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公开(公告)号：US20080039532A1
公开(公告)日：2008-02-14
申请号：US11579929
申请日：2005-05-06
CPC分类号： C07K14/005 , A61K47/542 , C12N2740/16122
摘要： The present application relates to a compound having a formula 1: B—R1-R2-M wherein B is a binding element for recognizing and binding a target; R1 is a first group of atoms for reacting with a functionality of the target so as to form a covalent bond with the target; R2 is a second group of atoms; R1 and R2 being such that the formation of the covalent bond between R1 and the target generates cleavage of the bond between R1 and R2 so as to free R2-M; and M is selected from the group consisting of a hydrogen atom and a pharmaceutically acceptable moiety. Alternatively, R1 and R2 can be inverted to form the formula II: B—R2-R1-M and being such that the formation of the covalent bond between R1 and the target generates cleavage of the bond between R1 and R2 so as to free R2-B.
摘要翻译： 本申请涉及具有式1的化合物：B-R1-R2-M其中B是用于识别和结合靶的结合元件; R1是与靶的功能性反应的第一组原子，以与靶形成共价键; R2是第二组原子; R1和R2使得R1和靶之间的共价键的形成产生R1和R2之间的键的切割，以游离R2-M; 并且M选自氢原子和药学上可接受的部分。 或者，可以将R1和R2反转以形成式II：B-R2-R1-M，并且使得R1和靶之间的共价键的形成产生R1和R2之间的键的切割，以释放R2 -B。
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公开(公告)号：US20090054332A1
公开(公告)日：2009-02-26
申请号：US12143780
申请日：2008-06-21
申请人： Jean-Philippe Estradier , Martin Robitaille , Karen Thibaudeau , Dominique P. Bridon , Xicai Huang , Omar Quraishi , Nathalie Bousquet-Gagnon
发明人： Jean-Philippe Estradier , Martin Robitaille , Karen Thibaudeau , Dominique P. Bridon , Xicai Huang , Omar Quraishi , Nathalie Bousquet-Gagnon
CPC分类号： A61K47/644 , A61K47/60 , A61K47/643 , A61K47/65
摘要： The present invention relates to compounds comprising modified thrombopoietin peptides and conjugates of such modified peptides to serum components, typically serum proteins or peptides. The compounds and conjugates of the invention comprise a reactive group or a residue of a reactive group, which is covalently attached to a modified peptide, optionally through a linking group. The present invention also provides methods for the covalent attachment of a modified peptide to a serum protein or peptide to form a conjugate of the invention. The conjugates of the invention typically exhibit a longer in vivo circulating half-life compared to the corresponding unconjugated peptides. The conjugates of the invention also retain at least some of the biological activity of the unconjugated peptides, and typically exhibit increased biological activity compared to the unconjugated peptides. The present invention also provides methods for the treatment and prevention of a disease or disorder comprising the administration of one or more of the compounds or conjugates of the invention to a subject in need of such treatment or prevention.
摘要翻译： 本发明涉及包含修饰的血小板生成素肽和这种修饰肽与血清成分（通常为血清蛋白或肽）的缀合物的化合物。 本发明的化合物和缀合物包含反应性基团或反应性基团的残基，其可任选地通过连接基团与修饰的肽共价连接。 本发明还提供了将修饰的肽共价连接到血清蛋白或肽以形成本发明的缀合物的方法。 与相应的未结合的肽相比，本发明的缀合物通常表现出较长的体内循环半衰期。 本发明的缀合物还保留非共轭肽的至少一些生物活性，并且与非共轭多肽相比通常表现出增加的生物学活性。 本发明还提供了治疗和预防疾病或病症的方法，包括将本发明的一种或多种化合物或缀合物施用于需要这种治疗或预防的受试者。
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公开(公告)号：US20060135428A1
公开(公告)日：2006-06-22
申请号：US11350703
申请日：2006-02-08
CPC分类号： C07K14/005 , A61K38/00 , C07K14/605 , C12N2740/16122
摘要： Modified anti-angiogenic peptides are disclosed. The modified peptides are capable of forming a peptidase stabilized anti-angiogenic peptide. The modified anti-angiogenic peptides, particularly modified kringle 5 peptides are capable of forming a conjugate with a blood protein. Conjugates are prepared from anti-angiogenic peptides, particularly kringle 5 peptides, by combining the peptide with a reactive functional group with a blood protein. The conjugates may be formed in vivo or ex vivo. The conjugates are administered to patients to provide an anti-angiogenic effect.
