Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1995-03-31
1997-01-14
Ford, John M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514205, 540222, 540227, C07D50146, A61K 31545
Patent
active
055939848
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/KR93/00087, filed Sep. 28, 1993.
TECHNICAL FIELD
The present invention relates to novel cephalosporin derivatives and processes for the preparation thereof; and more particularly, to novel cephalosporin derivatives and pharmaceutically acceptable non-toxic salts thereof, processes for preparing these compounds and to pharmaceutical compositions containing same as active ingredients.
BACKGROUND ART
Antibiotics of cephalosporin series are widely used in therapy for treatment of diseases which are caused by general pathogenic bacteria in mammals including human beings. There have been numerous studies aimed at increasing the efficacy and stability of the antibiotics of cephalosporin series, resulting in the development of various cephalosporin compounds.
For example, U.S. Pat. No. DES. 2,702,501 discloses various cephalosporin derivatives, including autibiotic known as cefotaxime, having a quaternary ammoniomethyl group in 3-position and/or 2-(2-aminothiazol-4-yl)-2-hydroxy (or substituted hydroxy) iminoacetamido group in the 7-position of cephem nucleus.
Among these known cephalosporin antibiotics, a compound known as ceftazidime, which is disclosed in DE U.S. Pat. No. 2,921,316 displays superior antibacterial activities against Gram-negative bacteria such as Pseudomonas aeruginosa, while it exhibits relatively inferior antibacterial activities against Gram-positive bacteria, in particular, Staphylococcus species. On the contrary, cefotaxime has been reported to have antibacterial activities against Staphylococcus species, while it possesses less effective antibacterial activities against Pseudomonas aeruginosa.
Accordingly, there have ensued further efforts to develop cephalosporin compounds having an excellent activity of broad spectrum, e.g., against both Gram-positive and Gram-negative bacteria including Pseudomonas aeruginosa.
For example, European Patent Application No. 47,977 discloses cephalosporin compounds having the following formula(A): ##STR2## wherein: n is 0 or 1; two carbon atoms); carbamoyl group; and tri(lower)alkyl ammonium, or pyridinium group having the formula of ##STR3## wherein: R.sup.c is an (lower)alkyl substituted with cycloalkyl, methyl, hydroxy, alkoxy, halogen, cyano, carbamoyl, carboxy or sulfonyl, (lower)alkenyl or (lower)alkylthio optionally substituted with carboxy, amino optionally monosubstituted by (lower)alkyl, (lower)alkanoyl or aminobenzenesulfonyl, di(lower)alkylamino, carbamoyl substituted with (lower)alkyl, hydroxy(lower)alkyl, (lower)alkoxy, hydroxy or cyano, di(lower)alkylcarbamoyl, thiocarbamoyl, cycloalkyl, phenyl, hydroxy, (lower)alkoxy, halogen, (lower)alkoxycarbonyl, (lower)alkanoyloxy, (lower)alkanoyl, carboxy, sulfocyano, nitro or hydroxysulfo(lower)alkyl group;
However, search for the desirable antibiotics with The broad spectrum is far from complete.
DISCLOSURE OF INVENTION
Accordingly, a primary object of the present invention is to provide novel cephalosporin derivatives and pharmaceutically acceptable non-toxic salts thereof which have strong antibacterial activities against a broad spectrum of pathogenic bacteria.
It is another object of the present invention to provide processes for preparing the cephalosporin derivatives and pharmaceutically acceptable non-toxic salts thereof.
It is still another object of the present invention to provide pharmaceutical compositions containing the above novel compounds as active ingredients.
In accordance with one aspect of the present invention, there are provided novel cephalosporin derivatives of formula(I) and pharmaceutically acceptable non-toxic salts thereof: ##STR4## wherein: R.sup.1 is a hydrogen or an optionally halogen-substituted C.sub.1-3 alkyl group, a propargyl group or --C(R.sup.a)(R.sup.b)COOH, wherein R.sup.a and R.sup.b are independently a hydrogen or a C.sub.1-3 alkyl group; hydrogen or halogen or a C.sub.1-3 alkyl, amino or hydroxy C.sub.1-3 alkylthio, cyano, carbamoyl, carboxyl, hydroxy C.sub.1-3 alkyl, nitro, acetyl or formyl group; and
In accordance w
REFERENCES:
patent: 4788185 (1988-11-01), Miyake et al.
Chae Jeong S.
Choi Young R.
Hyun Jae W.
Kang Heui I.
Lee Jong W.
Ford John M.
Yuhan Corporation
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