公开(公告)号：US3869437A

公开(公告)日：1975-03-04

申请号：US39021673

申请日：1973-08-21

Applicant: NAT RES DEV

Inventor： LINDSAY DAVID GORDON ,  SHALL SYDNEY

IPC: A61K38/00 ,  C07K14/62 ,  C07C103/52 ,  A61K17/02 ,  C07G7/00

CPC classification number: C07K14/62 ,  A61K38/00

Abstract: A physiologically acceptable insulin derivative has the terminal amino group of the B chain (B1, phenylalanine) protected by an acyl group or other blocking group containing up to seven carbon atoms and the amino group of the A chain (A1, glycine) is either free or protected by means of an acyl or other blocking group containing no more than four carbon atoms and preferably no more than three atoms other than hydrogen. Pharmaceutical preparations may be prepared containing an effective amount of such an insulin derivative together with a physiologically acceptable diluent. An insulin derivative of reduced antigenicity is obtainable from porcine or bovine insulin by reacting the insulin with an acylating agent or other blocking reagent to acylate or otherwise block the amino group of the B1 amino acid and optionally block the A1 and/or B29 amino acid, followed by purification of the derivative by various methods.

Abstract translation: 生理上可接受的胰岛素衍生物具有由酰基或其它含有至多7个碳原子的封闭基保护的B链（B1，苯丙氨酸）的末端氨基，A链（A1，甘氨酸）的氨基是游离的 或通过含有不超过四个碳原子，优选不超过三个除了氢原子的酰基或其它封闭基团来保护。 可以制备含有有效量的这种胰岛素衍生物和生理上可接受的稀释剂的药物制剂。 降低抗原性的胰岛素衍生物可通过使胰岛素与酰化剂或其它阻断试剂反应来从猪或牛胰岛素获得，以酰化或以其它方式阻断B1氨基酸的氨基并任选地阻断A1和/或B29氨基酸， 然后用各种方法纯化衍生物。