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1. 发明授权

US5236939A Substituted 1,3,4-oxa(thia)diazolinones process for their preparation and their use of combating endoparasites 失效
标题翻译：取代1,3,4-氧杂（噻吩）二唑啉酮的制备方法及其对抗内寄生虫
公开(公告)号：US5236939A
公开(公告)日：1993-08-17
申请号：US778023
申请日：1991-10-17
申请人： Gerhard Bonse , Nikolaus Muller , Achim Harder
发明人： Gerhard Bonse , Nikolaus Muller , Achim Harder
IPC分类号： A01N43/824 , C07D271/10 , C07D271/113 , C07D285/12 , C07D285/125 , C07D285/13
CPC分类号： C07D271/113 , C07D285/125 , C07D285/13
摘要： Substituted 1,3,4 -oxa- diazolinones of the formula (I) ##STR1## in which X represents O andY represents O or S,are disclosed as useful to combat endoparasites.
摘要翻译：公开了其中X代表O且Y代表O或S的式（I）的取代的1,3,4-恶二唑啉酮用于对抗内寄生虫。

2. 发明授权

US5093343A Substituted 1,3,4-oxa (thia) diazolinones process for their preparation and their use of combating endoparasites 失效
公开(公告)号：US5093343A
公开(公告)日：1992-03-03
申请号：US577970
申请日：1990-09-05
申请人： Gerhard Bonse , Nikolaus Muller , Achim Harder
发明人： Gerhard Bonse , Nikolaus Muller , Achim Harder
IPC分类号： A01N43/824 , A61K31/41 , A61K31/4245 , A61K31/433 , A61P33/10 , C07D271/10 , C07D271/113 , C07D285/12 , C07D285/125 , C07D285/13
CPC分类号： C07D271/113 , C07D285/125 , C07D285/13
摘要： Substituted 1,3,4-oxa- and thiadiazolinones of the formula (I) ##STR1## in which 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 among 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 or arylthio, which, in turn, can be sutstituted,R.sup.3 represents one or more identical or different radicals from among hydrogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, alkylenedioxy, halogenoalkylenedioxy, halogen, CN, NO.sub.2, alkylcarbonyl, carbalkoxy, alkylsulphonyl, arylsulphonyl, sulphamoyl, alkylsulphamoyl, dialkylsulphamoyl, aryl, aryloxy or arylthio, which, in turn, can be substituted,X represents O or S, andY represents O or S,with the exception of the compounds 5-phenoxy-3-(3,4-dichlorophenyl)-1,3,4-oxadiazol-2(3H)-one, and 5-phenoxy-3-(3-chloro-4-fluorophenyl)-1,3,4-oxadiazol-2-(3H)-one are disclosed as useful to combat endoparasites. Compositions containing these compounds and process for preparing them are also disclosed.The present invention relates to new substituted 1,3,4-oxa(thia)diazolinones, process for their preparation, and their use for combating endoparasites.Substituted 2-alkoxy-1,3,4-oxathiazolinones and their use against endoparasites are already known, but their actions are not always satisfactory (DE-OS (German Published Specification) 2,604,110). Previously described compounds are furthermore 2-aryloxy-1,3,4-oxadiazolinones (Pilgram, J. Heterocyclic Chem. 39, 823 (1982)); however, nothing is known about their use for combating endoparasites.The present invention relates to substituted 1,3,4-oxa-and thiadiazolinones of the formula (I) ##STR2## in which R.sup.1 represents hydrogen, alkyl, alkoxy, alkylthio, halogen, halogenoalkyl, halogenoalkoxy or halogeno-alkylthio,R.sup.2 represents one or more identical or different radicals from amongst hydrogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogeno-alkylthio, alkylenedioxy, halogenoalkylenedioxy, halogen, CN, NO.sub.2, NH.sub.2, alkylamino, dialkylamino, alkylcarbonyl, carbalkoxy, alkylsulphonyl, arylsulphonyl, sulphamoyl, alkylsulphamoyl, dialkyl-sulphamoyl, aryl, aryloxy or arylthio, which, in turn, can be substituted,R.sup.3 represents one or more identical or different radicals from amongst hydrogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogeno-alkylthio, alkylenedioxy, halogenoalkylenedioxy, halogen, CN, NO.sub.2, alkylcarbonyl, carbalkoxy, alkyl-sulphonyl, arylsulphonyl, sulphamoyl, alkyl-sulphamoyl, dialkylsulphamoyl, aryl, aryloxy or arylthio, which, in turn, can be substituted,X represents 0 or S, andY represents 0 or S,with the exception of the compounds 5-phenoxy-3-(3,4-dichlorophenyl)-1,3,4-oxadiazol-2(3H)-one and 5-phenoxy-(3-chloro-4-fluorophenyl)-1,3,4-oxadiazol-2-(3H)-one.The invention also relates to a process for the preparation of the new substituted 1,3,4-oxa- and thiadiazolinones of the formula ##STR3## in which R.sup.1 represents hydrogen, alkyl, alkoxy, alkylthio, halogen, halogenoalkyl, halogenoalkoxy or halogeno-alkylthio,R.sup.2 represents one or more identical or different radicals from amongst hydrogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogeno-alkylthio, alkylenedioxy, halogenoalkylenedioxy, halogen, CN, NO.sub.2, NH.sub.2, alkylamino, dialkylamino, alkylcarbonyl, carbalkoxy, alkylsulphonyl, aryl-sulphonyl, sulphamoyl, alkylsulphamoyl, dialkyl-sulphamoyl, aryl, aryloxy or arylthio, which, in turn, can be substituted,R.sup.3 represents one or more identical or different radicals from amongst hydrogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogeno-alkylthio, alkylenedioxy, halogenoalkylenedioxy, halogen, CN, NO.sub.2, alkylcarbonyl, carbalkoxy, alkyl-sulphonyl, arylsulphonyl, sulphamoyl, alkyl-sulphamoyl, dialkylsulphamoyl, aryl, aryloxy or arylthio, which, in turn, can be substituted,X represents O or S, andY represents O or S,with the exception of the compounds 5-phenoxy-3-(3,4-dichlorophenyl)-1,3,4-oxadiazol-2(3H)-one and 5-phenoxy-3-(3-chloro-4-fluorophenyl)-1,3,4-oxadiazol-2-(3H)-one, characterized in that compounds of the formula (II) ##STR4## in which X, Y, R.sup.1, R.sup.2 and R.sup.3 have the abovementioned meaning, are reacted with carbonylation reagents such as phosgene, phosgene or triphosgene, and the compounds obtained in this process, of the formula III ##STR5## in which X, Y, R.sup.1, R.sup.2 and R.sup.3 have the abovementioned meaning, are cyclized in the presence of bases.

