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公开(公告)号：US06346604B1
公开(公告)日：2002-02-12
申请号：US08969007
申请日：1997-11-12
IPC分类号： C07K102
摘要： Cyclic pentapeptides having a &ggr;-turn and a &bgr;-turn wherein the cyclic pentapeptide has the following formula (I): Cyclo(—A1—A2—A3—A4—A5—) (I) wherein A1, A2, A3, A4 and A5 are amino acid residues; said pentapeptide having amino acid residues in positions 1-2-3 to form a &ggr;-turn, and amino acid residues in positions 3-4-5-1 to form a &bgr;-turn in combination with the &ggr;-turn; in which D-&agr;-amino acid residues are selected for A1, A3 and A5 and L-&agr;-amino acid residues are selected for A2 and A4 or wherein L-&agr;-amino acid residues are selected for A1, A3 and A5 and D-&agr;-amino acid residues are selected for A2 and A4; are provided. Compounds having &ggr;-turns and &bgr;-turns can be systhesized, regardless of the kinds of amino acid residues, and it is possible to synthesize compounds in which desired amino acid residues are introduced into sites of &bgr;-turn and &ggr;-turn based on their importance from the viewpoint of biological activity. The present invention is therefore available for design of compounds having biological activity.
摘要翻译： 具有γ-匝和β-匝的环状五肽，其中环状五肽具有下式（I）：其中A1，A2，A3，A4和A5是氨基酸残基;所述五肽在1-2位具有氨基酸残基 -3以形成γ-匝数，以及位置3-4-5-1处的氨基酸残基与γ匝组合形成β-匝数;其中选择D-α-氨基酸残基用于A1， A2和A4选择A3和A5和L-α-氨基酸残基，或选择A1，A3和A5的L-α-氨基酸残基，A2和A4选择D-α-氨基酸残基; 具有γ-匝数和β-匝数的化合物可以被控制，而不管氨基酸残基的种类如何，并且可以合成将期望的氨基酸残基引入β-匝和γ-匝的位点的化合物 基于它们从生物活性的角度的重要性。 因此，本发明可用于设计具有生物活性的化合物。
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公开(公告)号：US06610655B2
公开(公告)日：2003-08-26
申请号：US09999432
申请日：2001-11-15
IPC分类号： C07K102
摘要： Cyclic pentapeptides are disclosed having the following formula (I)-Cyclo(-A1-A2-A3-A4-A5-)-wherein A1, A2, A3, A4 and A5 are amino acid residues. The pentapeptide has amino acid residues in positions 1-2-3 to form a &ggr;-turn, and amino acid residues in positions 3-4-5-1 to form a &bgr;-turn in combination with the &ggr;-turn. D-&agr;-amino acid residues are selected for A1, A3, and A5 and L-&agr;-amino acid residues are selected for A2 and A4. Compounds having &ggr;-turns and &bgr;-turns can be synthesized, regardless of the kinds of amino acid residues, and it is possible to synthesize compounds in which desired amino acid residues are introduced into sites of &bgr;-turn and &ggr;-turn based on their importance from the viewpoint of biological activity. The present invention is therefore available for design of compounds having biological activity.
摘要翻译： 公开了具有下式（I）-Cyclo（-A1-A2-A3-A4-A5-））的环五肽 - 其中A1，A2，A3，A4和A5是氨基酸残基。 五肽在1-2-3位具有氨基酸残基以形成γ-转角，并且3-4-5-1位置的氨基酸残基与γ转弯结合形成β-转角。 选择A1，A3和A5的D-α-氨基酸残基，A2和A4选择L-α-氨基酸残基。 可以合成具有γ-匝数和β-匝数的化合物，而不考虑氨基酸残基的种类，并且可以合成其中所需氨基酸残基被引入β-匝和γ-匝转位点的化合物 从生物活动的角度来看重要。 因此，本发明可用于设计具有生物活性的化合物。
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公开(公告)号：US5965526A
公开(公告)日：1999-10-12
申请号：US551251
申请日：1995-10-31
摘要： Cyclic pentapeptides are disclosed having the following formula (I) --Cyclo(-A.sub.1 -A.sub.2 -A.sub.3 -A.sub.4 -A.sub.5 -)-- wherein A.sub.1, A.sub.2, A.sub.3, A.sub.4 and A.sub.5, are amino acid residues. The pentapeptide has amino acid residues in positions 1-2-3 to form a .gamma.-turn, and amino acid residues in positions 3-4-5-1 to form a .beta.-turn in combination with the .gamma.-turn. D-.alpha.-amino acid residues are selected for A.sub.1, A.sub.3, and A.sub.5 and L-.alpha.-amino acid residues are selected for A.sub.2 and A.sub.4. Compounds having .gamma.-turns and .beta.-turns can be synthesized, regardless of the kinds of amino acid residues, and it is possible to synthesize compounds in which desired amino acid residues are introduced into sites of .beta.-turn and .gamma.-turn based on their importance from the viewpoint of biological activity. The present invention is therefore available for design of compounds having biological activity.
