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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.

Patent No.:

US 9963481 B1

PDFFull Text
Date of Patent:
May. 08, 2018

Filed:

Sep. 07, 2012

Chiral oligomeric pentenoate amides as bio-oligomer mimetics

Applicants:

Glenn C. Micalizio, Palm Beach Gardens, FL (US);

Thomas Kodadek, Jupiter, FL (US);

Mohosin Sarkar, Palm Beach Gardens, FL (US);

Inventors:

Glenn C. Micalizio, Palm Beach Gardens, FL (US);

Thomas Kodadek, Jupiter, FL (US);

Mohosin Sarkar, Palm Beach Gardens, FL (US);

Assignee:

The Scripps Research Institute, La Jolla, CA (US);

Attorneys:

Geoffrey K. Cooper

Thomas Fitting

Primary Examiner:

Valerie Rodriguez-Garcia

Int. Cl.
CPC ...
C07K 5/08 (2006.01); A61K 31/19 (2006.01); A61K 45/06 (2006.01); C07D 405/14 (2006.01); C07D 405/10 (2006.01); C07B 53/00 (2006.01); C07C 57/52 (2006.01); C07C 57/60 (2006.01); C07C 57/64 (2006.01); A61K 31/192 (2006.01); A61K 38/06 (2006.01); C07C 51/00 (2006.01); C07K 5/02 (2006.01); C07K 5/083 (2006.01); G01N 33/50 (2006.01); C07C 57/54 (2006.01);
U.S. Cl.
CPC ...
C07K 5/08 (2013.01); A61K 31/19 (2013.01); A61K 31/192 (2013.01); A61K 38/06 (2013.01); A61K 45/06 (2013.01); C07B 53/00 (2013.01); C07C 51/00 (2013.01); C07C 57/52 (2013.01); C07C 57/54 (2013.01); C07C 57/60 (2013.01); C07C 57/64 (2013.01); C07D 405/10 (2013.01); C07D 405/14 (2013.01); C07K 5/0205 (2013.01); C07K 5/0804 (2013.01); G01N 33/5008 (2013.01); C07B 2200/07 (2013.01); C07B 2200/11 (2013.01); G01N 2800/7028 (2013.01);
Abstract

Chiral oligomeric pentenoate amides are bio-oligomer mimetics possessing a high degree of conformation rigidity. Conformational rigidity is desirable in the design of molecules with high affinities for biological receptors and enzymes. Libraries of such oligomeric mimetics, such as of chiral oligomeric pentenoate amides can be used to probe biological systems. The present invention provides a method for preparation of chiral oligomeric pentanoate amides comprising conversion of a chiral oxazolidinone (4) to a chiral monomer of formula (1) which can be oligomerized to a chiral compound of formula (12) and so forth.

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