Tryptase-inhibitors

C - Chemistry – Metallurgy – 07 – C

Patent

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Details

C07C 271/20 (2006.01) A61K 31/192 (2006.01) A61K 31/194 (2006.01) A61P 11/00 (2006.01) C07D 213/30 (2006.01)

Patent

CA 2440482

Compounds of the formula I, wherein M, A1, A2, K1 and K2 have the meanings as indicated below are tryptase inhibitors. M is a central building block containing an acetylene containing linking group. A1 and A2 are carbonyl containing linking groups K1 is -B3-X1, -B3-Y1 or B3-Z1-B5-X1, K2 is -B4-X2, - B4-Y2 or -B4-Z2-B6-X2, B3 and B4 are identical or different and are a bond or 1-4C-alkylene, B5 and B6 are identical or different and are a bond or 1-2C- alkylene, X1 and X2 are identical or different and are amino, aminocarbonyl or amidino, Y1 and Y2 are imidazol -1-yl, Z1 and Z2 are identical or different and are 5,2-pyridinylene, 6-methyl-5,2-pyridinylene, 4,1-piperidinylene, 3,6- indazolylene, 3,6-indolylene, 1,3-phenylene, 1,4-phenylene, 1,3,-cyclohexalene or 1,4-cyclohexylene, the salts of these compounds, and the N-oxides of the nitrogen-containing heteroalryls, heteroarylenes and heterocycloalkylenes, and their salts, where all those compounds are excluded in which, owing to the meaning of the variables, there would be a direct linkage of two hereroatoms or two carbonyl groups.

L'invention concerne des composés de la formule I. Dans cette dernière, M, A1, A2, K1 et K2 ont des significations telles que décrites dans le descriptif et constituent de nouveaux inhibiteurs de la tryptase efficaces.

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