Indole and indazole keto sulphones as leukotriene antagonists

Details Indole and indazole keto sulphones as leukotriene antagonists Indole and indazole keto sulphones as leukotriene antagonists

C - Chemistry, Metallurgy

07

D

167/208, 260/300

C07D 209/22 (2006.01) C07D 209/08 (2006.01) C07D 209/12 (2006.01) C07D 209/24 (2006.01) C07D 231/56 (2006.01) C07D 403/06 (2006.01)

Patent

CA 1335450

This invention provides a series of novel keto sulfones of formula I Image in which the group =A- is selected from =C(Ra)- or =N- and the other radicals have the meanings defined, for example, wherein Ra is hydrogen or alkyl; the group R1.L- is an amidic radical of formula R1.W.CO.NH-, R1.W.CS.NH- or R1.NH.CO-, in which R1 is optionally substituted alkyl or phenyl-alkyl, cycloalkyl or cycloalkyl-alkyl, the cyclic moiety of any of which optionally may contain one unsaturated linkage; W is oxy, thio, imino or a direct link to R1; R2 is hydrogen, halogeno, alkyl or alkoxy; one of R3 and R4 is a radical of formula II: Image wherein Rb is hydrogen, alkyl or alkoxy, Rc is hydrogen, alkyl, alkoxy, trifluoromethyl or halogeno, and M is hydrogen, cyano, alkoxycarbonyl, optionally substituted alkyl or phenyl carbamoyl, or alkanoyl; and the other of R3 and R4 is hydrogen, halogeno (except for R3), cycloalkyl, or alkyl optionally containing one or two double or triple bonds, said alkyl additionally optionally bearing a substituent P selected from a group consisting of cyano, carboxy, 1H-tetrazol-5-yl, alkoxy, alkoxy-carbonyl, carbamoyl, ureido, carbamoyloxy, a carbamate, acylamino, acyloxy, and an optionally substituted alkyl or phenyl (optionally oxidized) thio group. The compounds of formula I are useful in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions. The invention also provides pharmaceutical compositions containing the formula I compounds, or their salts, and processes for the manufacture of the formula I compounds.

520793

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