C-31 desmethyl fr-900520 cyclic hemiketal immunosuppressant...

C - Chemistry – Metallurgy – 12 – P

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C12P 17/18 (2006.01) A61K 31/445 (2006.01) C07H 19/01 (2006.01) C12P 19/44 (2006.01)

Patent

CA 2074856

75/RJN36 18489 TITLE OF THE INVENTION NEW C-31 DESMETHYL FR-900520 CYCLIC HEMIKETAL IMMUNOSUPPRESSANT AGENT ABSTRACT OF THE DISCLOSURE Described is a process for producing a new immunosuppressant, a C-31 desmethyl, C-19/C-22 cyclic hemiketal biotransformation analog (Compound I) of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces, lavendulae ATCC No. 55209. Also disclosed is the C-31 methylated devivative (Compound II) of Compound I produced by enzymatic methylation using 31-O-des- methylimmunomycin O-methyl transferase, (DIMT), a methyl transferase enzyme. The macrolide 75/RJN36 - i - 18489 immunosuppressants are useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.

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