3-substituted-aminomethyl cephalosporin derivatives

Details 3-substituted-aminomethyl cephalosporin derivatives 3-substituted-aminomethyl cephalosporin derivatives

1986-12-09

1990-01-16

Rizzo, Nicholas S.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514201, 540222, 540221, C07D, A61K 31545

Patent

active

048943711

ABSTRACT:
An antibacterial cephalosporin derivative of the formula I: ##STR1## in which X is S,O,CH.sub.2 or S0; R2 is hydrogen, methoxy or formylamino; R3 is carboxy or a biodegradable ester thereof; R1 represents a variety of groups known in the cephalosporin art and R4 represents a group NR42R43 wherein R42 is hydrogen, lower alkyl or benzyl and R43 is one of a group of neutral heterocyclic species defined in the specification. Pharmaceutical compositions, manufacturing processes and intermediates are also described. In a specific embodiment, 3-substituted aminomethyl cephalosporin derivatives in which X is S or SO are disclosed.

REFERENCES:
patent: 4278793 (1981-07-01), Durckheimer et al.
patent: 4499088 (1985-02-01), Takaya et al.
patent: 4678781 (1987-07-01), Jung
Merck Index, Entries 1899, 1902, 1905, 1908 and 1916 (1983: Merck and Co.; Rahway, N.J.) pp. 268-272.
Angew. Chem. Int. Ed. Engl. 24 (1985) pp. 180-202-Durckheimer et al.
Heterocycles, vol. 13, 1979, pp. 197-202-Kishi

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