发明名称 Malonic acid based matrix metalloproteinase inhibitors
摘要 There is described the use of a compound represented by general formulae (I), (II) or (III), for the inhibition of matrix metalloproteinases (MMP), wherein X1 is oxygen or sulfur, R1 is OH, SH, CH2OH, CH2SH or NHOH, R2 is a residue of 2 to 10 hydrocarbon backbone atoms, which binds to the amino acid 161 of HNC, said residue being saturated or unsaturated, linear or branched, and contains preferably homocyclic or heterocyclic structures, X2 is oxygen or sulfur and binds as hydrogen acceptor on amino acid 160 of HNC, Y is a residue which binds to the S1' pocket of HNC and consists of at least 4 backbone atoms Z1-Z2-Z3-Z4-R3, and R3 is n-propyl, isopropyl, isobutyl or a residue with at least 4 backbone atoms, which is not larger than a tricyclic ring system. These compounds bind to MMPs in a manner different from the mode of binding of the inhibitors of the state of the art.
申请公布号 AU4303896(A) 申请公布日期 1996.06.26
申请号 AU19960043038 申请日期 1995.12.08
申请人 BOEHRINGER MANNHEIM GMBH 发明人 LUIS MORODER;WOLFRAM BODE;FRANK GRAMS;ROBERT HUBER
分类号 C07D307/52;A61K31/16;A61K31/165;A61K31/195;A61K31/34;A61K31/341;A61K31/495;A61K31/66;A61K38/00;A61P1/02;A61P1/04;A61P19/10;A61P29/00;A61P43/00;C07C233/54;C07C259/06;C07F9/30;C07F9/38;C07K5/06;C07K5/08;C07K5/097;C12N9/64 主分类号 C07D307/52
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