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1. 发明授权

US4611060A Intermediate(1,3-benzothiazol-2H-yl or 1,3-benzoxazol-2H-yl)4-oxy-or 4-thio-phenylurea derivatives 失效
标题翻译：中间体（1,3-苯并噻唑-2H-基或1,3-苯并恶唑-2H-基）4-氧基或4-硫代 - 苯基脲衍生物
公开(公告)号：US4611060A
公开(公告)日：1986-09-09
申请号：US784402
申请日：1985-10-04
申请人： Axel Haberkorn , Heinrich Kolling , Toyohiko Kume , Shinpei Kuyama
发明人： Axel Haberkorn , Heinrich Kolling , Toyohiko Kume , Shinpei Kuyama
IPC分类号： A23K1/16 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/53 , A61P33/02 , C07D263/58 , C07D277/68 , C07D277/74 , C07D413/12 , C07D417/12
CPC分类号： C07D413/12 , C07D417/12
摘要： 1-[-(Benzothia- or -oxazol-2-ylthio- or -2-yloxy)phenyl]-1,3,5-triazine-2,4,6(1H,3H,5H)-triones of the formula ##STR1## in which R is lower alkyl,R.sup.1 and R.sup.2 each independently is hydrogen, halogen, alkyl or alkoxy,R.sup.3 and R.sup.4 each independently is hydrogen, halogen, alkyl, alkoxy, alkylthio, fluoroalkyl, fluoroalkoxy or fluoroalkylthio, andX and Y each independently is sulphur or oxygen,or salts thereof, combat coccidioses, especially in poultry.
摘要翻译： 1 - [ - （苯并噻唑基 - 或 - 恶唑-2-基硫基 - 或-2-基氧基）苯基] -1,3,5-三嗪-2,4,6（1H，3H，5H） - 三 IMAGE>其中R是低级烷基，R 1和R 2各自独立地是氢，卤素，烷基或烷氧基，R 3和R 4各自独立地是氢，卤素，烷基，烷氧基，烷硫基，氟代烷基，氟代烷氧基或氟代烷硫基，X和Y各自独立地是硫或氧，或其盐，对抗球虫，特别是家禽。

2. 发明授权

US4005123A Substituted phenylisothioureas and processes for their preparation and use 失效
标题翻译：取代苯基异硫脲及其制备和使用方法
公开(公告)号：US4005123A
公开(公告)日：1977-01-25
申请号：US595040
申请日：1975-07-11
申请人： Heinrich Kolling , Herbert Thomas , Arno Widdig , Hartmund Wollweber
发明人： Heinrich Kolling , Herbert Thomas , Arno Widdig , Hartmund Wollweber
IPC分类号： A61K31/17 , A61K31/155 , C07C67/00 , C07C325/00 , C07C335/38 , C07C149/40
CPC分类号： C07C335/38
摘要： N-[2-(Substituted amido)phenyl]-N'-carbonyl-S-substituted isothioureas bearing an optionally substituted phenoxy, phenylthio, phenylsulfinyl or phenylsulfonyl group in the 4- or 5-position of the 2-(substituted amido)-phenyl group are anthelmintic agents. The compounds, of which N-(2-acetamido-4-phenoxyphenyl)-N'-carbomethoxy-S-methylthiourea is a typical example, are prepared through the reaction of S-substituted N-(mercaptohalomethylene)carbamic acid ester and an apropriately substituted 2-aminoanilide, or through alkylation of the corresponding S-unsubstituted thiourea.
摘要翻译：在2-（取代的酰胺基） - 苯并噻唑的4-或5-位上带有任选取代的苯氧基，苯硫基，苯基亚磺酰基或苯基磺酰基的N- [2-（取代的酰氨基）苯基] -N'-羰基-S-取代的异硫脲，苯基是驱肠剂。通过S-取代的N-（巯基甲基亚甲基）氨基甲酸酯和适当的反应制备N-（2-乙酰氨基-4-苯氧基苯基）-N'-甲酯基-S-甲基硫脲的化合物是典型的例子取代的2-氨基苯胺，或通过相应的S-未取代的硫脲的烷基化。

3. 发明授权

US3974204A Thionosalicylic acid anilides and salts thereof 失效
标题翻译：硫代水杨酸苯胺及其盐
公开(公告)号：US3974204A
公开(公告)日：1976-08-10
申请号：US549682
申请日：1975-02-13
申请人： Jurgen Kurz , Heinrich Kolling , Manfred Federmann
发明人： Jurgen Kurz , Heinrich Kolling , Manfred Federmann
IPC分类号： C07C153/067
摘要： New thionosalicylic acid anilides and salts with bases are provided which have parasiticidal activity in sheep and cattle particularly against adult liver flukes in sheep and cattle and other domestic animals, especially against juvenile liver flukes. The new compounds are produced by the reaction of poly-substituted phenols with substituted aromatic isothiocyanates, the hydrolysis products of oxo-thiono- or dithiono-dihydrobenzoxazines or by the reaction of N-phenyl-salicyl-imide chlorides with thio-compounds. Typical compounds are 3,5-dichloro-4'-bromo-thionosalicylic acid anilide and 2-acetoxy-3,5-dichloro-N-(2'-methyl-4'-chlorophenyl)-thionobenzamide. Novel benzoxazines obtainable from the above anilides are also provided and have similar properties. Typical compounds are 3-(3',5'-bis-trifluoromethyl-phenyl)-6,8-dibromo-2-oxo-4-thionodihydrobenzoxazine-(1,3), 3-(3',4'-dichlorophenyl)-6,8-dichloro-2,4-dithiono-dihydrobenzoxazine-(1,3) and 3-(4'-bromophenyl)-6-chloro-8-bromo-2,4-dithiono-dihydrobenzoxazine-(1,3). Methods for preparing a large number of both types of compounds are described. The compounds are administered orally or subcutaneously in doses of 2.5 to 100 mg/kg, preferably 5 to 15 mg/kg, of body weight.
摘要翻译：提供新的硫羟水杨酸和与碱的盐，其在绵羊和牛中具有杀寄生虫活性，特别是针对羊，牛和其他家畜中的成年肝吸虫，特别是针对幼鱼肝吸虫。新化合物是通过多取代苯酚与取代的芳族异硫氰酸酯的反应，氧代 - 硫代 - 或二硫代 - 二氢苯并恶嗪的水解产物或N-苯基 - 水杨酰基酰亚胺氯化物与硫代化合物的反应制备的。典型的化合物是3,5-二氯-4'-溴 - 硫代水杨酸酰苯胺和2-乙酰氧基-3,5-二氯-N-（2'-甲基-4'-氯苯基） - 硫代苯甲酰胺。还提供了可从上述酰苯胺获得的新型苯并恶嗪，具有相似的性质。典型的化合物是3-（3'，5'-双 - 三氟甲基 - 苯基）-6,8-二溴-2-氧代-4-硫代二氢苯并恶嗪 - （1,3），3-（3'，4'-二氯苯基）-6,8-二氯-2,4-二硫代二氢苯并恶嗪 - （1,3）和3-（4'-溴苯基）-6-氯-8-溴-2,4-二硫代 - 二氢苯并恶嗪 - （1， 3）。描述了制备大量两种类型化合物的方法。化合物以2.5至100mg / kg，优选5至15mg / kg体重的剂量口服或皮下给药。

4. 发明授权

US3970752A Coccidiocidal compositions utilizing 1-phenyl-substituted 1,3,5-triazine 失效
标题翻译：使用1-苯基取代的1,3,5-三嗪的杀微生物剂组合物
公开(公告)号：US3970752A
公开(公告)日：1976-07-20
申请号：US532221
申请日：1974-12-12
申请人： Gerd Aichinger , Axel Haberkorn , Heinrich Kolling , Eckart Kranz , Josef Reisdorff
发明人： Gerd Aichinger , Axel Haberkorn , Heinrich Kolling , Eckart Kranz , Josef Reisdorff
IPC分类号： A23K1/16 , C07C317/42 , C07C323/66 , A61K31/53
CPC分类号： C07C323/66 , A23K20/116 , C07C317/42
摘要： 1-Phenyl-substituted 1,3,5-triazines of the formula: ##SPC1##And pharmaceutically acceptable nontoxic salts thereofWherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub. 9 are the same or different and each is selected from the group consisting of hydrogen, straight or branched chain alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, halogen, nitro, cyano, amino, acylamino, alkoxycarbonylamino, carboxy, alkoxycarbonyl, carbamoyl, acyl, haloacyl, alkylsulphinyl, alkylsulphonyl, haloalkylsulphonyl and sulphamoyl;R.sub.10 is hydrogen, straight or branched chain alkyl, cycloalkyl, haloalkyl, alkoxy, alkoxyalkyl, haloalkoxyalkyl, alkylthioalkyl, haloalkylthioalkyl, alkenyl, alkynyl, alkoxycarbonyl, (alkylthio)carbonyl, (alkylthio)thiocarbonyl, acylamino, diacylamino, amino, dialkylamino, polymethyleneimino, polymethyleneimino interrupted by a heteroatom in the chain, or unsubstituted or substituted benzyl or aryl;R.sub.11 is hydrogen, or alkyl;X is sulphur, sulphinyl, or sulphonyl; andY is oxygen or sulphur,Are useful for their activity against coccidiosis in humans and animals.
摘要翻译：具有下式的1-苯基取代的1,3,5-三嗪：

