Cephalosporin derivatives

Details Cephalosporin derivatives Cephalosporin derivatives

C - Chemistry, Metallurgy

07

D

C07D 501/59 (2006.01) C07D 501/00 (2006.01)

Patent

CA 2140854

Many antibiotics of cephalosporin series useful as drugs are known, and many of them are administered parenterally because of low oral absorbability. Of the oral cephalosporin drugs used clinically, cephalexin and cefachlor show high oral absorbability, but have extremely inferior antibacterial activity against gram-negative bacteria to injectional cephalosporin drugs. Oral cephalosporin drugs of which the oral absorbability is elevated as so-called prodrug have been recently developed. These compounds have stronger anti- bacterial activity against gram-negative bacteria than cephalexin, etc., but remain the drawbacks of lowered antibacterial activity against gram-positive bacteria and the oral absorbability which is not so good. The present invention relates to cephalosporin derivatives represented by the formula: Image (I) (wherein R1 and R3 are each a hydrogen atom or a lower alkyl group, and R2 is a hydrogen atom or an in vivo hydrolyzable group) having both potent antibacterial activity and high oral absorbability and non-toxic salts thereof, and the drugs containing the compounds of the present invention as an effective ingredient have not only potent antibacterial activity against various phathogenic bacteria including gram-positive and gram- negative bacteria, but also excellent oral absorbability with low toxicity, and therefore, they are useful as antibiotics for oral administration.

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