JOO, Jung Hoon,주정훈,LEE, Sang Mi,이상미,YOO, Sang Eun,유상은,LEE, Mi Ok,이미옥,LEE, Ki Ho,이기호,PARK, Byoung Chul,박병철,LEE, Bo-Mi,이보미,YOUM, Tae-Hyun,염태현,CHO, Cheong-Weon,조정원,KIM, Jae Jong,김재종,WOO, Jin Suk,우진석,LIM,
申请号：
KRKR2012/006210
公开号：
WO2013/022238A3
申请日:
2012.08.03
申请国别(地区):
WO
年份:
2013
代理人:
摘要：
The present invention relates to a technique for producing tricyclic compound derivatives of novel structure by attaching a sugar to a tricyclic compound structure and relates to a glycosylation derivative synthesised by means of the technique the immunosuppressant function being retained, and water-solubility being improved by a maximum of at least 10,000 times. Also, the present invention relates to a pharmaceutical composition for suppressing immune diseases including allergic conjunctivitis and xerophthalmia and comprises a tacrolimus glycosylation derivative as an active ingredient.La présente invention concerne une technique de fabrication de dérivés de composés trycliques de nouvelle structure par fixation dun sucre à une structure de composé tricyclique et porte sur un dérivé de glycosylation synthétisé au moyen de la technique, la fonction immunosuppressive étant conservée, et la solubilité dans leau étant améliorée dun maximum dau moins 10000 fois. La présente invention concerne également une composition pharmaceutique pour supprimer des maladies immunitaires comprenant la conjonctivite allergique et la xérophtalmie et comprend un dérivé de glycosylation de tacrolimus comme principe actif.본 발명은 트리사이클로 화합물 구조에 당을 부착하여 신규 구조의 트리사이클로 화합물 유도체들을 만드는 기술 및 그 기술에 의해 합성되는 당화 유도체에 관한 것으로서, 면역억제 기능을 보유하며, 최대 10,000배 이상 수용성이 향상되었다. 또한, 본 발명은 알러지성 결막염, 안구 건조증을 포함하는 면역질환 억제용 약학 조성물에 관한 것으로서, 타크롤리무스 당화 유도체를 유효 성분으로 포함한다.
