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公开(公告)号：JP2009001583A
公开(公告)日：2009-01-08
申请号：JP2008187967
申请日：2008-07-18
发明人： BRIDON DOMINIQUE P , L ARCHEVEQUE BENOIT , EZRIN ALAN M , HOLMES DARREN L , LEBLANC ANOUK , ST PIERRE SERGE
IPC分类号： A61K38/00 , C07K14/47 , A61K35/14 , A61K35/16 , A61K38/22 , A61K38/26 , A61K38/28 , A61K47/22 , A61P3/08 , A61P3/10 , C07K5/103 , C07K7/06 , C07K7/08 , C07K14/16 , C07K14/435 , C07K14/575 , C07K14/605 , C07K14/765 , C07K19/00
CPC分类号： C07K14/005 , A61K38/00 , C07K14/605 , C12N2740/16122
摘要： PROBLEM TO BE SOLVED: To modify GLP-1, exendin 3, exendin 4 and other insulinotropic peptides to impart long lasting activity in vivo while keeping their low toxicity and merits in treatment. SOLUTION: The modified insulinotropic peptides consisting of exendin-4(1-39)-Lys 40 ( ε -MPA)-NH 2 , the modified insulinotropic peptides consisting of exendin-4(1-39)-Lys 40 ( ε -AEEA-MPA)-NH 2 , a conjugate containing the modified insulinotropic peptides linked to a blood component in a covalent bond, and a conjugate wherein the blood component is serum albumin are provided. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译： 待解决的问题：修饰GLP-1，毒蜥外泌肽3，毒蜥外泌肽素4和其他促胰岛素肽以在体内赋予持久的活性，同时保持其低毒性和治疗的优点。 解决方案：由毒蜥外泌肽-4（1-39）-Lys
40 -ASS -NH SB 组成的修饰的促胰岛素肽 >，由毒蜥外泌肽-4（1-39）-Lys 40（ ε -AEEA-MPA）-NH SB 2组成的修饰的促胰岛素肽 提供了含有与共价键中的血液成分连接的修饰的促胰岛素肽的缀合物和血液成分为血清白蛋白的结合物。 版权所有（C）2009，JPO＆INPIT -
公开(公告)号：JP2010168384A
公开(公告)日：2010-08-05
申请号：JP2010020780
申请日：2010-02-01
IPC分类号： A61K47/42 , C07K14/47 , A61K38/00 , A61K38/02 , A61K47/48 , A61P1/18 , A61P5/00 , A61P25/00 , A61P25/28 , A61P43/00 , C07K1/107 , C07K1/113 , C07K1/14 , C07K2/00 , C07K7/00 , C07K14/00 , C07K14/16 , C07K14/465 , C07K14/575 , C07K14/605 , C07K14/645
CPC分类号： C07K14/645 , A61K38/00 , A61K47/62 , C07K14/00 , C07K14/005 , C07K14/465 , C07K14/575 , C07K14/57545 , C07K14/605 , C07K14/62 , C07K14/76 , C07K2319/31 , C12N2740/16122
摘要： PROBLEM TO BE SOLVED: To provide a therapeutic method using a modified peptide by modifying a therapeutic peptide so as to protect the same from peptidase activity, offer longer duration of activity in-vivo and keep its toxicity low. SOLUTION: The modified therapeutic peptide is formable of a therapeutic peptide conjugate stabilized against peptidase activity, provided that the peptide includes a carboxy-terminal amino acid, an amino-terminal amino acid, a therapeutically active domain and a lowly therapeutically active domain identified through structure-activity analysis. The peptide contains a specific amino acid sequence having a reactive group that binds to an amino acid located within the lowly therapeutically active domain of the amino acid. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译： 要解决的问题：为了提供使用修饰的肽通过改变治疗肽以保护其不受肽酶活性的治疗方法，在体内提供更长的活性持续时间并保持其毒性低。 解决方案：修饰的治疗肽可形成针对肽酶活性稳定的治疗性肽缀合物，条件是肽包含羧基末端氨基酸，氨基末端氨基酸，治疗活性结构域和低治疗活性结构域 通过结构活动分析确定。 肽含有具有结合位于氨基酸的低治疗活性结构域内的氨基酸的反应性基团的特异性氨基酸序列。 版权所有（C）2010，JPO＆INPIT
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公开(公告)号：JP2009007371A
公开(公告)日：2009-01-15
申请号：JP2008187966
申请日：2008-07-18
发明人： BRIDON DOMINIQUE P , L ARCHEVEQUE BENOIT , EZRIN ALAN M , HOLMES DARREN L , LEBLANC ANOUK , ST PIERRE SERGE
IPC分类号： A61K38/00 , C07K14/575 , A61K35/14 , A61K35/16 , A61K38/04 , A61K38/22 , A61K38/26 , A61K38/28 , A61K47/42 , A61K47/48 , A61P3/04 , A61P3/08 , A61P3/10 , A61P25/08 , A61P25/14 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P41/00 , C07K5/103 , C07K7/06 , C07K7/08 , C07K14/16 , C07K14/435 , C07K14/605 , C07K14/765 , C07K19/00 , C12N15/09
CPC分类号： C07K14/005 , A61K38/00 , C07K14/605 , C12N2740/16122
