发明名称 METHOD FOR PRODUCING SMALL MOLECULE INHIBITOR FOR ROTAMASE ENZYME ACTIVITY
摘要 PROBLEM TO BE SOLVED: To provide a method for producing a compound as an inhibitor of an enzyme activity relating to a neurotrophic compound having an affinity to FKBP type immunophilin, i.e., an immunophilin protein, especially the inhibitor for a peptidyl-prolylisomerase or rotamase enzyme activity. SOLUTION: This method for producing the neurotrophic compound expressed by the formula below (wherein, R1 , Z are each a lipophilic group; X is O, S, or the like; and Y is O, NH, or the like), and a medicinal composition containing the same compound for the treatment of neuropathy, consist of (a) reacting L-proline methyl ester with methyloxalyl chloride, (b) forming an intermediate compound by a reaction of the obtained product with a carbon nucleophilic reagent, (C) reacting the intermediate compound with an alcohol, an amide and a blocked amino acid residue, (d) and further coupling the obtained product with a compound expressed by the formula: Y-Z [wherein, Y is OH or NHR2 (R2 is H or a 1-6C alkyl)].
申请公布号 JP2002371058(A) 申请公布日期 2002.12.26
申请号 JP20020113933 申请日期 2002.04.16
申请人 GUILFORD PHARMACEUT INC 发明人 HAMILTON GREGORY S;STEINER JOSEPH P
分类号 C12N9/99;A61K31/40;A61K31/401;A61K31/4025;A61K38/00;A61P21/00;A61P21/02;A61P25/00;A61P25/02;A61P25/16;A61P25/24;A61P25/28;A61P37/00;A61P43/00;C07B53/00;C07D207/16;C07D401/06;C07D405/06;C07D405/12;C07D407/04;C07D409/04;C07D409/12;C07D409/14;C07D417/04;C07D417/12;C07K5/078;(IPC1-7):C07D207/16 主分类号 C12N9/99
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