发明名称 MODIFIED CYCLOSPORINE WHICH CAN BE USED AS A PRO-DRUG AND USE THEREOF
摘要 The invention relates to a pro-drug comprising a cyclic undecapeptide wherei n the peptide chain thereof comprises at least one amino acid residue of gener al 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 whic h 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, a nd 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 hydroge n 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 whic h 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 linea r or branched.
申请公布号 CA2444278(A1) 申请公布日期 2002.10.31
申请号 CA20022444278 申请日期 2002.04.22
申请人 DEBIOPHARM S.A. 发明人 WENGER, ROLAND;MUTTER, MANFRED;HUBLER, FRANCIS;HAMEL, ARNAUD
分类号 A61K38/00;A61K38/13;A61P27/02;A61P31/18;A61P43/00;C07K7/64;(IPC1-7):C07K7/64;A61K47/48 主分类号 A61K38/00
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