초록 ▼

The compounds of the present invention comprise substituted phenolic thioethers represented by the formula: [Figure] (I) wherein: R1 and R2 are the same or different and independently represent tert-alkyl or phenyl; A represents methylene or methylene substituted by alkyl, dialkyl or hydroxy, provid

The compounds of the present invention comprise substituted phenolic thioethers represented by the formula: [Figure] (I) wherein: R1 and R2 are the same or different and independently represent tert-alkyl or phenyl; A represents methylene or methylene substituted by alkyl, dialkyl or hydroxy, provided that when A includes hydroxymethylene, the hydroxymethylene group is not adjacent to a heteroatom; B represents sulfur, sulfoxide, sulfone, oxygen, －NH－or nitrogen substituted by alkyl, phenyl, benzyl, substituted phenyl or substituted benzyl; C represents methylene or methylene substituted by alkyl; R3 represents CO2H, CO2-alkyl or a tetrazole group; m is 0 or 1, n is 2, 3 or 4 and p is 1, 2 or 3; amd the pharmaceutically acceptable salts thereof. The compounds of the present invention are specific inhibitors of 5-lipoxygenase and, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.

대표청구항 ▼

A compound of the formula: [Figure] or a pharmaceutically acceptable salt thereof wherein R1 and R2 are the same or different and independently represent tert-alkyl or phenyl; A represents methylene or methylene substituted by alkyl, dialkyl or hydroxy, provided that when A includes hydroxymethylene

A compound of the formula: [Figure] or a pharmaceutically acceptable salt thereof wherein R1 and R2 are the same or different and independently represent tert-alkyl or phenyl; A represents methylene or methylene substituted by alkyl, dialkyl or hydroxy, provided that when A includes hydroxymethylene, the hydroxymethylene group is not adjacent to a heteroatom; B represents sulfur, sulfoxide, sulfone, oxygen, －NH－or nitrogen substituted by alkyl, phenyl, benzyl, phenyl substituted by one or two substituents which may be the same or different and are independently selected from the group consisting of halogen, C1-C6 alkyl, hydroxy, C1-C6-alkoxy, acetoxy, carboxylic acid and C1-C6 alkyl esters thereof, nitro or phenyl or benzyl substituted by one or two substituents which may be the same or different and are independently selected from the group consisting of halogen, C1-C6 alkyl, hydroxy, C1-C6 alkoxy, acetoxy, carboxylic acid and C1-C6 alkyl esters thereof, nitro or phenyl; C represents methylene or methylene substituted by alkyl; R3 represents CO2H, CO2-alkyl, or a tetrazole group; m is 0 or 1, n is 2, 3, or 4 and p is 1, 2, or 3. A pharmaceutical composition for the treatment of inflammation and allergy conditions comprising a therapeutically effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier.