Substituted phenylisothioureas and processes for their preparation and
use
    2.
    发明授权
    Substituted phenylisothioureas and processes for their preparation and use 失效
    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

    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。

    Thionosalicylic acid anilides and salts thereof
    3.
    发明授权
    Thionosalicylic acid anilides and salts thereof 失效
    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

    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。

    Coccidiocidal compositions utilizing 1-phenyl-substituted 1,3,5-triazine
    4.
    发明授权
    Coccidiocidal compositions utilizing 1-phenyl-substituted 1,3,5-triazine 失效
    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

    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:

    1-(4-Phenoxy-phenyl)-1,3,5-triazines
    5.
    发明授权
    1-(4-Phenoxy-phenyl)-1,3,5-triazines 失效
    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

    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。

    2-Formamido phenylguanidines and processes for their preparation and use
    6.
    发明授权
    2-Formamido phenylguanidines and processes for their preparation and use 失效
    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

    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。

    Substituted phenylisothioureas and processes for their preparation and
use
    7.
    发明授权
    Substituted phenylisothioureas and processes for their preparation and use 失效
    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

    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。

    1-Phenyl-substituted 1,3,5-triazines
    9.
    发明授权
    1-Phenyl-substituted 1,3,5-triazines 失效
    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

    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: