Albany Molecular Research, Inc.

Jun-Ho Maeng

David Douglas Manning

Zhicai Yang

Bruce Francis Molino

Peter C Michels

Cheng Guo

Grant J Carr

Matthew W Chase

The present invention relates to novel therapeutics with antibacterial activity, processes for their preparation, and pharmaceutical, veterinary and nutritional compositions containing them as active ingredients. The present invention also relates to uses of the novel therapeutics, for example, as medicants or food additives in the treatment of bacterial infections or to aid body mass gain in a subject.

Antibacterial compounds, methods of making them, and uses thereof

The present invention relates to a process for preparation of a trans ISA247 compound of the formula: where R&#x2550;H or D; R&#x2550;H or D; and R&#x2550;H or D, by application of organozirconium chemistry. The process involves reacting an acetyl cyclosporin aldehyde with an organozirconium reagent to provide acetyl cyclosporin diene (the acetate of trans ISA247) and deacetylating the acetyl cyclosporin diene to produce the trans-isomer of ISA247. The present invention also relates to a process for preparing the same trans ISA247 compound, using olefin cross metathesis. The process involves: olefin cross metathesis of acetyl cyclosporin A to afford acetyl cyclosporin &#x3b1;,&#x3b2;-unsaturated aldehyde; Wittig reaction of the acetyl cyclosporin &#x3b1;,&#x3b2;-unsaturated aldehyde to provide acetyl cyclosporin diene; and deacetylation of the acetyl cyclosporin diene to produce the trans ISA247 compound. Also disclosed are processes for preparing an acetyl cyclosporin &#x3b1;,&#x3b2;-unsaturated aldehyde compound and a cyclosporin triene analogue compound. 

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Cohoes, NY, United States of America

Jun-Ho Maeng