BLENCH Toby Jonathan (IT),БЛЕНЧ Тоби Джонатан (IT),EDWARDS Christine (IT),ЭДВАРДС Кристин (IT),HEALD Robert Andrew (IT),ХИЛД Роберт Эндрю (IT),KULAGOWSKI Janusz Josef (IT),КУЛАГОВСКИЙ Януш Джозеф (IT),BLENCH Toby Jonathan,БЛЕНЧ Тоби Джонатан,EDWARDS Christine,ЭДВАРДС Кристин,HEALD Robert Andrew,ХИЛД Роберт Эндрю,KULAGOWSKI Janusz Josef,КУЛАГОВСКИЙ Януш Джозеф,SUTTON Jonathan Mark,САТТОН Джонатан Ма
申请号：
RU2014109451
公开号：
RU0002622643C2
申请日:
2012.09.12
申请国别(地区):
RU
年份:
2017
代理人:
摘要：
FIELD: pharmacology.SUBSTANCE: invention compounds have the properties of human neutrophil elastase (HNE) inhibitors. In formula IA 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 i
