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.:
Date of Patent:
Jun. 18, 2013
Filed:
Sep. 06, 2011
Harshani Lawrence, Tampa, FL (US);
Yiyu GE, Tampa, FL (US);
Said M. Sebti, Tampa, FL (US);
Wayne Guida, St. Petersburg, FL (US);
Harshani Lawrence, Tampa, FL (US);
Yiyu Ge, Tampa, FL (US);
Said M. Sebti, Tampa, FL (US);
Wayne Guida, St. Petersburg, FL (US);
University of South Florida, Tampa, FL (US);
H. Lee Moffitt Cancer Center and Research Institute, Inc., Tampa, FL (US);
Abstract
Disclosed herein is the use of HLM-008182, as well as its analogues formed via in-house synthesis, as a potent proteasome inhibitors. A new method was developed for HLM-008182 through a four-step protocol and the method was further optimized to a two step protocol. The synthesis in both protocols was regioselective with TiCl. The reaction was highly efficient with microwave assisted heating and THF as solvent. The modification around the molecule HLM-008182 established primary SAR, indicating that the proteasome inhibition activity was a function of the 2-side chain.