The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Dec. 12, 2000

Filed:

Oct. 30, 1998
Applicant:
Inventors:

Gary H Posner, Baltimore, MD (US);

Soon Hyung Woo, Pointe-Claire, CA;

Poonsakdi Ploypradith, Baltimore, MD (US);

Michael H Parker, Baltimore, MD (US);

Theresa A Shapiro, Towson, MD (US);

Jeffrey S Elias, Baltimore, MD (US);

John Northrop, Baltimore, MD (US);

Qun Y Zheng, Wayne, NJ (US);

Christopher Murray, Longmont, CO (US);

Randall J Daughenbaugh, Longmont, CO (US);

Assignees:

Hauser, Inc., Boulder, CO (US);

Johns Hopkins University, Baltimore, MD (US);

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
A61K / ; C07D / ;
U.S. Cl.
CPC ...
514450 ; 514422 ; 548518 ; 549320 ; 549348 ;
Abstract

The present invention provides a two-step procedure for the replacement of the pyranose anomeric 10-OH group in dihydroartemisinin by a variety of carbon nucleophiles, resulting in the novel C-10 carbon-substituted trioxanes of structure: ##STR1## wherein, when n is 1, R is selected from a group of unsubstituted or substituted aryls, heteroaryls, polyethylene glycol, acetylenics, or benzoylmethylenes, or alkanoylmethylenes; or when n is 2, R is selected from a group of unsubstituted or substituted aryls, heteroaryls, polyethylene glycol, alkenyls, alkyls, diketones or bis-acetylenes; or when n is 3, R is selected from a group of unsubstituted or substituted aryls, heteroaryls, polyethylene glycol, alkenyls, alkyls, diketones or bis-acetylenes.


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