Use of 3-hydroxybenzothiophenes for combating endoparasites,...

C - Chemistry – Metallurgy – 07 – D

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C07D 333/70 (2006.01) A61K 31/38 (2006.01) A61K 31/435 (2006.01) C07C 323/62 (2006.01) C07C 323/63 (2006.01) C07D 213/80 (2006.01) C07D 495/04 (2006.01)

Patent

CA 2019171

ABSTRACT OF THE DISCLOSURE A method of combating endoparasites in humans and animals which comprises administering to such humans and animals an endoparasiticidally effective amount of a 3-hydroxybenzothiophene of the formula Image (I) in which X represents =CH- or =N-, Y represents =O or =NH, R1 represents one or more identical or different radicals from the group consisting of hydrogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, alkylenedioxy, halogenoalkylene- dioxy, halogen, CN, NO2, NH2, alkylamino, dialkyl- amino, alkylcarbonyl, carbalkoxy, alkylsulphonyl, arylsulphonyl, sulphamoyl, alkylsulphamoyl, dialkyl- sulphamoyl, aryl, aryloxy and arylthio, which, in turn, may again be substituted, R2 represents optionally substituted alkoxy, cycloalkoxy or the radical -NR3R4, R3 represents hydrogen or alkyl, R4 represents an alkyl or carbocyclic or heterocyclic aromatic radical or the radical -COOR5, R3 and R4, together with the adjacent nitrogen atom, represent a 5- or 6-membered heterocycle which may contain O or N as further heteroatoms and is optionally substituted by C1-C4-alkyl, C1-C4-hydroxy- alkyl, C1-C4-halogenoalkyl or C1-C4-alkoxyalkyl R5 represents alkyl, cycloalkyl, aralkyl or aryl, which, in turn, may again be substituted, or optionally substituted-aryl. Many of the compounds are new, as well as their own intermediates. * * * Le A 26 892

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