发明授权
US5273979A C-31 desmethyl FR-900520 cyclic hemiketal immunosuppressant agent
失效
C-31脱甲基FR-900520循环半抗体免疫抑制剂
- 专利标题: C-31 desmethyl FR-900520 cyclic hemiketal immunosuppressant agent
- 专利标题(中): C-31脱甲基FR-900520循环半抗体免疫抑制剂
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申请号: US738997申请日: 1991-08-01
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公开(公告)号: US5273979A公开(公告)日: 1993-12-28
- 发明人: Shieh-Shung T. Chen , Raymond F. White , Georgette Dezeny , Byron H. Arison , Thomas R. Beattie , Amy M. Hale , Francis Dumont
- 申请人: Shieh-Shung T. Chen , Raymond F. White , Georgette Dezeny , Byron H. Arison , Thomas R. Beattie , Amy M. Hale , Francis Dumont
- 申请人地址: NJ Rahway
- 专利权人: Merck & Co., Inc.
- 当前专利权人: Merck & Co., Inc.
- 当前专利权人地址: NJ Rahway
- 主分类号: A61K31/445
- IPC分类号: A61K31/445 ; A61P37/06 ; C07D498/22 ; C07H19/01 ; C12N1/20 ; C12P17/18 ; C12P19/44 ; C12R1/56 ; A61K31/395 ; C07D491/16
摘要:
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 derivative (Compound II) of Compound I produced by enzymatic methylation using 31-O-desmethylimmunomycin O-methyl transferase, (DIMT), a methyl transferase enzyme. The macrolide immunosuppressants are useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.