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91. 发明授权

US4916120A Parasiticidal avermectin derivatives 失效
标题翻译：杀虫剂阿维菌素衍生物
公开(公告)号：US4916120A
公开(公告)日：1990-04-10
申请号：US230221
申请日：1988-08-01
申请人： Wolfgang Roben , Stendel Wilhelm , Peter Andrews
发明人： Wolfgang Roben , Stendel Wilhelm , Peter Andrews
IPC分类号： C07D493/22 , A61K31/365 , A61P33/00 , C07H17/08 , C07H19/01
CPC分类号： C07H19/01
摘要： Parasiticidally active avermectin derivatives of the formula ##STR1## in which R.sup.1 stands for hydrogen, OH, C.sub.1-5 -alkanoyloxy, .alpha.-L-oleandrosyloxy, .alpha.-L-oleandrosyl-.alpha.-L-oleandrosyloxy, 4'-C.sub.1-5 -alkanoyl-.alpha.-oleandrosyloxy or 4"-C.sub.1-5 -alkanoyl-.alpha.-L-oleandrosyl-.alpha.-L-oleandrosyloxy,R.sup.2 stands for hydrogen, OH, C.sub.1-5 -alkanoyloxy, or R.sup.2 stands for hydrogen when there is a double bond between C22 and C23,R.sup.3 stands for straight-chain or branched alkyl or alkenyl, andR.sup.4 stands for hydrogen, OH, C.sub.1-5 -alkanoyloxy, heterocyclylcarbonyloxy, or the bond between the C atoms C22 and C23 is a single or a double bond and the double bond of the cyclohexene ring can be between the C atoms C3 and C4 or between the C atoms C4 and C5.
摘要翻译：其中R1代表氢，OH，C1-5-烷酰氧基，α--L-烯丙基氧基，α-L-胆烷酰基-α-胆碱硫代酰氧基，4'-C1-5的分子式活性阿维菌素衍生物 - 烷酰基-α-链烷氧基或4'-“C 1 -C 5 - 烷酰基-α-L-胆烷酰基-α-胆碱酰氧基，R2代表氢，OH，C1-5-烷酰氧基，或当R2代表氢 C22和C23之间的双键，R3表示直链或支链烷基或烯基，R4表示氢，OH，C1-5-烷酰氧基，杂环基羰基氧基，或C原子之间的键C22和C23是单或双键并且环己烯环的双键可以在C原子C3和C4之间或C原子C4和C5之间。

92. 发明授权

US4914124A N-organooxycarbamic acid esters for combating endoparasites 失效
标题翻译： N-有机氧基氨基甲酸酯，用于抵抗内寄生虫
公开(公告)号：US4914124A
公开(公告)日：1990-04-03
申请号：US147469
申请日：1988-01-25
申请人： Nikolaus Muller , Peter Andrews
发明人： Nikolaus Muller , Peter Andrews
IPC分类号： A01N47/10 , A01N47/24 , A61K31/27 , A61K31/325 , C07C20060101
CPC分类号： C07C291/04 , A61K31/27
摘要： A method of combating endoparasites which comprises applying thereto or to an endoparasite habitat an endoparasiticidally effective amount of an N-organooxycarbamic acid ester of the formula ##STR1## in which R.sup.1 represents alkyl, cycloalkyl, alkenyl, alkinyl or aryl, which can optionally be substituted,R.sup.2 represents alkyl, alkenyl or alkinyl, which can optionally be substituted, andR.sup.3 represents alkyl, alkenyl or alkinyl, which can optionally be substituted.Those compounds wherein one of R.sup.2 and R.sup.3 is alkinyl are new.
摘要翻译：一种对付内寄生虫的方法，其包括向其内施用或内寄生物栖息地，其为内分泌有效量的式I的N-有机氧基氨基甲酸酯，其中R 1表示烷基，环烷基，烯基，炔基或芳基，其可任选地为取代的，R 2表示烷基，烯基或炔基，其可任选地被取代，并且R 3表示可任选被取代的烷基，烯基或炔基。其中R2和R3之一是炔基的那些化合物是新的。

