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    CYCLOSPORINE MODIFIEE UTILISABLE EN TANT QUE PRO-DROGUE ET SON UTILISATION
    2.
    发明公开
    CYCLOSPORINE MODIFIEE UTILISABLE EN TANT QUE PRO-DROGUE ET SON UTILISATION 无效
    修改药物PRE适用环孢菌素及其用途

    公开(公告)号：EP1379547A2

    公开(公告)日：2004-01-14

    申请号：EP02713992.2

    申请日：2002-04-22

    申请人： DEBIOPHARM S.A.

    发明人： WENGER, Roland ,  MUTTER, Manfred ,  HAMEL, Arnaud ,  HUBLER, Francis

    IPC分类号： C07K7/64 ,  A61K38/13 ,  A61K47/48

    CPC分类号： C07K7/645 ,  A61K38/00

    摘要： The invention relates to a pro-drug comprising a cyclic undecapeptide wherein the peptide chain thereof comprises at least one amino acid residue of general formula (1) wherein the carbon atom Ca is one of the links in said undecapeptide cycle; - substituents Y individually represent a hydrogen atom or form a bond together; - substitutents R?1 and R3¿ independently represent a hydrogen atom, an aralkyl group, an alkaryl group, a heteroalkyl group, a heterocyclic group, a heterocyclic alkyl group, an alkyl heterocyclic group or an alkyl group having 1-6 carbon atoms which is linear or branched, and which is optionally substituted by at least one of the groups chosen from among -COOH, -CONHR8, -NHC0=NH(NH¿2?), -NHC=NR?8(NH¿2), -NH2, -NHR8, -NR82, -N+R83, -OH, -OPO(OR8)2, -OPO(OH)(OR8), -OPO(OH)¿2?, -OSO(OR?8)¿2, -OSO(OH)(OR8), -OSO(OH)¿2?, and the different salts produced therefrom, each of the substituents R?8¿ independently representing an alkyl group which is linear or ramified having 1 - 6 carbon atoms; - substituents R?2 and R4¿ independently represent a hydrogen atom, an alkaryl group or an alkyl group having 1 - 6 carbon atoms which is linear or branched; - the substituents R?5 and R6¿ individually represent a hydrogen atom, an aralkyl group, an alkyl group having 1-6 carbon atoms which is linear or branched; and substituent R7 represents an alkaryl group, a heteroalkyl group, a heterocylic group,a heterocylic alkyl group, an alkyl heterocyclic group or an alkyl group having1 - 6 carbon atoms which is linear or branched.