The Scripps Research Institute

Optimer Pharmaceuticals, Inc.

Other

Merck Sharp + Dohme Corp.

Chan-Kou Hwang

Kyriacos Costa Nicolaou

Youe-Kong Shue

Yu-Hung Chiu

Alex Romero

Erik J Sorensen

Peter Emmanuel Maligres

Wilhelm Stahl

Adrian Leonard Smith

Erwin Paul Schreiner

Yoshitaka Ichikawa

Jonathan James Duffield

Wei-Min Dai

Toshio Suzuki

David Rabuka

Franklin W Okumu

Robert G Bergman

Farah Kondori Babakhani

Kenneth Marby

Pamela Sears

Sulan Yao

Robert E Minto

Robert Discordia

Steve Sucheck

Sebastian V Wendeborn

Chang-Hsing Liang

K C Nicolaou

Yoshi Ichikawa

Emmanuel Pitsinos

Jin-Jun Liu

Adrian L Smith

Sebastian V Wenderborn

Jonathan Duffield

Yoshiaki Ichikawa

Described herein are novel macrolides, the preparation of novel macrolides, the use of novel macrolides for preventing, treating, or ameliorating various conditions, and the use of novel macrolides as antibacterial agents.

Antibacterial agents

The present invention relates generally to the 18-membered macrocyclic antimicrobial agents called Tiacumicins, specifically, OPT-80 (which is composed almost entirely of the R-Tiacumicin B), pharmaceutical compositions comprising OPT-80, and methods using OPT-80. In particular, this compound is a potent drug for the treatment of bacterial infections, specificallyinfections.

18-membered macrocycles and analogs thereof

Described herein are novel macrolides, the preparation of novel macrolides, to the use of novel macrolides for preventing, treating, or ameliorating various conditions, and the use of novel macrolides as antibacterial agents.

A fused ring system compound is disclosed that contains an epoxide group on one side of the fused rings and an enediyne macrocyclic ring on the other side of the fused rings. The compounds have DNA-cleaving, antimicrobial and tumor growth-inhibiting properties. Chimeric compounds having the fused ring system compound as an aglycone bonded to (i) a sugar moiety as the oligosaccharide portion or (ii) a monoclonal antibody or antibody combining site portion thereof that immunoreacts with target tumor cells are also disclosed. Compositions containing a compound or a chimer are disclosed, as are methods of preparing a compound.

Dynemicin analogs: syntheses, methods of preparation and use

Open chain enediyne dihydroperoxides having eight carbons between the hydroperoxide groups that cleave DNA are disclosed, as are methods of making and using the same.

Open chain enediyne dihydroperoxides having DNA cleaving properties

Dynemicin analogs: synthesis, methods of preparation and use

A taxol intermediate selected from the group consisting of: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each selected from hydrogen, hydroxyl, or a protected hydroxyl; or R.sup.1 and R.sup.2 together form an oxo or a protected oxo; R.sup.3 is formyl, a protected formyl, or --CH(X)--OY wherein X is hydrogen or a monovalent metal and Y is hydrogen or a hydroxyl protecting group; and R.sup.4 and R.sup.5 are different and each selected from chloro or cyano; or R.sup.4 and R.sup.5 together form an oxo or a protected oxo, with the proviso that R.sup.1 and R.sup.2 are not both hydroxyl; R.sup.6 is hydroxyl or a protected hydroxyl; R.sup.7 is hydrogen, hydroxyl, or a protected hydroxyl; R.sup.8 is carboxyl, hydroxylmethyl, or a protected hydroxylmethyl; or R.sup.7 and R.sup.8 when taken together with carbon atoms 3 and 4, form an oxetane ring; or R.sup.6 and R.sup.8 when taken together with carbon atoms 1 and 4, form a bridged lactone; R.sup.9 is hydrogen or a hydroxyl protecting group; R.sup. 10 is hydroxyl or a protected hydroxyl; or R.sup.8 and R.sup.10 when taken together with carbon atoms 4 and 5, form a .gamma.-butyrolactone ring; R.sup.11 is alkoxycarbonyl, formyl, a protected formyl, hydroxylmethyl or a protected hydroxylmethyl; or R.sup.6 and R.sup.11 when taken together with carbon atoms 1 and 6, form a 2,2-dimethyl-1,3-dioxane ring; and the dotted line between the 2- and 3-positions of the six-membered ring represents an optional bond.

Intermediates for preparation of taxols

Chimeric analogs of calicheamicin that include an analog of calicheamicinone linked to an ester or glycoside, (-)-calicheamicinone and its analogs are disclosed.

Analogs of calicheamicin gamma1I, method of making and using the same

Macrocyclic enediynediols and enediynediones having a ten carbon ring and open chain enediyne dihydroperoxides having eight carbons between the hydroperoxide groups that cleave DNA are disclosed, as are methods of making and using the same.

Ten-membered ring enediynediols and enediynediones having DNA cleaving

Growing community of inventors

San Diego, CA, United States of America

Chan-Kou Hwang