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Title:
SUGAR MOIETY SILYL ETHER DERIVATIVE OF 5-AZACYTIDINE
Document Type and Number:
WIPO Patent Application WO/2017/183215
Kind Code:
A1
Abstract:
[Problem] To provide, as a substitute for a clinically used injected drug (5-azacytidine or 2'-deoxy-5-azacytidine), a 5-azacytidine or 2'-deoxy-5-azacytidine prodrug having high stability against the metabolic enzyme cytidine deaminase, as a therapeutic drug for various bone marrow tumors including myelodysplastic syndrome. [Solution] The aforementioned problem is solved by a compound, or salt thereof, represented in formula (1) (In the formula, R is an OR3 group or a hydrogen atom, R1, R2 and R3 are each a hydrogen atom or a silyl group represented by formula (2) (in that formula, R4, R5 and R6 are each an alkyl group optionally having a substituent, an aryl optionally having a substituent, or an arylalkyl group optionally having a substituent.) However, R1, R2 and R3 cannot all simultaneously be a hydrogen atom.).

Inventors:
SAKO MAGOICHI (JP)
SUGIYAMA SHINPEI (JP)
Application Number:
PCT/JP2016/065660
Publication Date:
October 26, 2017
Filing Date:
May 27, 2016
Export Citation:
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Assignee:
OHARA PHARMACEUTICAL CO LTD (JP)
International Classes:
C07H19/12; A61K31/706; A61P7/06; A61P35/00; A61P43/00
Domestic Patent References:
WO2016057828A12016-04-14
WO2013036846A22013-03-14
WO2004050665A12004-06-17
WO2004050666A12004-06-17
Foreign References:
JP2009509531A2009-03-12
Other References:
SIEDLECKI, PAWEL ET AL.: "Establishment and functional validation of a structural homology model for human DNA methyltransferase 1", BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, vol. 306, no. 2, 2003, pages 558 - 563, XP055066318
Attorney, Agent or Firm:
SHA Takuho (JP)
謝 卓峰 (JP)
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