Imidazolona and pyrazolone derivatives as inhibitors of Human neutrophils Elastase (HNE)

摘要

The derivatives of pidan and pyrazolum, which have the property of inhibiting the neutral elasticity of human beings, are used for treatment. 1. Requirement 1: a compound (1) with formula characteristics,or a pharmaceutically acceptable salt thereof, where X is -C or -N; Y is C or N, where X and Y are not simultaneously C or N; R¹ is selected from the group consisting of -C₁₋₆ linear or branched alkyl, -C₃₋₆ cycloalkyl, -C₃₋₆ heterocycloalkyl and aryl-C₁₋₆ alkylene-,a. In any of them, c83231;A select (2) from the formula group residues,where Q is -CH or N; R² is selected from the group consisting of -C₁₋₆ alkyl, aryl-C₁₋₆ alkylene- and heteroaryl-C₁₋₆ alkylene-;R³ is -C₁₋₆ alkylene-N⁺RᵃRᵇRᶜ or heteroaryl-C₁₋₆ alkylene; Rᵃ is -C₁₋₆ alkyl; Rᵇ is -C₁₋₆ alkyl; Rᶜ is selected from the group consisting of -C₁₋₆ alkyl, aryl-C₁₋₆ alkylene and heteroaryl-C₁₋₆ alkylene- or Rᵃ and Rᵇ can form a heterocycloalkyl with the atom N⁺,wherein said heterocycloalkyl and heteroaryl may be optionally substituted with one or more C₁₋₆ alkyl; where the nitrogen atom in the heterocycloalkyl and heteroaryl groups may be quaternized; and where the dotted lines connecting X to the carbon atom at position 4 and Y, indicate that when X is N, then the double bond is in position 4-5, and when Y is N, then the double bond is found in position 3 - 4.