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:
May. 02, 1995
Filed:
Oct. 16, 1992
David G Kingston, Blacksburg, VA (US);
Jingyu Liang, Nanjing, CN;
Virginia Tech Intellectual Properties, Inc., Blacksburg, VA (US);
Abstract
Substituted 2'-benzoyl and 2', 7-dibenzoyl taxol derivatives are synthesized which have improved water solubility and stability while maintaining bioactivity. In a preferred embodiment, taxol 2',7-di(sodium 1,2-benzenedicarboxylate) is synthesized by reacting taxol with phthalic anhydride, and subsequently neutralizing the resulting acid by an ion exchange resin. Taxol 2'-(sodium 1,4-benzenedicarboxylate) is prepared by reacting the monobenzyl ester of 1,4-benzene dicarboxylic acid with taxol in the presence of dicyclohexyl carbodiimide and dimethylaminopyridine, hydrogenolysing the resulting ester to remove the benzyl group, and neutralizing with ion exchange resin. Other taxol prodrugs are prepared by modifications of these routes. In a preferred embodiment, the compounds prepared have improved water-solubility as compared with taxol and demonstrate activity in the M109 mouse bioassay system.