HRP20221540T1 - Postupak za proizvodnju supstituiranog derivata policikličkog piridona i njegovog kristala - Google Patents
Postupak za proizvodnju supstituiranog derivata policikličkog piridona i njegovog kristala Download PDFInfo
- Publication number
- HRP20221540T1 HRP20221540T1 HRP20221540TT HRP20221540T HRP20221540T1 HR P20221540 T1 HRP20221540 T1 HR P20221540T1 HR P20221540T T HRP20221540T T HR P20221540TT HR P20221540 T HRP20221540 T HR P20221540T HR P20221540 T1 HRP20221540 T1 HR P20221540T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound
- formula
- salt
- image
- crystal
- Prior art date
Links
- 239000013078 crystal Chemical class 0.000 title claims 4
- 238000004519 manufacturing process Methods 0.000 title claims 4
- -1 polycyclic pyridone derivative Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 12
- 238000000034 method Methods 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- IUYHWZFSGMZEOG-UHFFFAOYSA-M magnesium;propane;chloride Chemical compound [Mg+2].[Cl-].C[CH-]C IUYHWZFSGMZEOG-UHFFFAOYSA-M 0.000 claims 4
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical group [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims 3
- 159000000003 magnesium salts Chemical class 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 150000002431 hydrogen Chemical group 0.000 claims 2
- 159000000000 sodium salts Chemical class 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical group CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 1
- KEAYESYHFKHZAL-UHFFFAOYSA-N Sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 claims 1
- WMJMABVHDMRMJA-UHFFFAOYSA-M [Cl-].[Mg+]C1CCCCC1 Chemical compound [Cl-].[Mg+]C1CCCCC1 WMJMABVHDMRMJA-UHFFFAOYSA-M 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 239000012312 sodium hydride Substances 0.000 claims 1
- 229910000104 sodium hydride Inorganic materials 0.000 claims 1
- CGRKYEALWSRNJS-UHFFFAOYSA-N sodium;2-methylbutan-2-olate Chemical compound [Na+].CCC(C)(C)[O-] CGRKYEALWSRNJS-UHFFFAOYSA-N 0.000 claims 1
- WBQTXTBONIWRGK-UHFFFAOYSA-N sodium;propan-2-olate Chemical compound [Na+].CC(C)[O-] WBQTXTBONIWRGK-UHFFFAOYSA-N 0.000 claims 1
- 125000005490 tosylate group Chemical group 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed systems
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B61/00—Other general methods
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Virology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Communicable Diseases (AREA)
- Pulmonology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pyridine Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2016121453 | 2016-06-20 | ||
| EP17815337.5A EP3473629B1 (en) | 2016-06-20 | 2017-06-19 | Method for producing substituted polycyclic pyridone derivative and crystal of same |
