EXENDIN-4 ANALOGUE PEGYLATED WITH POLYETHYLENE GLYCOL OR DERIVATIVE THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING DIABETES, CONTAINING SAME AS ACTIVE INGREDIENT
LEE, Sung Kwon,이성권,KIM, Won Bae,김원배,LEE, Seulki,이슬기,KIM, Tae Hyung,김태형
申请号：
KRKR2012/005137
公开号：
WO2013/002580A3
申请日:
2012.06.28
申请国别(地区):
WO
年份:
2013
代理人:
摘要：
The present invention relates to an exendin-4 analogue PEGylated with polyethylene glycol or a derivative thereof, a preparation method thereof, and a pharmaceutical composition for preventing or treating diabetes, containing the same as an active ingredient. According to the present invention, it is possible to increase the yield of a PEGylated exendin-4 analogue and to enhance the therapeutic effect of a drug through the selective PEGylation of cysteine using exendin-4 in which said cysteine (Cys) is introduced at position 40 of the C terminal, and thus it is possible to usefully employ the same in a composition for preventing or treating diseases caused by the hypersecretion of insulin.La présente invention concerne un analogue dexendine-4 pégylé par du polyéthylène glycol ou un dérivé de celui-ci, son procédé de préparation et une composition pharmaceutique pour prévenir ou traiter le diabète, le contenant en tant que principe actif. Selon la présente invention, il est possible daugmenter le rendement dun analogue dexendine-4 pégylé et daméliorer leffet thérapeutique dun médicament par la PEGylation sélective de cystéine à laide dexendine-4, ladite cystéine (Cys) étant introduite en position 40 de lextrémité terminale C, et il est ainsi possible dutiliser de façon utile celui-ci dans une composition pour prévenir ou traiter des maladies causées par lhypersécrétion dinsuline.본 발명은 폴리에틸렌글라이콜 또는 이의 유도체로 페길화된 엑센딘-4 유사체, 이의 제조방법 및 이를 유효성분으로 함유하는 당뇨병 예방 또는 치료용 약학적 조성물에 관한 것이다. 본 발명에 의하면 C-말단 40번 위치에 시스테인(Cys)이 도입된 엑센딘-4를 사용하여 상기 시스테인 선택적 페길화(PEGylation)을 통하여 페길화(PEGylation)된 엑센딘-4 유사체의 수율을 증가시킬 수 있고, 약물의 치료효과를 증가시킬 수 있어, 인슐린 과다분비에 의해 유발되는 질환의 예방 또는 치료용 조성물로 유용하게 사용할 수 있다.
