Leukotriene antagonists

C - Chemistry – Metallurgy – 07 – D

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167/233, 167/246

C07D 257/04 (2006.01) A61K 31/41 (2006.01)

Patent

CA 1329613

Abstract This invention provides benzene derivatives of the Formula I Image I wherein: R1 is hydrogen, C1-C6 alkyl, C3-C8 cycloalkyl, phenyl-substituted-(C1-C3 alkyl), phenyl, or phenyl substituted with a halo, C1-C4 alkyl, or C1-C4 alkoxy functionality; R2 is C1-C10 alkyl, C2-C6 alkenyl, benzyl, or 2-phenylethyl; R3 is hydrogen, bromo, or chloro; Z is -O-, -NR-, or Image ; A is -O-, Image , -NR-, Image , -CHOR- or straight or branched chain C1-C4 alkylidene; each p is independently 0, 1 or 2; Q is a bond or straight or branched chain C1-C4 alkylidene; R4 is COR9, 5-tetrazolyl, 3-(1,2,5-thiadiazolyl), or -CN; where each R is independently hydrogen, C1-C3 alkyl or C1-C4 alkanoyl; each R5 and R6 is independently hydrogen, C1-C3 alkyl, phenyl, or benzyl; R9 is hydroxy or C1-C4 alkoxy; and pharmaceutically acceptable salts thereof. These compounds are selective leukotriene antagonists that are useful in the treatment of conditions characterized by an excessive release of leukotrienes, as for example, asthma.

563376

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