1-carba(dethia)-3-cephem derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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540205, C07D47104, C07D41712, C07D41714, A61K 31435

Patent

active

048852910

ABSTRACT:
7.beta.-Acylamino-1-carba(dethia)-3-cephem-4-carboxylic acids represented by the formula ##STR1## wherein n is 1 or 2; R.sub.1 is C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 alkyl substituted by hydroxy, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, trifluoromethyl, carboxy, carbamoyl, amino, C.sub.1 -C.sub.4 alkylamino, di-(C.sub.1 -C.sub.4 alkyl)amino, halogen, cyano, phenyl, substituted phenyl as defined above; C.sub.2 -C.sub.6 alkenyl; C.sub.3 -C.sub.7 cycloalkyl; phenyl or substituted phenyl as defined above; or a 5- or 6-membered heterocycle selected from thienyl, furyl, pyrryl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, triazolyl, tetrazolyl, pyridyl, pyrimidyl, triazinyl, or pyrazinyl; the benzheterocycles, benzothienyl, benzofuryl, indolyl, benzimidazolyl, or benztriazolyl, and said 5- or 6-membered heterocycle and said benzheterocycle substituted by C.sub.1 -C.sub.4 alkyl, halogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, amino, carboxy, cyano, or carbamoyl; and when said heterocycle or benzheterocycle contains a basic ring nitrogen, the C.sub.1 -C.sub.4 alkyl quaternary salt thereof;
R.sub.2 is hydrogen, a carboxy-protecting group, or a group forming a biologically labile ester and, when R.sub.2 is hydrogen, the pharmaceutically acceptable non-toxic salts thereof; are antibiotics useful in the treatment of infectious disease.

REFERENCES:
patent: 4226866 (1980-10-01), Christenson
patent: 4673737 (1987-06-01), Evans et al.
patent: 4708956 (1987-11-01), Hirata et al.
patent: 4760060 (1988-07-01), Mochida
Scartazzini, Helv. Chem. Acta 58, 2437(1975).
Green, "Protective (Groups in Organic Synthesis" p. 161 (1981).
EPO Search Report in applicant's corresponding EPO Application No. 89300145.3.

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