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1. 发明授权

US4762830A 5-(azolyloxyphenylcarbamoyl)barbituric acid derivatives as anthelmintics 失效
标题翻译： 5-（阿唑酰氧基苯基氨基甲酰基）巴比妥酸衍生物作为驱肠虫剂
公开(公告)号：US4762830A
公开(公告)日：1988-08-09
申请号：US830430
申请日：1986-02-13
申请人： Elmar Sturm , Jean J. Gallay , Haukur Kristinsson , Georg Pissiotas
发明人： Elmar Sturm , Jean J. Gallay , Haukur Kristinsson , Georg Pissiotas
IPC分类号： C07D263/58 , A61K31/496 , A61K31/515 , A61P33/10 , C07D233/70 , C07D235/26 , C07D239/62 , C07D239/66 , C07D249/08 , C07D249/12 , C07D271/06 , C07D271/10 , C07D271/113 , C07D277/24 , C07D277/34 , C07D277/58 , C07D277/68 , C07D285/08 , C07D285/12 , C07D285/13 , C07D403/12 , C07D413/12 , C07D417/12 , A61K31/505 , C07D403/10
CPC分类号： C07D271/113 , C07D233/70 , C07D239/62 , C07D239/66 , C07D249/12 , C07D277/34 , C07D277/58 , C07D277/68 , C07D285/08 , C07D285/13 , C07D413/12 , C07D417/12
摘要： The invention relates to novel 5-(azolyloxyphenylcarbamoyl)barbituric acid derivatives of the general formula I ##STR1## wherein X is oxygen or sulfur;R.sub.1 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.6 cycloalkyl or allyl;R.sub.2 is C.sub.1 -C.sub.6 alkyl or allyl;R.sub.3 is an unsubstituted or substituted five-membered azole ring which is bound through carbon and is selected from the group consisting of benzimadazole, benzoxazole, benzothiazole, imidazole, oxazole, thiazole, oxadiazole, thiadiazole and triazole; andR.sub.4 and R.sub.5 are each independently of the other hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 haloalkoxy;and to the tautomers and salts thereof, as anthelmintic compounds. Together with suitable carriers and further assistants, these compounds may be used in particular for controlling helminths which are parasites of animals.
摘要翻译：本发明涉及通式I（I）的新的5-（azolyloxyphenylcarbamoyl）巴比土酸衍生物，其中X是氧或硫; R1是C1-C6烷基，C1-C6烷氧基，C3-C6环烷基或烯丙基; R2是C1-C6烷基或烯丙基; R3是通过碳结合的未取代或取代的五元唑环，选自苯并咪唑，苯并恶唑，苯并噻唑，咪唑，恶唑，噻唑，恶二唑，噻二唑和三唑; 并且R 4和R 5各自独立地为另一个氢，C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6烷氧基或C 1 -C 6卤代烷氧基; 和其互变异构体和盐，作为驱肠剂化合物。与合适的载体和进一步助剂一起，这些化合物可特别用于控制作为动物寄生虫的蠕虫。

