Compound 1 - cyano - 3-pyrrolidinyl - benzenesulfonamide Pharmaceutical composition containing same and their use for preparing a Medicament used to treat chronic obstructive pulmonary disease (COPD)

摘要

Compound of 1-cyano-3-pyrrolidinyl-benzenesulfonamide which are cathepsin C inhibitors of formula (1) or (2) and a salt thereof in which n is 1--5, each R1 is independently halo; OR2, C1-10 alkyl unsubstituted or substituted with halo or an unsubstituted or substituted heteroaromatic ring containing 1-3 heteroatoms selected from the group consisting of N, O or S; CN; C (O) NR3R4, NO2, NHC (O) NR5R6, NR7R8, a heteroaromatic ring containing 1-3 heteroatoms selected from the group consisting of N, O or S; aryl, unsubstituted or substituted with halo or C1-6 alkyl, C3-6 cycloalkyl, C4-6 cycloalkenyl, C1-10 alkenyl, C1-10 alkynyl or C (O) OR2; R2 is H, C1-6 alkyl,C1-6 haloalkyl, C (O) R9; R3 is H; C1-6 alkyl; C3-6 cycloalkyl or C3-6 heterocycloalkyl containing N, O or S and in which when the ring heteroatom is N is optionally substituted with CN; R4 is H, or C1-6 alkyl; R5 and R6 are independently H; C1-6 alkyl, aryl unsubstituted or substituted with halo, C1-4 alkoxy, C1-4 alkyl, or OR2; C1-10 alkyl unsubstituted or substituted with halo or C1-4 alkoxy, C3-6 cycloalkyl, C3-6 cycloalkylalkyl, C1-10 alkenyl, C1-10 alkynyl; C3-6 heterocycloalkyl, C3-6 heterocycloalkyl-C1-6 alkyl, C1-6 heteroarylalkyl or heteroaryl in which the heteroaryl ring is not substituted or is substituted by halo,1. C1-6 tar or C1-6 tar is replaced by halogenation; or arilalquilo C1-6, where arilo is not replaced by halogenation, or 2 or C (o);R7 and R8 are independently H; C1-10 alkyl, C1-6 arylalkyl in which the aryl group is unsubstituted or substituted by R9, halo, or C1-6 alkyl; C1-10 alkyl substituted with C3-6 cycloalkyl, one or more OH groups, halo; C1-6 heteroarylalkyl, or heteroaryl; or R9 is OH, C1-6 alkyloxy or NR2'R3 ',Where r2'o R3 is an independent h or C1-6. A pharmacist who understands this It is used to produce effective drugs (COPD) for the treatment of COPD.