93. 发明授权

US4287199A Benzimidazolylcarbamic acid esters substituted on the benzenoid nucleus by an oxy or thio substituent 失效
标题翻译：苯并咪唑基氨基甲酸酯通过氧基或硫取代基取代在苯环上
公开(公告)号：US4287199A
公开(公告)日：1981-09-01
申请号：US83883
申请日：1979-10-11
申请人： Hartmund Wollweber , Heinrich Kolling , Herbert Thomas , Peter Andrews
发明人： Hartmund Wollweber , Heinrich Kolling , Herbert Thomas , Peter Andrews
IPC分类号： A61K31/415 , A61K31/4184 , A61P33/10 , C07D235/32 , C07D401/12 , C07D403/12 , A61K31/445
CPC分类号： C07D235/32
摘要： The invention relates to 2-benzimidazolylcarbamic acid esters, substituted on the benzenoid nucleus by an aminoalkoxy, aminoalkylthio, an aminoalkylsulphinyl or an aminoalkylsulphonyl grouping. The invention also includes methods for making the compounds of the invention, compositions containing said compounds and the use of said compounds and compositions as anthelminitic agents.
摘要翻译：本发明涉及2-苯并咪唑基氨基甲酸酯，其通过氨基烷氧基，氨基烷硫基，氨基烷基亚磺酰基或氨基烷基磺酰基在苯类核上取代。本发明还包括制备本发明化合物的方法，含有所述化合物的组合物以及所述化合物和组合物作为anthelminitic剂的用途。

94. 发明授权

US4247546A Phosphonylureidobenzene derivatives and their medicinal use 失效
标题翻译：膦酰基脲衍生物及其药用
公开(公告)号：US4247546A
公开(公告)日：1981-01-27
申请号：US967035
申请日：1978-12-06
申请人： Hartmund Wollweber , Herbert Thomas , Peter Andrews
发明人： Hartmund Wollweber , Herbert Thomas , Peter Andrews
IPC分类号： A61K9/00 , A61K31/66 , A61K31/665 , A61K31/67 , A61K31/675 , A61P33/10 , C07F9/24 , C07F9/572 , C07F9/6539 , C07F9/6571 , C07F9/6574 , C07F9/6578 , A01N57/32 , A01N57/22
CPC分类号： C07F9/6539 , A61K31/66 , C07F9/2487 , C07F9/5727 , C07F9/657154
摘要： The invention includes phosphonylureidobenzene compounds of the general formula ##STR1## or pharmaceutically acceptable salts in whichR.sup.1 and R.sup.2 are identical or different and represent an alkyl group, orR.sup.1 and R.sup.2 together represent a dimethylene group, a trimethylene group or a tetramethylene group,X and Y are identical or different and represent an oxygen atom or a sulphur atom andR.sup.3 and R.sup.4 are identical or different and represent an alkyl group, orR.sup.3 and R.sup.4 together represent a trimethylene group or a tetramethylene group, orR.sup.3 and R.sup.4, together with the carbon atom and nitrogen atom between them, form a thiazolidine ring system, which are used medicinally as parasiticides.The compounds are particularly effective in combatting helminths in carnivores.Also included in the invention are pharmaceutical compositions containing said phosphonylureidobenzene compounds and methods for the treatment of warm-blooded animals by administering said compounds or compositions.
摘要翻译：本发明包括通式为（I）的膦酰基脲基化合物或其中R 1和R 2相同或不同并且表示烷基的药学上可接受的盐，或者R 1和R 2一起表示二亚甲基，三亚甲基或四亚甲基基，X和Y相同或不同，表示氧原子或硫原子，R3和R4相同或不同，表示烷基，或R3和R4一起表示三亚甲基或四亚甲基，或R 3和R 4 与它们之间的碳原子和氮原子一起形成噻唑烷环体系，它们在医药上用作杀寄生虫剂。这些化合物特别有效地对抗食肉动物的蠕虫。本发明还包括含有所述膦酰基脲基化合物的药物组合物和通过施用所述化合物或组合物治疗温血动物的方法。

95. 发明授权

US4162319A Ring substituted pyrazino-isoquinoline derivatives and their preparation 失效
公开(公告)号：US4162319A
公开(公告)日：1979-07-24
申请号：US931576
申请日：1978-08-07
申请人： Jurgen Seubert , Rolf Pohlke , Herbert Thomas , Peter Andrews
发明人： Jurgen Seubert , Rolf Pohlke , Herbert Thomas , Peter Andrews
IPC分类号： C07D217/14 , A61K31/495 , C07D401/02 , C07D405/02
CPC分类号： C07D217/14
摘要： Isoquinolines of the formula ##STR1## wherein R.sup.1 is H, OH, alkyl; R.sup.2 is H, or an unsubstituted or substituted carbonyl, carbonyloxy or thiocarbonyl group; R.sup.3 is H, alkyl or hydroxy alkyl; R.sup.4 is H, alkyl or phenyl; R.sup.5 is O, H,H or H and alkyl, phenyl, halo or hydroxy; R.sup.6 and R.sup.7 are optional substituents; and R.sup.8 is H or alkyl, R.sup.2 being a thiocarbonyl or carbonyloxy group when R.sup.1 and R.sup.3 to R.sup.8 are H and X is O; and their physiologically acceptable salts, are antihelmintics, especially against cestodes and trematodes; some also possessing CNS activity, e.g., psychotropic and blood pressure regulating activity.

