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    Depsipeptides and drugs containing the same as the active ingredient
    15.
    发明授权
    Depsipeptides and drugs containing the same as the active ingredient 有权
    含有与活性成分相同的多肽和药物

    公开(公告)号：US06255286B1

    公开(公告)日：2001-07-03

    申请号：US09214002

    申请日：1998-12-24

    申请人： Makoto Yanai ,  Masashi Suzuki ,  Norio Oshida ,  Koji Kawamura ,  Shigeru Hiramoto ,  Orie Yasuda ,  Nobuhiro Kinoshita ,  Akiko Shingai ,  Masako Takasu

    发明人： Makoto Yanai ,  Masashi Suzuki ,  Norio Oshida ,  Koji Kawamura ,  Shigeru Hiramoto ,  Orie Yasuda ,  Nobuhiro Kinoshita ,  Akiko Shingai ,  Masako Takasu

    IPC分类号： A61K3800

    CPC分类号： C07K5/1021 ,  A61K38/00 ,  C07K5/06043 ,  C07K5/06052 ,  C07K5/06104 ,  C07K5/101 ,  C07K7/06 ,  C07K11/00

    摘要： Depsipeptides represented by the formula (1): (wherein: R1 is a straight or branched alkyl group of 5-20 carbon atoms or a straight or branched alkoxymethyl group of 5-15 carbon atoms; R2 is —A—B, —A—B—W, —A—B—W—D or —A—B—W—D—E, R3 is a hydroxyl group, a lower alkoxy group, a benzyloxy group, —Z, —Z—G or —Z—G—J, the above A, B, D, E, G and J independently each other are a residue of an amino acid selected from alanine, valine, leucine, isoleucine, serine, threonine, lysine, hydroxylysine, arginine, cysteine, methionine, phenylalanine, tyrosine, aspartic acid, asparagine, glutamic acid, glutamine and the like or an N—(C1-C4) alkyl derivative of these amino acid residues; the above W and Z independently each other are a residue of an amino acid selected from aspartic acid, asparagine, glutamic acid, glutamine, alanine, serine or lysine) or pharmacologically acceptable salts thereof. The depsipeptides have an activity of promoting the production of apolipoprotein E and are useful as a therapeutic agent for neurologic damages, especially for dementia, and further as a therapeutic agent for hyperlipemia.

    摘要翻译： 由式（1）表示的缩肽：其中：R1是5-20个碳原子的直链或支链烷基或5-15个碳原子的直链或支链烷氧基甲基; R2是-AB，-ABW，-ABWD 或-ABWDE，R3是羟基，低级烷氧基，苄氧基，-Z，-ZG或-ZGJ，上述A，B，D，E，G和J彼此独立地是氨基的残基 选自丙氨酸，缬氨酸，亮氨酸，异亮氨酸，丝氨酸，苏氨酸，赖氨酸，羟赖氨酸，精氨酸，半胱氨酸，甲硫氨酸，苯丙氨酸，酪氨酸，天冬氨酸，天冬酰胺，谷氨酸，谷氨酰胺等的N-酸或N-（C1-C4） 这些氨基酸残基的烷基衍生物;上述W和Z彼此独立地是选自天冬氨酸，天冬酰胺，谷氨酸，谷氨酰胺，丙氨酸，丝氨酸或赖氨酸的氨基酸的残基）或其药理学上可接受的盐。脱脂肽具有 促进载脂蛋白E的产生的活性并且可用作治疗 用于神经损伤的特异剂，特别是对于痴呆，并且作为高脂血症的治疗剂。

    Depsipeptides containing N-substituted glycine residue
    18.
    发明授权
    Depsipeptides containing N-substituted glycine residue 失效
    含有N-取代的甘氨酸残基的三肽

    公开(公告)号：US06316406B1

    公开(公告)日：2001-11-13

    申请号：US09379614

    申请日：1999-08-24

    申请人： Makoto Yanai ,  Masashi Suzuki ,  Norio Oshida ,  Koji Kawamura ,  Shigeru Hiramoto ,  Orie Yasuda ,  Nobuhiro Kinoshita ,  Akiko Shingai ,  Masako Takasu

    发明人： Makoto Yanai ,  Masashi Suzuki ,  Norio Oshida ,  Koji Kawamura ,  Shigeru Hiramoto ,  Orie Yasuda ,  Nobuhiro Kinoshita ,  Akiko Shingai ,  Masako Takasu

    IPC分类号： A61K3815

    CPC分类号： C07K7/06 ,  A61K38/00

    摘要： A depsipeptide containing N-substituted glycine residue having the formula (1) or (2): (wherein R1 is a straight or branched alkyl group of 5-20 carbon atoms or a straight or branched alkoxymethyl group of 5-15 carbon atoms; R2 is a group of the formula —A—B—W—(D)m—(E)n, —A—B—W—(D)m—(E)n—F or —A—B—W—(D)m—(E)n—F—Z; R3 is a hydroxyl group, a lower alkoxy group, a benzyloxy group, or a group of the formula —Z, —Z—G or —Z—G—J; A, B, D, E, F, G and J independently are an N-substituted glycine residue or a residue of an amino acid selected from the group consisting of alanine, valine, leucine, serine, etc.; W and Z independently are a residue of an amino acid selected from the group consisting of an aspartic acid, a glutamic acid, etc.; at least one of A, B, D, E, F, G and J is an N-substituted glycine residue) or a pharmacologically acceptable salt thereof. The above depsipeptides have a promoting activity on the production of apolipoprotein E, and are useful as a therapeutic agent for neurologic damages, especially dementia, and hyperlipemia.