5. 发明授权

US3966725A 1-(4-Phenoxy-phenyl)-1,3,5-triazines 失效
标题翻译： 1-（4-苯氧基 - 苯基）-1,3,5-三嗪
公开(公告)号：US3966725A
公开(公告)日：1976-06-29
申请号：US559562
申请日：1975-03-18
申请人： Josef Helmut Reisdorff , Gerd Aichinger , Axel Haberkorn , Heinrich Kolling , Eckart Kranz
发明人： Josef Helmut Reisdorff , Gerd Aichinger , Axel Haberkorn , Heinrich Kolling , Eckart Kranz
IPC分类号： C07D251/34 , A23K1/16 , A61K31/53 , A61P33/02 , C07C273/18 , C07C275/36 , C07C319/20 , C07C323/20 , C07D251/38
CPC分类号： C07D251/26 , A23K20/116 , C07C273/1827 , C07C319/20
摘要： 1-(4-Phenoxy-phenyl)-1,3,5-triazine derivatives of the formula ##SPC1##And pharmaceutically-acceptable, nontoxic salts thereof whereinR.sub.1 to R.sub.9 are the same or different and each is hydrogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, halo, nitro, cyano, amino, acylamino, alkoxycarbonylamino, carboxy, alkoxycarbonyl, carbamoyl, acyl, haloacyl, alkylsulphinyl, alkylsulphonyl, haloalkylsulphinyl, haloalkylsulphonyl or sulphamoyl; provided that at least one of R.sub.1 to R.sub.9 is haloalkyl, haloalkylthio, haloalkylsulphinyl or haloalkylsulphonyl;R.sub.10 is hydrogen, alkyl, cycloalkyl, haloalkyl, alkoxy, alkoxyalkyl, haloalkoxyalkyl, alkylthioalkyl, haloalkylthioalkyl, alkenyl, alkinyl, alkoxycarbonyl, alkylthiocarbonyl, alkylthiothiocarbonyl, acylamino, diacylamino, dialkylamino, polymethylene-imino, polymethylene-imino interrupted by a heteroatom, unsubstituted or substituted benzyl or unsubstituted or substituted aryl;R.sub.11 is hydrogen or alkyl; andY is oxygen or sulphur;Are useful in treating coccidiosis in humans and animals.
摘要翻译： 1-（4-苯氧基 - 苯基）-1,3,5-三嗪衍生物及其药学上可接受的，其中R 1至R 9相同或不同并且各自为氢，烷基，卤代烷基，烷氧基，卤代烷氧基的非对映体烷硫基，卤代烷硫基，卤素，硝基，氰基，氨基，酰氨基，烷氧基羰基氨基，羧基，烷氧基羰基，氨基甲酰基，酰基，卤代酰基，烷基亚磺酰基，烷基磺酰基，卤代烷基亚磺酰基，卤代烷基磺酰基或氨磺酰基。条件是R 1至R 9中的至少一个为卤代烷基，卤代烷硫基，卤代烷基亚磺酰基或卤代烷基磺酰基; R 10为氢，烷基，环烷基，卤代烷基，烷氧基，烷氧基烷基，卤代烷氧基烷基，烷硫基烷基，卤代烷硫基烷基，烯基，炔基，烷氧基羰基，烷硫基羰基，烷基硫代羰基，酰氨基，二酰基氨基，二烷基氨基，聚亚甲基亚氨基，被杂原子中断的聚亚甲基亚氨基，取代的苄基或未取代或取代的芳基; R11是氢或烷基; Y为氧或硫; 有用于治疗人类和动物的结核病。

