5-(alkylidene-cycloalkyl)- and...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 403/04 (2006.01) A61K 31/4439 (2006.01) A61K 31/497 (2006.01) A61K 31/53 (2006.01) C07D 401/04 (2006.01)

Patent

CA 2411015

The present invention relates to 5-(alkylidene- cycloalkyl)-pyrazoles and 5-(alkylidene-heterocyclyl)- pyrazoles of the formula I: Image wherein the ring of the formula (R 5) -A- (SO m R 4) is a substituted phenyl, pyridinyl, pyrimidinyl, pyridazinyl, or triazinyl; m is 0, 1 or 2; R 1 is H, vitro, cyano, alkyl, substituted sulfonyl, formyl, ketone, ester or optionally substituted amino; R 2 is H, vitro, cyano, optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, alkoxy, cycloalkyloxy, aryloxy, heteroaryloxy, heterocyclyloxy, formyl, ester, ketone, substituted amide, substituted amino or alkylthiol; B is -O-, -S-, or -NR3; R 3 is H or alkyl; R 4 is optionally substituted amino, substituted-amide or substituted cyano; R 5 is H, halo, hydroxy, substituted alkyl, alkoxy, alkenyl, alkynyl, cycloalkyl, cyano, formyl, ketone, ester, substituted amino, substituted amide or alkylthio; G is cycloalkyl or heterocyclyl; R 6 and R 7 are each H, alkyl, alkenyl, alkynyl cycloalkyl, aryl, heteroaryl, heterocyclyl, formyl, amide, ester, ketone or alkylthio. The present invention also relates to pharmaceutical compositions containing compounds of formula I and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.

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