Patent IL-119256-A (IL)
Title: 2-cyano-3-mercaptocrotonamide derivatives, a process for their preparation and pharmaceutical compositions containing them
IPC: C07C323/60
Filed: 1996-09-17
Abstract: Compounds of the formula and/or optionally stereoisomeric forms and/or physiologically tolerable salts thereof where R1 a hydrogen atom, (C1-C17)-alkyl, (C1-C4)-alkyl, mono- or polysubsituted by fluorine, chlorine, bromine or iodine, phenyl, phenyl, mono-or polysubstituted by fluorine, chlorine, bromine or iodine, nitro, cyano, (C1-C4) - alkyl, (C1-C4)- alkyl, mono- or polysubstituted by fluorine, chlorine, bromine or iodine, (C1-C4) - alkoxy, (C1-C4) - alkoxy, mono- or polysubstituted by fluorine, chlorine, bromine or iodine, 1636 ד' באב התשס" א - July 24, 2001 benzyl, (C3-C7) - cycloalkyl, alkenyl having 2 or 3 carbon atoms or alkynyl having 2 or 3 carbon atoms; R2 is a hydrogen atom, (C1-C4) - alkyl, phenyl, phenyl - (C1-C2) - alkyl or alkenyl having 2 to 3 carbon atoms, R3 is a mono-, di-or trinuclear, unsaturated heterocyclic radical having 3 to 13 carbon atoms and 1 to 4 heteroatoms from the group consisting of oxygen, sulfur and nitrogen, of which at most one of the heteroatoms in the ring system is other than nitrogen, and is unsubstituted or mono- or polysubstituted by fluorine, chlorine, bromine or iodine, (C1-C4) - alkyl, (C1-C4) - alkyl, mono- or polysubstituted by fluorine, chlorine, bromine or iodine, (C1-C4) - alkoxy, (C1-C4) - alkoxy, mono- or polysubsituted by fluorine, chlorine, bromine or iodine, nitro, hydroxyl, carboxyl, carbamoyl or an oxo group, (b) a radical of the formula in which R4, R5 and R6 can be identical or different and are a hydrogen atom, (C1-C4) - alkyl, (C1-C4) - alkyl, mono- or polysubstituted by fluorine. chlorine. bromine or iodine, in which R4 is a hydrogen atom and R5 and R6, together with the phenyl ring of the formula II, form a naphthalene ring. in which R4 is a hydrogen atom and R5 and R6 form a methylenedioxy radical, (C1-C4) - alkoxy, (C1-C4) - alkoxy, mono-or polysubsituted by fluorine, chlorine, bromine or iodine, (C1-C4) - alkylmercapto (C1-C4) - alkylmercapto, mono- or polysubstituted by fluorine, chlorine, bromine or iodine, fluorine. chlorine, bromine or iodine, nitro, cyano, hydroxyl, carboxyl, (C1-C4) - alkylsulfonyl, alkoxycarbonyl, having 1 to 3 carbon atoms in the alkyl chain, benzoyl, benzoyl, mono- or polysubstituted by fluorine, chlorine, bromine or iodine. (C1-C4) - alkyl or (C1-C4) - alkoxy, phenyl, phenyl, mono- or polysubstituted by (C1-C4) - alkoxy, fluorine, chlorine, bromine or iodine or (C1-C4) - alkyl, phenoxy, or phenoxy, mono- or polysubstituted by (C1-C3)-alkoxy, mono-or polysubstituted by fluorine, chlorine, bromine or iodine, (C1-C3)-alkyl, mono- or polysubstituted by fluorine, chlorine, bromine or iodine, or fluorine, chlorine, bromine or iodine, a radical of the formula -(CH2)n-COOR10 in which R10 is a hydrogen atom or (C1-C4) - alkyl and n is an integer from 1 to 12, or R2 and R3, together with the nitrogen atom to which they are bonded, form a 4- to 7-membered ring, which is unsubstituted or substituted by carbonyl on the carbon atom adjacent to the nitrogen atom, or R2 and R3, together with the nitrogen atom to which they are bonded, form a 5- to 6-membered ring of the formula 1637 ד' באב התשס" א - July 24, 2001 in which W is