Pyrrolidine derivatives as inhibitors of the protease that activates the respiratory tract

摘要

Pyrrolidine derivatives relates to compounds of formula (1) where J is a Ring monociclico 5 to 12 members, aryl, heteroaryl, among others; r1 is - L - NR2 (CR2) - L - (CR2), NRC (NR) - NR2 (CR2), - L - C (= NR - NR2) or a Heterocyclic Ring of 5 to 7 members, where r is H, alkyl (C1 - C6), alquenilo (C2 - C6 Alquinilo) or (C2 - C6); R2 is alkyl (C1 - C6), alquenilo (C2 - C6), alquinilo (C2 - C6)Among others; or (CR2) is W - K - K - S (CR2), S (k) (CR2) or oC (OR) (CR2), where K And l are each of 0 to 6; R3 is nr7r8 or R6, R7 and R8 are each h, alkyl (C1 - C6), alquenilo (C2 - C6), among others; R4 and R5 are each h, alkyl, alkoxy (C1 - C6) (C1 - C6), among others, R10 is Halo, alkyl, alkoxy (C1 - C6) R6, among others; and x are each a Ring carbociclico 5 to 7 members,A Heterocyclic ring, aryl or heteroaryl; R is 0 OR 1; M and N are each 1 to 6; p is 0 to 3. Preferred compounds are compounds of formula (ii), (iii), among others. It also relates to a Pharmaceutical composition.These compounds are inhibitors of proteases that Activate the respiratory tract (CAP) to be useful in the treatment of cystic fibrosis, Lung Cancer, chronic bronchitis, asthma