Metastin derivative and use thereof

Details Metastin derivative and use thereof Metastin derivative and use thereof

C - Chemistry, Metallurgy

07

K

C07K 14/47 (2006.01) A61K 38/00 (2006.01) A61P 1/18 (2006.01) A61P 3/04 (2006.01) A61P 3/06 (2006.01) A61P 3/10 (2006.01) A61P 7/02 (2006.01) A61P 9/10 (2006.01) A61P 13/00 (2006.01) A61P 15/00 (2006.01) A61P 15/06 (2006.01) A61P 15/08 (2006.01) A61P 25/28 (2006.01) A61P 35/00 (2006.01) A61P 35/04 (2006.01) A61P 43/00 (2006.01)

Patent

CA 2511858

A metastin derivative or salt thereof excelling in stability in blood and exhibiting cancerous metastasis inhibitory action or cancerous hyperplasia inhibitory action. The metastin derivative is represented by the formula: (I) wherein each of Z1, Z3, Z5 and Z7 is H or C1-C3 alkyl; each of Z2, Z4, Z6 and Z8 is H, O or S; R1 is H, carbamoyl, etc.; R2 is H, cyclic C1-C10 alkyl, etc.; R3 is C1-C8 alkyl having a basic group, etc.; R4 is C6-C12 aromatic hydrocarbon ring group, etc.; X is -NHCH(Q1)YQ2C(=Z9)- (wherein Q1 is C6-C12 aromatic hydrocarbon ring group, etc.; Q2 is CH2, etc.; Y is CONH, etc.; and Z9 is H, etc.); and P is arbitrary amino acid residues discontinuously bonded or continuous from the C-terminal side of 1st-48th amino acid sequence segment of specified amino acid sequence, etc.

L'invention concerne un dérivé de la métastine ou son sel, qui présente une excellente stabilité dans le sang et une action inhibitrice de la métastase cancéreuse ou une action inhibitrice de l'hyperplasie cancéreuse. Le dérivé de la métastine est représenté par la formule (I), dans laquelle chacun des éléments Z?1¿, Z?3¿, Z?5¿ et Z?7¿ est H ou alkyle C¿1?-C¿3?; chacun des éléments Z?2¿, Z?4¿, Z?6¿ et Z?8¿ est H, O ou S; R?1¿ est H, carbamoyle, etc.; R?2¿ est H, alkyle C¿1?-C¿10? cyclique, etc.; R?3¿ est alkyle C¿1?-C¿8? pré

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