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61. 发明授权

US5428047A Use of substituted 1,2,4-oxadiazole derivatives for combating endoparasites, new substituted 1,2,4-oxadiazole derivatives, and processes for their preparation 失效
标题翻译：使用取代的1,2,4-恶二唑衍生物对抗内寄生虫，新的取代的1,2,4-恶二唑衍生物及其制备方法
公开(公告)号：US5428047A
公开(公告)日：1995-06-27
申请号：US124909
申请日：1993-09-21
申请人： Peter Jeschke , Werner Lindner , Achim Harder , Norbert Mencke
发明人： Peter Jeschke , Werner Lindner , Achim Harder , Norbert Mencke
IPC分类号： A01N43/82 , A01N43/836 , A61K31/41 , A61K31/4245 , A61P33/00 , A61P33/10 , C07D271/06 , C07D413/06
CPC分类号： C07D271/06 , A01N43/82 , A61K31/41
摘要： The present invention relates to the use of substituted 1,2,4-oxadiazole derivatives of the general formula I ##STR1## in which R.sup.1 represents hydrogen, alkyl which is optionally substituted by halogen, alkoxy, hydroxyl, amino, alkylamino, dialkylamino, cycloalkylamino as well as cycloalkyl, optionally substituted aryl or hetaryl,R.sup.2 represents hydrogen and alkyl,X represents O, S, SO, SO.sub.2 and N-R.sup.3,R.sup.3 represents hydrogen, alkyl, alkylcarbonyl or halogenoalkylcarbonylR.sup.4 represents identical or different radicals from the series comprising hydrogen, halogen, cyano, nitro, isothiocyanato, amino, aminoacyl, alkylamino, dialkylamino, trialkylammonium halide, sulphonylamino, hydroxyl, mercapto, alkyl, aralkyl, halogenoalkyl, alkoxy, aralkoxy, halogenoalkoxy, aryl, aryloxy, arylthio, arylsulphinyl, arylsulphonyl, alkylthio, halogenoalkylthio, alkylsulphinyl, halogenoalkylsulphinyl, alkylsulphonyl, halogenoalkylsulphonyl, alkoxycarbonyl, alkylcarbonyl, alkylcarbonyloxy, alkoxyalkyl, alkoxyalkoxy, hydroxyalkoxy, hetarylmethyleneoxy,for combating endoparasites in medicine and veterinary medicine, and new compounds of the formula (I) and their preparation.
摘要翻译：本发明涉及通式Ⅰ的取代的1,2,4-恶二唑衍生物（Ⅰ），其中R1代表氢，任选被卤素，烷氧基，羟基，氨基，烷基氨基，二烷基氨基，环烷基氨基以及环烷基，任选取代的芳基或杂芳基，R 2表示氢和烷基，X表示O，S，SO，SO 2和N-R 3，R 3表示氢，烷基，烷基羰基或卤代烷基羰基R 4表示相同或不同的基团，氨基，氨基酰基，烷基氨基，二烷基氨基，三烷基卤化铵，磺酰基氨基，羟基，巯基，烷基，芳烷基，卤代烷基，烷氧基，芳烷氧基，卤代烷氧基，芳基，芳氧基，芳硫基，芳基亚磺酰基，芳基磺酰基，烷硫基，卤代烷硫基，烷基亚磺酰基，卤代烷基亚磺酰基，烷基磺酰基，卤代烷基磺酰基，烷氧基羰基，烷基羰基，烷基羰基氧基，烷氧基烷基，烷氧基烷氧基，羟基烷氧基，杂芳基亚甲氧基，用于对抗医药和兽药中的内寄生虫，以及式（I）的新化合物及其制备。

