： 公开了抑制胰岛淀粉多胺的某些活性但也用作其他胰淀素活性的胰岛淀粉样多肽激动剂的化合物。 这些化合物可用于治疗哺乳动物的燃料代谢紊乱，包括但不限于糖尿病，包括I型糖尿病和II型糖尿病，葡萄糖耐量降低，胰岛素抵抗和X综合症。本发明还涉及 治疗I型糖尿病，有利地调节胃肠蠕动，治疗葡萄糖耐量降低，治疗餐后高血糖症，治疗肥胖症和治疗Syndromne X，包括施用治疗有效量的某些化合物，如本文所述。

    Inotropic and diuretic effects of GLP-1 and GLP-1 agonists
    7.
    发明授权
    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：US07442680B2

    公开(公告)日：2008-10-28

    申请号：US10656093

    申请日：2003-09-05

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

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

    IPC分类号： 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。

    Phenylaminocarbonyl derivatives
    10.
    发明授权
    Phenylaminocarbonyl derivatives 失效
    苯基氨基羰基衍生物

    公开(公告)号：US5550137A

    公开(公告)日：1996-08-27

    申请号：US77284

    申请日：1993-06-14

    申请人： Nigel R. A. Beeley ,  Thomas A. Millican

    发明人： Nigel R. A. Beeley ,  Thomas A. Millican

    IPC分类号： C07C233/29 ,  C07C233/75 ,  C07C235/46 ,  C07C235/56 ,  C07D213/75 ,  C07D213/81 ,  C07D239/42 ,  A61K31/44 ,  C07D213/30

    CPC分类号： C07D213/75 ,  C07C233/29 ,  C07C233/75 ,  C07C235/46 ,  C07C235/56 ,  C07D213/81 ,  C07D239/42 ,  C07C2101/08

    摘要： ##STR1## Compounds of formula (1) are described wherein Y represents a halogen atom or a group --OR
    1 where R
    1 represents an optionally substituted alkyl group; R
    2 represents an optionally substituted cycloalkyl, cycloalkenyl or polycycloalkyl group; R
    3 represents a hydrogen atom or an alkyl, aryl or aralkyl group; R
    4 represents an aryl or heteroaryl group; X represents --O--, --S--, --CH
    2 -- or --N(R
    5 )--, where R
    5 is a hydrogen atom or an alkyl group; n is zero or an integer or value 1, 2 or 3; and the salts, solvates and hydrates thereof. The compounds are selective phosphodiesterase IV inhibitors and are useful for the prophylaxis or treatment of inflammatory diseases.

    摘要翻译： （1）式（1）化合物，其中Y表示卤素原子或-OR1基团，其中R 1表示任选取代的烷基; R2表示任选取代的环烷基，环烯基或多环烷基; R3表示氢原子或烷基，芳基或芳烷基; R4表示芳基或杂芳基; X表示-O - ， - S - ， - CH 2 - 或-N（R 5） - ，其中R 5是氢原子或烷基; n为零或整数或值1,2或3; 及其盐，溶剂化物和水合物。 该化合物是选择性磷酸二酯酶IV抑制剂，可用于预防或治疗炎性疾病。