| PCT/JP2017/022478 WO2017221869A1 (ja) | 2016-06-20 | 2017-06-19 | 置換された多環性ピリドン誘導体の製造方法およびその結晶 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20221540T1 true HRP20221540T1 (hr) | 2023-03-03 |
Family
ID=60783429
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20221540TT HRP20221540T1 (hr) | 2016-06-20 | 2017-06-19 | Postupak za proizvodnju supstituiranog derivata policikličkog piridona i njegovog kristala |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US11261198B2 (https=) |
| EP (2) | EP4194459A1 (https=) |
| JP (2) | JP6212678B1 (https=) |
| KR (2) | KR102447711B1 (https=) |
| CN (2) | CN113717198B (https=) |
| AR (1) | AR108812A1 (https=) |
| AU (1) | AU2017282305B2 (https=) |
| BR (1) | BR112018076600A2 (https=) |
| ES (1) | ES2936077T3 (https=) |
| HR (1) | HRP20221540T1 (https=) |
| IL (1) | IL263812B2 (https=) |
| MX (1) | MX2018016267A (https=) |
| PL (1) | PL3473629T3 (https=) |
| SG (1) | SG11201810655QA (https=) |
| SI (1) | SI3473629T1 (https=) |
| TW (1) | TWI750188B (https=) |
| WO (1) | WO2017221869A1 (https=) |
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| SG11201804348SA (en) | 2015-12-15 | 2018-06-28 | Shionogi & Co | Medicine for treating influenza characterized by comprising combination of cap-dependent endonuclease inhibitor with anti-influenza drug |
| US11261198B2 (en) * | 2016-06-20 | 2022-03-01 | Shionogi & Co., Ltd. | Process for preparing substituted polycyclic pyridone derivative and crystal thereof |
| KR20190018469A (ko) | 2016-08-10 | 2019-02-22 | 시오노기세야쿠 가부시키가이샤 | 치환된 다환성 피리돈 유도체 및 그의 프로드러그를 함유하는 의약 조성물 |
| US11104689B2 (en) | 2017-09-18 | 2021-08-31 | Sunshine Lake Pharma Co., Ltd. | Influenza virus replication inhibitor and use thereof |
| CN111386276B (zh) | 2017-10-06 | 2023-06-23 | 盐野义制药株式会社 | 制备取代的多环吡啶酮衍生物的立体选择性方法 |
| CN110357850A (zh) * | 2018-03-26 | 2019-10-22 | 广东东阳光药业有限公司 | 一种含硫杂环化合物的制备方法 |
| IL278161B2 (en) | 2018-04-24 | 2024-12-01 | Shionogi & Co | Solid dosage form with excellent stability |
| KR102501180B1 (ko) | 2018-04-24 | 2023-02-21 | 시오노기세야쿠 가부시키가이샤 | 안정성이 우수한 고형 제제 |
| CN108558907B (zh) * | 2018-06-01 | 2019-08-09 | 海化生命(厦门)科技有限公司 | 一种关键中间体2的制备方法 |
| CN110872247A (zh) * | 2018-08-29 | 2020-03-10 | 上海复星星泰医药科技有限公司 | Xofluza含硫杂环化合物、其中间体及制备方法 |
| CN109134428A (zh) * | 2018-10-25 | 2019-01-04 | 南京科技职业学院 | 一种巴洛沙韦中间体的制备方法 |
| CN111170875B (zh) * | 2018-11-09 | 2022-12-27 | 广东东阳光药业有限公司 | 一种二烷氧基胺类化合物的制备方法 |
| CN109721585B (zh) * | 2018-12-19 | 2020-09-29 | 浙江工业大学 | 一种巴洛沙韦关键中间体的制备方法 |
| CN109516998B (zh) * | 2018-12-25 | 2021-06-25 | 深圳市华先医药科技有限公司 | 一种巴洛沙韦中间体的合成方法 |
| CN109504721B (zh) * | 2018-12-26 | 2021-07-09 | 杭州科巢生物科技有限公司 | 一种抗流感药物的合成方法 |
| CN111484508B (zh) * | 2019-01-29 | 2022-11-25 | 北京四环制药有限公司 | 一种用于制备巴罗萨韦或其衍生物的化合物及其制备方法和其应用 |
| CN111574386B (zh) * | 2019-02-19 | 2024-02-23 | 广东东阳光药业股份有限公司 | 一种氧代乙胺化合物的纯化方法 |
| WO2020181025A1 (en) | 2019-03-05 | 2020-09-10 | Assia Chemical Industries Ltd | Solid state forms of baloxavir marboxil |
