SUGAR MOIETY SILYL ETHER DERIVATIVE OF 5-AZACYTIDINE

WIPO Patent Application WO/2017/183217

A1

[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.).

SAKO MAGOICHI (JP)
SUGIYAMA SHINPEI (JP)

PCT/JP2016/072010

October 26, 2017

July 27, 2016

Click for automatic bibliography generation  

OHARA PHARMACEUTICAL CO LTD (JP)

C07H19/12; A61K31/706; A61P7/06; A61P35/00; A61P43/00

WO2016057828A1	2016-04-14
WO2013036846A2	2013-03-14
WO2004050665A1	2004-06-17
WO2004050666A1	2004-06-17
WO2004050665A1	2004-06-17
WO2004050666A1	2004-06-17

JP2009509531A	2009-03-12
US3816619A	1974-06-11
DE1922702A1	1969-11-20

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
ONCOLOGY, vol. 30, no. 5, 1974, pages 405 - 422
EXPERT OPINION ON PHARMACOTHERAPY, vol. 14, no. 9, 2013, pages 1255 - 1268
THE JOURNAL OF CLINICAL INVESTIGATION, vol. 124, no. 1, 2014, pages 40 - 46
THE JOURNAL OF CLINICAL INVESTIGATION, vol. 53, 1974, pages 922 - 931
BUNSEKI, vol. 7, 2008, pages 332 - 336
JOURNAL OF AMERICAN CHEMICAL SOCIETY, vol. 94, 1972, pages 6190 - 6191
TETRAHEDRON LETTERS, vol. 22, 1981, pages 3455 - 3458
SYNTHESIS, 1996, pages 1031 - 1069
PROTECTIVE GROUPS IN ORGANIC SYNTHESIS, 1999
TETRAHEDRON, vol. 60, 2004, pages 5833 - 5871
TETRAHEDRON, vol. 69, 2013, pages 2383 - 2417
COLLECTIN OF CZECHOSLOVAK CHEMICAL COMMUNICATION, vol. 61, 1996, pages S23 - S25
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATION, vol. 306, 2003, pages 558 - 563
JOURNAL OF AMERICAN CHEMICAL SOCIETY, vol. 134, 2012, pages 7978 - 7982
NANO LETTERS, vol. 14, no. 3, 2014, pages 1472 - 1476
COREY, E.J ET AL., J. AM. CHEM. SOC., vol. 94, 1972, pages 6190
MORITA, T ET AL., TETRAHEDRON LETT., vol. 21, 1980, pages 835
Y. KITA ET AL., TETRAHEDRON LETT., 1979, pages 4311
LALONDE, M.; CHAN, T. H., SYNTHESIS, 1985, pages 817 - 845
JOURNAL OF CLINICAL PATHOLOGY, vol. 59, 2006, pages 947 - 951

SHA Takuho (JP)

View/Download PDF      PDF Help

Previous Patent: DEVICE FOR MANUFACTURING THREE-DIMENSIONAL CONNECTED FILAMENT AND METHOD FOR MANUFACTURING THREE-DIM...

Next Patent: MULTILAYER CUSHION AND MATTRESS EQUIPPED WITH SAME