Eli Lilly and Company

Robert Theodore Vasileff

John Michael Morin, Jr

Michael Dean Kinnick

Daniel Jon Sall

Matthew Joseph Fisher

Joseph A Jakubowski

Allen D Kline

Anne Marie Happ

Marshall A Skelton

Michael J Martinelli

William H Lunn

Theo Schotten

Wolfgang Stenzel

Michael Paal

Kenneth James Ruterbories

Jason Scott Sawyer

Douglas Wade Beight

Nicholas J Bach

Ho-Shen Lin

Jolie Anne Bastian

Michael Enrico Richett

Richard Waltz Harper

Robert D Dillard

Michael LeRoy Phillips

Benjamin Alan Anderson

Susan Elizabeth Draheim

Tulio Suarez

Edward David Mihelich

Michael Lyle Denney

Nancy Kay Harn

Gerd Ruhter

Gary A Hite

Richard Walter Schevitz

John Mcneill McGill, Iii

Richard James Loncharich

Larry W Hertel

William T Jackson

Gerd R&uuml;hter

A class of novel tricyclics is disclosed together with the use of such compounds for inhibiting sPLA mediated release of fatty acids for treatment of conditions such as septic shock.

Substituted tricyclics

This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.

Glycoprotein IIB/IIIA antagonists

This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, benzopyran, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.

Glycoprotein IIb/IIIa antagonists

A class of novel tricyclics is disclosed together with the use of such compounds for inhibiting sPLA,mediated release of fatty acids for treatment of conditions such as septic shock.

Glycoprotein IIB IIIA antagonists

This invention provides novel indenone derivatives, their pharmaceutical formulations and their use for the inhibition of leukocyte adherence to cells.

Cell adhesion inhibitors

A process for photochemically converting 3-exomethylene cephams (or 1-carba(1-dethia)cephams or and 1-oxa(1-dethia)cephams) from the corresponding 3-alkyl-3-cephem (or 1-carba(1-dethia)cephem or 1-oxa(1-dethia)cephem) is provided. Further provided are 3-cephams useful as intermediates to 3-cephem compounds.

Photochemical conversion of cephalosporins,

Cephalosporin compounds substituted in the 7-position by a 2-(5- or 6-membered heterocyclic)-2-oximinoacetylamino group and in the 3-position with a thienopyridinium methyl group or a furopyridinium methyl group are broad spectrum antibiotics highly effective in combating bacterial infections of gram-negative and gram-positive microorganisms. The cephalosporins are best prepared by reacting a silylated 7-[2-(heterocyclic)-2-oximinoacetylamino]-3-iodomethyl-3-cephem-4-carboxyl ic acid with the thienopyridine or the furopyridine. Pharmaceutical formulations comprising a compound of the invention and a method for treating bacterial infections comprising their use are also provided.

Thieno and furopyridinium-substituted cephalosporins

Cephalosporin compounds substituted in the 7-position by a 2-(5- or 6-membered heterocyclic)-2-oximinoacetylamino group and in the 3-position with a thienopyridinium methyl group or a furopyridinium methyl group are broad spectrum antibiotics highly effective in combating bacterial infections of gram-negative and gram-positive microorganisms. The cephalosporins are best prepared by reacting a silylated 7-[2-(heterocyclic)-2-oximinoacetylamino-3-iodomethyl-3-cephem-4-carboxyli c acid with the thienopyridine or the furopyridine. Pharmaceutical formulations comprising a compound of the invention and a method for treating bacterial infections comprising their use are also provided.

Broad spectrum cephalosporin antibiotics represented by the betaine structure of the formula ##STR1## wherein R is a 5-membered amino-substituted heterocyclic containing oxygen and nitrogen; R' is e.g., hydrogen or C.sub.1 -C.sub.4 alkyl; and bicyclicpyridinium is a thienopyridinium or a furopyridinium group; are prepared by reacting a silylated 3-iodomethyl cephalosporin with a thienopyridine, e.g., thieno[2,3-b]pyridine or a furopyridine. The compounds are potent antibacterials against gram-positive and gram-negative organisms. Pharmaceutical compositions and a method for treating bacterial infections are also provided.

Oxazole and oxadiazole cephalosporins

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Indianapolis, IN, United States of America

Robert Theodore Vasileff