Shaman Pharmaceuticals, Inc.

University of Michigan

Axys Pharmaceuticals, Inc.

Jeffrey M Dener

Donald E Bierer

Thien V Truong

Michael S Tempesta

Bernard Loev

Masato Koreeda

Anthony R Gangloff

Wu Yang

Elaine Yee-Lin Kuo

Ken Duane Rice

Richard Hector

Joane Litvak

Steven Row King

Reimar C Bruening

Larisa G Dubenko

Guohua Mao

Shivanand D Jolad

Thien V Troung

John E Kuo

Novel compounds, compositions and methods effective for the prevention and treatment of mast-cell mediated inflammatory disorders are described. The compounds, compositions and methods are effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis, as well as other types of immunomediated inflammatory disorders, such as rheumatoid arthritis, conjunctivitis and inflammatory bowel disease, various dermatological conditions, as well as certain viral conditions. The compounds comprise potent and selective inhibitors of the mast cell protease tryptase. The compositions for treating these conditions include oral, inhalant, topical and parenteral preparations as well as devices comprising such preparations.

Compositions and methods for treating mast-cell mediated conditions

This invention pertains to a synthetic process for obtaining a unique phosphocholine derivative which has been isolated from the leaves of the plant Irbachia alata, identified to be 1,22-bis�2-(trimethylammonium)ethylphosphatyl! docosane is disclosed. Also disclosed is a synthetic process for obtaining a novel class of mono- and bis(phosphocholine) derivatives which are useful as antiinfective agents. The compounds are particularly effective in treating fungal infections, especially those caused by Candida albicans, Cryptococcus neoformans, and Aspergillus fumigatus.

Process for the preparation of mono-  and bis(phosphocholine)

Class of phosphocholine derivatives having antifungal activity

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 1,2-dithiin compounds useful as antifungal or anti-infective agents, as well as methods for their use as such, are described. The 1,2-dithiin compounds are particularly effective in treating infections, especially those caused by Candida albicans, Cryptococcus neoformans, Aspergillus fumigatus, Candida krusei, Candida parapsilosis, Candida tropicalis, Trichophyton rubrum, Epidermophyton species, Microsporum species, Sporothrix species, Blastomyces dermatitidis, Coccidiodes immiitis, Histoplasma capsulatum, Herpes virus, Influenza virus, Cytomegalovirus, human immunodeficiency virus, retrovirus, Adenovirus, Papillomavirus, Paravirus, Arenavirus, Bunyavirus, Coronavirus, Paramyxovirus, Picornavirus, Rhabdovirus, Togavirus, Hepadnavirus, Staphylococcus aureus, Streptococcus faecalis, Escherichia coli, Pseudomonas aeruginosa, Enterobacter aerogenes, Klebsiella pneumoniae, Staphylococcus epidermis, Zanthomonus maltrophilia, Acinetobacter, Enterobacter cloacae, Serratia marscens, Listeria, Monocytogenes, Enterococcus faecalis, Streptococcus pyogenes; Streptococcus pneumonia, Viridans streptococci, Haemophilus influenzae, Proteus mirabills, Proteus vulgaris and Bacterioides fragilis.

1,2-dithiins having antifungal activity

The present invention provides an improved procedure for the preparation of 3,6-disubstituted-1,2-dithiin derivatives, especially unsymmetrical 1,2-dithiins. In addition, the process offers significant process, scaleup, and safety advantages over the previously reported synthetic processes. The compounds synthesized by this new process and described herein are particularly effective in treating fungal infections, especially those caused by Candida albicans, Cryptococcus neoformans, Aspergillus fumigatus, Trichophyton rubrum, Candida parapsilosis, Candida tropicalis, or Candida krusei.

Preparation of symmetrical and unsymmetrical

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Daly City, CA, United States of America

Jeffrey M Dener