Abstract: The present invention provides: a method for identifying a blood cancer patient who may benefit from a monotherapy using a drug comprising a DNA methyl transferase inhibitor and a combination therapy using the aforesaid drug together with another epigenetic controller; a pharmaceutical composition to be used in treating a patient who has been identified or selected by the method; and a kit for identifying such a patient. More particularly, the aforesaid method comprises a step for measuring the expression amount of DUSP5 in a sample obtained from a blood cancer patient. When the expression amount measured in this step is lower than a reference expression amount of DUSP5, then the patient is identified or selected as a blood cancer patient who may benefit from a treatment using the drug comprising a DNA methyl transferase inhibitor.

Abstract: [Problems] The object is to provide a compound as a therapeutic or prophylactic agent for TKI-resistant CML to replace the injection “Dacogen®” which has been clinically used as a therapeutic agent for high-risk myelodysplastic syndrome and acute myeloid leukemia. The said compound has remarkable stability against cytidine deaminase, a hydrolytic enzyme, and is absorbed in vivo even by oral administration, incorporated into the biosynthesis route of nucleic acid, and exhibits the effect of inhibiting DNA methyltransferase (DNMT).

Abstract: To provide, in place of injected agents (nucleoside-based anticancer agents or antivirus agents) clinically used as therapeutic drugs for cancer or virus infections, a medicine that has high stability with respect to various hydrolytic metabolic enzymes, is absorbed into the body even by oral administration, and exhibits a cytocidal effect by being incorporated into a DNA and RNA biosynthetic route and inhibiting the modification and extension of DNA and RNA or inhibiting reverse transcriptases or inhibiting protein synthesis. The aforementioned problem is solved by a novel compound represented by formula (I). (In the formula, D is the 5?-position moiety of a nucleoside-based anticancer agent or an antivirus agent, and R1 and R2 are each a benzyl group that may have the same substituent or different substituents.

Abstract: 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?-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 OR3 or a hydrogen atom, R1, R2, and R3 are each independently hydrogen atom or silyl group represented by formula (2): wherein, R4, R5, and R6 are 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 R1, R2, and R3 are not hydrogen atom simultaneously.

Abstract: 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?-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 OR3 or a hydrogen atom, R1, R2, and R3 are each independently hydrogen atom or silyl group represented by formula (2): wherein, R4, R5, and R6 are 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 R1, R2, and R3 are not hydrogen atom simultaneously.

Abstract: 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?-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 OR3 or a hydrogen atom, R1, R2, and R3 are each independently hydrogen atom or silyl group represented by formula (2): wherein, R1, R5, and R6 are 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 R1, R2, and R3 are not hydrogen atom simultaneously.

Abstract: 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?-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 OR3 or a hydrogen atom, R1, R2, and R3 are each independently hydrogen atom or silyl group represented by formula (2): wherein, R1, R5, and R6 are 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 R1, R2, and R3 are not hydrogen atom simultaneously.

Abstract: The present invention relates to a novel compound represented by formula (1), or salt thereof, wherein R is hydroxy group or hydrogen atom; R1 and R2 are the same or different, and are each independently benzyl group which may have a substituent. The present invention provides therapeutically agents, which have remarkable stability against cytidine deaminase, a metabolic enzyme, can be absorbed in vivo by oral administration and inhibit protein synthesis by being incorporated easily into nucleic acid bio-synthesis in vivo for replacing injection agent (5-azacytidine or 2?-deoxy-5-azacytidine) used in clinic for treating myeloma.

Abstract: The present invention relates to a novel compound represented by formula (1), or salt thereof, wherein R is hydroxy group or hydrogen atom; R1 and R2 are the same or different, and are each independently benzyl group which may have a substituent. The present invention provides therapeutically agents, which have remarkable stability against cytidine deaminase, a metabolic enzyme, can be absorbed in vivo by oral administration and inhibit protein synthesis by being incorporated easily into nucleic acid bio-synthesis in vivo for replacing injection agent (5-azacytidine or 2?-deoxy-5-azacytidine) used in clinic for treating myeloma.

Abstract: Novel 1,5-benzothiazepine derivatives having the formula; ##STR1## (wherein R.sub.1, R.sub.2 and R.sub.3 each denotes hydrogen, a halogen, a lower alkyl group, a lower alkoxy group or a hydroxy group; R.sub.4 denotes a lower alkyl group, an allyl group, a lower alkoxyalkyl group, a lower alkyl group substituted with a hydroxy group or a halogen, a lower alkylaminoalkyl group or a morpholino lower alkyl group; X denotes a halogen or hydrogen) are produced from corresponding 1,4-benzothiazine by a ring expansion reaction with trimethylhalosilane, hydrogen peroxide and water. The derivatives have analgesic, antipyretic and antiarrythmic activities.