发明名称 Benzamide derivatives
摘要 The present invention relates to a new compound of formula I <IMAGE> with one of the symbols R1, R2, R3, R4 and R5 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 Art Nitrothiazole compound PH 5776 (2-(acetolyloxy)-N-(5-nitro 2-thiazolyl) benzamide) is a compound of formula II <IMAGE> in which R1=O-COCH3 R2=R3=R4=R5=H The 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 <IMAGE> This reaction is not suitable for the preparation of pure compound of formula I <IMAGE> in which one of the symbols R1, R2, R3, R4 and R5 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 <IMAGE> with one of the symbols R1, R2, R3, R4 and R5 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.
申请公布号 US5578621(A) 申请公布日期 1996.11.26
申请号 US19940301407 申请日期 1994.09.08
申请人 ROSSIGNOL, JEAN-FRANCOIS 发明人 ROSSIGNOL, JEAN-FRANCOIS
分类号 A61K31/425;A61K31/426;C07D277/58;(IPC1-7):A61K31/425 主分类号 A61K31/425
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