FIELD: pharmacology.
SUBSTANCE: invention compounds have the properties of human neutrophil elastase (HNE) inhibitors. In formula I
A represents CH; R1 is selected from hydrogen; a (C1-C6) alkyl; a (C1-C6)alkylNR7R8group; a (C1-C4)alkenyl; a (C1-C6)alkylphenyl, where the phenyl ring is possibly substituted by a (C1-C6)alkylNR15R16 group or a (C1-C6)alkylN+R15R16R17group; a -(CH2)nCONR5R6group; a -CH2-(CH2)nNR5SO2R6group; a -(CH2)t-(C6H4)-SO2(C1-C4)alkyl group; a -(CH2)rSO2(C1-C4)alkyl group, wherein such (C1-C4)alkyl is possibly substituted by a -N+R15R16R17group; a -SO2-phenyl group. Such phenyl ring is possibly substituted by a (C1-C6)alkylNR7R8group; and a -(CH2)n-W group, where W represents a 6-membered heteroaryl ring with one heteroatom N, which is possibly substituted by a group -SO2(C1-C4)alkyl; n means 1; t means zero, 1; r means 2, 3; R5 is selected from the group consisting of hydrogen, a (C1-C6)alkyl, a (C1-C6)alkylNR16R15group and a (C1-C6)alkylN+R17R15R16group; R6 represents hydrogen or a (C1-C6)alkyl; R7 is selected from the group consisting of a (C1-C6)alkyl, a carbonyl(C1-C6)alkyl group, a -SO2(C1-C4)alkyl group and a (C1-C6)alkylNR16R15group; R8 represents a (C1-C6 )alkyl; alternatively, R7 and R8 can form, together with the nitrogen atom to which they are attached, a (C5-C7)heterocycloalkyl ring system, which is possibly substituted by oxo; R16 represents a (C1-C6)alkyl; R15 represents a (C1-C6)alkyl; R17 represents a (C1-C6)alkyl; R2 represents hydrogen or -SO2R4, where R4 is selected from a (C1-C6)alkyl; R14 represents a cyano group or a -C(O)-XR3group; X is a divalent group selected from -O- and -NH-; R3 represents a group selected from hydrogen; a (C1-C6)alkyl; a group of formula -[Alk1]-Z, where Alk1 represents a (C1-C4)alkylene radical, and Z represents NR9R10, where R9 and R10 independently represent a (C1-C6)alkyl. The invention also relates to pharmaceutical compositions and to a method of treating a disease or a condition in which HNE is involved.
EFFECT: new formula compounds obtained, having the properties of human neutrophil elastase inhibitors.
16 cl, 1 tbl, 39 ex
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