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公开(公告)号：US20060241019A1
公开(公告)日：2006-10-26
申请号：US10565900
申请日：2004-07-26
CPC分类号： A61K38/28 , A61K47/643 , C07K14/62
摘要： The present invention relates to an insulin derivative comprising an insulin molecule and a reactive group for covalently bonding a blood component, wherein preferably the insulin molecule is human natural insulin molecule and the reactive group is coupled to an amino acid of the insulin molecule at a position selected from the positions Gly A1, Phe B1 and Lys B29.
摘要翻译： 本发明涉及包含胰岛素分子和用于共价键合血液成分的反应性基团的胰岛素衍生物，其中优选地，胰岛素分子是人天然胰岛素分子，并且反应性基团与胰岛素分子的氨基酸在位置 选自Gly A1，Phe B1和Lys B29。
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公开(公告)号：US20050176643A1
公开(公告)日：2005-08-11
申请号：US11067556
申请日：2005-02-25
申请人： Dominique Bridon , Roger Leger , Xicai Huang , Karen Thibaudeau , Martin Robitaille , Peter Milner
发明人： Dominique Bridon , Roger Leger , Xicai Huang , Karen Thibaudeau , Martin Robitaille , Peter Milner
CPC分类号： C07K14/57545 , A61K38/00 , C07K19/00 , C07K2319/01
摘要： The present invention relates to a compound comprising a PYY peptide or a functional derivative thereof, which is coupled to a reactive group. Such a reactive group is capable of reacting on a blood component so as to form a stable covalent bond therewith. The present invention also relates to a conjugate comprising such a compound which is covalently bonded to a blood component. Moreover, the invention also relates to a method of enhancing, in a patient, the anti-obesity activity of a PYY peptide or functional derivative thereof.
摘要翻译： 本发明涉及包含与反应性基团偶联的PYY肽或其功能性衍生物的化合物。 这样的反应性基团能够对血液成分进行反应，与其形成稳定的共价键。 本发明还涉及包含共价键合到血液成分上的化合物的缀合物。 此外，本发明还涉及在患者中增强PYY肽或其功能性衍生物的抗肥胖活性的方法。
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公开(公告)号：US07144854B1
公开(公告)日：2006-12-05
申请号：US09657431
申请日：2000-09-07
申请人： Dominique P. Bridon , Michele Rasamoelisolo , Karen Thibaudeau , Xicai Huang , Richard Beliveau
发明人： Dominique P. Bridon , Michele Rasamoelisolo , Karen Thibaudeau , Xicai Huang , Richard Beliveau
IPC分类号： A61K38/00
CPC分类号： C12N9/6408
摘要： Modified anti-angiogenic peptides are disclosed. The modified peptides are capable of forming a peptidase stabilized anti-angiogenic peptide. The modified anti-angiogenic peptides, particularly modified kringle 5 peptides are capable of forming a conjugate with a blood protein. Conjugates are prepared from anti-angiogenic peptides, particularly kringle 5 peptides, by combining the peptide with a reactive functional group with a blood protein. The conjugates may be formed in vivo or ex vivo. The conjugates are administered to patients to provide an anti-angiogenic effect.
摘要翻译： 公开了修饰的抗血管生成肽。 修饰的肽能够形成肽酶稳定的抗血管生成肽。 修饰的抗血管生成肽，特别是修饰的三环5肽能够与血液蛋白形成缀合物。 通过将肽与反应性官能团与血液蛋白结合，由抗血管生成肽，特别是kringle 5肽制备缀合物。 缀合物可以在体内或离体形成。 向患者施用共轭物以提供抗血管生成作用。
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公开(公告)号：US07906482B2
公开(公告)日：2011-03-15
申请号：US11923222
申请日：2007-10-24
申请人： Dominique P. Bridon , Roger Leger , Xicai Huang , Karen Thibaudeau , Martin Robitaille , Peter G. Milner
发明人： Dominique P. Bridon , Roger Leger , Xicai Huang , Karen Thibaudeau , Martin Robitaille , Peter G. Milner
CPC分类号： C07K14/57545 , A61K38/00 , C07K19/00 , C07K2319/01
摘要： The present invention relates to a compound comprising a PYY peptide or a functional derivative thereof, which is coupled to a reactive group. Such a reactive group is capable of reacting on a blood component so as to form a stable covalent bond therewith. The present invention also relates to a conjugate comprising such a compound which is covalently bonded to a blood component. Moreover, the invention also relates to a method of enhancing, in a patient, the anti-obesity activity of a PYY peptide or functional derivative thereof.
