GLUCAGON-LIKE PEPTIDE-1 DERIVATIVES AND THEIR PHARMACEUTICAL USE
    81.
    发明申请
    GLUCAGON-LIKE PEPTIDE-1 DERIVATIVES AND THEIR PHARMACEUTICAL USE 有权
    GLUCAGON-LIKE PEPTIDE-1衍生物及其药物用途

    公开(公告)号:US20110082079A1

    公开(公告)日:2011-04-07

    申请号:US12676451

    申请日:2008-09-05

    CPC分类号: C07K14/605 A61K38/26

    摘要: The invention relates to protracted Glucagon-Like Peptide-1 (GLP-1) derivatives and therapeutic uses thereof. The GLP-1 derivative of the invention comprises a modified GLP-1(7-37) sequence having a total of 2-12 amino acid modifications, including Glu22 and Arg26, and being derivatised with an albumin binding residue or pegylated in position 18, 20, 23, 30, 31, 34, 36, 37, or 39. These compounds are useful in the treatment or prevention of diabetes type 2 and related diseases. The compounds are potent, stable, have long half-lives, a high affinity of binding to albumin, and/or a high affinity of binding to the extracellular domain of the GLP-1 receptor (GLP-1R), all of which is of potential relevance for the overall aim of achieving long-acting, stable and active GLP-1 derivatives with a potential for once weekly administration.

    摘要翻译: 本发明涉及长效的胰高血糖素样肽-1(GLP-1)衍生物及其治疗用途。 本发明的GLP-1衍生物包含具有总共2-12个氨基酸修饰的修饰的GLP-1(7-37)序列,包括Glu22和Arg26,并用白蛋白结合残基衍生或在18位聚乙二醇化, 20,23,30,31,34,36,37或39.这些化合物可用于治疗或预防2型糖尿病和相关疾病。 该化合物是有效的,稳定的,具有长的半衰期,与白蛋白结合的高亲和力,和/或与GLP-1受体(GLP-1R)细胞外结构域结合的高亲和力,所有这些都是 对于实现长效,稳定和活性的GLP-1衍生物的总体目标的潜在相关性,具有每周一次行政的潜力。

    Peptides for Use in the Treatment of Obesity
    84.
    发明申请
    Peptides for Use in the Treatment of Obesity 审中-公开
    用于治疗肥胖症的肽

    公开(公告)号:US20100016238A1

    公开(公告)日:2010-01-21

    申请号:US12522477

    申请日:2008-01-17

    CPC分类号: C07K14/68

    摘要: The present invention relates to novel peptide compounds which are effective in modulating one or more melanocortin receptor types, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of obesity as well as a variety of diseases or conditions associated with obesity.

    摘要翻译: 本发明涉及有效调节一种或多种黑皮质素受体类型的新型肽化合物,治疗中化合物的用途,包括向有需要的患者施用化合物的治疗方法,以及使用 药物制造中的化合物。 本发明的化合物在治疗肥胖以及与肥胖相关的各种疾病或病症方面特别有意义。

    Urea Glucokinase Activators
    85.
    发明申请
    Urea Glucokinase Activators 失效
    尿素葡萄糖激酶活化剂

    公开(公告)号:US20100009989A1

    公开(公告)日:2010-01-14

    申请号:US12522286

    申请日:2008-01-08

    CPC分类号: C07D277/48 C07D417/12

    摘要: This application relates to novel urea glucokinase activators and use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes. Further encompassed is a pharmaceutical composition comprising a compound according to the invention and a process for preparing such.

    摘要翻译: 本申请涉及新型尿素葡萄糖激酶激活剂和本发明化合物在制备用于治疗各种疾病的药物中的用途。 用于治疗2型糖尿病。 进一步包括的是包含根据本发明的化合物和其制备方法的药物组合物。