Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1988-01-14
1989-12-05
Berch, Mark L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
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:
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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.
Berch Mark L.
Eli Lilly and Company
Scanlon William B.
Whitaker Leroy
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