发明名称 A MODIFIED CYCLOSPORINE WHICH CAN BE USED AS PRODRUGS. AND APPLICATION THEREOF
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 R1 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(NH2), -NHC=NR8(NH2), -NH2, -NHR8, -NR82, -N+R83, -OH, -OPO(OR8)2, -OPO(OH)(OR8), -OPO(OH)2, -OSO(OR8)2, -OSO(OH)(OR8), -OSO(OH)2, and the different salts produced therefrom, each of the substituents R8 independently representing an alkyl group which is linear or ramified having 1-6 carbon atoms; - substituents R2 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 R5 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 heterocyclic group, a heterocyclic alkyl group, an alkyl heterocyclic group or an alkyl group having 1-6 carbon atoms which is linear or branched.
申请公布号 UA75136(C2) 申请公布日期 2004.01.15
申请号 UA20031110436 申请日期 2002.04.22
申请人 DEBIOPHARM S.A. 发明人
分类号 A61K38/00;A61K38/13;A61P27/02;A61P31/18;A61P43/00;C07K7/64 主分类号 A61K38/00
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