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11.发明授权Protection of endogenous therapeutic peptides from peptidase activity through conjugation to blood components 失效通过与血液成分缀合，保护内源性治疗肽免受肽酶活性的影响公开(公告)号：US06887470B1
公开(公告)日：2005-05-03
申请号：US09657276
申请日：2000-09-07
CPC分类号： C07K19/00
摘要： A method for protecting a peptide from peptidase activity in vivo, the peptide being composed of between 2 and 50 amino acids and having a C-terminus and an N-terminus and a C-terminus amino acid and an N-terminus amino acid is described. In the first step of the method, the peptide is modified by attaching a reactive group to the C-terminus amino acid, to the N-terminus amino acid, or to an amino acid located between the N-terminus and the C-terminus, such that the modified peptide is capable of forming a covalent bond in vivo with a reactive functionality on a blood component. In the next step, a covalent bond is formed between the reactive group and a reactive functionality on a blood component to form a peptide-blood component conjugate, thereby protecting said peptide from peptidase activity. The final step of the method involves the analyzing of the stability of the peptide-blood component conjugate to assess the protection of the peptide from peptidase activity.
摘要翻译： 描述了一种在体内保护肽免受肽酶活性的方法，所述肽由2-50个氨基酸组成且具有C末端和N末端以及C末端氨基酸和N-末端氨基酸 。 在该方法的第一步中，通过将反应性基团连接到C末端氨基酸，N末端氨基酸或位于N末端和C末端之间的氨基酸来修饰肽， 使得修饰的肽能够在体内与血液成分上的反应性官能团形成共价键。 在下一步骤中，在反应性基团和血液成分上的反应性官能团之间形成共价键以形成肽 - 血液成分缀合物，从而保护所述肽免受肽酶活性。 该方法的最后步骤包括分析肽 - 血液成分缀合物的稳定性，以评估肽对肽酶活性的保护。
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12.发明授权Protection of endogenous therapeutic peptides from peptidase activity through conjugation to blood components 失效通过与血液成分缀合，保护内源性治疗肽免受肽酶活性的影响公开(公告)号：US07256253B2
公开(公告)日：2007-08-14
申请号：US11066697
申请日：2005-02-25
CPC分类号： C07K19/00
摘要： A secretin or secretin derivative protected against peptidase activity. The secretin or derivative comprises a peptidic sequence and a reactive group selected from the group consisting of succinimidyl and maleimido groups capable of reacting with an amino group, hydroxyl group or thiol group on a blood component to form a stable covalent bond. The reactive group is attached at a position along the peptidic sequence that provides, when conjugated to a blood component, a higher stability against peptidase degradation than the unconjugated secretin or derivative, and therefore an increased maintenance of the therapeutic activity compared to the unconjugated secretin or derivative. Such a compound is thus effective to provide a source of secretin having a high stability against peptidases. A method for synthesizing such a compound is also described.
摘要翻译： 保护蛋白酶活性的促胰液素或促胰液素衍生物。 分泌素或衍生物包含肽类序列和选自能够与血液成分上的氨基，羟基或硫醇基反应形成稳定的共价键的琥珀酰亚胺基和马来酰亚胺基的反应性基团。 反应性基团连接在沿着肽序列的位置，当与血液成分缀合时，其比非共轭分泌素或衍生物具有比肽酶降解更高的稳定性，因此与未缀合的促胰液素相比，治疗活性的维持得到增加 衍生物。 因此，这样的化合物有效地提供对肽酶具有高稳定性的促胰液素来源。 还描述了合成这种化合物的方法。
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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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14.发明授权Method of treatment of diabetes and/or obesity with reduced nausea side effect 失效减少恶心副作用的糖尿病和/或肥胖症的治疗方法公开(公告)号：US08039432B2
公开(公告)日：2011-10-18
申请号：US11595576
申请日：2006-11-09
CPC分类号： A61K38/26 , A61K47/643
摘要： The present invention provides methods of administering an insulinotropic peptide in an amount effective to treat a disorder or condition while reducing nausea side effect by administering to a subject in need thereof an insulinotropic peptide conjugated to albumin. The present invention also provides methods of selecting a subject for administration of a conjugated insulinotropic peptide. Exemplary disorders or conditions treatable with an insulinotropic peptide include obesity and type II diabetes.
摘要翻译： 本发明提供以有效治疗病症或病症的量施用促胰岛素肽的方法，同时通过向有需要的受试者施用与白蛋白缀合的促胰岛素肽来减轻恶心副作用。 本发明还提供了选择用于给予共轭促胰岛素肽的受试者的方法。 用促胰岛素肽治疗的示例性疾病或病症包括肥胖症和II型糖尿病。
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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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公开(公告)号：US20090099074A1
公开(公告)日：2009-04-16
申请号：US11965288
申请日：2007-12-27
CPC分类号： A61K38/22 , A61K47/643
摘要： The present disclosure relates to a conjugate comprising a PYY peptide or a functional derivative thereof which is coupled to a reactive group. Such a reactive group reacts with albumin so as to form a stable covalent bond therewith. The disclosure further provides methods of reducing water or food intake and reducing food intake between meals by administering such conjugates.