6. 发明授权

US4127670A 2-Formamido phenylguanidines and processes for their preparation and use 失效
标题翻译： 2-甲酰氨基苯胍及其制备和使用方法
公开(公告)号：US4127670A
公开(公告)日：1978-11-28
申请号：US770389
申请日：1977-02-22
申请人： Hartmund Wollweber , Heinrich Kolling , Herbert Thomas
发明人： Hartmund Wollweber , Heinrich Kolling , Herbert Thomas
IPC分类号： C07C279/24 , C07C149/437 , A61K31/27
CPC分类号： C07C279/24
摘要： N-(2-formamidophenyl)-N',N"-bis-carbonylguanidines bearing an optionally substituted phenoxy, phenylthio, phenylsulfinyl or phenylsulfonyl group in the 4- or 5-position of the 2-(formamido)-phenyl group are anthelminetic agents. The compounds, of which N-(2-formamido-4-phenylthiophenyl)-N',N"-bis-carbomethoxyguanidine is a typical example, are prepared through the reaction of isothiourea-S-alkyl ether and an appropriately substituted 2-aminoformanilide.
摘要翻译：在2-（甲酰氨基） - 苯基的4-或5-位带有任意取代的苯氧基，苯硫基，苯基亚磺酰基或苯基磺酰基的N-（2-甲酰氨基苯基）-N'，N“ - 双 - 羰基胍具有抗激动作用代理商其中N-（2-甲酰氨基-4-苯硫基苯基）-N'，N“ - 双 - 甲酯基胍的化合物是典型的例子，是通过异硫脲-S-烷基醚和适当取代的2- 氨基甲酰苯胺。

7. 发明授权

US4021571A Substituted phenylisothioureas and processes for their preparation and use 失效
标题翻译：取代苯基异硫脲及其制备和使用方法
公开(公告)号：US4021571A
公开(公告)日：1977-05-03
申请号：US693097
申请日：1976-06-04
申请人： Heinrich Kolling , Herbert Thomas , Arno Widdig , Hartmund Wollweber
发明人： Heinrich Kolling , Herbert Thomas , Arno Widdig , Hartmund Wollweber
IPC分类号： A61K31/17 , A61K31/155 , C07C67/00 , C07C325/00 , C07C335/38 , A01N9/12
CPC分类号： C07C335/38
摘要： N-[2-(Substituted amido)phenyl]-N'-carbonyl-S-substituted isothioureas bearing an optionally substituted phenoxy, phenylthio, phenylsulfinyl or phenylsulfonyl group in the 4- or 5-position of the 2-(substituted amido)-phenyl group are anthelmintic agents. The compounds, of which N-(2-acetamido-4-phenoxyphenyl)-N'-carbomethoxy-S-methylthiourea is a typical example, are prepared through the reaction of S-substituted N-(mercaptohalomethylene)carbamic acid ester and an appropriately substituted 2-aminoanilide, or through alkylation of the corresponding S-unsubstituted thiourea.
摘要翻译：在2-（取代的酰胺基） - 苯并噻唑的4-或5-位上带有任选取代的苯氧基，苯硫基，苯基亚磺酰基或苯基磺酰基的N- [2-（取代的酰氨基）苯基] -N'-羰基-S-取代的异硫脲，苯基是驱肠剂。通过S-取代的N-（巯基甲基亚甲基）氨基甲酸酯与合适的反应制备N-（2-乙酰氨基-4-苯氧基苯基）-N'-甲酯基-3-甲硫基脲的典型实例的化合物取代的2-氨基苯胺，或通过相应的S-未取代的硫脲的烷基化。

