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1. 发明授权

US4205077A Benzimidazole sulphides as anthelmintic agents 失效
标题翻译：苯并咪唑硫化物作为驱肠剂
公开(公告)号：US4205077A
公开(公告)日：1980-05-27
申请号：US894974
申请日：1978-04-10
申请人： Ernst Aufderhaar , Jean J. Gallay , Manfred Kuhne , Alfred Meyer , Oswald Rechsteiner , Max Schellenbaum , Jean-Paul Fumeaux
发明人： Ernst Aufderhaar , Jean J. Gallay , Manfred Kuhne , Alfred Meyer , Oswald Rechsteiner , Max Schellenbaum , Jean-Paul Fumeaux
IPC分类号： A01N43/52 , A61K31/415 , A61K31/4184 , A61P33/00 , C07D235/28 , C07D235/20
CPC分类号： C07D235/28 , A01N43/52
摘要： Benzimidazole derivatives of the formula ##STR1## in which R and R.sub.1 independently of one another are each hydrogen, an alkanoyl group having 1 to 4 carbon atoms, an alkoxycarbonyl group having 1 to 4 carbon atoms, an alkylsulphonyl group having 1 to 4 carbon atoms, a benzoyl group, a phenylsulphonyl group or a p-methylphenylsulphonyl group; R.sub.2 and R.sub.4 independently of one another are each hydrogen, halogen or a methyl group, R.sub.3 is hydrogen, halogen, a methyl group or a methoxy group; X is oxygen or sulphur; Y is halogen, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a methylthio group, a methylsulphinyl group, a methylsulphonyl group, a trifluoromethyl group, a nitro group, a hydroxyl group, a cyano group or an acetyl group; and m is 0, 1, 2 or 3; and if one of the two radicals R or R.sub.1 is hydrogen, the position of the other of these radicals on the N atoms cannot be clearly established, including, when at least one of the two radicals R or R.sub.1 is hydrogen, the possible tautomeric compounds of the formula I; and the disulphides obtainable by oxidation of compounds of the formula I. The compounds are useful for combating helminths in domestic animals and productive animals.
摘要翻译：其中R和R 1彼此独立的式“IMAGE”的苯并咪唑衍生物各自为氢，具有1至4个碳原子的烷酰基，具有1至4个碳原子的烷氧基羰基，具有1至4个碳原子的烷基磺酰基，苯甲酰基，苯基磺酰基或对甲基苯基磺酰基; R 2和R 4彼此独立地各自为氢，卤素或甲基，R 3为氢，卤素，甲基或甲氧基; X是氧或硫; Y是卤素，具有1至4个碳原子的烷基，具有1至4个碳原子的烷氧基，甲硫基，甲基亚磺酰基，甲基磺酰基，三氟甲基，硝基，羟基，氰基组或乙酰基; m为0,1,2或3; 并且如果两个基团R或R 1中的一个为氢，则这些基团中另一个基团在N原子上的位置不能清楚地确定，包括当两个基团R或R 1中的至少一个为氢时，可能的互变异构化合物的式I; 和通过氧化式I化合物可获得的二硫化物。该化合物可用于在家畜和生产性动物中对抗蠕虫。

2. 发明授权

US4197307A 2-Alkylthio-, 2-alkylsulphinyl- and 2-alkylsulfonyl-6-phenylbenzimidazoles as anthelmintic agents 失效
标题翻译： 2-烷基硫代，2-烷基亚磺酰基和2-烷基磺酰基-6-苯基苯并咪唑作为驱肠剂
公开(公告)号：US4197307A
公开(公告)日：1980-04-08
申请号：US894973
申请日：1978-04-10
申请人： Jean-Jacques Gallay , Manfred Kuhne , Alfred Meyer , Oswald Rechsteiner , Max Schellenbaum
发明人： Jean-Jacques Gallay , Manfred Kuhne , Alfred Meyer , Oswald Rechsteiner , Max Schellenbaum
IPC分类号： A61K31/415 , A61K31/4184 , A61P33/00 , A61P33/10 , C07D235/28
CPC分类号： C07D235/28
摘要： Benzimidazole derivatives of the formula ##STR1## in which R is an alkyl group having 1 to 6 carbon atoms, an alkenyl group having 3 to 5 carbon atoms, an alkynyl group having 3 to 5 carbon atoms or a benzyl group, which is unsubstituted or monosubstituted to disubstituted by a methyl group, halogen or a nitro group;R.sub.1 is hydrogen, an alkanoyl group having 1 to 4 carbon atoms, an alkoxycarbonyl group having 1 to 4 carbon atoms, a N,N-dialkylcarbamoyl group or N,N-dialkylthiocarbamoyl group, each having 1 to 4 carbon atoms in the alkyl groups, an alkylsulphonyl group having 1 to 4 carbon atoms, a benzoyl group, a phenylsulphonyl group, a 4-methylphenylsulphonyl group or the radical, ##STR2## in which Q is a carbonyl group, a thiocarbonyl group or an oxalyl group;R.sub.2 is hydrogen, halogen or a methyl group;R.sub.3 is hydrogen, halogen, a methyl group or an alkoxy group having 1 to 4 carbon atoms;R.sub.4 is hydrogen, halogen or a methyl group; X is oxygen or sulphur;Y is halogen, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a methylthio group, a methylsulphinyl group, a methylsulphonyl group, a trifluoromethyl group, a nitro group, a hydroxyl group, a cyano group or an alkanoyl group having 1 to 4 carbon atoms in the alkyl moiety m is 0, 1, 2 or 3; andn is 0, 1 or 2.Included are, if R.sub.1 is not hydrogen, the tautomeric compounds of the formula I. The compounds are effective for combating helminths in domestic and useful animals.
摘要翻译：其中R是具有1至6个碳原子的烷基，具有3至5个碳原子的烯基，具有3至5个碳原子的炔基或苄基的式“IMAGE”的苯并咪唑衍生物，其是未取代的或被甲基，卤素或硝基单取代至二取代; R 1为氢，碳原子数为1〜4的烷酰基，碳原子数1〜4的烷氧基羰基，N，N-二烷基氨基甲酰基或N，N-二烷基硫代氨基甲酰基，烷基中为碳原子数为1〜，具有1至4个碳原子的烷基磺酰基，苯甲酰基，苯基磺酰基，4-甲基苯基磺酰基或基团，其中Q是羰基，硫代羰基或草酰基的 R2是氢，卤素或甲基; R3是氢，卤素，甲基或具有1-4个碳原子的烷氧基; R4是氢，卤素或甲基; X是氧或硫; Y是卤素，具有1至4个碳原子的烷基，具有1至4个碳原子的烷氧基，甲硫基，甲基亚磺酰基，甲基磺酰基，三氟甲基，硝基，羟基，氰基基团或在烷基部分m中具有1至4个碳原子的烷酰基为0,1,2或3; 并且n为0,1或2.如果R 1不是氢，则包括式I的互变异构化合物。该化合物对于在家用和有用动物中对抗蠕虫是有效的。

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