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:
Jul. 12, 1977
Filed:
Dec. 03, 1975
Carl P Schaffner, Trenton, NJ (US);
Witold Mechlinski, New Brunswick, NJ (US);
Rutgers Research and Educational Foundation, New Brunswick, NJ (US);
Abstract
Derivatives of amphoteric polyene macrolide antibiotics which carry, on the lactone ring, a carboxyl group and an amino sugar characterized by a primary amine group, consist of (a) the methyl, ethyl or propyl ester formed by esterification of the carboxyl group, and (b) salts of such polyene esters constituted as acid addition salts formed with the amine group. The derivatives (a) and (b) have effective antimicrobial activity, e.g. antifungal potency, comparable to the base antibiotics, and the acid salts (b), produced by suitable acids, e.g. hydrochlorides, can be made to have good water solubility which is normally unattainable with the base compounds and is of special advantage in a compound which retains strong activity. Other addition salts are also of value, for example to provide lipid-soluble forms of these antifungal polyenes. Esterification of these chemically sensitive antibiotics is unusually successful using diazomethane, diazoethane or diazopropane with tetrahydrofurane as solvent to produce the ester dissolved therein, avoiding degradation of the base antibiotic or of its potency.