8. 发明授权

US3993682A Substituted phenylguanidines and processes for their preparation and use 失效
标题翻译：取代的苯胍及其制备和使用的方法
公开(公告)号：US3993682A
公开(公告)日：1976-11-23
申请号：US572224
申请日：1975-04-28
申请人： Heinrich Kolling , Herbert Thomas , Arno Widdig , Hartmund Wollweber
发明人： Heinrich Kolling , Herbert Thomas , Arno Widdig , Hartmund Wollweber
IPC分类号： A61K31/27 , A61K31/155 , A61K31/16 , A61K31/165 , A61P33/00 , A61P33/10 , B01D45/04 , B01D47/06 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/43 , C07C241/00 , C07C247/20 , C07C277/08 , C07C279/20 , C07C279/24 , C07C313/00 , C07C315/02 , C07C315/04 , C07C317/40 , C07C317/42 , C07C317/44 , C07C317/46 , C07C317/50 , C07C323/43 , C07C323/44 , C07C149/40
CPC分类号： B01D45/04 , A61K31/155 , B01D47/06
摘要： N-[2-(Substituted amido)phenyl]-N',N"-bis-carbonylguanidines bearing an optionally substituted phenoxy, phenylthio, phenylsulfinyl or phenylsulfonyl group in the 4- or 5-position of the 2-(substituted amido)phenyl group are anthelmintic agents. The compounds, of which N-(2-acetamido-4-phenylthiophenyl)-N',N"-bis-carbomethoxyguanidine is a typical example, are prepared through the reaction of isothiourea-S-alkyl ether and an appropriately substituted 2-aminoanilide.
摘要翻译：在2-（取代的酰氨基）苯甲酸的4-或5-位上带有任选取代的苯氧基，苯硫基，苯基亚磺酰基或苯基磺酰基的N- [2-（取代的酰胺基）苯基] -N'，N“ - 双 - 羰基胍苯基是驱肠剂。其中N-（2-乙酰氨基-4-苯硫基苯基）-N'，N“ - 双 - 甲酯基胍的化合物是典型的例子，通过异硫脲-S-烷基醚和适当取代的2- 氨基苯胺。

9. 发明授权

US3948893A 1-Phenyl-substituted 1,3,5-triazines 失效
标题翻译： 1-苯基取代的1,3,5-三嗪
公开(公告)号：US3948893A
公开(公告)日：1976-04-06
申请号：US452140
申请日：1974-03-18
申请人： Gerd Aichinger , Axel Haberkorn , Heinrich Kolling , Eckart Kranz , Josef Reisdorff
发明人： Gerd Aichinger , Axel Haberkorn , Heinrich Kolling , Eckart Kranz , Josef Reisdorff
IPC分类号： C07D251/34 , A23K1/16 , A61K31/53 , C07C317/42 , C07C323/44 , C07C323/66 , C07D209/48 , C07D251/04 , C07D251/38 , C07D51/26
CPC分类号： C07D209/48 , A23K20/116 , C07C317/42 , C07C323/44 , C07C323/66
摘要： 1-Phenyl-substituted 1,3,5-triazines of the formula: ##SPC1##And pharmaceutically acceptable nontoxic salts thereof whereinR.sub.1, r.sub.2, r.sub.3, r.sub.4, r.sub.5, r.sub.6, r.sub.7, r.sub.8 and R.sub.9 are the same or different and each is selected from the group consisting of hydrogen, straight or branched chain alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, halogen, nitro, cyano, amino, acylamino, alkoxycarbonylamino, carboxy, alkoxycarbonyl, carbamoyl, acyl, haloacyl, alkylsulphinyl, alkylsulphonyl, haloalkylsulphonyl and sulphamoyl;R.sub.10 is hydrogen, straight or branched chain alkyl, cycloalkyl, haloalkyl, alkoxy, alkoxyalkyl, haloalkoxyalkyl, alkylthioalkyl, haloalkylthioalkyl, alkenyl, alkynyl, alkoxycarbonyl, (alkylthio)carbonyl, (alkylthio)thiocarbonyl, acylamino, diacylamino, amino, dialkylamino, polymethyleneimino, polymethyleneimino interrupted by a heteroatom in the chain, or unsubstituted or substituted benzyl or aryl;R.sub.11 is hydrogen, or alkyl;X is sulphur, sulphinyl, or sulphonyl; andY is oxygen or sulphur,Are useful for their activity against coccidiosis in humans and animals.
摘要翻译：具有下式的1-苯基取代的1,3,5-三嗪：

10. 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。

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