公开(公告)号：EP2925786A1

公开(公告)日：2015-10-07

申请号：EP12889309.6

申请日：2012-11-29

申请人： Mediplex Corp. ,  SNU R&DB Foundation ,  ST Pharm Co. Ltd.

发明人： BYUN, Young Ro ,  AHMED, Al-Hilal Taslim ,  JEON, Ok Cheol ,  MOON, Hyun Tae ,  YUN, Yisuk ,  KIM, Kyungjin

IPC分类号： C07K17/02 ,  C07K14/575 ,  C08B37/00 ,  A61K47/06

CPC分类号： A61K47/48123 ,  A61K9/0053 ,  A61K31/727 ,  A61K38/16 ,  A61K38/26 ,  A61K47/542 ,  A61K47/554 ,  A61K49/0423 ,  B82Y5/00 ,  C07K14/605 ,  C07K14/62

摘要： The present invention relates to a method for preparing an end site-specific macromolecule-bile acid oligomer conjugate, comprising conjugating a bile acid oligomer which is prepared by oligomerization of two or more bile acid monomers to the terminal site of a macromolecule; a method for body absorption of an end site-specific macromolecule-bile acid oligomer conjugate, comprising administering the macromolecule-bile acid oligomer conjugate prepared by the above method to a subject orally; an end site-specific macromolecule-bile acid oligomer conjugate wherein the bile acid oligomer is conjugated to the terminal site of macromolecule; a composition comprising the conjugate; an oral formulation for macromolecule comprising the conjugate, a solubilizer, an excipient, a disintegrant, a binder, and a lubricant; a pharmaceutical composition comprising a heparin-bile acid oligomer conjugate wherein the bile acid oligomer is conjugated to the terminal site of heparin; and a method for treating thrombosis using said composition.

摘要翻译： 本发明涉及一种制备末端位点特异性大分子 - 胆汁酸低聚物缀合物的方法，包括将通过将两种或多种胆汁酸单体低聚制备的胆汁酸低聚物与大分子的末端部位缀合; 一种终点特异性大分子胆汁酸低聚物缀合物的身体吸收方法，其特征在于，将通过上述方法制备的高分子 - 胆汁酸低聚物缀合物口服给予对象; 末端位点特异性大分子 - 胆汁酸低聚物缀合物，其中胆汁酸低聚物与大分子的末端位点共轭; 包含该缀合物的组合物; 包含缀合物，增溶剂，赋形剂，崩解剂，粘合剂和润滑剂的用于大分子的口服制剂; 包含肝素 - 胆汁酸低聚物缀合物的药物组合物，其中所述胆汁酸低聚物与肝素的末端位点缀合; 以及使用所述组合物治疗血栓形成的方法。

公开(公告)号：EP2925786B1

公开(公告)日：2018-10-03

申请号：EP12889309.6

申请日：2012-11-29

申请人： ST Pharm Co., Ltd.

发明人： BYUN, Young Ro ,  AHMED, Al-Hilal Taslim ,  JEON, Ok Cheol ,  MOON, Hyun Tae ,  YUN, Yisuk ,  KIM, Kyungjin

IPC分类号： A61K47/54 ,  A61K9/00 ,  A61K38/16 ,  A61K38/26 ,  A61K49/04 ,  A61K31/727 ,  B82Y5/00 ,  C07K14/605 ,  C07K14/62

CPC分类号： A61K31/727 ,  A61K9/0053 ,  A61K38/16 ,  A61K38/26 ,  A61K47/542 ,  A61K47/554 ,  A61K49/0423 ,  B82Y5/00 ,  C07K14/605 ,  C07K14/62

摘要： The present invention relates to a method for preparing an end site-specific macromolecule-bile acid oligomer conjugate, comprising conjugating a bile acid oligomer which is prepared by oligomerization of two or more bile acid monomers to the terminal site of a macromolecule; a method for body absorption of an end site-specific macromolecule-bile acid oligomer conjugate, comprising administering the macromolecule-bile acid oligomer conjugate prepared by the above method to a subject orally; an end site-specific macromolecule-bile acid oligomer conjugate wherein the bile acid oligomer is conjugated to the terminal site of macromolecule; a composition comprising the conjugate; an oral formulation for macromolecule comprising the conjugate, a solubilizer, an excipient, a disintegrant, a binder, and a lubricant; a pharmaceutical composition comprising a heparin-bile acid oligomer conjugate wherein the bile acid oligomer is conjugated to the terminal site of heparin; and a method for treating thrombosis using said composition.