会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 16. 发明授权
    • Benzamide derivatives
    • 苯甲酰胺衍生物
    • US5578621A
    • 1996-11-26
    • US301407
    • 1994-09-08
    • Jean-Francois Rossignol
    • Jean-Francois Rossignol
    • A61K31/425A61K31/426C07D277/58
    • C07D277/58A61K31/425A61K31/426
    • The present invention relates to a new compound of formula I ##STR1## with one of the symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 representing OH, whereas the remaining symbols represent H; to a pharmaceutical composition containing the said compound, and to the use of said compound as anti-parasital, anti-bacterial, anti-fungal agent.The Prior ArtNitrothiazole compound PH 5776 (2-(acetolyloxy)-N-(5-nitro 2-thiazolyl) benzamide) is a compound of formula II ##STR2## in which R.sub.1 =O--COCH3 R.sub.2 =R.sub.3 =R.sub.4 =R.sub.5 =HThe preparation and uses of this compound are disclosed in U.S. Pat. No. 3,950,351, as well as in publication made by Applicant.In U.S. Pat. No. 3,950,351, the compound of formula II is prepared by reacting ##STR3## This reaction is not suitable for the preparation of pure compound of formula I ##STR4## in which one of the symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent OH, whereas the remaining symbols represent H.Moreover, contrary to what could be expected from the prior art, i.e. that the presence of an acyloxy group was necessary for rendering the compound active and efficient against bacteria, parasites, . . . , it has now been found that the compound of formula I ##STR5## with one of the symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 representing OH, whereas the remaining symbols represent H; had an excellent efficiency against parasites, bacteria, fungus although it does not contain an acyloxy group.The compound of formula I had a substantially immediate action against parasite, fungus, bacteria.
    • 本发明涉及一种新的式I化合物,其中符号R1,R2,R3,R4和R5之一代表OH,而其余符号代表H; 涉及含有所述化合物的药物组合物,以及所述化合物作为抗寄生虫,抗菌,抗真菌剂的用途。 现有技术硝基噻唑化合物PH5776(2-(乙酰基氧基)-N-(5-硝基2-噻唑基)苯甲酰胺)是式II化合物,其中R1 = O-COCH3R2 = R3 = R4 = R5 = 该化合物的制备和用途在美国专利No. 3,950,351号以及申请人出版的刊物。 在美国专利 式3,950,351中,式II化合物通过反应制备,该反应不适用于制备纯化合物Ⅰ“IMAGE”,其中R1,R2,R3,R4和R5之一代表OH 而其余符号代表H.此外,与现有技术可以预期的相反,即,需要存在酰氧基以使化合物对细菌,寄生虫有效和有效。 。 。 现在已经发现,具有代表OH的符号R1,R2,R3,R4和R5之一的式I化合物,而其余的符号代表H; 尽管它不含有酰氧基,但对寄生虫,细菌,真菌具有极好的效力。 式I的化合物对寄生虫,真菌,细菌具有基本上立即的作用。