62. 发明授权

US5118680A Combating endoparasites with 3-hydroxybenzothiophenes 失效
标题翻译：与3-羟基苯并噻吩组合内给药
公开(公告)号：US5118680A
公开(公告)日：1992-06-02
申请号：US721901
申请日：1991-06-20
申请人： Nikolaus Muller , Werner Hallenbach , Achim Harder , Werner Lindner
发明人： Nikolaus Muller , Werner Hallenbach , Achim Harder , Werner Lindner
IPC分类号： C07D333/64 , A61K31/38 , A61K31/381 , A61K31/435 , A61P33/00 , A61P33/10 , C07C323/62 , C07C323/65 , C07C323/67 , C07D333/70 , C07D409/06 , C07D413/06 , C07D495/04
CPC分类号： C07D495/04 , C07C323/62 , C07D333/70
摘要： 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 ##STR1## in which X represents .dbd.CH-- or .dbd.N--,Y represents .dbd.O or .dbd.NH,R.sup.1 represents one or more identical or different radicals from the group consisting of hydrogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, alkylenedioxy, halogenoalkylenedioxy, halogen, CN, NO.sub.2, NH.sub.2, alkylamino, dialkylamino, alkylcarbonyl, carbalkoxy, alkylsulphonyl, arylsulphonyl, sulphamoyl, alkylsulphamoyl, dialkylsulphamoyl, aryl, aryloxy and arylthio, which, in turn, may again be substituted,R.sup.2 represents optionally substituted alkoxy, cycloalkoxy or the radical --NR.sup.3 R.sup.4,R.sup.3 represents hydrogen or alkyl,R.sup.4 represents an alkyl or carbocyclic or heterocyclic armoatic radical or the radical --COOR.sup.5,R.sup.3 and R.sup.4, 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 C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -hydroxyalkyl, C.sub.1 -C.sub.4 -halogenoalkyl or C.sub.1 -C.sub.4 -alkoxyalkylR.sup.5 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.
摘要翻译：一种对抗人和动物内寄生虫的方法，其包括向所述人和动物施用内寄生有效量的式（I）的3-羟基苯并噻吩，其中X表示= CH-或= N-，Y表示= O或= NH，R 1表示与氢，烷基，烷氧基，烷硫基，卤代烷基，卤代烷氧基，卤代烷硫基，亚烷基二氧基，卤代亚烷基二氧基，卤素，CN，NO 2，NH 2，烷基氨基，二烷基氨基，烷基羰基中的一个或多个相同或不同的基团，烷基磺酰基，芳基磺酰基，氨磺酰基，烷基氨磺酰基，二烷基氨磺酰基，芳基，芳氧基和芳硫基，其又可以被取代，R 2表示任选取代的烷氧基，环烷氧基或基-NR 3 R 4，R 3表示氢或烷基，R 4表示烷基或碳环或杂环杂环基团或基团-COOR 5，R 3和R 4与相邻的氮原子一起代表5-或6-元杂环可以含有O或N作为其它杂原子并且任选被C 1 -C 4 - 烷基，C 1 -C 4 - 羟基烷基，C 1 -C 4 - 卤代烷基或C 1 -C 4 - 烷氧基烷基取代的O 2可以表示烷基，环烷基，芳烷基或芳基，又可以是取代的或任选取代的芳基。许多化合物是新的，以及它们自己的中间体。

