E. R. Squibb Sons, Inc.

Koster, William H.

Ermann, Peter H.

Sundeen, Joseph E.

Treuner, Uwe D.

Straub, Henner

Peter H Ermann

Henner Straub

Uwe D Treuner

Joseph E Sundeen

Jakob-Matthias Drossard

William H Koster

Sailesh A Varia

Kent Amsberry

Michael Fakes

Richard H Mueller

Hermann Breuer

William A Slusarchyk

Joseph O'Sullivan

Douglas W Phillipson

Antibacterial activity is exhibited by novel compounds having the formula ##STR1## where R.sub.1, R.sub.2, and M are as defined herein and X is --(CH.sub.2).sub.n -- wherein n is 0, 1, 2, 3 or 4 or CR.sub.3 R.sub.4 wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen, --CH.sub.3 or --C.sub.2 H.sub.5 or R.sub.3 and R.sub.4 taken together with the carbon atom to which they are attached form a 3, 4, 5, 6 or 7-membered cycloalkyl ring.

Hereroaryl derivatives of monocyclic beta-lactam antibiotics

Antibacterial activity is exhibited by novel compounds having the formula ##STR1## where R.sub.1, R.sub.2, and M are as defined herein and X is --(CH.sub.2).sub.n -- wherein n is 0, 1, 2, 3 or 4 or CR.sub.3 R.sub.4 wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen, --CH.sub.3 or --C.sub.2 H.sub.5 or R.sub.3 and R.sub.4 taken together with the carbon atom to which they are attached form a 3, 4, 5, 6 or 7-membered cycloalkyl ring. Also described are various intermediates for the preparation of compounds of formula 1.

Intermediates for the preparation of heteroaryl derivatives of

Antibacterial activity has been found in compounds of the formula. Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein: A is a bond or alkylene;

Heterocyclic hydrazide derivatives of monocyclic .beta.-lactam

Heteroaryl derivatives of monocyclic beta-lactam antibiotics

Novel antibiotic substances, including novel natural products, having the general formula ##STR1## wherein R.sub.1 and R.sub.2 are as defined herein, are disclosed. These compounds have been found to be cytochrome P450 inhibitors.

4-methoxy-5-methyl-pyran-3-ol natural products and derivatives thereof

Novel antibiotic substances, having the general formula ##STR1## wherein A, R.sub.1 and R.sub.2 are as defined herein.

Substituted pyran derivatives having antiinfective activity

Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof and possessing antibacterial activiy, and intermediates to compounds of formula I having the formula ##STR2##

6,7-dihydroxyquinoxalines as intermediates to beta-lactam antibiotics

Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof and possessing antibacterial activity, and intermediates to compounds of formula I having the formula

Heteroaroylhydrazide derivatives of monocyclic beta-lactam antibiotics

Antibacterial activity is exhibited by 2-azetidinones having a 3-acylamino substituent and having an activating group in the 1-position of the formula ##STR1## wherein R.sub.4 is ##STR2## wherein A.sub.1 is a single bond, ##STR3## --NH-- or ##STR4## A.sub.2 is a single bond, --NH--, --CH.sub.2 --CH.sub.2 --NH-- or ##STR5## A.sub.3 is a single bond, --CH.dbd.CH--, --(CH.sub.2).sub.t --, --NH--(CH.sub.2).sub.p -- or ##STR6## wherein t is 1, 2, 3 or 4 and p is 0 or 1; and A.sub.4 is a single bond --CH.sub.2 --, --NH--CH.sub.2 --, or --N.dbd.CH--.

2-Oxo-1-[[(substituted sulfonyl)amino]-carbonyl]azetidines

Antibacterial activity is exhibited by .beta.-lactams having a 3-acylamino substituent and having in the 1-position an activating group of the formula ##STR1## wherein R is

2-oxo-1-(((substituted sulfonyl)amino)-carbonyl)azetidines

Antibacterial activity is exhibited by 3-acylamino-2-oxoazetidines having in the 1-position an activating group of the formula ##STR1## wherein R is ##STR2## and R.sub.4 is ##STR3##

2-oxo-1-[[(substituted sulfonyl)amino]-carbonyl]azetidines

Processes for preparing the useful intermediates having the formula ##STR1## are disclosed herein, utilizing novel chemical compounds having the formula ##STR2##

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Donaustauf, Germany

Peter H Ermann