JP2022022550A - アピキサバンの新規製造方法 - Google Patents
アピキサバンの新規製造方法 Download PDFInfo
- Publication number
- JP2022022550A JP2022022550A JP2020110365A JP2020110365A JP2022022550A JP 2022022550 A JP2022022550 A JP 2022022550A JP 2020110365 A JP2020110365 A JP 2020110365A JP 2020110365 A JP2020110365 A JP 2020110365A JP 2022022550 A JP2022022550 A JP 2022022550A
- Authority
- JP
- Japan
- Prior art keywords
- apixaban
- reaction
- compound
- formamide
- production method
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- CQEYGVVPQQVSNL-UHFFFAOYSA-N CCOC(c(c(CCN1c(cc2)ccc2NC(CCCCCl)=O)c2C1=O)n[n]2-c(cc1)ccc1OC)=O Chemical compound CCOC(c(c(CCN1c(cc2)ccc2NC(CCCCCl)=O)c2C1=O)n[n]2-c(cc1)ccc1OC)=O CQEYGVVPQQVSNL-UHFFFAOYSA-N 0.000 description 2
- QNZCBYKSOIHPEH-UHFFFAOYSA-N COc(cc1)ccc1-[n]1nc(C(N)=O)c(CCN2c(cc3)ccc3N(CCCC3)C3=O)c1C2=O Chemical compound COc(cc1)ccc1-[n]1nc(C(N)=O)c(CCN2c(cc3)ccc3N(CCCC3)C3=O)c1C2=O QNZCBYKSOIHPEH-UHFFFAOYSA-N 0.000 description 2
Classifications
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hematology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2020110365A JP2022022550A (ja) | 2020-06-26 | 2020-06-26 | アピキサバンの新規製造方法 |
| PCT/JP2021/020478 WO2021261172A1 (ja) | 2020-06-26 | 2021-05-28 | アピキサバンの新規製造方法 |
| CN202180059664.3A CN116137814A (zh) | 2020-06-26 | 2021-05-28 | 阿哌沙班的新型制造方法 |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2020110365A JP2022022550A (ja) | 2020-06-26 | 2020-06-26 | アピキサバンの新規製造方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2022022550A true JP2022022550A (ja) | 2022-02-07 |
| JP2022022550A5 JP2022022550A5 (enExample) | 2022-11-29 |
Family
ID=79282492
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020110365A Pending JP2022022550A (ja) | 2020-06-26 | 2020-06-26 | アピキサバンの新規製造方法 |
Country Status (3)
| Country | Link |
|---|---|
| JP (1) | JP2022022550A (enExample) |
| CN (1) | CN116137814A (enExample) |
| WO (1) | WO2021261172A1 (enExample) |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007001385A2 (en) * | 2004-09-28 | 2007-01-04 | Bristol-Myers Squibb Company | Process for preparing 4,5-dihydro-pyrazolo [3,4-c] pyrid-2-ones |
| CN104045637A (zh) * | 2014-04-18 | 2014-09-17 | 河北科技大学 | 一种阿哌沙班的制备方法 |
| JP2017521437A (ja) * | 2014-07-11 | 2017-08-03 | ラボラトリオス、レスビ、ソシエダッド、リミターダLaboratorios Lesvi,S.L. | アピキサバンの製造方法 |
| CN110862389A (zh) * | 2018-08-28 | 2020-03-06 | 江苏康缘药业股份有限公司 | 一种阿哌沙班晶型的制备方法 |
| WO2020120485A1 (en) * | 2018-12-11 | 2020-06-18 | Krka, D.D., Novo Mesto | Process for preparing apixaban |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200303201A (en) * | 2001-12-10 | 2003-09-01 | Bristol Myers Squibb Co | Synthesis of 4,5-dihydro-pyrazolo [3,4-c] pyrid-2-ones |
| CN104892601B (zh) * | 2015-06-09 | 2017-09-19 | 江苏中邦制药有限公司 | 一种抗血栓药物阿哌沙班的制备方法 |
| CN110615788B (zh) * | 2019-10-17 | 2021-07-06 | 江西国药有限责任公司 | 一种高纯度阿哌沙班的制备工艺 |
-
2020
- 2020-06-26 JP JP2020110365A patent/JP2022022550A/ja active Pending
-
2021
- 2021-05-28 CN CN202180059664.3A patent/CN116137814A/zh active Pending
- 2021-05-28 WO PCT/JP2021/020478 patent/WO2021261172A1/ja not_active Ceased
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007001385A2 (en) * | 2004-09-28 | 2007-01-04 | Bristol-Myers Squibb Company | Process for preparing 4,5-dihydro-pyrazolo [3,4-c] pyrid-2-ones |
| CN104045637A (zh) * | 2014-04-18 | 2014-09-17 | 河北科技大学 | 一种阿哌沙班的制备方法 |
| JP2017521437A (ja) * | 2014-07-11 | 2017-08-03 | ラボラトリオス、レスビ、ソシエダッド、リミターダLaboratorios Lesvi,S.L. | アピキサバンの製造方法 |
| CN110862389A (zh) * | 2018-08-28 | 2020-03-06 | 江苏康缘药业股份有限公司 | 一种阿哌沙班晶型的制备方法 |
| WO2020120485A1 (en) * | 2018-12-11 | 2020-06-18 | Krka, D.D., Novo Mesto | Process for preparing apixaban |
Non-Patent Citations (1)
| Title |
|---|
| WANG, Y. ET AL.: "Design, synthesis, and structure-activity relationship of novel and effective apixaban derivatives a", BIOORG. MED. CHEM., vol. 24, JPN6021024814, 2016, pages 5646 - 5661, ISSN: 0005169685 * |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2021261172A1 (ja) | 2021-12-30 |
| CN116137814A (zh) | 2023-05-19 |
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