KR102087080B1 - 에독사반의 제조용 중간체의 제조 방법 및 에독사반의 제조 방법 - Google Patents

에독사반의 제조용 중간체의 제조 방법 및 에독사반의 제조 방법 Download PDF

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KR102087080B1
KR102087080B1 KR1020180065951A KR20180065951A KR102087080B1 KR 102087080 B1 KR102087080 B1 KR 102087080B1 KR 1020180065951 A KR1020180065951 A KR 1020180065951A KR 20180065951 A KR20180065951 A KR 20180065951A KR 102087080 B1 KR102087080 B1 KR 102087080B1
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edoxaban
compound
formula
preparing
represented
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KR20190139463A (ko
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정헌석
니라사 자야프라카시
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주식회사 가피바이오
동방에프티엘(주)
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Priority to KR1020180065951A priority Critical patent/KR102087080B1/ko
Priority to JP2018175006A priority patent/JP2019210273A/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/26—Radicals substituted by halogen atoms or nitro radicals
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020180065951A 2018-06-08 2018-06-08 에독사반의 제조용 중간체의 제조 방법 및 에독사반의 제조 방법 Active KR102087080B1 (ko)

Priority Applications (3)

Application Number Priority Date Filing Date Title
KR1020180065951A KR102087080B1 (ko) 2018-06-08 2018-06-08 에독사반의 제조용 중간체의 제조 방법 및 에독사반의 제조 방법
JP2018175006A JP2019210273A (ja) 2018-06-08 2018-09-19 エドキサバンの製造方法
JP2023101357A JP7664971B2 (ja) 2018-06-08 2023-06-21 エドキサバンの製造方法

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
KR1020180065951A KR102087080B1 (ko) 2018-06-08 2018-06-08 에독사반의 제조용 중간체의 제조 방법 및 에독사반의 제조 방법

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KR20190139463A KR20190139463A (ko) 2019-12-18
KR102087080B1 true KR102087080B1 (ko) 2020-03-10

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20210152213A (ko) * 2020-06-08 2021-12-15 주식회사 파마코스텍 신규한 에독사반 벤젠술폰산염 1 수화물의 제조방법
KR20250049636A (ko) 2023-10-05 2025-04-14 주식회사 파마코스텍 신규한 에독사반 제조방법

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102090912B1 (ko) * 2019-12-18 2020-03-18 유니셀랩 주식회사 신규한 결정형 형태의 에독사반 및 이의 제조방법
CN111393456B (zh) * 2020-03-31 2022-07-12 内蒙古京东药业有限公司 一种由三氯乙酮鎓盐衍生物制备依度沙班的方法
CN111763222B (zh) * 2020-08-03 2021-05-25 珠海市海瑞德新材料科技有限公司 用于制备依度沙班游离碱的中间体及其制备方法和应用
WO2023223346A1 (en) * 2022-05-16 2023-11-23 Mylan Laboratories Limited An improved process for the preparation of edoxaban intermediate
CN115594613B (zh) * 2022-10-31 2024-04-19 上海柏狮生物科技有限公司 依度沙班中间体及其制备方法
CN116332958A (zh) * 2023-03-30 2023-06-27 浙江九洲药业股份有限公司 一种依度沙班对甲苯磺酸盐的制备方法
CN116332957A (zh) * 2023-03-30 2023-06-27 浙江九洲药业股份有限公司 一种FXa抑制剂化合物的制备方法
WO2024197723A1 (zh) * 2023-03-30 2024-10-03 浙江九洲药业股份有限公司 一种依度沙班对甲苯磺酸盐的制备方法

Citations (5)

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Publication number Priority date Publication date Assignee Title
JP2010120852A (ja) 2007-03-09 2010-06-03 Daiichi Sankyo Co Ltd 新規なジアミド誘導体
JP5666424B2 (ja) 2009-03-10 2015-02-12 第一三共株式会社 ジアミン誘導体の製造方法
CN104761571A (zh) 2015-03-10 2015-07-08 山东科兴生物制品有限公司 一种依度沙班的合成方法
CN105399667A (zh) * 2015-12-15 2016-03-16 南京艾德凯腾生物医药有限责任公司 一种依度沙班中间体的制备方法
CN107641131A (zh) * 2016-07-22 2018-01-30 江苏威凯尔医药科技有限公司 一种抗血栓药物的制备方法

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JP4128138B2 (ja) 2001-06-20 2008-07-30 第一三共株式会社 ジアミン誘導体
WO2010131663A1 (ja) * 2009-05-15 2010-11-18 第一三共株式会社 オキサミド誘導体
KR102371784B1 (ko) * 2014-02-18 2022-03-07 다이이찌 산쿄 가부시키가이샤 활성화 혈액 응고 제 X 인자 (FXa) 의 저해약의 제조 방법

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010120852A (ja) 2007-03-09 2010-06-03 Daiichi Sankyo Co Ltd 新規なジアミド誘導体
JP5666424B2 (ja) 2009-03-10 2015-02-12 第一三共株式会社 ジアミン誘導体の製造方法
CN104761571A (zh) 2015-03-10 2015-07-08 山东科兴生物制品有限公司 一种依度沙班的合成方法
CN105399667A (zh) * 2015-12-15 2016-03-16 南京艾德凯腾生物医药有限责任公司 一种依度沙班中间体的制备方法
CN107641131A (zh) * 2016-07-22 2018-01-30 江苏威凯尔医药科技有限公司 一种抗血栓药物的制备方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
논문 Organic Process Research and Development (2009)*

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20210152213A (ko) * 2020-06-08 2021-12-15 주식회사 파마코스텍 신규한 에독사반 벤젠술폰산염 1 수화물의 제조방법
KR102513519B1 (ko) * 2020-06-08 2023-03-23 주식회사 파마코스텍 신규한 에독사반 벤젠술폰산염 1 수화물의 제조방법
KR20250049636A (ko) 2023-10-05 2025-04-14 주식회사 파마코스텍 신규한 에독사반 제조방법

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JP2019210273A (ja) 2019-12-12
JP2023116769A (ja) 2023-08-22
KR20190139463A (ko) 2019-12-18

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