Ohara Pharmaceutical Co., Ltd.

Shinpei Sugiyama

Magoichi Sako

The present invention relates to a prodrug of 5-azacytidine or 2'-deoxy-5-azacytidine having remarkable stability against cytidine deaminase, a metabolic hydrolyzing enzyme in replacement of current injections (5-azacytidine or 2&#x2032;-deoxy-5-azacytidine) which are clinically used as therapeutic agents for various myelomas including myelodysplastic syndrome. The present invention provides a compound represented by formula (1), or salt thereof, wherein, R is ORor a hydrogen atom, R, R, and Rare each independently hydrogen atom or silyl group represented by formula (2): wherein, R, R, and Rare each independently alkyl group which may have a substituent, aryl group which may have a substituent, or arylalkyl group which may have a substituent, with the provision that R, R, and Rare not hydrogen atom simultaneously.

Silyl etherified derivatives of 5-azacytidines in carbohydrate moiety

The present invention relates to a prodrug of 5-azacytidine or 2'-deoxy-5-azacytidine having remarkable stability against cytidine deaminase, a metabolic hydrolyzing enzyme in replacement of current injections (5-azacytidine or 2&#x2032;-deoxy-5-azacytidine) which are clinically used as therapeutic agents for various myelomas including myelodysplastic syndrome. The present invention provides a compound represented by formula (1), or salt thereof,  

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Shiga, Japan

Shinpei Sugiyama