Compound 1 - cyano - 3-pyrrolidinyl - N - substituted sulfonamide, their use for preparing a drug used to treat chronic obstructive pulmonary disease and Pharmaceutical composition containing same

摘要

Compound of 1-cyano-3-pyrrolidinyl-N-substituted-sulfonamide which is a cathepsin C inhibitor, of formula (1) or a salt thereof, in which Rx is C1-6 alkyl or aryl or aryl-C1- alkyl 6 wherein aryl is unsubstituted or substituted by halo, C1-6alkyl, halo-substituted-C1-6alkyl, C1-6alkoxy optionally substituted by halo, or S (O) and where y is 0-2, n is 1-5; each R1 is independently halo, OR2, C1-10 alkyl unsubstituted or substituted by halo, 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 by halo or C1-6alkyl, C3-6cycloalkyl,C4-6cycloalkenyl, C1-10alkenyl, C1-10alkynyl, or C (O) OR2, R2 is H, C1-6alkyl, halo-C1-6alkyl, C (O) R9; R3 is H, C1-6 alkyl, C3-6 cycloalkyl, or C3-6 heterocycloalkyl containing N, O, or S and wherein when the ring heteroatom is N is optionally substituted by CN; R4 is H, or C1-6 alkyl; R5 and R6 are independently H, C1-6alkyl, aryl unsubstituted or substituted by halo, C1-4alkoxy, C1-4alkyl, or OR2; C1-10 alkyl unsubstituted or substituted by halo or C1-4 alkoxy; C3-6 cycloalkyl, C3-6 cycloalkyl-alkyl, C1-10 alkenyl, C1-10 alkynyl, C3-6 heterocycloalkyl, C3-6 heterocycloalkyl-C1-6 alkyl,1. C1-6 type non-n-acrylonitrile, in this case, non-n-acrylonitrile is not replaced or replaced by halogen, C1-6 type tar or halogen substitute, and C1-6 type tar or aril-c1-6 type tar is not replaced or replaced by halogen, or2 or C (o);R7 and R8 are independent h, C1-10 tar, aril-c1-6 tar, in which arilo is not replaced or replaced by R9, halo or C1-6 tar, C1-10 tar is replaced by C3-6 cyclododecane, or consists of one or more groups Oh, halo, heterosexual C1-6 or heterosexual; or R9 is oh, c1-6-oxy or NR2. Where R2 or R3 is an independent h or C1-6. Use this compound to produce effective drugs for COPD. Including the pharmaceutical components of this compound