2. 发明授权

US4753940A Barbituric acid derivatives 失效
标题翻译：巴比妥酸衍生物
公开(公告)号：US4753940A
公开(公告)日：1988-06-28
申请号：US827118
申请日：1986-02-07
申请人： Elmar Sturm , Jean J. Gallay , Georg Pissiotas
发明人： Elmar Sturm , Jean J. Gallay , Georg Pissiotas
IPC分类号： A61K31/515 , A61K31/517 , A61K31/53 , A61P33/00 , A61P33/10 , C07D215/20 , C07D215/22 , C07D215/227 , C07D237/00 , C07D237/14 , C07D237/16 , C07D237/32 , C07D239/34 , C07D239/56 , C07D239/62 , C07D239/66 , C07D239/80 , C07D239/88 , C07D241/18 , C07D241/44 , C07D251/34 , C07D251/38 , C07D251/42 , C07D401/12 , C07D403/12 , A61K31/495 , C07D253/04 , C07D403/10
CPC分类号： C07D215/227 , C07D237/14 , C07D237/16 , C07D239/34 , C07D239/56 , C07D239/62 , C07D239/66 , C07D241/18 , C07D241/44 , C07D251/34 , C07D251/38 , C07D251/42 , C07D401/12 , C07D403/12
摘要： The invention relates to novel phenylcarbamoylbarbituric acid derivatives of the general formula ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.3 alkoxy, allyl or C.sub.3 -C.sub.6 cycloalkyl,R.sub.2 is C.sub.1 -C.sub.4 alkyl or allyl,R.sub.3 is an unsubstituted or substituted heteroaromatic 6-membered ring which contains 2 or 3 nitrogen atoms, or is an unsubstituted or substituted heteroaromatic 6-membered ring which is fused to a benzene ring and which contains 1 to 3 nitrogen atoms,R.sub.4 and R.sub.5 are each independently of the other hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.3 haloalkyl andX is an oxygen or sulfur atom,and to the tautomers and salts thereof.These compounds may be used for controlling helminths which are parasites of animals.
摘要翻译：本发明涉及通式为：其中R 1为C 1 -C 4烷基，C 1 -C 3烷氧基，烯丙基或C 3 -C 6环烷基，R 2为C 1 -C 4烷基或烯丙基的新型苯基氨基甲酰基巴比妥酸衍生物，R 3为未取代或未取代的含有2或3个氮原子的取代的杂芳族六元环，或者是未被取代或取代的杂芳族六元环，其与苯环稠合并且含有1至3个氮原子，R 4和R 5各自独立地为氢，C 1 -C 4烷基，C 1 -C 4烷氧基或C 1 -C 3卤代烷基，X是氧或硫原子，以及其互变异构体和盐。这些化合物可用于控制作为动物寄生虫的蠕虫。

3. 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。

4. 发明授权

US4670441A Thiobarbituric acid derivatives and their use as anthelminthics 失效
标题翻译：硫代巴比妥酸衍生物及其作为抗凝药物的用途
公开(公告)号：US4670441A
公开(公告)日：1987-06-02
申请号：US751715
申请日：1985-07-05
申请人： Manfred Kuhne , Jean J. Gallay
发明人： Manfred Kuhne , Jean J. Gallay
IPC分类号： C07D213/64 , A61K31/505 , A61K31/515 , A61P33/10 , C07C65/24 , C07C265/12 , C07D213/643 , C07D239/66 , C07D401/12 , C07D239/68
CPC分类号： C07D213/643 , C07C265/12 , C07C65/24 , C07D239/66 , C07D401/12
摘要： The invention relates to novel 5-phenylcarbamoylthiobarbituric acid derivatives of the general formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently C.sub.1 -C.sub.5 alkyl or methoxy,R.sub.3 is unsubstituted phenyl, unsubstituted pyridyl, or phenyl which is substituted by 1 to 3 identical or different members selected from the group consisting of C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.4 cyanoalkyl, halogen, nitro and C.sub.1 -C.sub.5 haloalkyl containing 1 to 5 halogen atoms, or is pyridyl which is substituted by 1 to 3 identical or different members selected from the group consisting of C.sub.1 -C.sub.5 alkyl, halogen, nitro and C.sub.1 -C.sub.5 haloalkyl containing 1 to 5 halogen atoms andR.sub.4 and R.sub.5 are each independently hydrogen, halogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.2 haloalkyl containing 1 to 3 halogen atoms, or are C.sub.1 -C.sub.3 -alkoxy or nitro,and to the tautomers and salts thereof, as anthelmintics.The compounds may be used by themselves or together with suitable carriers and further adjuvants for controlling helminths which are parasites of animals.
摘要翻译：本发明涉及通式为：其中R 1和R 2各自独立地为C 1 -C 5烷基或甲氧基，R 3为未取代的苯基，未被取代的吡啶基或被1位取代的苯基的新的5-苯基氨基甲酰硫代巴比妥酸衍生物至3个选自C 1 -C 5烷基，C 1 -C 4氰基烷基，卤素，硝基和含有1至5个卤原子的C 1 -C 5卤代烷基的相同或不同的成员，或者是被1至3个相同或不同的成员所取代的吡啶基，由C1-C5烷基，卤素，硝基和含有1-5个卤素原子的C1-C5卤代烷基组成的组，R4和R5各自独立地为氢，卤素，C1-C5烷基，含1-3个卤素原子的C1-C2卤代烷基，或C1- C3-烷氧基或硝基，以及其互变异构体和盐，作为驱肠虫剂。这些化合物本身或与合适的载体一起使用，以及用于控制作为动物寄生虫的蠕虫的另外的辅助剂。

