Calpain inhibitors for the treatment of neurodegenerative...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 5/08 (2006.01) A61K 31/16 (2006.01) A61K 31/195 (2006.01) A61K 31/27 (2006.01) A61K 31/33 (2006.01) A61K 38/05 (2006.01) A61K 38/06 (2006.01) C07C 237/10 (2006.01) C07C 237/20 (2006.01) C07C 243/28 (2006.01) C07C 271/20 (2006.01) C07C 323/60 (2006.01) C07K 5/06 (2006.01) C07K 5/078 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2224721

Novel amino acid analogs are provided having the formula (I): Z-A3-A2-A1-Q, wherein Z is H or a protecting group; A3 and A2 are independently an optionally protected valine, leucine, alanine, isoleucine, phenylalnine, tyrosine, glycine, 2-arylglycine having either <u>D</u> or <u>L</u> stereochemistry or a chemical bond; A1 is an optionally protected valine, leucine, isoleucine, alanine, phenylalnine, tyrosine, 2-phenyl-glycine, 2- phenethyl-glycine, 2-aryl-glycine; Q is H, CH2OCOL, CH2OL, CH2SL, CH2X, NHNHCOCH2OCOL, NHNHCOCH2OL, NHNHCOCH2SL, wherein L is an optionally substituted aryl or optionally substituted hereroaryl; and X is CI, Br or F, and a pharmaceutically acceptable salt thereof.

L'invention concerne de nouveaux analogues d'acides aminés, et un de leurs sels pharmacologiquement acceptable, de formule (I): Z-A¿3?-A¿2?-A¿1?-Q, dans laquelle Z représente H ou un groupe de protection; A¿3? et A¿2? représentent indépendemment valine, leucine, alanine, isoleucine, phénylalnine, tyrosine, glycine, 2-arylglycine, toutes éventuellement protégées, et présentant une stéréochimie <u>D</u> ou <u>L</u> ou une liaison chimique; A¿1? représente valine, leucine, isoleucine, alanine, phénylalnine, tyrosine, 2-phényl-glycine, 2-phénéthyl-glycine, 2-aryl-glycine, toutes éventuellement protégées; Q représente H, CH¿2?OCOL, CH¿2?OL, CH¿2?SL, CH¿2?X, NHNHCOCH¿2?OCOL, NHNHCOCH¿2?OL, NHNHCOCH¿2?SL, où L représente aryle ou hétéroaryle éventuellement substitués; et X représente CI, Br ou F.

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