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Last Updated: December 22, 2024

Claims for Patent: 3,923,785

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Summary for Patent: 3,923,785

Title:	(R)-3-(2-deox y-.beta.-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[4,][1,3]diaz epin-8-ol
Abstract:	Essentially pure (R)-3-(2-deoxy-.beta.-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[ 4,5-d][1,3]-diazepin-8-ol and the process for the production of (R)-3-(2-deoxy-.beta.-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[ 4,5-d][1,3]diazepin-8-ol by inoculating an aqueous nutrient medium, preferably containing sources of assimilable carbon and nitrogen and added inorganic salt and having a pH between about 6 and 8, with a (R)-3-(2-deoxy-.beta.-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[ 4,5-d][1,3]diazepin-8-ol producing strain of Streptomyces antibioticus, such as the strain corresponding to NRRL 3238, conducting a fermentation under aseptic aerobic conditions at a temperature between about 20 and 45.degree.C. until a substantial quantity of (R)-3-(2-deoxy-.beta.-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo- [4,5-d][1,3]diazepin-8-ol is formed, and isolating the desired product from the fermentation mixture are disclosed. The (R)-3-(2-deoxy-.beta.-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[ 4,5-d][1,3]diazepin-8-ol potentiates the activity of 9-(.beta.-D-arabinofuranosyl)adenine as an antiviral agent that is active in vitro and in vivo against DNA viruses such as herpes and vaccinia viruses.
Inventor(s):	Ryder; Albert (Detroit, MI), Dion; Henry W. (Detroit, MI), Woo; Peter W. (Ann Arbor, MI), Howells; John D. (Grosse Pointe Woods, MI)
Assignee:	Parke, Davis & Company (Detroit, MI)
Application Number:	05/462,826
Patent Claims:	1. An essentially pure compound having the name (R)-3-(2-deoxy-.beta.-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[ 4,5-d][1,3]diazepin-8-ol. 2. A mixture consisting of the compound of claim 1 and 9-(.beta.-D-arabinofuranosyl)adenine. 3. The mixture of claim 2 wherein the ratio of (R)-3-(2-deoxy-.beta.-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[ 4,5-d][1,3]diazepin-8-ol to 9-(.beta.-D-arabinofuranosyl)adenine is from about 0.005 to 0.2:1.

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