5. 发明授权

US4511567A 6-[(4-Substituted piperazin-l-yl)thiocarbonylamino]benzazoles and their use 失效
标题翻译： 6 - [（4-取代的哌嗪-1-基）硫代羰基氨基]苯并唑及其用途
公开(公告)号：US4511567A
公开(公告)日：1985-04-16
申请号：US418955
申请日：1982-09-16
申请人： Jean J. Gallay , Ernst Schweizer
发明人： Jean J. Gallay , Ernst Schweizer
IPC分类号： A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/495 , A61K31/496 , A61P33/10 , C07D235/06 , C07D235/08 , C07D235/10 , C07D263/56 , C07D277/64 , C07D277/66 , C07D417/12 , C07D413/12
CPC分类号： C07D263/56 , C07D235/08 , C07D235/10 , C07D277/64
摘要： The invention relates to a process for the manufacture of novel benzazole derivatives of the formula I ##STR1## in which R.sub.1 represents an optionally 4-substituted piperazino group or a group of the formula R.sub.2 --alk--X.sub.2 --,R.sub.2 represents optionally esterified carboxy or represents hydroxymethyl,alk represents lower alkylene or lower alkylidene,X.sub.1 and X.sub.2, independently of one another, each represents oxygen or sulphur,Ph represents 1,2-phenylene optionally substituted as well as by the group R.sub.1 --C(.dbd.X.sub.1)--NH--,X.sub.3 represents oxygen, sulphur or optionally substituted imino, andR.sub.3 represents optionally fluorine-substituted lower alkyl or cycloalkyl,and their salts.The compounds of the formula I, which have proved to be excellent micro- and macrofilaricides and schistosomacides, are manufactured according to methods known per se.
摘要翻译：本发明涉及一种制备式I（I）的新的苯并唑衍生物的方法，其中R 1表示任选的4-取代的哌嗪子基或式R2-alk-X2-的基团，R2代表任选地酯化羧基或代表羟甲基，烷基代表低级亚烷基或低级亚烷基，X 1和X 2各自独立地表示氧或硫，Ph表示可以被取代的1,2-亚苯基以及R1-C（= X1 ）-NH-，X3表示氧，硫或任选取代的亚氨基，R 3表示任选氟取代的低级烷基或环烷基，及其盐。根据本身已知的方法制备已证明是优异的微米和大型杀丝菌剂和血吸虫病剂的式I化合物。

6. 发明授权

US4748178A 5-(pyridyloxy- or pyridylthio-phenyl)carbamoyl barbituric acid derivatives 失效
标题翻译： 5-（吡啶氧基 - 或吡啶基硫基 - 苯基）氨基甲酰基巴比妥酸衍生物
公开(公告)号：US4748178A
公开(公告)日：1988-05-31
申请号：US829589
申请日：1986-02-13
申请人： Urs Burckhardt , Jean J. Gallay , Manfred Kuhne
发明人： Urs Burckhardt , Jean J. Gallay , Manfred Kuhne
IPC分类号： C07D239/62 , A01N20060101 , A01N43/54 , A23K1/16 , A61K20060101 , A61K31/515 , A61P33/00 , A61P33/10 , C07D20060101 , C07D213/00 , C07D239/00 , C07D401/12 , C07D405/12 , A61K31/495 , C07D401/10
CPC分类号： C07D401/12 , A01N43/54 , C07D239/62
摘要： Novel phenylcarbamoylbarbituric acid derivatives of the general formula I ##STR1## and tautomeric forms and salts thereof in which R.sub.1 and R.sub.2 independently of one another are C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.3 -alkoxy, C.sub.3 -C.sub.6 -cycloalkyl, allyl or phenyl; R.sub.3 is substituted or unsubstituted pyridyl as herein defined; and X is oxygen or sulfur; they possess anthelmintic activity. The active substances can be employed in conjunction with suitable carriers and further adjuncts for controlling zooparasitic helminths.
摘要翻译：新的通式I的苯基氨基甲酰基巴比妥酸衍生物，其中R 1和R 2彼此独立地是C 1 -C 5 - 烷基，C 1 -C 3 - 烷氧基，C 3 -C 6 - 环烷基，烯丙基或苯基; R 3是如本文定义的取代或未取代的吡啶基; X为氧或硫; 他们具有驱虫活动。活性物质可以与合适的载体一起使用，另外还可用于控制火山喷发蠕虫。