96. 发明授权

US4120961A Ring substituted pyrazino-isoquinoline derivatives and their preparation 失效
标题翻译：环取代的吡嗪异喹啉衍生物及其制备方法
公开(公告)号：US4120961A
公开(公告)日：1978-10-17
申请号：US817467
申请日：1977-07-20
申请人： Jurgen Seubert , Rolf Pohlke , Herbert Thomas , Peter Andrews
发明人： Jurgen Seubert , Rolf Pohlke , Herbert Thomas , Peter Andrews
IPC分类号： C07D217/14 , A61K31/495 , C07D241/36
CPC分类号： C07D217/14
摘要： Isoquinolines of the formula ##STR1## wherein R.sup.1 is H, OH, alkyl; R.sup.2 is H, or an unsubstituted or substituted carbonyl, carbonyloxy or thiocarbonyl group; R.sup.3 is H, alkyl or hydroxy alkyl; R.sup.4 is H, alkyl or phenyl; R.sup.5 is O, H,H or H and alkyl, phenyl, halo or hydroxy; R.sup.6 and R.sup.7 are optional substituents; and R.sup.8 is H or alkyl, R.sup.2 being a thiocarbonyl or carbonyloxy group when R.sup.1 and R.sup.3 to R.sup.8 are H and X is O; and their physiologically acceptable salts, are antihelmintics, especially against cestodes and trematodes; some also possessing CNS activity, e.g., psychotropic and blood pressure regulating activity.
摘要翻译：其中R 1是H，OH，烷基; R2是H或未取代或取代的羰基，羰基氧基或硫代羰基; R3是H，烷基或羟基烷基; R4是H，烷基或苯基; R5是O，H，H或H，烷基，苯基，卤素或羟基; R6和R7是任选的取代基; 当R 1和R 3至R 8为H且X为O时，R 8为H或烷基，R 2为硫代羰基或羰基氧基; 和它们的生理学上可接受的盐，是抗炎药，特别是针对绦虫和吸虫; 一些还具有CNS活性，例如精神病和血压调节活性。

97. 发明授权

US4114717A Motor vehicle oil drip pan apparatus device for at least indirectly saving lives and accidents on a highway 失效
标题翻译：机动车油滴灌装置装置，至少间接节省公路上的生命和事故
公开(公告)号：US4114717A
公开(公告)日：1978-09-19
申请号：US722887
申请日：1976-09-13
申请人： Peter Andrews
发明人： Peter Andrews
IPC分类号： F16N31/00 , B62D25/20
CPC分类号： F16N31/006
摘要： A substantially skidpan apparatus device of which at least one portion thereof is hooked and/or removably secured to at least one cross member or to at least one other structural portion of a first type of motor vehicle of the race car, automobile or car, truck and bus type. At least one portion of oil or fluid drippings which have dripped from at least one portion of the above disclosed motor vehicles are retained therein. The apparatus device is also for specific use in a boat type of non-highway used motor vehicle to prevent at least one portion of th inland waters from being oil polluted. The oil or fluid drippings being generally captured and retained in at least one portion of a fluid retaining receptacle portion of the apparatus device and/or at least one portion of a separate material or a nestable receptacle which may be retained in the fluid retaining receptacle portion of the apparatus device. A roadway's, race track's, highway's (car, truck and bus) motor vehicle travelling surface is thereby substantially prevented from "summer icing" of the disclosed motor vehicles traveled surfaces and "viscous hydroplaning" of the motor vehicle's tires thereon, is substantially prevented at and especially when the four first type of motor vehicle's are abruptly started, stopped, curving or curving in and out at a high rate of speed or even merely traveling at a very high rate of speed.
摘要翻译：一种基本的防滑装置，其至少一部分被钩住和/或可移除地固定到赛车，汽车或汽车，卡车的至少一个横向构件或至少一个其他结构部分的第一类型的机动车辆和总线类型。从上述公开的机动车辆的至少一部分滴下的至少一部分油或液体滴落物被保留在其中。装置装置还用于特定用于非公路二级汽车的船型，以防止内陆水域的至少一部分被油污染。油或液体滴液通常被捕获并保持在装置装置的流体保持容纳部分的至少一部分中和/或可以保持在流体保持容纳部分中的单独材料或可嵌套的容器的至少一部分的装置装置。因此，基本上防止了道路，赛道，高速公路（汽车，卡车和公共汽车）机动车辆行驶表面上的摩托车行驶表面的“夏季结冰”和机动车辆的轮胎的“粘性滑水” 特别是当四种第一类型的机动车辆以高速率突然起动，停止，弯曲或弯曲时，甚至仅以非常高的速度行驶时。

