Leukotriene antagonists

Details Leukotriene antagonists Leukotriene antagonists

C - Chemistry, Metallurgy

07

C

167/179, 260/312

C07C 59/40 (2006.01) C07C 43/178 (2006.01) C07C 43/225 (2006.01) C07C 57/58 (2006.01) C07C 59/66 (2006.01) C07C 59/68 (2006.01) C07D 257/04 (2006.01) C07D 257/06 (2006.01) C07D 295/088 (2006.01)

Patent

CA 1242195

Abstract This invention provides novel compounds which are leukotriene antagonists, certain novel intermedi- ates to the compounds, formulations of the compounds, and a method of using the compounds for the treatment of conditions characterized by an excessive release of leukotrienes. The novel compounds are of the general formula Image I or a pharmaceutically acceptable salt thereof, wherein: R1 is Image or halo; R2 is halo or hydroxy; R3 is C1-C12 alkyl, hydroxy-substituted C1-C12 alkyl, or C2-C6 alkenyl; Y is -O-, Image or -CR6R7-; Z is -O-, Image or -CR8R9, or when taken together, -Y-Z is -CH=C. n is 1-10; D is CN, SCN or QR4; Image or a bond; R4 is -COR10, hydroxy, -NR11R12, -SC(=NH)NH2, or Image where R is hydrogen or C1-C3 alkyl; R5 is hydrogen, C1-C6 alkyl, C3-C8 cycloalkyl, or phenyl optionally substituted with halo, C1-C4 alkyl, or C1-C4 alkoxy; each of R6, R7, R8, and R9 is independently hydrogen, C1-C10 alkyl, phenyl, or benzyl; R10 is hydroxy, C1-C4 alkoxy, -NHOH, or -NR11R12; each of R11 and R12 is independently hydrogen, C1-C3 alkyl, or when taken together with the nitrogen atom form a morpholine or N-methyl piperazine ring; and p is 0, 1, or 2; with the provisions that: a) when R1 is R5-?- R2 may not be hydroxy; b) when one of Y and Z is -O- or Image , the other of Y and Z may not be -O- or Image ; and c) when R is COR10, hydroxy, -NR11R12, or -SC(=NH)NH2, Q may only be a bond.

458595

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