Patents Assigned to OHARA PHARMACEUTICAL CO., LTD.
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Patent number: 11173174Abstract: [Problem] To provide, in place of injected agents (such as Vidaza® and Dacogen®) clinically used as therapeutic drugs for high-risk myelodysplastic syndromes, a medicine as a therapeutic drug or a prophylactic drug for various advanced solid tumors, said medicine having high stability with respect to cytidine deaminase which is a hydrolytic metabolic enzyme, being absorbed into the body even by oral administration, and having an effect of being integrated into a nucleic acid biosynthetic route and inhibiting DNA methyltransferases, i.e., DNMTs. [Solution] The aforementioned problem is solved by a novel compound represented by formula (I). (In the formula, R is a hydroxyl group or a hydrogen atom, and R1 and R2 are each a benzyl group that may have a substituent.Type: GrantFiled: April 24, 2018Date of Patent: November 16, 2021Assignee: Ohara Pharmaceutical Co., Ltd.Inventors: Sako Magoichi, Toshikazu Ushijima, Naoko Hattori
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Patent number: 10227374Abstract: 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.Type: GrantFiled: February 22, 2018Date of Patent: March 12, 2019Assignee: Ohara Pharmaceutical Co., Ltd.Inventors: Magoichi Sako, Shinpei Sugiyama
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Publication number: 20180179246Abstract: 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.Type: ApplicationFiled: February 22, 2018Publication date: June 28, 2018Applicant: OHARA PHARMACEUTICAL CO., LTD.Inventors: Magoichi Sako, Shinpei SUGIYAMA
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Patent number: 9901641Abstract: 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.Type: GrantFiled: November 18, 2016Date of Patent: February 27, 2018Assignee: Ohara Pharmaceutical Co., Ltd.Inventors: Magoichi Sako, Shinpei Sugiyama
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Publication number: 20170304337Abstract: 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.Type: ApplicationFiled: November 18, 2016Publication date: October 26, 2017Applicant: OHARA PHARMACEUTICAL CO., LTD.Inventors: Magoichi SAKO, Shinpei SUGIYAMA
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Patent number: 9670238Abstract: 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.Type: GrantFiled: November 18, 2016Date of Patent: June 6, 2017Assignee: Ohara Pharmaceutical Co., Ltd.Inventors: Magoichi Sako, Xiong Luo
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Publication number: 20170152275Abstract: 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.Type: ApplicationFiled: November 18, 2016Publication date: June 1, 2017Applicant: OHARA PHARMACEUTICAL CO., LTD.Inventors: MAGOICHI SAKO, XIONG LUO