Novel Peptides for Use in the Treatment of Obesity
    111.
    发明申请
    Novel Peptides for Use in the Treatment of Obesity 审中-公开
    用于治疗肥胖症的新型肽

    公开(公告)号:US20080039387A1

    公开(公告)日:2008-02-14

    申请号:US11666799

    申请日:2005-11-04

    IPC分类号: A61K38/16 C07K14/00

    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。

    Cyclic peptides as potent and selective melanocortin-4 receptors agonists
    114.
    发明申请
    Cyclic peptides as potent and selective melanocortin-4 receptors agonists 失效
    循环肽作为有效和选择性的黑皮质素-4受体激动剂

    公开(公告)号:US20040171793A1

    公开(公告)日:2004-09-02

    申请号:US10483309

    申请日:2004-01-08

    发明人: Maria A. Bednarek

    IPC分类号: A61K038/12 C07K007/64

    CPC分类号: C07K14/68 A61K38/00 C07K7/56

    摘要: Cyclic peptides of formula I are potent and selective agonists 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 diagnoses, treatment or prevention of disorders or diseases mediated through the MC-4 receptor.

    摘要翻译: 式I的循环肽是黑皮质素-4受体的有效和选择性激动剂,因此是测定MC-4受体的生理作用以及用于诊断,治疗或预防疾病的有用的研究工具, 通过MC-4受体介导的疾病。

    Melanocortin receptor ligands
    115.
    发明授权
    Melanocortin receptor ligands 失效
    黑皮质素受体配体

    公开(公告)号:US06613874B1

    公开(公告)日:2003-09-02

    申请号:US09537789

    申请日:2000-03-29

    IPC分类号: C07K750

    摘要: Disclosed are cyclic peptide analogs that are MC-4 and/or MC-3 receptor ligands, the analogs having a structure according to Formula (I): wherein B, X, E, Z, D, G, M′, W, R, R1, R1′, R11, m, n, p and q are as described in the specification. The peptide analogs are useful in treating diseases that are mediated by the MC-4 and/or the MC-3 receptor. As such, the invention is directed to methods of treating body weight disorders, such as obesity, anorexia, and cachexia. The invention also relates to the treatment of CNS depression, behavior-related disorders, memory-related disorders, cardiovascular function, inflammation, sepsis, septic shock, cardiogenic shock, hypovolemic shock, sexual dysfunction, erectile dysfunction, muscle atrophy, diseases associated with nerve growth and repair, and intrauterine fetal growth. Also disclosed are pharmaceutical compositions comprising the peptide analogs of Formula (I).

    摘要翻译: 公开了作为MC-4和/或MC-3受体配体的环肽类似物,该类似物具有式(I)的结构:其中B,X,E,Z,D,G,M',W,R ,R1,R1',R11,m,n,p和q如说明书中所述。 肽类似物可用于治疗由MC-4和/或MC-3受体介导的疾病。 因此,本发明涉及治疗体重障碍,例如肥胖症,厌食症和恶病质的方法。 本发明还涉及CNS抑郁症,行为相关障碍,记忆相关障碍,心血管功能,炎症,败血症,败血症休克,心源性休克,血容量不足休克,性功能障碍,勃起功能障碍,肌肉萎缩,与神经相关的疾病 生长和修复,宫内胎儿生长。 还公开了包含式(I)的肽类似物的药物组合物。

    Melanocortin receptor ligands and methods of using same
    117.
    发明授权
    Melanocortin receptor ligands and methods of using same 失效
    黑皮质素受体配体及其使用方法

    公开(公告)号:US06350430B1

    公开(公告)日:2002-02-26

    申请号:US09027108

    申请日:1998-02-20

    IPC分类号: A61K5100

    摘要: The invention provides ligands for melanocortin receptors. For example, the invention provides the melanocortin receptor peptide ligand Ac-Nlc-Gln-His-(p(I)-D-Phe)-Arg-(D-Trp)-Cly-NH2, (SEQ ID NO: 1), where the iodo group is unlabeled or radioactively labeled. The invention additionally provides methods of assaying for melanocortin receptors in a cell or tissue such as brain. The invention also relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a melanocortin receptor ligand and to methods of administering the pharmaceutical composition to a subject. The invention further provides tetrapeptide ligands for melanocortin receptors and methods of altering melanocortin receptor activity.

    摘要翻译: 本发明提供黑皮质素受体的配体。 例如,本发明提供黑皮质素受体肽配体Ac-Nlc-Gln-His-(p(I)-D-Phe)-Arg-(D-Trp)-Cly-NH 2,(SEQ ID NO:1) 其中碘基团未标记或放射性标记。 本发明另外提供了测定细胞或组织如脑中黑皮质素受体的方法。 本发明还涉及包含药学上可接受的载体和黑皮质素受体配体的药物组合物以及向受试者施用该药物组合物的方法。 本发明还提供了黑皮质素受体的四肽配体和改变黑皮质素受体活性的方法。

    Cyclic peptides as potent and selective melanocortin-4 receptor antagonists
    118.
    发明申请
    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:US20020016291A1

    公开(公告)日:2002-02-07

    申请号:US09761046

    申请日:2001-01-16

    发明人: Maria A. Bednarek

    IPC分类号: A61K038/12 C07K007/50

    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,因此是测定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。