Leukotriene antagonists

Details Leukotriene antagonists Leukotriene antagonists

C - Chemistry, Metallurgy

07

C

167/179, 260/312

C07C 59/90 (2006.01) C07C 45/64 (2006.01) C07C 45/67 (2006.01) C07C 45/71 (2006.01) C07C 49/82 (2006.01) C07C 49/825 (2006.01) C07C 49/84 (2006.01) C07C 65/40 (2006.01) C07D 257/04 (2006.01) C07D 311/24 (2006.01)

Patent

CA 1242196

Abstract This invention provides novel benzene deriva- tives which are leukotriene antagonists, formulations of those derivatives, intermediates for preparing the derivatives, and a method of using those derivatives for the treatment of conditions characterized by an exces- sive release of leukotxienes. More specifically the invention as disclosed provides compounds of the Formula I Image and pharmaceutically acceptable salts thereof, wherein: R1 is hydrogen, C1-C6 alkyl, C3-C8 cycloalkyl, phenyl-substituted-(C1-13 alkyl), phenyl, or phenyl substituted with halo, C1-C4 alkyl, or C1-C4 alkoxy; R2 is C1-C10 alkyl, C2-C6 alkenyl, benzyl, or 2-phenylethyl; R3 is hydrogen, bromo, or chloro; Z is -O , -NR-, or Image , or when taken together, Image m is 0-4; A is a bond, -o-, Image -NR, -?-'', or -CHOH-; n is 0-4, Q is a bond, -O-, Image , or -NR " -; and R4 is -CN, hydroxy, -SC(=NH)NH2, -NR14-R15, Image Image Image or Image ; where each of R, R', and R'' is independently hydrogen or C1-C3 alkyl; each of R5 and R6 is independently hydrogen, C1-C3 alkyl, phenyl, or benzyl; R9 is hydroxy, Cl-C4 alkoxy, -NHOH, or -NR14R15; R10 is hydrogen, hydroxy, C1-C4 alkoxy, halo, C1-C4 alkyl, amino, mono- or di-(C1-C3 alkyl)amino, or (C1-C3 alkyl)CONH-; R11 is - (CR16R17) r-COR9, -O-(CR16R17)s-COR9, -(CR16R17)r-T-CN, -O-(CR16R17)s-T-CN, Image or Image ; R12 is hydrogen or C1-C3 alkyl; R13 is hydrogen or methyl; each of R14 and R15 is independently hydrogen, C1-C3 alkyl, or when taken together with the nitrogen atom form a morpholine or N-methyl piperazine ring; each of R16 and R17 is independently hydrogen or C1-C3 alkyl; r is 0-4; s is 1-4; T is a bond or -S-, W is a bond, -o-, -NR'''-, or Image ; R''' is hydrogen or C1-C3 alkyl; and p is 0, 1, or 2; provided that: (a) when R4 is -CN, -COR9, hydroxy, -NR11R12, or -SC(=NH3~2, Q may only be a bond and n may not be 0; (b) when A is -O-, Image , -NR'-, or -CHOH-, and Z is -o-, Image , or -NR-, m may not be 0; (c) when A is -o-, Image , -NR'-, or -CHOH-, and Q is -O-, Image , or -NR " -, n may not be 0; (d) when Z is -O-, Image , or -NR-, Q is -O-, Image , or NR " -, and A is a bond, m and n may not both be 0; and Image (e) if A is (1) when Z is Image m may not be 0, (2) when Q is Image , n may not be 0, and (3) when Z is -C- or -NR- and Q is -O- or -NR " -, m and n may not both be 0. Also provided are certain intermediates useful in preparing the compounds of Formula I. These compounds have the general formula Image XVI wherein R1, R2, R3, R5, and R6 are the same as previously defined and G is halo, hydroxy, thiol, -NR18R19, or -P(C6H5)3X', where each of R18 and R19 is independently hydrogen or C1-C3 alkyl, and X' is halo.

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