Thioformamide derivatives

Details Thioformamide derivatives Thioformamide derivatives

C - Chemistry, Metallurgy

07

C

167/228, 167/268

C07C 327/46 (2006.01) A61K 31/165 (2006.01) C07D 213/59 (2006.01)

Patent

CA 1326485

(1) ABSTRACT OF THE DISCLOSURE: The invention relates to thioformamide derivatives of the formula: Image (I) wherein R represents a straight- or branched-chain alkyl radical containing from 1 to 4 carbon atoms, Ar represents a phenyl group substituted in the 3 or 5 or 3 and 5 positions by a substituent selected from the group consisting of cyano, nitro, trifluoromethyl, carbamoyl, carboxy, C2-5-alkanoyl, C2-5-alkoxycarbonyl, C1-4-alkyl- sulphonyl, fluorine, chlorine or bromine, or a phenyl group substituted in the 3 or 5 or 3 and 5 positions by a substituent selected from the group consisting of cyano, nitro, trifluoromethyl, carbamoyl, carboxy, C2-5-alkanoyl, C2-5-alkoxycarbonyl, C1-4-alkylsulphonyl, fluorine, chlorine or bromine and further substituted by halogen, C1-4-alkyl or C6-12-aryl, or Ar is a naphthyl group, Y represents an ethylene or methylene radical or a valency bond, and X represents a carbonyl or hydroxymethylene group or a group of the formula: >C=NOR1, >C=NN(R1)2 or >C=NN(R1)CON(R1)2 in which the symbols R1, which may be the same or different, each represents a hydrogen atom of a straight- or branched- chain alkyl radical containing from 1 to 4 carbon atoms which is unsubstituted or substituted by one or more substituents selected from C2-4-alkenyl, carboxy, C2-5- alkoxycarbonyl, hydroxy, C1-4-alkoxy, carbamoyl (unsubstituted or substituted by one or two C1-4-alkyl groups), amino, C1-4- (2) alkylamino and di-C1-4-alkylamino groups or represents a benzyl, phenethyl, 1-naphthylmethyl, 2-naphthylmethyl or pyrid-3-ylmethyl radical each of which may be substituted on the ring by one or more halogen atoms, hydroxy, C1-4-alkyl, C14-alkoxy (alkoxy being unsubstituted or substituted as defined for alkyl groups represented by R1), cyano, nitro, trifluoromethyl, carboxy, C1-4-alkylamino, C2-5-alkanoylamino or C2-5-alkoxy-carbonyl groups or two R1 substituents on the same nitrogen atom may together form a straight- or branched-chain alkylene radical containing from 4 to 6 carbon atoms in the chain which is unsubstituted or substituted as defined for alkyl radicals represented by R1, and pharmaceutically acceptable salts thereof. These derivatives are useful as medicine. The invention also relates to processes for their preparation and compositions containing them.

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