摘要： PROBLEM TO BE SOLVED: To modify GLP-1, Exendin3, Exendin4 and other insulinotropic peptides to impart long lasting activity in vivo while keeping their low toxity and merits in treatment. SOLUTION: A modified insulinotropic peptides consists of an Exendin-4(1-39)-Lys 40 (ε-MPA)-NH 2 , a modified insulinotropic peptides consists of an Exendin-4(1-39)-Lys 40 (ε-AEEA-MPA)-NH 2 , a conjugate containing modified insulinotropic peptides linked to a blood component in a covalent bond, a conjugate wherein the blood component is serum albumin. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译： 要解决的问题：修饰GLP-1，毒蜥外泌肽3，毒蜥外泌肽4和其他促胰岛素肽，以在体内赋予持久的活性，同时保持其低毒性和治疗的优点。 解决方案：修饰的促胰岛素肽由Exendin-4（1-39）-Lys SP30（ε-MPA）-NHS2S / SB>，修饰的促胰岛素肽 由含有与血液成分连接的修饰的促胰岛素肽的共轭物组成的毒蜥外泌肽-4（1-39）-Lys
40 （ε-AEEA-MPA）-NH 2 在共价键中，其中血液成分是血清白蛋白的结合物。 版权所有（C）2009，JPO＆INPIT -
公开(公告)号：JP2009079048A
公开(公告)日：2009-04-16
申请号：JP2008246982
申请日：2008-09-25
IPC分类号： A61K47/42 , C07K14/00 , A61K38/00 , A61K38/02 , A61K47/48 , A61P1/18 , A61P5/00 , A61P25/00 , A61P25/28 , A61P43/00 , C07K1/107 , C07K1/113 , C07K1/14 , C07K2/00 , C07K7/00 , C07K14/16 , C07K14/465 , C07K14/575 , C07K14/605 , C07K14/645
CPC分类号： C07K14/645 , A61K38/00 , A61K47/62 , C07K14/00 , C07K14/005 , C07K14/465 , C07K14/575 , C07K14/57545 , C07K14/605 , C07K14/62 , C07K14/76 , C07K2319/31 , C12N2740/16122
摘要： PROBLEM TO BE SOLVED: To provide a method for modifying peptides used for treatment to protect them from a peptidase activity, providing a longer retention time of in vivo activity and on the other hand, maintaining a low toxicity and also holding the advantageous points of treatments with the modified peptide. SOLUTION: This modified peptide used for the treatment is provided by forming a peptidase-stabilized peptide conjugate for the treatment. The peptide contains a carboxyl terminal amino acid, an amino terminal amino acid, a treatment active region and a lower treatment active region identified by a structure activity analysis. The peptide contains a peptide YY having a reactive group to be bonded with an amino acid positioned in the lower treatment active region of the amino acids, or its derivative. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译： 要解决的问题：提供一种修饰用于治疗肽类的方法，以保护它们免于肽酶活性，提供更长的体内活性保留时间，另一方面，保持低毒性，并且还具有优势 改良肽处理点。 解决方案：用于治疗的修饰肽通过形成用于治疗的肽酶稳定的肽缀合物来提供。 该肽含有羧基末端氨基酸，氨基末端氨基酸，处理活性区和通过结构活性分析鉴定的较低处理活性区。 肽含有具有与位于氨基酸的较低处理活性区域中的氨基酸结合的反应性基团的肽YY或其衍生物。 版权所有（C）2009，JPO＆INPIT
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公开(公告)号：JP2008150384A
公开(公告)日：2008-07-03
申请号：JP2008008555
申请日：2008-01-17
IPC分类号： A61K47/42 , C07K14/47 , A61K38/00 , A61K38/02 , A61K47/48 , A61P1/18 , A61P5/00 , A61P25/00 , A61P25/28 , A61P43/00 , C07K1/107 , C07K1/113 , C07K1/14 , C07K2/00 , C07K7/00 , C07K14/00 , C07K14/16 , C07K14/465 , C07K14/575 , C07K14/605 , C07K14/645 , C07K19/00
CPC分类号： C07K14/645 , A61K38/00 , A61K47/62 , C07K14/00 , C07K14/005 , C07K14/465 , C07K14/575 , C07K14/57545 , C07K14/605 , C07K14/62 , C07K14/76 , C07K2319/31 , C12N2740/16122
摘要： PROBLEM TO BE SOLVED: To modify a therapeutic peptide to be protected from peptidase activity and to give long lasting of activities in vivo while the peptide keeps low toxicity and retains therapeutic merits of the modified peptide. SOLUTION: A modified therapeutic peptide is provided, which therapeutic peptide can form a peptidase-stabilized therapeutic peptide conjugate, and which peptide contains carboxy-terminal amino acids, amino-terminal amino acid, and therapeutically active regions and lowly therapeutically active regions, identified by structural activity-concerning analysis. The peptide is characterized by containing a specific derivative having a reactive group to be bonded with amino acid positioned in the lowly therapeutically active region of amino acid. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译： 待解决的问题：为了修饰待保护的治疗肽不受肽酶活性的影响，并且在肽保持低毒性并且保持修饰肽的治疗优点的同时在体内给予持久的活性。 解决方案：提供修饰的治疗肽，该治疗肽可以形成肽酶稳定的治疗性肽缀合物，并且该肽含有羧基末端氨基酸，氨基末端氨基酸和治疗活性区域和低治疗活性区域 ，由结构活动相关分析确定。 该肽的特征在于含有具有与位于氨基酸的低治疗活性区域中的氨基酸结合的反应性基团的特异性衍生物。 版权所有（C）2008，JPO＆INPIT
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