| 摘要 |
(1) This invention provides benzene derivatives of the Formula I <IMG> I wherein: R1 is hydrogen, C1-C6 alkyl, C3-C8 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, chloro, C1-C3 alkyl, nitro, or -NRR; Z is -O-, -NR- , or <IMG>; p is 0, 1 or 2; each A is a bond or a straight or branched chain C1-C10 alkylidene, C5-C10 cyclic alkylidene, or C2-C4 alkenylidene group; Q is -?- or -CHOH-; Y is -?-, -CHOH, -O-, or a bond, or -A-Q-A-Y-, when taken together with two adjacent carbon atoms of the phenyl ring to which A is attached, is <IMG>, where E is a bond, -CH2-, -S-, or -O-; and R4 is -COR9, 5-tetrazolyl, 3-(1,2,5-thiadiazolyl), 2-thioxo-4-thiazolidinonyl, or -CN; where each R is hydrogen or C1-C3 alkyl; each R5 and R6 is independently hydrogen, C1-C3 alkyl, phenyl, or benzyl; each R7 and R8 is independently hydrogen, C1-C3 alkoxy, halo, amino, hydroxy, or C1-C3 alkyl; and R9 is hydroxy or C1-C4 alkoxy; provided that (a) all three A groups may not be a bond at the same time; and (b) when Y is a group other than a bond, the A group between Q and Y may not be a bond; 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.
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