Abstract: A compound of the formula ##STR1## wherein R is hydrogen, alkali metal, ##STR2## or ##STR3## R.sub.1 is hydrogen or methyl; R.sub.2 is hydrogen or methyl;R.sub.3 is hydrogen, lower alkyl or lower alkylphenyl;R.sub.4 is hydrogen, --OCONH.sub.2, ##STR4## R.sub.7 is hydrogen or lower alkyl; R.sub.8 is hydrogen or --CONH.sub.2 ;R.sub.9 is hydrogen, lower alkyl, ##STR5## or --(CH.sub.2).sub.p --N--(lower alkyl).sub.2 ; R.sub.10 is hydrogen or lower alkyl;R.sub.11 is hydrogen, sodium or potassium;n is 1, 2, 3 or 4;m is 0, 1 or 2;p is 1, 2, 3 or 4.
Abstract: A process for removing the acyl sidechain from penicillins and cephalosporins which comprises chlorinating the acyl compound and treating the resulting iminochloride with an o-aminothiophenol to obtain the corresponding 6.beta.-aminopenicillin or 7.beta.-aminocephalosporin.
Type:
Grant
Filed:
July 6, 1979
Date of Patent:
February 24, 1981
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
William A. Slusarchyk, Christopher M. Cimarusti
Abstract: New derivatives of 8H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]pyrido[3,4-e]pyrimidine have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.
Abstract: Penicillin esters and their acid addition salts of the formula ##STR1## wherein X is hydrogen, methyl, methoxy, chloro, or bromo and n is an integer from 1 to 3 provided that n is 2 or 3 only when X is hydrogen or methoxy; are disclosed. Upon oral administration, these esters provide improved absorption and result in high concentrations of the antibacterially active parent penicillin in the blood, tissues and urine.
Type:
Grant
Filed:
August 31, 1978
Date of Patent:
June 3, 1980
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
William E. Brown, Christopher M. Cimarusti
Abstract: New derivatives of 8H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]-pyrido[3,4-e]pyrimidine have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.
Abstract: Imidazolylethoxy derivatives of pyridin-5-methanols having the general formula ##STR1## and their acid addition salts are useful as antifungal and antibacterial agents.