Pyridine compounds, process for the preparation thereof and...

C - Chemistry – Metallurgy – 07 – D

Patent

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167/210, 167/223

C07D 401/12 (2006.01) A61K 31/55 (2006.01) C07D 213/56 (2006.01) C07D 213/57 (2006.01) C07D 213/61 (2006.01) C07D 213/64 (2006.01) C07D 213/643 (2006.01) C07D 213/65 (2006.01) C07D 213/70 (2006.01) C07D 213/72 (2006.01) C07D 213/80 (2006.01) C07D 213/89 (2006.01) C07D 401/14 (2006.01) C07D 491/056 (2006.01)

Patent

CA 1262726

- 1 - Abstract The invention relates to compounds of the formula: Image wherein X is alkylene or -(CR6-CR7)r- wherein R6 is H, alkyl or phenyl, R7 is H, alkyl, cyano or phenyl, and r is 1 or 2; A is alkylene or alkylene interrupted by at least one double bond; R1 is H, halogen, alkyl, alkoxy, alkylthio, cyclo- alkyloxy, cycloalkylthio, alkoxycarbonyl, carboxy, phenyl, phenoxy, phenylthio, 3-pyridyloxy or 3-pyridylthio; R2 is H, hydroxy, alkanoyloxy or alkoxycarbonyloxy, or adjacent R1 and R2 may combine to form tetramethylene or -CH2OCR8R9O- (R8 and R9 are alkyl); R3 is H, alkyl or hydroxyalkyl; R4 is H or alkyl; R5 is phenyl, heteroaryl or -(CH2)m-CHR10R11 (R10 is H or phenyl, R11 is phenyl or pyridyl and m is 0 to 2); p is 0 or 1; and q is 2 or 3; the phenyl group or moiety being optionally substituted, and salts thereof. The invention also provides processes for the preparation of the compounds, and pharmaceutical compositions contain- ing the same. The compounds and salts thereof show good antiallergic activity mainly because of their 5-lipoxy- genase inhibiting activity, antihistamine activity and/or inhibitory activity against chemical mediator release. The compounds are accordingly useful for the treatment of allergic diseases.

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