New diaza-phosphorine derivs. active against ectoparasites - e.g. helminths, esp. nematodes, cestodes and trematodes infecting warm blooded animal

摘要

Diazaphosphorine derivs. of formula (I), their tautomers N-oxides and salts are new. In (I): X = O or S; R = alkyl, alkenyl, alkynyl or (hetero) aryl all opt. substd.; R1, R3 = H, aryl, alkenyl or (ar)alkyl; or one of R2 and R3 = opt. substd. cycloalkyl; Y = O or S; R4 = pyridyl opt. substd. by a gp. A, or pyrimidinyl opt. substd. by a gp. A or a gp. B. A = 1-4 C(halo)alkyl, 2-4C alkoxyalkyl, 1-4C (halo)alkoxy, 1-4C(halo)alkylthio, 1-4Calkylsulphinyl, 1-4Calkylsulphonyl, amino, 1-3Calkylamino, di(1-3Calkyl)amino, allyl, propargyl, halo, NO2, CN; phenyl, SCN, NCS, 1-5Calkanoyl, benzyl or benzoyl opt. substd. by 1-3C(halo)alkyl, 1-3Calkoxy or halo; R5, R6 = H, halo, 1-4C(halo)alkyl, 1-4Calkoxy or 1-4Calkylthio. 7 Cpds. are claimed e.g. N-(4-(3-chloro-5-trifluoro methyl-2-pyridyloxy)-phenyl)-hexahydro -1,2,3-trimethyl-2,4,6 trioxo-2-phenyl-1,3,2-:azaphosphorin-5-carboxamide. USE - (I) are active against endoparasites e.g. anthelmintics esp. active against nematodes, cestodes and trematodes in domestic and working animals esp. mammals. Dosage is 1-500 mg/kg. Admin. is p.o. parenteral, s.c. or topical.