63. 发明授权

US5095032A Parasiticidal new substituted thienopyranones 失效
标题翻译： PARASITICIDAL新取代的三烯衍生物
公开(公告)号：US5095032A
公开(公告)日：1992-03-10
申请号：US555553
申请日：1990-07-19
申请人： Heinz-Jurgen Bertram , Nikolaus Muller , Achim Harder
发明人： Heinz-Jurgen Bertram , Nikolaus Muller , Achim Harder
IPC分类号： A01N43/16 , A61K31/38 , A61P33/00 , A61P33/10 , C07D495/04
CPC分类号： C07D495/04
摘要： Parasiticidal new substituted thienopyranones of the formula ##STR1## in which X represents O or S,R.sup.1 and R.sup.2 independently of one another represent hydrogen, halogen, CN, NO.sub.2, alkyl, aralkyl, aryl, alkylcarbonyl or alkoxycarbonyl, or, together with the adjacent C atoms, form a carbocyclic ring which is optionally interrupted by heteroatoms,R.sup.3 represents optionally substituted alkyl or phenyl,R.sup.4 represents hydrogen or alkyl,R.sup.3 and R.sup.4, together with the adjacent nitrogen atom, represent a heterocyclic 5- or 6-membered ring.Some of the intermediates for making them are also new.
摘要翻译：其中X表示O或S，R1和R2彼此独立地表示式XI的间隔性新取代的噻吩吡喃酮代表氢，卤素，CN，NO 2，烷基，芳烷基，芳基，烷基羰基或烷氧基羰基，或与相邻的C原子形成任选被杂原子中断的碳环，R 3表示任选取代的烷基或苯基，R 4表示氢或烷基，R 3和R 4与相邻的氮原子一起代表杂环的5-或6-元环。一些制造它们的中间体也是新的。

64. 发明授权

US5095024A Substituted 1,3,4-thiadizaolinones, processes for their preparation, and their use for combating endoparasites 失效
标题翻译：取代1,3,4-噻唑烷酮，其制备方法及其用于组合内生菌的用途
公开(公告)号：US5095024A
公开(公告)日：1992-03-10
申请号：US581934
申请日：1990-09-13
申请人： Nikolaus Muller , Gerhard Bonse , Werner Lindner , Achim Harder
发明人： Nikolaus Muller , Gerhard Bonse , Werner Lindner , Achim Harder
IPC分类号： A01N43/824 , A61K31/41 , A61K31/433 , A61P33/00 , A61P33/10 , C07C243/28 , C07C337/02 , C07C337/06 , C07D285/12 , C07D285/125 , C07D285/13
CPC分类号： C07D285/13 , C07C337/02 , C07D285/125
摘要： Substituted 1,3,4-thiadiazolinones of the formula (I), ##STR1## in which X represents O or S,R.sup.1 represents hydrogen, alkyl, alkoxy, alkylthio, halogen, halogenoalkyl, halogenoalkoxy or halogenoalkylthio,R.sup.2 represents one or more identical or different radicals from the series comprising hydrogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, alkylenedioxy, halogenoalkylenedioxy, halogen, CN, NO.sub.2, NH.sub.2, alkylamino, dialkylamino, alkylcarbonyl, carbalkoxy, alkylsulphonyl, arylsulphonyl, sulphamoyl, alkylsulphamoyl, dialkylsulphamoyl, aryl, aryloxy and arylthio, each of which can, in turn, be substituted as well, andR.sup.3 represents alkyl, alkenyl or alkynyl, each of which can optionally be substituted,with the exception of the compound 5-methylmercapto-3-phenyl-1,3,4-thiadiazol-2-(3H)-one, are disclosed as being useful to combat endoparasites. Compositions containing these compounds, process for preparing them, and novel intermediates are also disclosed.
摘要翻译：取代的式（I）的1,3,4-噻二唑啉酮，其中X代表O或S，R1代表氢，烷基，烷氧基，烷硫基，卤素，卤代烷基，卤代烷氧基或卤代烷硫基，R2代表一或更多相同或不同的基团，其包含氢，烷基，烷氧基，烷硫基，卤代烷基，卤代烷氧基，卤代烷硫基，亚烷基二氧基，卤代亚烷基二氧基，卤素，CN，NO 2，NH 2，烷基氨基，二烷基氨基，烷基羰基，烷氧基，烷基磺酰基，芳基磺酰基，氨磺酰基，烷基氨磺酰基，二烷基氨磺酰基，芳基，芳氧基和芳硫基，其中每一个也可以被取代，并且R 3表示烷基，烯基或炔基，其中每一个可任选被取代，除了化合物5-甲基巯基 - 3-苯基-1,3,4-噻二唑-2-（3H） - 酮被公开用于对抗内寄生虫。还公开了含有这些化合物的组合物，其制备方法和新型中间体。

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