| AU2019433734B2 (en) | 2019-03-12 | 2025-08-28 | Shionogi & Co., Ltd. | Treating influenza using substituted polycyclic pyridone derivatives and prodrugs thereof in a subject having influenza and a complication risk factor |
| CN111825699B (zh) * | 2019-04-15 | 2023-02-21 | 上海复星星泰医药科技有限公司 | 含硫杂环化合物及其制备方法 |
| CN110143941B (zh) * | 2019-06-04 | 2021-05-25 | 北京四环制药有限公司 | 一种巴罗萨韦玛波酯中间体的合成方法 |
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| CN112521386B (zh) * | 2019-09-19 | 2023-05-26 | 周雨恬 | 具有抗病毒作用的多环吡啶酮化合物及其药物组合和用途 |
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| CN112707862B (zh) * | 2019-10-24 | 2022-09-27 | 广东东阳光药业有限公司 | 一种并环吡啶酮化合物的制备方法 |
| CN111057070A (zh) * | 2019-10-30 | 2020-04-24 | 浙江工业大学 | 一种巴洛沙韦关键中间体的合成方法 |
| WO2021093860A1 (zh) * | 2019-11-13 | 2021-05-20 | 南京知和医药科技有限公司 | 取代的双三环化合物及其药物组合物和用途 |
| WO2021129602A1 (zh) * | 2019-12-23 | 2021-07-01 | 石家庄迪斯凯威医药科技有限公司 | 取代的多环化合物及其药物组合物和用途 |
| CN119080592A (zh) * | 2020-03-07 | 2024-12-06 | 广东东阳光药业股份有限公司 | 一种杂环化合物的合成方法 |
| CN111875619B (zh) * | 2020-07-30 | 2021-06-25 | 深圳市新阳唯康科技有限公司 | 巴洛沙韦酯的晶型及其制备方法 |
| CN114539285B (zh) * | 2020-11-25 | 2025-10-17 | 上海迪赛诺生物医药有限公司 | 一种玛巴洛沙韦的制备方法 |
| EP4262983A1 (en) | 2020-12-15 | 2023-10-25 | Synthon B.V. | Solid forms of baloxavir, salts of baloxavir and cocrystals of baloxavir |
| CN114671889A (zh) * | 2020-12-24 | 2022-06-28 | 江苏威凯尔医药科技有限公司 | 一种取代三环吡啶酮衍生物的晶型及其制备方法 |
| CN115594692B (zh) * | 2021-07-08 | 2025-04-11 | 重庆博腾制药科技股份有限公司 | 一种制备抗流感病毒药物中间体的方法 |
| WO2023286078A1 (en) * | 2021-07-13 | 2023-01-19 | Natco Pharma Limited | An improved process for the preparation of an intermediate of baloxavir morboxil |
| CN113717199B (zh) * | 2021-08-13 | 2022-04-01 | 北京北朋科技有限公司 | 巴洛沙韦的氘代衍生物及其在抗流感病毒中的应用 |
| CN113717200B (zh) * | 2021-09-13 | 2022-11-22 | 石药集团中奇制药技术（石家庄）有限公司 | 一种巴洛沙韦中间体的制备方法 |
| CN114014874B (zh) * | 2021-12-20 | 2023-04-28 | 中国科学院上海药物研究所 | 一种玛巴洛沙韦中间体的制备方法 |
| CN116730962A (zh) * | 2022-03-02 | 2023-09-12 | 上海迪赛诺化学制药有限公司 | 一种2-羟乙基-3-戊氧基-4-吡喃酮的制备方法 |
| CN116751214A (zh) * | 2022-03-05 | 2023-09-15 | 重庆博腾制药科技股份有限公司 | 一种制备(r)-多环吡啶衍生物的方法、应用及其制备玛巴洛沙韦的方法 |
| CN116082361B (zh) * | 2023-04-11 | 2023-06-13 | 和鼎（南京）医药技术有限公司 | 一种制备玛巴洛沙韦中间体和玛巴洛沙韦的方法 |
| CN116891485A (zh) * | 2023-08-24 | 2023-10-17 | 迪嘉药业集团股份有限公司 | 一种玛巴洛沙韦中间体化合物的晶型及其制备方法 |
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| US11261198B2 (en) * | 2016-06-20 | 2022-03-01 | Shionogi & Co., Ltd. | Process for preparing substituted polycyclic pyridone derivative and crystal thereof |
| KR20190018469A (ko) | 2016-08-10 | 2019-02-22 | 시오노기세야쿠 가부시키가이샤 | 치환된 다환성 피리돈 유도체 및 그의 프로드러그를 함유하는 의약 조성물 |
| US9862675B1 (en) | 2017-07-05 | 2018-01-09 | King Fahd University Of Petroleum And Minerals | Method of N-formylating amines with a phosphonic anhydride |
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