7. 发明授权

US4602912A Mothproofing and beetleproofing composition: 5-(pyridyloxy- or thiothenylcarbamoyl)barbituric acid 失效
标题翻译：防虫和防虫组合物：5-（吡啶氧基 - 或硫代苯基氨基甲酰基）巴比妥酸
公开(公告)号：US4602912A
公开(公告)日：1986-07-29
申请号：US748282
申请日：1985-06-24
申请人： Bernardo de Sousa , Urs Burckhardt , Jean J. Gallay , Manfred Kuhne , Ernst Beriger , Dieter Reinehr
发明人： Bernardo de Sousa , Urs Burckhardt , Jean J. Gallay , Manfred Kuhne , Ernst Beriger , Dieter Reinehr
IPC分类号： A01N43/54 , A01N53/00 , A01N53/08 , A01N57/00 , D06M16/00 , A23F3/34 , D06M3/00 , D06P5/00
CPC分类号： D06M16/006 , A01N53/00 , Y10S8/917
摘要： The invention relates to a composition for protecting keratinous material, in particular woollen textiles, from attack by pests that feed on keratin, in particular moth and beetle larvae, which composition contains, as active ingredient combination, a specifically substituted 5-(pyridyloxyphenylcarbamoyl)barbituric acid or a salt thereof and a synthetic pyrethroid, as well as to a process comprising the use of this active ingredient combination for providing said material with a protective finish against attack by pests that feed on keratin.
摘要翻译：本发明涉及一种用于保护角质材料，特别是羊毛纺织物的组合物，不受角蛋白侵害的害虫特别是蛾和甲虫幼虫的攻击，该组合物含有作为活性成分组合的特异性取代的5-（吡啶基氧基苯基氨基甲酰基）巴比妥酸或其盐和合成拟除虫菊酯，以及包括使用这种活性成分组合的方法来提供所述材料具有防止食用角蛋白的害虫的保护作用。

8. 发明授权

US4428957A 6-Isothiocyano-5-methoxy-2-tert.-butylbenzthiazole and a method of controlling ruminant liver flukes therewith 失效
标题翻译： 6-异硫氰酸-5-甲氧基-2-叔丁基苯并噻唑及其反刍动物肝吸虫的防治方法
公开(公告)号：US4428957A
公开(公告)日：1984-01-31
申请号：US260651
申请日：1981-05-04
申请人： Joseph C. Boray , Jean J. Gallay , Gedeon Sarasin
发明人： Joseph C. Boray , Jean J. Gallay , Gedeon Sarasin
IPC分类号： C07D277/64 , A61K31/425
CPC分类号： C07D277/64
摘要： The isothiocyanobenzothiazole derivative of the formula ##STR1## and also salts thereof nontoxic to warm-blooded animals have, besides generally good anthelmintic properties, especially a particularly pronounced action against filariasis, schistosomiasis and gastrointestinal helminths in warm-blooded organisms and equally against liver flukes in sheep. The active substance, together with suitable carriers and additives, is administered perorally or via the abomasum, in the form of solutions, emulsions, suspensions, powders, tablets, boluses and capsules.
摘要翻译：除了通常具有良好的驱虫特性之外，式“IMAGE”的异硫氰酸苯并噻唑衍生物以及对温血动物无毒的盐尤其是对温血生物中的丝虫病，血吸虫病和胃肠蠕虫特别明显的作用，同样地抗肝吸虫羊。活性物质与合适的载体和添加剂一起以溶液，乳剂，悬浮液，粉末，片剂，丸剂和胶囊的形式经口或经由皱胃施用。

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