Cyclic peptides as potent and selective melanocortin-4 receptor antagonists
    3.
    发明授权
    Cyclic peptides as potent and selective melanocortin-4 receptor antagonists 失效
    循环肽作为有效和选择性的黑皮质素-4受体拮抗剂

    公开(公告)号:US06693165B2

    公开(公告)日:2004-02-17

    申请号:US09761046

    申请日:2001-01-16

    申请人: Maria A. Bednarek

    发明人: Maria A. Bednarek

    IPC分类号: C07K750

    摘要: Cyclic peptides of formula I are potent and selective antagonists of melanocortin-4 receptors, and as such are useful research tool for the determination of the physiological roles of the MC-4 receptor, as well as for the diagnosis, treatment or prevention of disorders or diseases mediated through the MC-4 receptor.

    摘要翻译: 式I的环肽是黑皮质素-4受体的有效和选择性拮抗剂,因此是确定MC-4受体的生理作用以及用于诊断,治疗或预防疾病或疾病的有用的研究工具 通过MC-4受体介导的疾病。

    Melanin-concentrating hormone analogs
    4.
    发明授权
    Melanin-concentrating hormone analogs 失效
    黑色素浓缩激素类似物

    公开(公告)号:US07220720B2

    公开(公告)日:2007-05-22

    申请号:US10182509

    申请日:2001-02-01

    申请人: Maria A. Bednarek

    发明人: Maria A. Bednarek

    IPC分类号: C07K7/08 A61K38/00

    CPC分类号: C07K7/08 A61K38/00

    摘要: The present invention features truncated MCH analogs active at the MCH receptor. The truncated MCH analogs are optionally modified peptide derivatives of mammalian MCH. The analogs can bind to the MCH receptor and, preferably, bring about signal transduction. MCH analogs have a variety of different uses including being used as a research tool and being used therapeutically.

    摘要翻译: 本发明具有在MCH受体上有活性的截短的MCH类似物。 截短的MCH类似物是哺乳动物MCH的任选修饰的肽衍生物。 类似物可以结合MCH受体,并且优选地引起信号转导。 MCH类似物具有各种不同的用途,包括用作研究工具并被用于治疗。

    Melanin-concentrating hormone antagonists
    6.
    发明授权
    Melanin-concentrating hormone antagonists 失效
    黑色素浓缩激素拮抗剂

    公开(公告)号:US07335723B2

    公开(公告)日:2008-02-26

    申请号:US10485682

    申请日:2002-08-02

    申请人: Maria A. Bednarek

    发明人: Maria A. Bednarek

    IPC分类号: A61K38/12 A61K38/00 A01N37/18

    摘要: The present invention features MCH antagonists active at the MCH-1R. The antagonists are optionally modified peptides able to inhibit the effect of MCH at MCH-1R. MCH antagonists have a variety of uses including being used as a research tool and being used to achieve a beneficial effect in a subject.

    摘要翻译: 本发明具有在MCH-1R活性的MCH拮抗剂。 拮抗剂是能够抑制MCH-1R对MCH的作用的任选修饰的肽。 MCH拮抗剂具有多种用途,包括用作研究工具并用于在受试者中实现有益效果。

    Selective melanin-concentrating hormone type-1 receptor agonists
    7.
    发明授权
    Selective melanin-concentrating hormone type-1 receptor agonists 失效
    选择性黑色素浓缩激素1型受体激动剂

    公开(公告)号:US07273846B2

    公开(公告)日:2007-09-25

    申请号:US10500672

    申请日:2003-01-06

    申请人: Maria A. Bednarek

    发明人: Maria A. Bednarek

    IPC分类号: C07K7/08 A61K38/00

    CPC分类号: C07K14/575 A61K38/00

    摘要: The present invention features truncated hMCH analogs selectively active at MCH-1R over MCH-2R. Using amino acid numbering provided in hMCH, the featured analogs contain an X6 which is either a D-amino acid, 5-guanidinopropionic acid or its lower or higher homolog, or a derivative thereof; and a X10 which is either asparagine, glutamine, alanine, leucine, isoleucine, valine, norleucine, cyclohexylalanine, phenylalanine, (2′)-naphthylalanine, tyrosine, histidine, tryptophan, lysine, serine, threonine, methionine, or a derivative thereof.

    摘要翻译: 本发明的特征在于在MCH-1R上通过MCH-2R选择性活性的截短的hMCH类似物。 使用hMCH中提供的氨基酸编号,特征类似物含有D-氨基酸,5-胍基丙酸或其较低或较高同源物或其衍生物的X 6 S 6。 和天冬酰胺,谷氨酰胺,丙氨酸,亮氨酸,异亮氨酸,缬氨酸,正亮氨酸,环己基丙氨酸,苯丙氨酸,(2') - 萘丙氨酸,酪氨酸,组氨酸,色氨酸,赖氨酸,丝氨酸,苏氨酸的X 10 ,甲硫氨酸或其衍生物。