98. 发明授权

US4015012A 4-Acylaminophenylacetamidines and a method for their preparation 失效
标题翻译： 4-酰氨基苯基乙酰胺及其制备方法
公开(公告)号：US4015012A
公开(公告)日：1977-03-29
申请号：US579446
申请日：1975-05-21
申请人： Hartmund Wollweber , Ekkehard Niemers , Hans Peter Schulz , Herbert Thomas , Peter Andrews
发明人： Hartmund Wollweber , Ekkehard Niemers , Hans Peter Schulz , Herbert Thomas , Peter Andrews
IPC分类号： A61K31/155 , A61K31/165
CPC分类号： A61K31/155
摘要： New 4-acylaminophenylacetamidines of the formula: ##STR1## in which R is a straight or branched chain alkoxyalkyl having 3 to 8 carbon atoms or straight or branched chain alkenyloxyalkyl having 3 to 8 carbon atoms wherein the alkoxy moiety or alkenyloxy moiety may substituted by alkoxy or phenyl, and including the non-toxic pharmacologically acceptable salts thereof. The products have utility as parasiticides.The products are obtained by either of two methods: (1) via the reaction of an N'-(4-aminophenyl)-N,N-dimethylacetamidine with an acylating agent or (2) via the reaction of a 4-acylaminoaniline with an N,N-dimethylacetamide or N,N-dimethylthioacetamide.
摘要翻译：新的具有3-8个碳原子的直链或支链烷氧基烷基或具有3-8个碳原子的直链或支链链烯氧基烷基的4-氨基苯基乙酰胺，其中R是具有3-8个碳原子的直链或支链烷氧基烷基，其中烷氧基部分或烯氧基部分可被烷氧基取代或苯基，并且包括其无毒的药理学上可接受的盐。该产品具有作为杀寄生虫剂的作用。

99. 发明授权

US3993760A Pyrazinoisoquinolines as anthelmintic agents 失效
标题翻译：吡嗪异喹啉作为驱肠剂
公开(公告)号：US3993760A
公开(公告)日：1976-11-23
申请号：US481792
申请日：1974-06-21
申请人： Rolf Pohlke , Friedrich Loebich , Jurgen Seubert , Herbert Thomas , Peter Andrews
发明人： Rolf Pohlke , Friedrich Loebich , Jurgen Seubert , Herbert Thomas , Peter Andrews
IPC分类号： C07D217/14 , C07D471/04 , A61K31/495
CPC分类号： C07D471/04 , C07D217/14
摘要： (-)-2-Benzoyl-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline is prepared by benzoylation of (-)-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline, or cyclization of a compound of the formula ##SPC1##Wherein X is F, Cl, Br, I or O-tosyl and which has the optical configuration of the final product, or cyclization of a compound of the formula ##SPC2## wherein Y is OH, alkoxy, F, Cl, Br or I under HY-removing reaction conditions and which has the optical configuration of the final product, which is an anthelmintic.
摘要翻译：（ - ） - 2-苯甲酰基-4-氧代-1,2,3,6,7,11b-六氢-4H-吡嗪并[2,1-a]异喹啉线是通过（ - ） - 4-氧代 -1,2,3,6,7,11b-六氢-4H-吡嗪并[2,1-a]异喹啉，或式WHEREIN X的化合物与F，Cl，Br，I或O-甲苯磺酰基和其具有最终产物的光学构型，或在HY-去除反应条件下环化下式化合物其中Y是OH，烷氧基，F，Cl，Br或I，并且具有最终产物的光学构型，其中是一个驱魔。

100. 发明授权

US3970699A 4-Acylaminophenylacetamidines and a method for their preparation 失效
标题翻译： 4-酰氨基苯基乙酰胺及其制备方法
公开(公告)号：US3970699A
公开(公告)日：1976-07-20
申请号：US505738
申请日：1974-09-13
申请人： Hartmund Wollweber , Ekkehard Niemers , Hans Peter Schulz , Herbert Thomas , Peter Andrews
发明人： Hartmund Wollweber , Ekkehard Niemers , Hans Peter Schulz , Herbert Thomas , Peter Andrews
IPC分类号： A61K31/165 , A61K31/155 , A61P33/10 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C239/00 , C07C257/14 , C07C257/20 , C07C103/34
CPC分类号： A61K31/155
摘要： New 4-acylaminophenylacetamidines of the formula: ##SPC1##In which R is a straight or branched chain alkoxyalkyl having 3 to 8 carbon atoms or straight or branched chain alkenyloxyalkyl having 3 to 8 carbon atoms wherein the alkoxy moiety or alkenyloxy moiety may substituted by alkoxy or phenyl, and including the non-toxic pharmacologically acceptable salts thereof. The products have utility as parasiticides.The products are obtained by either of two methods: (1) via the reaction of an N'-(4-aminophenyl)-N,N-dimethylacetamidine with an acylating agent or (2) via the reaction of a 4-acylaminoaniline with an N,N-dimethylacetamide or N,N-dimethylthioacetamide.
摘要翻译：新的4-酰基氨基苯基乙酰胺的下式：

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