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COMPOSÉ PEPTIDE CYCLIQUE OU SEL PHARMACEUTIQUEMENT ADMIS DE CE COMPOSÉ, ET PROCÉDÉ DE PRODUCTION CORRESPONDANT
专利权人:
KWANSEI GAKUIN EDUCATIONAL FOUNDATION
发明人:
HIRAI, YOHEI,OKUGAWA, YOJI
申请号:
EP11803647
公开号:
EP2592088A4
申请日:
2011.07.06
申请国别(地区):
EP
年份:
2014
代理人:
摘要:
Provided are a cyclic peptide compound or a pharmacologically acceptable salt thereof capable of inhibiting parakeratosis of skin, and a method for producing the same. This method comprises subjecting a cyclic peptide compound of Formula (I): or a pharmacologically acceptable salt thereof, wherein Xaa 1 and Xaa 5 are each optionally substituted Ser, optionally substituted Thr, or optionally substituted Tyr; Xaa 2 is optionally substituted Ile, optionally substituted Val, or optionally substituted Leu; Xaa 3 and Xaa 4 are each optionally substituted Asn, optionally substituted Gln, optionally substituted Asp, or optionally substituted Glu; and R 1 is a group of Formula (II): €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ-CO-(CH 2 ) n -NH-€ƒ€ƒ€ƒ€ƒ€ƒ(II) or Formula (III): €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ-NR-(CH 2 ) n -CO-€ƒ€ƒ€ƒ€ƒ€ƒ(III) wherein n is the same as defined above, and in Formula (I), the linkage between Cys and Cys is a peptide bond or a disulfide bond, and the other linkages are peptide bonds, to cyclization with a compound of Formula (IV): €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒCys-R 1 -Xaa 1 -Xaa 2 -Xaa 3 -Xaa 4 -Xaa 5 -Cys€ƒ€ƒ€ƒ€ƒ€ƒ(IV) wherein, Xaa 1 , Xaa 2 , Xaa 3 , Xaa 4 , Xaa 5 , and R 1 are the same as defined above.
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中国工程科技知识中心
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