β-Superfamily conotoxins
    4.
    发明授权
    β-Superfamily conotoxins 有权
    β-超家族芋螺毒素

    公开(公告)号:US07115708B2

    公开(公告)日:2006-10-03

    申请号:US11198847

    申请日:2005-08-08

    IPC分类号: C07K4/12 A61K51/08

    CPC分类号: C07K14/43504

    摘要: The present invention is directed to β-superfamily conotoxin peptides, derivatives or pharmaceutically acceptable salts thereof. The present invention is further directed to the use of this peptide, derivatives thereof and pharmaceutically acceptable salts thereof for the treatment of disorders associated with voltage-gated ion channels, ligand gated channels and other receptors. The invention is further directed to nucleic acid sequences encoding the β-superfamily conotoxin peptides and encoding β-superfamily conotoxin propeptides, as well as the β-superfamily conotoxin propeptides.

    摘要翻译: 本发明涉及β-超家族荚果毒素肽,其衍生物或药学上可接受的盐。 本发明进一步涉及该肽,其衍生物和其药学上可接受的盐在治疗与电压门控离子通道,配体门控通道和其它受体相关的病症中的用途。 本发明还涉及编码β-超家族荚果毒素肽和编码β-超家族荚果毒素前肽以及β-超家族荚果毒素前肽的核酸序列。

    Contryphan peptides
    5.
    发明授权
    Contryphan peptides 有权
    对角han肽

    公开(公告)号:US06441132B1

    公开(公告)日:2002-08-27

    申请号:US09297771

    申请日:1999-12-14

    IPC分类号: C07K412

    CPC分类号: C07K7/06 A61K38/00

    摘要: The present invention is directed to contryphan peptides having 6-12 amino acids, preferably including one or more D-tryptophan residues. More specifically, the present invention is directed to contryphan peptides having the general formula Xaa1-Cys-Xaa2-Xaa3-Glu-Pro-Trp-Cys (SEQ ID NO:1), wherein Xaa1 is Gly or des-Xaa1, Xaa2 is Pro or 4-trans-hydroxyproline and Xaa3 is D-Trp or L-Trp, preferably D-Trp. The present invention is further directed to the peptides contryphan R and des-Gly1 contryphan R. In contryphan R, Xaa1 is Gly and Xaa3 is D-Trp. These contryphans are useful as anticonvulsant or neuroprotective agents.

    摘要翻译: 本发明涉及具有6-12个氨基酸的优选肽,优选包括一个或多个D-色氨酸残基。 更具体地,本发明涉及具有通式Xaa1-Cys-Xaa2-Xaa3-Glu-Pro-Trp-Cys(SEQ ID NO:1)的反式肽,其中Xaa1是Gly或des-Xaa1,Xaa2是Pro 或4-反式 - 羟基脯氨酸,Xaa3是D-Trp或L-Trp,优选D-Trp。 本发明进一步针对R和des-Gly1对应的肽。相反,Raa,Xaa1是Gly,Xaa3是D-Trp。 这些拮抗剂可用作抗惊厥药或神经保护剂。

    Uses of &agr;-conotoxin peptides
    7.
    发明授权
    Uses of &agr;-conotoxin peptides 有权
    α-芋螺毒素肽的使用

    公开(公告)号:US06265541B1

    公开(公告)日:2001-07-24

    申请号:US09219446

    申请日:1998-12-23

    IPC分类号: C07K1400

    摘要: The present invention relates to the use of &agr;-conotoxin peptides having the general formula Xaa1-Xaa2-Cys-Cys-Xaa3-Xaa4-Pro-Xaa5-Cys-Xaa6-Cys (SEQ ID NO: 1) for treating disorders regulated at neuronal nicotinic acetylcholine receptors. Such disorders include, but are not limited to, cardiovascular disorders, gastric motility disorders, urinary incontinence, nicotine addiction, mood disorders (such as bipolar disorder, unipolar depression, dysthymia and seasonal effective disorder) and small cell lung carcinoma, as well as the localization of small cell lung carcinoma. In this formula, Xaa1 is des-Xaa1, Tyr, mono-iodo-Tyr or di-iodo-Tyr, Xaa2 is any amino acid, Xaa3 is any amino acid, Xaa4 is any amino acid, Xaa5 is any amino acid and Xaa6 represents a peptide of 3-7 amino acids. Disulfide linkages exist between the first and third cysteines and the second and fourth cysteines. Pro may be replaced with hydroxy-Pro. The C-terminus may contain a hydroxyl or an amide group, preferably an amide group.

    摘要翻译: 本发明涉及具有用于治疗在神经元烟碱乙酰胆碱受体调节的病症的通式的α-芋螺毒素肽的用途。 这些病症包括但不限于心血管疾病,胃动力障碍,尿失禁,尼古丁成瘾,情绪障碍(例如双相情感障碍,单极抑郁,精神抑郁和季节性有效障碍)和小细胞肺癌,以及 小细胞肺癌的定位。 在该式中,Xaa1是des-Xaa1,Tyr,单碘-Tyr或二碘-Tyr,Xaa2是任何氨基酸,Xaa3是任何氨基酸,Xaa4是任何氨基酸,Xaa5是任何氨基酸,Xaa6表示 3-7个氨基酸的肽。 第一和第三半胱氨酸与第二和第四半胱氨酸之间存在二硫键。 Pro可以用羟基替代。 C末端可以含有羟基或酰胺基,优选酰胺基。