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:
Jun. 27, 2017

Filed:

Jul. 06, 2015
Applicant:

President and Fellows of Harvard College, Cambridge, MA (US);

Inventors:

Andrew G. Myers, Boston, MA (US);

David A. Kummer, La Jolla, CA (US);

Derun Li, Roselle Park, NJ (US);

Evan Hecker, Arlington, MA (US);

Amelie Dion, Cambridge, MA (US);

Peter M. Wright, Cambridge, MA (US);

Assignee:
Attorney:
Primary Examiner:
Int. Cl.
CPC ...
A61K 31/423 (2006.01); C07D 261/20 (2006.01); C07C 45/67 (2006.01); C07C 45/69 (2006.01); C07C 49/637 (2006.01); C07C 237/26 (2006.01); C07C 311/05 (2006.01); C07D 207/16 (2006.01); C07D 209/58 (2006.01); C07D 213/30 (2006.01); C07D 213/74 (2006.01); C07D 233/61 (2006.01); C07D 277/24 (2006.01); C07D 277/64 (2006.01); C07D 295/15 (2006.01); C07D 295/155 (2006.01); C07D 498/04 (2006.01); C07F 7/08 (2006.01); C07C 29/32 (2006.01); C07C 45/00 (2006.01); C07C 45/29 (2006.01); C07D 261/18 (2006.01); C07F 7/18 (2006.01);
U.S. Cl.
CPC ...
C07D 261/20 (2013.01); C07C 29/32 (2013.01); C07C 45/00 (2013.01); C07C 45/29 (2013.01); C07C 45/67 (2013.01); C07C 45/673 (2013.01); C07C 45/69 (2013.01); C07C 49/637 (2013.01); C07C 237/26 (2013.01); C07C 311/05 (2013.01); C07D 207/16 (2013.01); C07D 209/58 (2013.01); C07D 213/30 (2013.01); C07D 213/74 (2013.01); C07D 233/61 (2013.01); C07D 261/18 (2013.01); C07D 277/24 (2013.01); C07D 277/64 (2013.01); C07D 295/15 (2013.01); C07D 295/155 (2013.01); C07D 498/04 (2013.01); C07F 7/0814 (2013.01); C07F 7/188 (2013.01); C07B 2200/07 (2013.01); C07C 2101/02 (2013.01); C07C 2101/08 (2013.01); C07C 2103/46 (2013.01); C07C 2103/66 (2013.01);
Abstract

The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.


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