摘要翻译： 公开了具有下式（I）-Cyclo（-A1-A2-A3-A4-A5-））的环五肽，其中A1，A2，A3，A4和A5是氨基酸残基。 五肽在1-2-3位具有氨基酸残基以形成γ转角，并且3-4-5-1位置的氨基酸残基与γ转角组合形成β转角。 A1，A3和A5选择D-α-氨基酸残基，A2和A4选择L-氨基酸残基。 可以合成具有γ-转角和β-转角的化合物，而不管氨基酸残基的种类如何，并且可以合成其中所需氨基酸残基被引入β-转角和γ转角的位点的化合物，基于它们 从生物活动的角度来看重要。 因此，本发明可用于设计具有生物活性的化合物。
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公开(公告)号：US20070202099A1
公开(公告)日：2007-08-30
申请号：US10594773
申请日：2005-03-29
IPC分类号： A61K39/395
CPC分类号： C07K16/18 , A61K47/6843
摘要： The present invention provides an agent for improving the blood stability of an endogenous ligand, which comprises an antibody that has affinity to the mammalian endogenous ligand but substantially does not neutralize the same, and the above-described agent for the prophylaxis and/or treatment for a disease for which an increase in the blood concentration of the endogenous ligand and/or an prolonged blood half-life is prophylactically or therapeutically effective. Provided that the above-described agent is administered alone to a mammal without co-administering the same or substantially the same compound as the endogenous ligand, the blood stability of the endogenous ligand increases and the receptor activity-regulatory action thereof is enhanced.
摘要翻译： 本发明提供了一种用于改善内源性配体的血液稳定性的试剂，其包含对哺乳动物内源性配体具有亲和力但基本上不中和其的抗体，以及上述用于预防和/或治疗 内源性配体的血液浓度的增加和/或延长的血液半衰期的预防或治疗有效的疾病。 假设将上述药剂单独施用于哺乳动物而不与内源性配体相同或基本相同的化合物共同施用，则内源性配体的血液稳定性增加，并且其受体活性调节作用增强。
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公开(公告)号：US09175037B2
公开(公告)日：2015-11-03
申请号：US13263630
申请日：2010-04-08
申请人： Taiji Asami , Hiroshi Inooka , Naoki Nishizawa
发明人： Taiji Asami , Hiroshi Inooka , Naoki Nishizawa
摘要： An object of the present invention is to provide a novel anorectic agent. Another object of the invention is to provide an NMU derivative which exhibits a high anorectic effect even when administered in a usual manner, for example, peripherally. These objects can be achieved by the compound represented by formula (I) or a salt thereof. In formula (I), Y represents a polypeptide containing an amino acid sequence set forth in SEQ ID NO.: 1 wherein 1 to 4 amino acids are substituted; X represents a methoxypolyethylene glycol; X′ is absent or represents a methoxypolyethylene glycol; and a moiety represented by formula: La-Lb-[Lc]j represents a linker.
