University of Michigan

Shaman Pharmaceuticals, Inc.

Harrier Inc.

Masato Koreeda

Brian Keith Shull

Roeland J Tuinman

Wu Yang

Todd A Houston

Bernard Loev

Donald E Bierer

Clarke Slemon

Jeffrey M Dener

Michael S Tempesta

Thien V Truong

Richard Hector

R Erich Klemke

R -Erich Klemke

Novel analogs of fusidic acid are described with one or more carbohydrate units attached. Certain glycosylated analogs of fusidic acid have enhanced solubility properties in diluents or excipient of choice as compared to unmodified fusidic acid. Certain glycosylated analogs may be employed as chemotherapeutic agents and particular analogs may be useful for fighting anti-microbial infections.

Glycosylated analogs of fusidic acid

Novel glycosides, especially steroidal and non-steroidal glycosides are provided. The steroidal and non-steroidal glycosides preferably are prepared from aglycons which possess valuable properties such as pharmacological properties. The glycosides are prepared from useful aglycons and possess useful properties which are the same as those of their respective unglycosylated aglycons. The glycosides are provided in acylated and deacylated form. The acylated glycosides after hydrolysis of the acyl groups possess enhanced water solubility properties, as illustrated in the case where the aglycon is acetominophen.

Glycoside compounds and methods of synthesis

The present invention relates to chemotherapeutic agents, and more particularly, to novel analogs of camptothecin. The camptothecin analogs display increased solubility through the hydrophilicity of added non-ionic sugar substituents. In accordance with the present invention, a member from the class of novel camptothecin analogs is to be delivered in vivo as a chemotherapeutic agent to fight cancer growth in the body.

Process for preparing glycosylated analogs of camptothecin

Glycoside derivatives of acetaminophen

Glycosylated analogs of camptothecin

This invention pertains to a novel group of 1,2-dithiin compounds useful as antiinfective agents, and a novel synthetic process to produce the same. The compounds are particularly effective in treating fungal infections, especially those caused by Candida albicans, Cryptococcus neoformans or Aspergillus fumigatus.

1,2-dithiin antiinfective agents

Novel water-soluble mono and disaccharides of 1,2-dithiins, as well as methods for their synthesis and the synthesis of 3,6-bis(hydroxymethyl)-1,2-dithiin, are provided. The water-soluble compounds have useful medicinal applications, e.g., as an antifungal agent or antibacterial agent in a pharmaceutically acceptable carrier.

Water-soluble glycosylated derivatives of 1,2-dithiin compounds

The invention concerns C-glycosylated derivatives of soft carbon nucleophile compounds, particularly compounds which contain acid-labile structural units. The invention further concerns a mild, cost-effective, non-hazardous and stereoselective method of general application employing a glycal as a glycosyulating agent and iodine as a catalyst for the preparation of C-glycosylated soft carbon nucleophile compounds.

Synthesis of C-glycosylated compounds with the use of a mild,

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Ann Arbor, MI, United States of America

Masato Koreeda