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    Peptide fragments
    2.
    发明授权
    Peptide fragments 失效
    肽片段

    公开(公告)号：US5891848A

    公开(公告)日：1999-04-06

    申请号：US637418

    申请日：1996-04-25

    申请人： Yutaka Oomura

    发明人： Yutaka Oomura

    IPC分类号： A61K38/00 ,  C07K14/50

    CPC分类号： C07K14/501 ,  A61K38/00

    摘要： Peptide fragments and their pharmaceutically acceptable salts, and therapeutic agents containing one or more of them as an effective component possess excellent therapeutic activity for improving cerebral function and protecting cerebral neurons and are useful as pharmaceutical agents. The peptide fragments of the present invention are amino acid residue peptide fragments of acid fibroblast growth factor (aFGF) of mammalian animals or humans which do not contain cysteine at the 16-position. The compounds include a 1-29 amino acid residue peptide fragment of acid fibroblast growth factor in which cysteine, an amino acid at the 16-position, is substituted with another amino acid, such as alanine, serine, or glutamic acid, and pharmaceutically acceptable salts thereof. The compounds also include a 1-15 amino acid residue fragment of acid fibroblast growth factor of mammalian animals or humans and pharmaceutically acceptable salts thereof. The protein fragments may have an N-terminal group which is in amide form or free form. In a passive avoidance learning test and in a maze-learning test in water, the peptides of the present invention exhibit an excellent action of improving the learning and the remembering ability of senility-accelerated mice in which remembering and learning abilities were reduced. The peptide fragments also exhibit a protective effect against the death of cerebral neurons caused by ischemia. As such, the compounds of the present invention show excellent improvement of brain functions and protection of cerebral neurons. The compounds are useful as a pharmaceutical agent for dementia and other diseases caused by reduction of various brain functions.

    摘要翻译： 肽片段及其药学上可接受的盐和含有一种或多种作为有效成分的治疗剂对于改善脑功能和保护脑神经元具有优异的治疗活性，并且可用作药剂。 本发明的肽片段是在16位不含有半胱氨酸的哺乳动物或人类的酸性成纤维细胞生长因子（aFGF）的氨基酸残基肽片段。 化合物包括酸性成纤维细胞生长因子的1-29个氨基酸残基肽片段，其中16位氨基酸的半胱氨酸被另一个氨基酸如丙氨酸，丝氨酸或谷氨酸取代，并且药学上可接受的 的盐。 所述化合物还包括哺乳动物或人的酸成纤维细胞生长因子的1-15个氨基酸残基片段及其药学上可接受的盐。 蛋白质片段可以具有酰胺形式或游离形式的N-末端基团。 在被动回避学习测试和水中的迷宫学习测试中，本发明的肽表现出改善衰老加速小鼠的学习和记忆能力的优异作用，其中记忆和学习能力降低。 肽片段也表现出对缺血引起的脑神经元死亡的保护作用。 因此，本发明的化合物显示脑功能的极好改善和对脑神经元的保护。 该化合物可用作由各种脑功能降低引起的痴呆症和其它疾病的药剂。