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    • 9. 发明公开
    • TRYPTASE-INHIBITORS
    • 类胰蛋白酶抑制剂
    • EP1370518A2
    • 2003-12-17
    • EP02724222.1
    • 2002-03-12
    • ALTANA Pharma AG
    • MARTIN, ThomasULRICH, Wolf-RüdigerBÄR, ThomasSTADLWIESER, JosefWOLLIN, Stefan-LutzZECH, KarlSOMMERHOFF, Christian, P.
    • C07C271/20A61K31/192A61K31/194A61P11/00C07D213/30
    • C07C271/20
    • 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.
    • 其中M,A1,A2,K1和K2具有如下所示含义的式I化合物是类胰蛋白酶抑制剂。 M是含有含乙炔连接基团的中央构件。 A1和A2是含羰基连接基团,K1是-B3-X1,-B3-Y1或B3-Z1-B5-X1,K2是-B4-X2,-B4-Y2或-B4-Z2-B6-X2,B3 和B 4是相同或不同的并且是键或1-4C-亚烷基,B 5和B 6相同或不同并且是键或1-2C-亚烷基,X 1和X 2相同或不同并且是氨基,氨基羰基或脒基, Y1和Y2是咪唑-1-基,Z1和Z2相同或不同,并且是5,2-亚吡啶基,6-甲基-5,2-亚吡啶基,4,1-亚哌啶基,3,6-吲唑基,3,6 - 亚苯基,1,3-亚苯基,1,4-亚苯基,1,3-环己烯或1,4-亚环己基,这些化合物的盐以及含氮杂芳基,亚杂芳基和杂环亚烷基的N-氧化物, 和它们的盐,其中排除了所有这些化合物,其中由于这些变量的含义,将存在两个下游或两个羰基的直接连接。