3. 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。

4. 发明授权

US06329338B1 Derivatives of cyclodepsipeptide PF1022 substance 失效
标题翻译：环糊精PF1022物质的衍生物
公开(公告)号：US06329338B1
公开(公告)日：2001-12-11
申请号：US09043558
申请日：1998-05-20
申请人： Osamu Sakanaka , Yumiko Okada , Makoto Ohyama , Maki Matsumoto , Masaaki Takahashi , Yasushi Murai , Katsuharu Iinuma , Achim Harder , Norbert Mencke , Gerhard Bonse , Peter Jeschke
发明人： Osamu Sakanaka , Yumiko Okada , Makoto Ohyama , Maki Matsumoto , Masaaki Takahashi , Yasushi Murai , Katsuharu Iinuma , Achim Harder , Norbert Mencke , Gerhard Bonse , Peter Jeschke
IPC分类号： A61K3812
CPC分类号： C07D273/00 , Y02P20/55
摘要： Novel derivatives of PF1022 substance, which are cyclodepsipeptides represented by the general formula (I) shown below or their salts are useful as anthelmintic agent for prevention or treatment of parasitic infections.
摘要翻译： PF1022物质的新型衍生物，其为由下述通式（I）表示的环缩缩肽或其盐，可用作预防或治疗寄生虫感染的驱肠剂。

5. 发明授权

US06265537B1 Thiodepsipeptides for combating endoparasites and a method for producing the same 失效
标题翻译：用于抵抗内寄生虫的硫代肽类及其制备方法
公开(公告)号：US06265537B1
公开(公告)日：2001-07-24
申请号：US09381946
申请日：1999-09-27
申请人： Peter Jeschke , Achim Harder , Georg von Samson-Himmelstjerna , Norbert Mencke , Gerhard Bonse , Katsuharu Iinuma , Osamu Sakanaka
发明人： Peter Jeschke , Achim Harder , Georg von Samson-Himmelstjerna , Norbert Mencke , Gerhard Bonse , Katsuharu Iinuma , Osamu Sakanaka
IPC分类号： C07K506
CPC分类号： C07D273/00 , C07D407/12 , C07D407/14 , C07D413/14
摘要： The present invention relates to cyclic thiodepsipeptides, in particular 18 to 24-membered cyclothiodepsipeptides, their endoparasitical compositions, and methods of making and using the same.
摘要翻译：本发明涉及环状硫代脂肽，特别是18至24元环磺酸肽，其内在政治组合物及其制备和使用方法。