摘要翻译： 本发明的目的是提供一种新型的厌食剂。 本发明的另一个目的是提供即使以常规方式（例如外周）施用也显示出高的厌食症的NMU衍生物。 这些目的可以通过式（I）表示的化合物或其盐来实现。 式（I）中，Y表示含有1〜4个氨基酸被取代的SEQ ID NO：1所示的氨基酸序列的多肽。 X表示甲氧基聚乙二醇; X'不存在或表示甲氧基聚乙二醇; 并且由式：La-Lb- [Lc] j表示的部分代表连接体。
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公开(公告)号：US20120094899A1
公开(公告)日：2012-04-19
申请号：US13263630
申请日：2010-04-08
申请人： Taiji Asami , Hiroshi Inooka , Naoki Nishizawa
发明人： Taiji Asami , Hiroshi Inooka , Naoki Nishizawa
摘要： An object of the present invention is to provide a novel anorectic agent. Another object of the invention is to provide an NMU derivative which exhibits a high anorectic effect even when administered in a usual manner, for example, peripherally. These objects can be achieved by the compound represented by formula (I) or a salt thereof. In formula (I), Y represents a polypeptide containing an amino acid sequence set forth in SEQ ID NO.: 1 wherein 1 to 4 amino acids are substituted; X represents a methoxypolyethylene glycol; X′ is absent or represents a methoxypolyethylene glycol; and a moiety represented by formula: La-Lb-[Lc]j represents a linker.
摘要翻译： 本发明的目的是提供一种新型的厌食剂。 本发明的另一个目的是提供即使以常规方式（例如外周）施用也显示出高的厌食症的NMU衍生物。 这些目的可以通过式（I）表示的化合物或其盐来实现。 式（I）中，Y表示含有1〜4个氨基酸被取代的SEQ ID NO：1所示的氨基酸序列的多肽。 X表示甲氧基聚乙二醇; X'不存在或表示甲氧基聚乙二醇; 并且由式：La-Lb- [Lc] j表示的部分代表连接体。
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公开(公告)号：US20100286035A1
公开(公告)日：2010-11-11
申请号：US12681747
申请日：2008-10-06
申请人： Tetsuya Ohtaki , Yasushi Masuda , Satoshi Kumano , Hiroshi Inooka
发明人： Tetsuya Ohtaki , Yasushi Masuda , Satoshi Kumano , Hiroshi Inooka
CPC分类号： C07K14/575 , A61K38/00 , A61K47/60
摘要： The objective of the present invention is to provide a new antifeedant. The other objective of the present invention is to provide a NMU derivative showing a high antifeedant activity even in common administration forms such as peripheral administration. A neuromedin U derivative wherein a methoxypolyethylene glycol is bound via a linker having a specific structure to a polypeptide which contains at least 8 amino acids of the C-terminus of an amino acid sequence of neuromedin U and which consists of the same or substantially the same amino acid sequence as the amino acid sequence of neuromedin U.
摘要翻译： 本发明的目的是提供一种新的拒食剂。 本发明的另一个目的是提供即使在常规给药形式如外周给药中也显示高抗拒食活性的NMU衍生物。 一种神经介素U衍生物，其中甲氧基聚乙二醇通过具有特定结构的连接体与包含神经介肽U的氨基酸序列的至少8个氨基酸的多肽结合，所述多肽含有相同或基本相同的氨基酸序列 氨基酸序列作为神经介素U的氨基酸序列。
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公开(公告)号：US20100112601A1
公开(公告)日：2010-05-06
申请号：US12309998
申请日：2007-08-07
申请人： Masahiro Shirakawa , Hiroshi Inooka
发明人： Masahiro Shirakawa , Hiroshi Inooka
IPC分类号： G01N33/567 , C07K16/00
CPC分类号： C07K16/28 , C07K2317/55 , C07K2317/76 , C07K2317/92 , G01N33/56966 , G01N33/74 , G01N2333/726
摘要： The present invention provides an anti-PAC1 monoclonal antibody capable of recognizing a PAC1 having a native structure, a PAC1 activity regulator (in particular, activity inhibitor) containing the antibody, a prophylactic/therapeutic agent for a disease associated with accentuation of a bioactivity of PAC1, containing the antibody, a diagnostic reagent for a disease associated with an abnormality of PAC1 activity, containing the antibody, and a screening method for a substance that regulates the expression of PAC1, using the antibody and a PAC1-expressing cell.
摘要翻译： 本发明提供能够识别具有天然结构的PAC1的抗PAC1单克隆抗体，含有抗体的PAC1活性调节剂（特别是活性抑制剂），与增加生物活性相关的疾病的预防/治疗剂 含有抗体的PAC1，含有抗体的PAC1活性异常的疾病的诊断试剂，以及使用抗体和PAC1表达细胞调节PAC1的表达的物质的筛选方法。
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