E. R. Squibb Sons, Inc.

Bristol-myers Squibb Compnay

Squibb Corporation

Uwe D Treuner

Hermann Breuer

Theodor Denzel

Peter H Ermann

Henner Straub

William H Koster

Joseph E Sundeen

Sailesh A Varia

Michael Fakes

Kent Amsberry

Gregory S Bisacchi

William A Slusarchyk

Jakob-Matthias Drossard

Robert Zahler

Yan Shi

James Clifford Sutton

Shung C Wu

Peter W Glunz

Guohua Zhao

George C Morton

Xiaojun Zhang

Daniel L Cheney

E Scott Priestley

Alexandra Holubec

Theodore Denzel

Tetsuo Miyadera

Compounds having the formula (I), or a stereoisomer or pharmaceutically-acceptable salt, or hydrate thereof, are useful as factor VIIa inhibitors, wherein X is &#x2014;NRS(O)R; W is hydrogen or &#x2014;(CRR)W; Wis hydrogen or a bond with R; Z is a-membered heteroaryl group, a five to six membered heterocyclo or cycloalkyl group, atomembered bicyclic aryl or heteroaryl, or a six membered aryl or heteroaryl, and R, R, R, R, R, and Rare as defined in the specification.

Phenylglycine derivatives useful as serine protease inhibitors

Acid derivatives useful as serine protease inhibitors

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

Heteroaryl derivatives of monocyclic beta-lactam antibiotics

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

Antibiotic substances having the general formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined herein.

Aminoalkylphosphonic acid esters of natural

Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof which possess antibacterial activity.

Monobactam hydrazide derivatives

Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, exhibit antibacterial activity wherein R is ##STR2##

Certain (2-carboxy or 2-propenoic or 2-carbonyl)-3-halo-4,5-dioxy

Componds having the formula ##STR1## and pharmaceutically acceptable salts thereof, exhibit antibacterial activity wherein R is ##STR2##

2-oxo-[[(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 2-azetidinones having a 3-acylamino substituent and having an activating group in the 1-position of the formula ##STR1## wherein R is ##STR2## A.sub.1 is --NH-- or ##STR3## A.sub.2 is ##STR4## or --CH.dbd.CH--.

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

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##

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

.beta.-Lactams having a sulfonic acid salt substituent in the 1-position, an acylamino substituent in the 3-position and an --NR.sub.2 R.sub.3 substituent in the 4-position wherein R.sub.2 and R.sub.3 are the same or different and each is ##STR1## or R.sub.2 and R.sub.3 together with the nitrogen atom to which they are attached are ##STR2## R.sub.4 is alkyl, aryl or arylalkyl; and R.sub.5 and R.sub.6 are the same or different and each is hydrogen, halogen, alkyl, alkoxy, alkylthio, alkoxycarbonyl, carboxyl or a carboxyl salt; have antibacterial activity.

4-amino derivatives of 2-oxo-1-azetidinesulfonic acid salts

Compounds having the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently hydrogen or alkyl of 1 to 4 carbon atoms, or R.sub.1 and R.sub.2 together with the carbon atom to which they are attached form a cycloalkyl ring;

Growing community of inventors

Wuppertal, Germany

Uwe D Treuner