摘要翻译： 本发明涉及包含与反应性基团偶联的PYY肽或其功能性衍生物的化合物。 这样的反应性基团能够对血液成分进行反应，与其形成稳定的共价键。 本发明还涉及包含共价键合到血液成分上的化合物的缀合物。 此外，本发明还涉及在患者中增强PYY肽或其功能性衍生物的抗肥胖活性的方法。
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公开(公告)号：US07601691B2
公开(公告)日：2009-10-13
申请号：US11067556
申请日：2005-02-25
申请人： Dominique P. Bridon , Roger Leger , Xicai Huang , Karen Thibaudeau , Martin Robitaille , Peter G. Milner
发明人： Dominique P. Bridon , Roger Leger , Xicai Huang , Karen Thibaudeau , Martin Robitaille , Peter G. Milner
CPC分类号： C07K14/57545 , A61K38/00 , C07K19/00 , C07K2319/01
摘要： The present invention relates to a compound comprising a PYY peptide or a functional derivative thereof, which is coupled to a reactive group. Such a reactive group is capable of reacting on a blood component so as to form a stable covalent bond therewith. The present invention also relates to a conjugate comprising such a compound which is covalently bonded to a blood component. Moreover, the invention also relates to a method of enhancing, in a patient, the anti-obesity activity of a PYY peptide or functional derivative thereof.
摘要翻译： 本发明涉及包含与反应性基团偶联的PYY肽或其功能性衍生物的化合物。 这样的反应性基团能够对血液成分进行反应，与其形成稳定的共价键。 本发明还涉及包含共价键合到血液成分上的化合物的缀合物。 此外，本发明还涉及在患者中增强PYY肽或其功能性衍生物的抗肥胖活性的方法。
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公开(公告)号：US07741286B2
公开(公告)日：2010-06-22
申请号：US11350703
申请日：2006-02-08
申请人： Dominique P. Bridon , Michele Rasamoelisolo , Karen Thibaudeau , Xicai Huang , Richard Beliveau
发明人： Dominique P. Bridon , Michele Rasamoelisolo , Karen Thibaudeau , Xicai Huang , Richard Beliveau
IPC分类号： A61K38/00
CPC分类号： C07K14/005 , A61K38/00 , C07K14/605 , C12N2740/16122
摘要： Modified anti-angiogenic peptides are disclosed. The modified peptides are capable of forming a peptidase stabilized anti-angiogenic peptide. The modified anti-angiogenic peptides, particularly modified kringle 5 peptides are capable of forming a conjugate with a blood protein. Conjugates are prepared from anti-angiogenic peptides, particularly kringle 5 peptides, by combining the peptide with a reactive functional group with a blood protein. The conjugates may be formed in vivo or ex vivo. The conjugates are administered to patients to provide an anti-angiogenic effect.
摘要翻译： 公开了修饰的抗血管生成肽。 修饰的肽能够形成肽酶稳定的抗血管生成肽。 修饰的抗血管生成肽，特别是修饰的三环5肽能够与血液蛋白形成缀合物。 通过将肽与反应性官能团与血液蛋白结合，由抗血管生成肽，特别是kringle 5肽制备缀合物。 缀合物可以在体内或离体形成。 向患者施用共轭物以提供抗血管生成作用。
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公开(公告)号：US20110071082A1
公开(公告)日：2011-03-24
申请号：US12759153
申请日：2010-04-13
申请人： Dominique P. Bridon , Michele Rasamoelisolo , Karen Thibaudeau , Xicai Huang , Richard Beliveau
发明人： Dominique P. Bridon , Michele Rasamoelisolo , Karen Thibaudeau , Xicai Huang , Richard Beliveau
CPC分类号： C07K14/005 , A61K38/00 , C07K14/605 , C12N2740/16122
摘要： Modified anti-angiogenic peptides are disclosed. The modified peptides are capable of forming a peptidase stabilized anti-angiogenic peptide. The modified anti-angiogenic peptides, particularly modified kringle 5 peptides are capable of forming a conjugate with a blood protein. Conjugates are prepared from anti-angiogenic peptides, particularly kringle 5 peptides, by combining the peptide with a reactive functional group with a blood protein. The conjugates may be formed in vivo or ex vivo. The conjugates are administered to patients to provide an anti-angiogenic effect.
摘要翻译： 公开了修饰的抗血管生成肽。 修饰的肽能够形成肽酶稳定的抗血管生成肽。 修饰的抗血管生成肽，特别是修饰的三环5肽能够与血液蛋白形成缀合物。 通过将肽与反应性官能团与血液蛋白结合，由抗血管生成肽，特别是kringle 5肽制备缀合物。 缀合物可以在体内或离体形成。 向患者施用共轭物以提供抗血管生成作用。
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