Malonic acid based matrix metalloproteinase inhibitors

Details Malonic acid based matrix metalloproteinase inhibitors Malonic acid based matrix metalloproteinase inhibitors

C - Chemistry, Metallurgy

07

D

C07D 307/54 (2006.01) A61K 31/16 (2006.01) A61K 31/165 (2006.01) A61K 31/34 (2006.01) A61K 31/395 (2006.01) A61K 31/66 (2006.01) A61K 38/05 (2006.01) C07C 233/54 (2006.01) C07C 259/06 (2006.01) C07C 327/12 (2006.01) C07F 9/38 (2006.01) C07F 9/655 (2006.01) C07K 5/06 (2006.01) C07K 5/062 (2006.01) C07K 5/097 (2006.01) C12N 9/64 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2206665

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.

L'invention concerne l'utilisation d'un composant représenté par les formules générales (I), (II), ou (III), servant à inhiber les métalloprotéinases matricielles (MMP). Dans ces formules, X¿1? représente oxygène ou soufre; R¿1? représente OH, SH, CH¿2?OH, CH¿2?SH ou NHOH; R¿2? représente un radical comportant 2 à 10 atomes du squelette hydrocarboné, qui se fixe à l'acide aminé 161 de HNC, ce radical étant saturé ou non, linéaire ou ramifié, et renfermant de préférence des structures homocycliques ou hétérocycliques; X¿2? représente oxygène ou soufre et se fixe sous forme d'accepteur d'hydrogène sur l'acide aminé 160 de HNC; Y représente un radical qui se fixe au sous-site S1' de HNC et comporte une structure Z¿1?-Z¿2?-Z¿3?-Z¿4?-R¿3? à au moins 4 atomes du squelette; et R¿3? représente n-propyle, isopropyle, isobutyle ou un radical comportant au moins 4 atomes du squelette, de taille inférieure à un système tricyclique. Ces composés se fixent aux MMP selon un mode différent du mode de fixation des inhibiteurs de la technique antérieure.

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