N,N,N-Trimethyl derivatives of polyene amphoteric antibiotics, p

Drug – bio-affecting and body treating compositions – Conjugate or complex of monoclonal or polyclonal antibody,... – Conjugated via claimed linking group – bond – chelating agent,...

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536 17, A61K 3171

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active

041443284

ABSTRACT:
The present invention relates to novel substances; namely, to N,N,N-trimethyl derivatives of polyene amphoteric antibiotics, and to a process of producing same, said substances having the following general formula: ##STR1## wherein R is aglycone of a polyene amphoteric antibiotic, without the carboxyl group.
The process of producing N,N,N-trimethyl derivatives of polyene amphoteric antibiotics is carried out in an organic solvent medium wherein said polyene amphoteric antibiotics are subjected to complete amino-group methylation by means of a methylating agent with subsequent separation of the end product. N,N,N-trimethyl derivatives of polyene amphoteric antibiotics possess high antibiotic activity thus inhibiting the growth of yeast, yeast-like microorganisms, and filamentous fungi. Said compounds are used in medicine to treat fungal diseases.

REFERENCES:
patent: 3945993 (1976-03-01), Schaffner et al.
patent: 4002741 (1977-01-01), Kulbakh et al.
Noller, "Chemistry of Organic Compounds", 3rd Ed., 1965, pp. 252-253, W. B. Saunders Co., Phila., Pa.

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