Pyrazole derivatives

Details Pyrazole derivatives Pyrazole derivatives

C - Chemistry, Metallurgy

07

D

260/300, 260/386

C07D 231/20 (2006.01)

Patent

CA 1079728

Abstract of the Disclosure Pyrazole derivatives of the formula: Image and pharmaceutically acceptable nontoxic salts thereof wherein R is hydrogen, trifluoromethyl or alkyl; R1 is hydrogen or alkyl; R2 is alkyl; R3 is aryl substituted by: (a) one or two of the same or different substi- tuents selected from the group consisting of halogen, trifluoromethyl, alkyl, alkenyl and alkoxy; (b) one substituent selected from the group con- sisting of alkylamino, dialkylamino wherein the alkyl moieties may form a heterocyclic ring with the nitrogen atom to which they are attached, cycloalkyl, cycloalkenyl, trifluoro- methoxy, nitro, cyano, carbonamido unsubsti- tuted or substituted by 1 or 2 alkyl moieties, sulphonamido unsubstituted or substituted by 1 or 2 alkyl moieties, and SOn-alkyl wherein n is 0, 1 or 2; (c) one substituent selected from the group con- sisting of alkylamino, dialkylamino wherein the alkyl moieties may form a heterocyclic ring with the nitrogen atom to which they are attached, cycloalkyl, cycloalkenyl, trifluoro- methoxy, nitro, cyano, carbonamido unsubsti- tuted or substituted by 1 or 2 alkyl moieties, sulphonamido unsubstituted or substituted by 1 or 2 alkyl moieties, and SOn-alkyl wherein n is 0, 1 or 2, and by one or two substituents selected from the group consisting of alkyl, alkenyl, alkoxy, halogen and trifluoromethyl; or (d) two substituents on the aryl moiety form a branched or unbranched saturated or unsaturated 5- to 7-membered isocyclic or heterocyclic ring, which ring can also have 1 or 2 oxygen atoms or sulfur atoms; or SOn-alkyl wherein ? is 0, 1 or 2; or R3 is naphthyl or pyridyl; and R4 is R5CO wherein R5 is alkyl unsubstituted or sub- stituted by 1, 2 or 3 halogen moieties, by alkoxy, or by mono- or dialkylamino; lower alkoxy; dialkyl- amino; thiophene; phenyl unsubstituted or substi- tuted by 1 or 2 alkyl, trifluoromethyl, alkoxy, nitro or halogen moieties; or a 5- to 7-membered heterocycle unsubstituted or substituted by 1 or 2 halogen, alkyl or nitro moieties; or R4 is Z-SO2 wherein Z is alkyl, phenyl or phenyl substi- tuted by 1 or 2 alkyl, halogen, nitro, trifluoro- methyl or trifluoromethylsulphonyl moieties, or by dichloroquinoxalinyl. The pyrazole derivatives and their salts are useful as di- uretics, saluretics and antihypertensives.

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