发明授权
- 专利标题: Cytidine nucleoside compound
- 专利标题(中): 胞苷核苷化合物
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申请号: US654019申请日: 1976-01-30
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公开(公告)号: US4096324A公开(公告)日: 1978-06-20
- 发明人: Robert C. Kelly , William J. Wechter
- 申请人: Robert C. Kelly , William J. Wechter
- 申请人地址: MI Kalamazoo
- 专利权人: The Upjohn Company
- 当前专利权人: The Upjohn Company
- 当前专利权人地址: MI Kalamazoo
- 主分类号: C07H19/06
- IPC分类号: C07H19/06 ; C07H19/08
摘要:
5'-Esters of ara-cytidine (1-.beta.-D-arabinofuranosylcytosine) are prepared by reacting ara-cytidine with .beta.,.beta.,.beta.-trihaloethoxycarbonyl halide or other protective agency to form a protective amido group on the primary amino nitrogen of ara-cytidine and then reacting the thus-protected compound with a reagent reactive with the 5'-O-hydroxyl group, e.g., an acylating agent, to form the 5'-O-derivative. The .beta.,.beta.,.beta.-trihaloethoxycarbonyl or other protective group is then removed. Alternately, the primary amino group of ara-cytidine can be protected from acylation by protonation. The 5'-O-derivatives in their free base of salt form are characterized in that they display the property of sustained release of the compound, ara-cytidine, when administered intramuscularly or subcutaneously. Ara-cytidine is known for its anti-viral action and for its usefulness as an agent for controlling leukemias, including acute leukemia, and the sustained release property extends the usefulness of ara-cytidine for these purposes and as an inmunosuppressive agent. The 5'-O-derivartives of this invention can also be administered orally.
公开/授权文献
- US5016156A High voltage stabilizing circuit 公开/授权日:1991-05-14