C-21 hydroxylated fk-506 antagonist

Details C-21 hydroxylated fk-506 antagonist C-21 hydroxylated fk-506 antagonist

C - Chemistry, Metallurgy

12

P

C12P 17/18 (2006.01) A61K 31/435 (2006.01) A61K 31/445 (2006.01) C07D 498/18 (2006.01) C12N 1/20 (2006.01)

Patent

CA 2071332

175/RJN114 18452Y TITLE OF THE INVENTION NEW C-21 HYDROXYLATED FK-506 ANTAGONIST ABSTRACT OF THE DISCLOSURE Described is a process for producing a new FK-506 antagonist agent, a C-21 hydroxylated analog of FR-900520 under novel fermentation conditions utilizing the novel microorganism, Streptomvces hvgroscopicus (Merck Culture Collection MA 6832) ATCC No. 55166. The macrolide antagonist is useful in preventing and/or counteracting accidental or inadvertent FK-506 overdosage in an FK-506 thera- peutic program designed to prevent autoimmune diseases or human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.

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