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公开(公告)号:EP2253326B1
公开(公告)日:2018-04-04
申请号:EP09715976.8
申请日:2009-02-27
发明人: MORISHITA, Mariko , TAKAYAMA, Kozo , NISHIO, Reiji , IDA, Nobuo
CPC分类号: A61K38/215 , A61K9/0043 , A61K38/10 , A61K38/28 , A61K47/42 , C07K14/43581 , A61K2300/00
摘要: By a pharmaceutical composition for nasal administration comprising a hydrophilic bioactive substance and any one of (a) to (c) below, a hydrophilic bioactive substance having a low transmucosal absorption capability which has conventionally been able to be administered by only injection can be nasally administered. Such a pharmaceutical composition is useful for improvement of the pain and the inconvenience of patients caused by administration by injection. (a) A peptide having the amino acid sequence shown in SEQ ID NO: 1. (b) A peptide having the same amino acid sequence as shown in SEQ ID NO: except that one or several amino acids are deleted, substituted and/or added, the peptide having nasal mucosal permeability. (c) A peptide having an amino acid sequence represented by the reverse sequence of (a) or (b), the peptide having nasal mucosal permeability.
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公开(公告)号:EP2433953A1
公开(公告)日:2012-03-28
申请号:EP10777770.8
申请日:2010-05-19
发明人: MORISHITA, Mariko , TAKAYAMA, Kozo , NISHIO, Reiji , IDA, Nobuo
CPC分类号: C07K7/08 , A61K9/0053 , A61K9/007 , A61K9/0073 , A61K38/10 , C07K14/43581
摘要: A cell-penetrating peptide described in any of (A) to (D) below gives cell membrane permeability and further transmucosal absorbability to a physiologically active substance:
(A) a peptide having the amino acid sequence represented by SEQ ID NO:1;
(B) a peptide having an amino acid sequence which is the same as the amino acid sequence represented by SEQ ID NO:1 except that one or several basic amino acids are substituted, deleted, inserted and/or added, which peptide has cell membrane permeability;
(C) a peptide having an amino acid sequence which is the same as the amino acid sequence represented by SEQ ID NO:1 except that 1 to 5 amino acids are substituted, deleted, inserted and/or added, which peptide has cell membrane permeability;
(D) a peptide having: an amino acid sequence represented by the reverse sequence of any of (A) to (C); an amino acid sequence which is the same as the amino acid sequence represented by the reverse sequence of (A) except that one or several basic amino acids are substituted, deleted, inserted and/or added; or an amino acid sequence which is the same as the amino acid sequence represented by the reverse sequence of (A) except that 1 to 5 amino acids are substituted, deleted, inserted and/or added; which peptide has cell membrane permeability.摘要翻译: 下述(A)〜(D)中任一项所述的细胞穿透肽赋予生理活性物质的细胞膜通透性及其进一步的粘膜吸收性:(A)具有SEQ ID NO:1所示的氨基酸序列的肽。 (B)具有与SEQ ID NO:1所示的氨基酸序列相同的氨基酸序列的肽,除了一个或多个碱基氨基酸被取代,缺失,插入和/或添加,该肽具有细胞膜 渗透性; (C)具有与SEQ ID NO:1所示的氨基酸序列相同的氨基酸序列的肽,除了1〜5个氨基酸被取代,缺失,插入和/或添加之外,该肽具有细胞膜渗透性 ; (D)具有由(A)〜(C)中任一项的相反序列表示的氨基酸序列的肽; 与(A)的逆序列表示的氨基酸序列相同的氨基酸序列,除了一个或多个碱性氨基酸被取代,缺失,插入和/或添加; 或与(A)的逆序列表示的氨基酸序列相同的氨基酸序列,除了1〜5个氨基酸被取代,缺失,插入和/或添加; 哪种肽具有细胞膜通透性。
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公开(公告)号:EP2433953B1
公开(公告)日:2015-07-08
申请号:EP10777770.8
申请日:2010-05-19
发明人: MORISHITA, Mariko , TAKAYAMA, Kozo , NISHIO, Reiji , IDA, Nobuo
IPC分类号: C07K7/08 , C07K14/435
CPC分类号: C07K7/08 , A61K9/0053 , A61K9/007 , A61K9/0073 , A61K38/10 , C07K14/43581
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公开(公告)号:EP2253326A1
公开(公告)日:2010-11-24
申请号:EP09715976.8
申请日:2009-02-27
发明人: MORISHITA, Mariko , TAKAYAMA, Kozo , NISHIO, Reiji , IDA, Nobuo
CPC分类号: A61K38/215 , A61K9/0043 , A61K38/10 , A61K38/28 , A61K47/42 , C07K14/43581 , A61K2300/00
摘要: By a pharmaceutical composition for nasal administration comprising a hydrophilic bioactive substance and any one of (a) to (c) below, a hydrophilic bioactive substance having a low transmucosal absorption capability which has conventionally been able to be administered by only injection can be nasally administered. Such a pharmaceutical composition is useful for improvement of the pain and the inconvenience of patients caused by administration by injection.
(a) A peptide having the amino acid sequence shown in SEQ ID NO: 1.
(b) A peptide having the same amino acid sequence as shown in SEQ ID NO: except that one or several amino acids are deleted, substituted and/or added, the peptide having nasal mucosal permeability.
(c) A peptide having an amino acid sequence represented by the reverse sequence of (a) or (b), the peptide having nasal mucosal permeability.
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