6. 发明授权

US6033879A Process for the preparation of substituted aryl lactic acid containing cyclodepsipeptides with 24 ring atoms 失效
标题翻译：制备具有24个环原子的含有缩水甘油酯的取代芳基乳酸的方法
公开(公告)号：US6033879A
公开(公告)日：2000-03-07
申请号：US077913
申请日：1998-06-04
申请人： Peter Jeschke , Gerhard Bonse , Gerhard Thielking , Winfried Etzel , Achim Harder , Norbert Mencke , Horst Kleinkauf , Rainer Zocher , Katsuharu Iinuma , Kouichi Miyamoto
发明人： Peter Jeschke , Gerhard Bonse , Gerhard Thielking , Winfried Etzel , Achim Harder , Norbert Mencke , Horst Kleinkauf , Rainer Zocher , Katsuharu Iinuma , Kouichi Miyamoto
IPC分类号： C12P21/02 , C07D273/00 , C07K11/00 , C12P1/00 , C12P17/14 , C12R1/645 , C12P21/04 , C12P1/02
CPC分类号： C07D273/00 , C12P1/00 , C12P17/14 , Y10S435/911
摘要： The present invention relates to a new process for the preparation of substituted aryllactic acid-containing cyclodepsipeptides having 24 ring atoms of the formula (I): ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 have the meaning given in the description,with the aid of fungal strains of the species Agonomycetales or enzymatic preparations isolated therefrom.
摘要翻译： PCT No.PCT / EP96 / 05190 Sec。 371日期：1998年6月4日 102（e）1998年6月4日PCT PCT 1996年11月25日PCT公布。出版物WO97 / 20945 日期：1997年6月12日本发明涉及具有式（I）的24个环原子的具有取代芳基乳酸的环缩缩肽的新方法：其中R1，R2，R3，R4具有在说明书中给出的含义借助于种属Agonomycetales的真菌菌株或从其分离的酶制剂。

7. 发明授权

US5821222A Cyclic depsipeptides having 18 ring atoms for combating endoparasites 失效
标题翻译：具有18个环原子的环状脱肽用于对抗内寄生虫
公开(公告)号：US5821222A
公开(公告)日：1998-10-13
申请号：US728106
申请日：1996-10-09
申请人： Gerhard Bonse , Michael Londershausen , Erwin Bischoff , Hartwig Muller , Achim Harder , Nobert Mencke , Peter Kurka , Peter Jeschke , Jurgen Scherkenbeck
发明人： Gerhard Bonse , Michael Londershausen , Erwin Bischoff , Hartwig Muller , Achim Harder , Nobert Mencke , Peter Kurka , Peter Jeschke , Jurgen Scherkenbeck
IPC分类号： A61K31/395 , A61P31/00 , A61P33/00 , C07C227/18 , C07C229/06 , C07C229/12 , C07C229/14 , C07C229/22 , C07C229/34 , C07C231/02 , C07C233/36 , C07C235/12 , C07C271/22 , C07D273/00 , A61K38/15 , C07K11/02
CPC分类号： C07D273/00 , C07C229/12 , C07C229/14 , C07C235/12 , C07C271/22
摘要： The present invention relates to the use of cyclic depsipeptides having 18 ring atoms of the general formula (I) ##STR1## in which R.sup.1 to R.sup.6 have the meaning given in the description, and to their optical isomers and racemates, in medicine and veterinary medicine for combating endoparasites, to their preparation, and to new cyclic depsipeptides having 18 ring atoms.
摘要翻译：本发明涉及具有通式（I）的具有18个环原子的环状缩水甘油酯的用途，其中R1至R6具有说明书中给出的含义，以及其在医学上的旋光异构体和外消旋体以及用于对抗内寄生虫及其制备的兽药，以及具有18个环原子的新的环状缩肽。

8. 发明授权

US5624897A Cyclic depsipeptides having 18 ring atoms, and their use for combating endoparasites 失效
标题翻译：具有18个环原子的环状缩肽，以及它们用于对抗内寄生虫的用途
公开(公告)号：US5624897A
公开(公告)日：1997-04-29
申请号：US353409
申请日：1994-12-09
申请人： Peter Jeschke , Jurgen Scherkenbeck , Gerhard Bonse , Erwin Bischoff , Norbert Mencke , Achim Harder , Michael Londershausen , Hartwig Muller
发明人： Peter Jeschke , Jurgen Scherkenbeck , Gerhard Bonse , Erwin Bischoff , Norbert Mencke , Achim Harder , Michael Londershausen , Hartwig Muller
IPC分类号： A01N43/72 , A61K31/395 , A61K38/00 , A61P33/00 , A61P33/10 , C07D273/00 , C07K11/02 , A61K38/15
CPC分类号： C07D273/00
摘要： New cyclic depsipeptides having 18 ring atoms, of the general formula (I) ##STR1## in which R represents hydrogen, straight-chain or branched or cyclic alkyl having up to 8 carbon atoms, and their optical isomers and racemates,and their use for combating endoparasites in the field of medicine and veterinary medicine.
摘要翻译：具有18个环原子的具有18个环原子的具有通式（I）的化合物（I）其中R表示氢，具有至多8个碳原子的直链或支链或环状烷基及其旋光异构体和外消旋物，以及它们用于打击医药和兽医领域的内寄生虫。

9. 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。

10. 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。

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