    摘要翻译： 含有具有式（1）或（2）的N-取代甘氨酸残基的缩酚酸肽:(其中R 1是5-20个碳原子的直链或支链烷基或5-15个碳原子的直链或支链烷氧基甲基; R2 是式-ABW-（D）m-（E）n，-ABW-（D）m-（E）nF或-ABW-（D）m-（E）nFZ的基团; R3是羟基 ，低级烷氧基，苄氧基或式-Z，-ZG或-ZGJ的基团; A，B，D，E，F，G和J独立地为N-取代的甘氨酸残基或 选自丙氨酸，缬氨酸，亮氨酸，丝氨酸等的氨基酸; W和Z独立地是选自天冬氨酸，谷氨酸等的氨基酸的残基;至少 A，B，D，E，F，G和J之一是N-取代的甘氨酸残基）或其药理学上可接受的盐。 上述脱脂肽对载脂蛋白E的产生具有促进作用，可用作神经损伤的治疗剂，特别是痴呆和高脂血症。

    Depsipeptides containing N-substituted glycine residue
    20.
    发明授权
    Depsipeptides containing N-substituted glycine residue 失效
    含有N-取代的甘氨酸残基的三肽

    公开(公告)号：US6001815A

    公开(公告)日：1999-12-14

    申请号：US218125

    申请日：1998-12-21

    申请人： Makoto Yanai ,  Masashi Suzuki ,  Norio Oshida ,  Koji Kawamura ,  Shigeru Hiramoto ,  Orie Yasuda ,  Nobuhiro Kinoshita ,  Akiko Shingai ,  Masako Takasu

    发明人： Makoto Yanai ,  Masashi Suzuki ,  Norio Oshida ,  Koji Kawamura ,  Shigeru Hiramoto ,  Orie Yasuda ,  Nobuhiro Kinoshita ,  Akiko Shingai ,  Masako Takasu

    IPC分类号： A61K38/00 ,  C07K7/06

    CPC分类号： C07K7/06 ,  A61K38/00

    摘要： A depsipeptide containing N-substituted glycine residue having the formula (1) or (2): ##STR1## (wherein R.sub.1 is a straight or branched alkyl group of 5-20 carbon atoms or a straight or branched alkoxymethyl group of 5-15 carbon atoms; R.sub.2 is a group of the formula --A--B--W--(D).sub.m --(E).sub.n, --A--B--W--(D).sub.m --(E).sub.n --F or --A--B--W--(D).sub.m --(E).sub.n --F--Z; R.sub.3 is a hydroxyl group, a lower alkoxy group, a benzyloxy group, or a group of the formula --Z, --Z--G or --Z--G--J; A, B, D, E, F, G and J independently are an N-substituted glycine residue or a residue of an amino acid selected from the group consisting of alanine, valine, leucine, serine, etc.; W and Z independently are a residue of an amino acid selected from the group consisting of an aspartic acid, a glutamic acid, etc.; at least one of A, B, D, E, F, G and J is an N-substituted glycine residue) or a pharmacologically acceptable salt thereof.The above depsipeptides have a promoting activity on the production of apolipoprotein E, and are useful as a therapeutic agent for neurologic damages, especially dementia, and hyperlipemia.

    摘要翻译： 含有具有式（1）或（2）的N-取代甘氨酸残基的depsipeptide：（其中R1是5-20个碳原子的直链或支链烷基或5-15个碳原子的直链或支链烷氧基甲基; R2 是式-ABW-（D）m-（E）n，-ABW-（D）m-（E）nF或-ABW-（D）m-（E）nFZ的基团; R3是羟基 ，低级烷氧基，苄氧基或式-Z，-ZG或-ZGJ的基团; A，B，D，E，F，G和J独立地为N-取代的甘氨酸残基或 选自丙氨酸，缬氨酸，亮氨酸，丝氨酸等的氨基酸; W和Z独立地是选自天冬氨酸，谷氨酸等的氨基酸的残基;至少 A，B，D，E，F，G和J之一是N-取代的甘氨酸残基）或其药理学上可接受的盐。 上述脱脂肽对载脂蛋白E的产生具有促进作用，可用作神经损伤的治疗剂，特别是痴呆和高脂血症。