摘要翻译： 本公开涉及包含与反应性基团偶联的PYY肽或其功能性衍生物的缀合物。 这样的反应性基团与白蛋白反应，从而与其形成稳定的共价键。 本公开进一步提供了通过施用这种缀合物来减少水分或食物摄入并减少膳食之间的食物摄取的方法。
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公开(公告)号：US20090175821A1
公开(公告)日：2009-07-09
申请号：US11982033
申请日：2007-10-31
CPC分类号： C07K14/57563 , A61K38/38 , A61K47/62 , A61K47/643
摘要： A method for protecting a peptide from peptidase activity in vivo, the peptide being composed of between 2 and 50 amino acids and having a C-terminus and an N-terminus and a C-terminus amino acid and an N-terminus amino acid is described. In the first step of the method, the peptide is modified by attaching a reactive group to the C-terminus amino acid, to the N-terminus amino acid, or to an amino acid located between the N-terminus and the C-terminus, such that the modified peptide is capable of forming a covalent bond in vivo with a reactive functionality on a blood component. In the next step, a covalent bond is formed between the reactive group and a reactive functionality on a blood component to form a peptide-blood component conjugate, thereby protecting said peptide from peptidase activity. The final step of the method involves the analyzing of the stability of the peptide-blood component conjugate to assess the protection of the peptide from peptidase activity.
摘要翻译： 描述了一种在体内保护肽免受肽酶活性的方法，所述肽由2-50个氨基酸组成且具有C末端和N末端以及C末端氨基酸和N-末端氨基酸 。 在该方法的第一步中，通过将反应性基团连接到C末端氨基酸，N末端氨基酸或位于N末端和C末端之间的氨基酸来修饰肽， 使得修饰的肽能够在体内与血液成分上的反应性官能团形成共价键。 在下一步骤中，在反应性基团和血液成分上的反应性官能团之间形成共价键以形成肽 - 血液成分缀合物，从而保护所述肽免受肽酶活性。 该方法的最后步骤包括分析肽 - 血液成分缀合物的稳定性，以评估肽对肽酶活性的保护。
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18.发明授权Protection of endogenous therapeutic peptides from peptidase activity through conjugation to blood components 失效通过与血液成分缀合，保护内源性治疗肽免受肽酶活性的影响公开(公告)号：US06849714B1
公开(公告)日：2005-02-01
申请号：US09623548
申请日：2000-05-17
CPC分类号： C07K1/1077 , A61K38/00 , Y02P20/55
摘要： A method of synthesizing a modified therapeutic peptide capable of forming a peptidase-stabilized therapeutic peptide conjugate, the peptide having between 3 and 50 amino acids, is k. In a first step of the method, a therapeutic peptide having a carboxy terminal amino acid and amino terminal amino acid is synthesized. In a second step, pairs of cysteine residues present in the therapeutic peptide are sequentially and selectively oxidized to form disulfide bridges in the therapeutic peptide. In a third step, a protecting group is attached to remaining cysteine residues that do not form disulfide bridges in the therapeutic peptide. Finally, the peptide is coupled to a reactive group capable of reacting with amino groups, hydroxyl groups or thiol groups on a blood component to form a covalent bond therewith.
摘要翻译： 描述了能够形成肽酶稳定的治疗性肽缀合物的修饰的治疗肽的方法，所述肽具有3至50个氨基酸。 在该方法的第一步中，合成具有羧基末端氨基酸和氨基末端氨基酸的治疗肽。 在第二步中，存在于治疗肽中的成对的半胱氨酸残基被顺序地和选择性氧化，以在治疗肽中形成二硫键。 在第三步中，将保护基连接到在治疗肽中不形成二硫键的剩余半胱氨酸残基。 最后，肽与能够与血液成分上的氨基，羟基或硫醇基反应以形成与其共价键的反应性基团偶联。
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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：US07982018B2
公开(公告)日：2011-07-19
申请号：US11873291
申请日：2007-10-16
IPC分类号： A61K38/35 , A61K38/38 , C07K14/695 , C07K14/76 , C07K14/765
CPC分类号： C07K14/57509 , A61K38/00 , A61K47/64 , A61K47/643 , A61K47/644 , A61K47/6889
摘要： The present invention relates to compounds comprising modified corticotrophin releasing factor peptide and specifically urocortin and urocortin-related peptides, modified derivatives thereof, and conjugates of such modified peptides and derivatives to serum components, preferably serum proteins or peptides. The compounds and conjugates of the invention comprise a reactive group, which is covalently attached to a modified peptide or derivative, optionally through a linking group. The present invention also provides methods for the covalent attachment of a modified peptide or derivative to a serum protein or peptide to form a conjugate of the invention. The conjugates of the invention preferably 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 preferably 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促肾上腺皮质激素释放因子肽，特别是尿皮质素和尿皮质素相关肽，其修饰的衍生物，以及这些修饰肽和衍生物与血清成分，优选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，其任选地通过连接基团共价连接到修饰的肽或衍生物上。 本发明还提供了将修饰的肽或衍生物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，本发明的缀合物优选表现出更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优选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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