Title:
PARAMYCIN METABOLITE
Document Type and Number:
Japanese Patent JP3183554
Kind Code:
B2
Abstract:
PURPOSE: To obtain a rapamycin metabolite useful for treating transplantation rejection, host vs. graft disease, autoimmune diseases, solid tumors and fungal infections as an immunosuppressant, an antiinflammation agent, an antitumor agent and an antifungal agent.
CONSTITUTION: This rapamycin metabolite, e.g. 41-O-desmethyl rapamycin, has a deprotonated molecular ion detected at a mass to charge ratio of 899, and a characteristic desorption chemical ionization mass spectroscopic fragmentation pattern comprising ions detected at mass to charge ratios of 591, 569, 559, 543, 529, 421 and 308. The compound is obtained, e.g. by isolating human liver microsome, controlling the concentration of the protein, adding the acetonitrile/water solution of the rapamycin to the microsome solution, and reacting the rapamycin with the microsome in the presence of a NADPH regeneration system prepared by dissolving DETA, MgCl, NADP, isocitric acid and isocitric acid dehydrogenase in a phosphate buffer solution.
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Inventors:
Uwe Christians
Karl Friedrich Sewing
Martin Zatler
Karl Friedrich Sewing
Martin Zatler
Application Number:
JP11881192A
Publication Date:
July 09, 2001
Filing Date:
May 12, 1992
Export Citation:
Assignee:
American Home Products Corporation
International Classes:
A61P29/00; A61P31/04; A61P37/06; C07D498/18; C12P17/18; A61K31/435; (IPC1-7): C07D498/18; A61K31/435; A61P29/00; A61P37/06
Attorney, Agent or Firm:
Aoyama Ryo (1 person outside)
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