American Cyanamid Company

Other

Gregg Brian Feigelson

Carl B Ziegler

William V Curran

Yang-I Lin

Panayota Bitha

Karen Bush

Timothy W Strohmeyer

Subas Sakya

David Michael Blum

Kenneth E Green

Edward R Ruso

Alex R Jurgens

Mellard N Jennings

Carbapenem antibiotic compounds of the general formula: ##STR1## wherein the moiety ##STR2## is a 4, 5 or 6 membered mono, di- or tri-substituted oxygen or sulfur containing ring; wherein Z is oxygen, sulfur, sulfoxide and sulfone, pharmaceutical compositions thereof useful for the treatment of bacterial infections, processes for preparing the compounds and new intermediates useful in the process.

2-thiosubstituted carbapenems

Carbapenem antibiotic compounds of the general formula: ##STR1## wherein the moiety ##STR2## is a 4, 5 or 6 membered mono, di- or tri- substituted oxygen or sulfur containing ring; wherein Z is oxygen, sulfur, sulfoxide and sulfone, pharmaceutical compositions thereof useful for the treatment of bacterial infections, method of inhibiting a Beta-lactamase enzyme by administering said compounds, processes for preparing the compounds and new intermediates useful in the process are disclosed.

Method of inhibiting a .beta.-lactamase enzyme by administering novel

New 4-substituted azetidinones having the formulae I and II: ##STR1## wherein X is oxygen, sulfur or a moiety of the formula NR.sup.6 where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are defined hereafter, which are intermediates for the preparation of carbapenem and carbacephem antibacterials and processes for producing such antibacterials through the utilization of an acid mediated ring closure reaction.

4-substituted azetidinones as precursors to 2-substituted-3-carboxy

Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.4, R.sup.5, R.sup.12, R.sup.16 and R.sup.17 are defined in the specification are provided. These compounds are useful as intermediates for the preparation of carbapenem antibacterials.

Tetrahydrofuanyl compounds of the following formulae: ##STR1## are disclosed.

Method for producing tetrahydrofuranyl compounds

Carbapenem antibiotic compounds of the general formula: ##STR1## wherein the moiety ##STR2## is a 4, 5 or 6 membered mono, di- or tri- substituted oxygen or sulfur containing ring; wherein Z is oxygen, sulfur, sulfoxide and sulfone, pharmaceutical compositions thereof useful for the treatment of bacterial infections, processes for preparing the compounds and new intermediates useful in the process.

The invention provides substituted allylazetidinone compounds having the formula: ##STR1## and propargyl azetidinone compounds having the formula: ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.30, X, Y and Q are defined in the specification.

2-substituted alkyl-3-carboxy carbapenems as antibiotics and a method of

The invention relates to new 2-substituted alkyl-3-carboxy carbapenems having the formula: ##STR1## with R.sup.1, R.sup.2, R.sup.3, X and Y defined hereafter as antibiotics and beta lactamase inhibitors produced by a novel Michael addition-elimination reaction of a substituted allyl azetidinone in the reaction shown: ##STR2## with R.sup.1, R.sup.2, Q, X and Y defined hereafter.

2-substituted alkyl-3-carboxy carbopenems as antibiotics and a method of

The invention is an improved process for the large scale production of acetic acid, (dimethoxyphosphinyl) [[1,1-dimethylethyl)dimethylsilyl]oxy]-, (4-nitrophenyl)methyl ester.

Process for the synthesis of acetic acid, (dimethoxyphosphinyl)

New 4-substituted azetidinones having the formulea I and II: ##STR1## with R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and X defined hereafter, which are intermediates for the preparation of carbapenem and carbacephem antibacterials and processes for producing such antibacterials through the utilization of an acid mediated ring closure reaction.

Growing community of inventors

Airmont, NY, United States of America

Gregg Brian Feigelson