Bristol-myers Squibb Compnay

Bristol-myers Company

Schering Corporation

Jerzy Golik

Dolatrai M Vyas

John F Kadow

John K Thottathil

Murray A Kaplan

Mark D Wittman

Yasutsugu Ueda

John J Wright

John D Matiskella

Henry S Wong

Wen-Sen Li

Robert K Perrone

John Beutler

Pat Clark

John Ross

John Roach

William B Lebherz, Iii

Gary Muschik

Thomas W Hudyma

Mahesh G Patel

Ann C Horan

James A Matson

Chung-Pin H Chen

The present invention concerns antitumor compounds. More particularly, the invention provides novel taxane derivatives, pharmaceutical compositions thereof, and their use as antitumor agents.

Phosphonooxymethyl ethers of taxane derivatives

Water soluble prodrugs of azole compounds

Water soluble prodrugs of azole antifungal agents are provided by quaternizing a nitrogen atom of the azole ring with a phosphonooxymethyl group.

Water-soluble prodrugs of azole compounds

The present invention concerns novel paclitaxel derivatives, their use as antitumor agents, and pharmaceutical formulations.

7-methylthiooxomethyl and 7-methylthiodioxomethyl paclitaxels

An antitumor antibiotic designated BMY-41339 is produced by fermentation of certain strains of Actinomadura verrucosospora. BMY-41339 exhibits antimicrobial activity and also inhibits the growth of tumors in experimental animals.

Antitumor antibiotic

Antitumor antibiotic BMY-41339

There is provided new antitumor antibiotic substances designated herein as BBM-1675C and BBM-1675D, said substances being produced by selective chemical hydrolysis of the bioactive components BBM-1675A.sub.1 (esperamicin A.sub.1) or BBM-1675A.sub.2 (esperamicin A.sub.2). The new antitumor antibiotics exhibit both antimicrobial activity and antitumor activity.

BBM-1675c and d antitumor antibiotics

Novel N-acetyl derivatives designated N-acetyl-esperamicins A.sub.1, A.sub.2 and A.sub.1b are prepared by acetylating known antitumor antibiotics. The new derivatives exhibit both antimicrobial and antitumor activity and have the structures ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or ##STR2## and R.sup.3 is --CH(CH.sub.3).sub.2 or --CH.sub.2 CH.sub.3.

Esperamicin derivatives

Actinomadura melliaura nov. sp. (ATCC 39691) produces four novel compounds which we have designated AT 2433 A.sub.1, AT 2433 A.sub.2, AT 2433 B.sub.1 and AT 2433 B.sub.2. The novel compounds or pharmaceutically acceptable salts thereof exhibit antibacterial and antitumor activity.

Antibiotic, antitumor compounds and their use

Growing community of inventors

Southington, CT, United States of America

Jerzy Golik