JP6162349B1 - ５−アザシチジン類の糖部シリルエーテル誘導体 - Google Patents

５−アザシチジン類の糖部シリルエーテル誘導体 Download PDF

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Publication number
JP6162349B1
JP6162349B1 JP2016565699A JP2016565699A JP6162349B1 JP 6162349 B1 JP6162349 B1 JP 6162349B1 JP 2016565699 A JP2016565699 A JP 2016565699A JP 2016565699 A JP2016565699 A JP 2016565699A JP 6162349 B1 JP6162349 B1 JP 6162349B1
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Prior art keywords
group
azacytidine
compound
salt
formula
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Japanese (ja)
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JPWO2017183217A1 (ja
Inventor
孫市 酒向
孫市 酒向
晋平 杉山
晋平 杉山
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Ohara Pharmaceutical Co Ltd
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Ohara Pharmaceutical Co Ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/12—Triazine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H23/00—Compounds containing boron, silicon or a metal, e.g. chelates or vitamin B12

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
JP2016565699A 2016-04-21 2016-07-27 ５−アザシチジン類の糖部シリルエーテル誘導体 Active JP6162349B1 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
JP2016085145 2016-04-21
JP2016085145 2016-04-21
PCT/JP2016/065660 WO2017183215A1 (ja) 2016-04-21 2016-05-27 ５－アザシチジン類の糖部シリルエーテル誘導体
JPPCT/JP2016/065660 2016-05-27
PCT/JP2016/072010 WO2017183217A1 (ja) 2016-04-21 2016-07-27 ５－アザシチジン類の糖部シリルエーテル誘導体

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2017092160A Division JP2017197539A (ja) 2016-04-21 2017-05-08 ５−アザシチジン類の糖部シリルエーテル誘導体

Publications (2)

Publication Number Publication Date
JP6162349B1 true JP6162349B1 (ja) 2017-07-12
JPWO2017183217A1 JPWO2017183217A1 (ja) 2018-04-26

Family

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Family Applications (2)

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JP2016565699A Active JP6162349B1 (ja) 2016-04-21 2016-07-27 ５−アザシチジン類の糖部シリルエーテル誘導体
JP2017092160A Pending JP2017197539A (ja) 2016-04-21 2017-05-08 ５−アザシチジン類の糖部シリルエーテル誘導体

Family Applications After (1)

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JP2017092160A Pending JP2017197539A (ja) 2016-04-21 2017-05-08 ５−アザシチジン類の糖部シリルエーテル誘導体

Country Status (7)

Country Link
US (1) US9901641B2 (enExample)
EP (2) EP3543249A1 (enExample)
JP (2) JP6162349B1 (enExample)
KR (1) KR102579485B1 (enExample)
CN (1) CN108368148B (enExample)
MY (1) MY182327A (enExample)
WO (2) WO2017183215A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025142803A1 (ja) * 2023-12-25 2025-07-03 大原薬品工業株式会社 Ｄｎｍｔ阻害剤の経口投与用の医薬組成物

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10227374B2 (en) * 2016-04-21 2019-03-12 Ohara Pharmaceutical Co., Ltd. Silyl etherified derivatives of 5-azacytidines in carbohydrate moiety
WO2019160127A1 (ja) * 2018-02-19 2019-08-22 大原薬品工業株式会社 Ｄｎｍｔ阻害剤の用途
CN112638422B (zh) * 2018-10-30 2023-03-17 大原药品工业株式会社 医药组合物
JPWO2021060341A1 (enExample) * 2019-09-26 2021-04-01
WO2022031759A1 (en) * 2020-08-04 2022-02-10 Herophilus, Inc. Decitabine induced mecp2 expression and uses thereof
CN116940365A (zh) * 2021-02-23 2023-10-24 大原药品工业株式会社 慢性髓性白血病干细胞抑制剂
WO2025263591A1 (ja) * 2024-06-21 2025-12-26 大原薬品工業株式会社 経口用ｄｎｍｔ阻害剤の結晶形態

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5527077B1 (enExample) * 1970-03-14 1980-07-17
JP2009509531A (ja) * 2005-09-29 2009-03-12 スーパージェン インコーポレイテッド ５−アザ−シトシンを組み込んだオリゴヌクレオチドアナログ
WO2013036846A2 (en) * 2011-09-09 2013-03-14 Koronis Pharmaceuticals, Incorporated N4 derivatives of deoxycytidine prodrugs
WO2016057828A1 (en) * 2014-10-08 2016-04-14 Epigenetics Pharma Llc Silylated pyrimidine prodrugs and methods of their use

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3816619A (en) 1965-08-25 1974-06-11 Upjohn Co Ladakamycin and process for preparing same
CH527207A (de) 1968-05-08 1972-08-31 Ceskoslovenska Akademie Ved Verfahren zur Herstellung von 1-Glycosyl-5-azacytosinen
GB0227906D0 (en) * 2002-11-29 2003-01-08 Amedis Pharm Ltd Compounds and their use
AU2003302624A1 (en) * 2002-11-29 2004-06-23 Amedis Pharmaceuticals Ltd. Silicon compounds
KR100866399B1 (ko) 2002-12-10 2008-11-03 엘지엔시스(주) 매체자동지급기의 모듈부 스톱퍼장치
KR100897924B1 (ko) 2002-12-10 2009-05-18 엘지엔시스(주) 금융통합단말기 프린터부의 용지가이드 장치
CN102010455B (zh) * 2009-09-05 2012-07-11 山东新时代药业有限公司 一种地西他滨的制备方法
CN103619864A (zh) * 2011-03-31 2014-03-05 细胞基因国际有限公司 5-氮杂胞苷的合成
KR101922702B1 (ko) 2016-05-10 2018-11-29 주식회사 씨엔제이 기판용 필름의 재활용 칩 제작방법 및 장치

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5527077B1 (enExample) * 1970-03-14 1980-07-17
JP2009509531A (ja) * 2005-09-29 2009-03-12 スーパージェン インコーポレイテッド ５−アザ−シトシンを組み込んだオリゴヌクレオチドアナログ
WO2013036846A2 (en) * 2011-09-09 2013-03-14 Koronis Pharmaceuticals, Incorporated N4 derivatives of deoxycytidine prodrugs
WO2016057828A1 (en) * 2014-10-08 2016-04-14 Epigenetics Pharma Llc Silylated pyrimidine prodrugs and methods of their use

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, vol. 306, no. 2, JPN6017003086, 2003, pages 558 - 563, ISSN: 0003541881 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025142803A1 (ja) * 2023-12-25 2025-07-03 大原薬品工業株式会社 Ｄｎｍｔ阻害剤の経口投与用の医薬組成物

Also Published As

Publication number Publication date
WO2017183217A1 (ja) 2017-10-26
JP2017197539A (ja) 2017-11-02
CN108368148A (zh) 2018-08-03
WO2017183215A1 (ja) 2017-10-26
EP3252067B1 (en) 2019-05-29
MY182327A (en) 2021-01-19
EP3252067A1 (en) 2017-12-06
EP3252067A4 (en) 2017-12-06
EP3543249A1 (en) 2019-09-25
CN108368148B (zh) 2021-11-05
KR20180134835A (ko) 2018-12-19
US20170304337A1 (en) 2017-10-26
JPWO2017183217A1 (ja) 2018-04-26
US9901641B2 (en) 2018-02-27
KR102579485B1 (ko) 2023-09-20

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