The invention provides 4′-C-ethynyl pyrimidine nucleosides (other than 4′-C-ethynylthymidine) represented by formula [I]:
1
wherein B represents a base selected from the group consisting of pyrimidine and derivatives thereof; X represents a hydrogen atom or a hydroxyl group; and R represents a hydrogen atom or a phosphate residue; and a pharmaceutical composition containing any one of the compounds and a pharmaceutically acceptable carrier. Preferably, the composition is used as an anti-HIV agent or a drug for treating AIDS.
4′-C-ethynyl pyrimidine nucleosides and pharmaceutical compositions thereof
申请人:Yamasa Corporation
公开号:US06403568B1
公开(公告)日:2002-06-11
The invention provides 4′-C-ethynyl pyrimidine nucleosides (other than 4′-C-ethynylthymidine) represented by formula [I]:
wherein B represents a base selected from the group consisting of pyrimidine and derivatives thereof; X represents a hydrogen atom or a hydroxyl group; and R represents a hydrogen atom or a phosphate residue; and a pharmaceutical composition containing any one of the compounds and a pharmaceutically acceptable carrier. Preferably, the composition is used as an anti-HIV agent or a drug for treating AIDS.
4′-C-ethynyl pyrimidine nucleoside compounds and pharmaceutical compositions
申请人:Yamasa Corporation
公开号:US06291670B1
公开(公告)日:2001-09-18
The invention provides 4′-C-ethynyl pyrimidine nucleosides (other than 4′-C-ethynylthymidine) represented by formula [I]:
wherein B represents a base selected from the group consisting of pyrimidine and derivatives thereof; X represents a hydrogen atom or a hydroxyl group; and R represents a hydrogen atom or a phosphate residue; and a pharmaceutical composition containing any one of the compounds and a pharmaceutically acceptable carrier. Preferably, the composition is used as an anti-HIV agent or a drug for treating AIDS.
The invention provides 4′-C-ethynyl purine nucleosides represented by formula [I]:
wherein B represents a base selected from the group consisting of purine and derivatives thereof; X represents a hydrogen atom or a hydroxyl group; and R represents a hydrogen atom or a phosphate residue; and a pharmaceutical composition containing any one of the compounds and a pharmaceutically acceptable carrier. Preferably, the composition is used as an anti-HIV agent or a drug for treating AIDS.
A process for immobilizing cells is described, particularly procaryotic cells, which includes a step of adsorbing said cells on a resin, wherein such a resin is a weak anionic exchange resin and preferably has amino moieties; when the immobilized cells are UPase and/or PNPase producing cells, nucleosides can be produced by reaction of a pentose-1-phosphate with a purine or pyrimidine base, and transglycosylation reactions can be performed; advantageously, as immobilized UPase or PNPase producing cells,
Escherichia
cells of the DH5alpha strain transformed by the plasmid vectors having the sequences reported in Seq. Id. No. 1 and 2. are used.