JP7179014B2 - ニラパリブの製造方法 - Google Patents
ニラパリブの製造方法 Download PDFInfo
- Publication number
- JP7179014B2 JP7179014B2 JP2019557567A JP2019557567A JP7179014B2 JP 7179014 B2 JP7179014 B2 JP 7179014B2 JP 2019557567 A JP2019557567 A JP 2019557567A JP 2019557567 A JP2019557567 A JP 2019557567A JP 7179014 B2 JP7179014 B2 JP 7179014B2
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- Prior art keywords
- formula
- salt
- acid
- compound
- monohydrate
- Prior art date
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
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- 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
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
- C07C303/32—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of salts of sulfonic acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
- C07C303/42—Separation; Purification; Stabilisation; Use of additives
- C07C303/44—Separation; Purification
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D211/70—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D211/74—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
-
- 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)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Medicinal Preparation (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Saccharide Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762489415P | 2017-04-24 | 2017-04-24 | |
| US201762489387P | 2017-04-24 | 2017-04-24 | |
| US62/489,387 | 2017-04-24 | ||
| US62/489,415 | 2017-04-24 | ||
| PCT/US2018/029131 WO2018200517A1 (en) | 2017-04-24 | 2018-04-24 | Methods of manufacturing of niraparib |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020517668A JP2020517668A (ja) | 2020-06-18 |
| JP2020517668A5 JP2020517668A5 (enExample) | 2021-06-17 |
| JP7179014B2 true JP7179014B2 (ja) | 2022-11-28 |
Family
ID=63919973
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019557567A Active JP7179014B2 (ja) | 2017-04-24 | 2018-04-24 | ニラパリブの製造方法 |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US11161834B2 (enExample) |
| EP (1) | EP3615513B1 (enExample) |
| JP (1) | JP7179014B2 (enExample) |
| KR (1) | KR102582624B1 (enExample) |
| CN (2) | CN118271233A (enExample) |
| AU (2) | AU2018258274C1 (enExample) |
| CA (1) | CA3060715C (enExample) |
| ES (1) | ES2926255T3 (enExample) |
| IL (1) | IL270068B (enExample) |
| MA (1) | MA48475A (enExample) |
| MX (1) | MX393879B (enExample) |
| SG (1) | SG11201909807TA (enExample) |
| TW (1) | TWI783993B (enExample) |
| WO (1) | WO2018200517A1 (enExample) |
| ZA (1) | ZA201906944B (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20240136T1 (hr) | 2016-06-29 | 2024-04-12 | Tesaro, Inc. | Metode liječenja raka jajnika |
| AU2018246214B2 (en) | 2017-03-27 | 2021-07-08 | Merck Sharp & Dohme Llc | Niraparib compositions |
| WO2018200517A1 (en) | 2017-04-24 | 2018-11-01 | Tesaro, Inc. | Methods of manufacturing of niraparib |
| TW202444417A (zh) | 2017-05-09 | 2024-11-16 | 美商提薩羅有限公司 | 治療癌症的組合療法 |
| CN110913911A (zh) | 2017-05-18 | 2020-03-24 | 特沙诺有限公司 | 用于治疗癌症的组合疗法 |
| CN111278433A (zh) | 2017-09-26 | 2020-06-12 | 特沙诺有限公司 | 尼拉帕尼制剂 |
| WO2019067978A1 (en) | 2017-09-30 | 2019-04-04 | Tesaro, Inc. | POLYTHERAPIES FOR THE TREATMENT OF CANCER |
| US11801240B2 (en) | 2017-10-06 | 2023-10-31 | Tesaro, Inc. | Combination therapies and uses thereof |
| US12297184B2 (en) | 2018-10-03 | 2025-05-13 | Tesaro, Inc. | Niraparib salts |
| CN112300074B (zh) * | 2019-08-02 | 2023-12-29 | 北京盈科瑞创新药物研究有限公司 | 一种吲唑甲酰胺类化合物及其制备方法和应用 |
| US20250352534A1 (en) | 2022-02-15 | 2025-11-20 | Tesaro, Inc. | Use of Niraparib for the Treatment of Brain Cancer |
| WO2024142096A1 (en) * | 2022-12-29 | 2024-07-04 | Dr. Reddy’S Laboratories Limited | Process for preparation of niraparib tosylate and its intermediates |
| WO2025017711A1 (en) * | 2023-07-20 | 2025-01-23 | Natco Pharma Limited | An improved process for the preparation of niraparib tosylate monohydrate |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010515715A (ja) | 2007-01-10 | 2010-05-13 | イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・ピー・アー | ポリ(adp−リボース)ポリメラーゼ(parp)阻害剤としてのアミド置換インダゾール |
| JP2011509252A (ja) | 2008-01-08 | 2011-03-24 | メルク シャープ エンド ドーム リミテッド | 2−{4−[(3s)−ピペリジン−3−イル]フェニル}−2h−インダゾール−7−カルボキサミドの薬学的に許容される塩 |
| WO2014088983A1 (en) | 2012-12-07 | 2014-06-12 | Merck Sharp & Dohme Corp. | Regioselective n-2 arylation of indazoles |
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| US5605793A (en) | 1994-02-17 | 1997-02-25 | Affymax Technologies N.V. | Methods for in vitro recombination |
| US6335160B1 (en) | 1995-02-17 | 2002-01-01 | Maxygen, Inc. | Methods and compositions for polypeptide engineering |
| US5837458A (en) | 1994-02-17 | 1998-11-17 | Maxygen, Inc. | Methods and compositions for cellular and metabolic engineering |
| FI104465B (fi) | 1995-06-14 | 2000-02-15 | Valio Oy | Proteiinihydrolysaatteja allergioiden hoitamiseksi tai estämiseksi, niiden valmistus ja käyttö |
| DE69841075D1 (de) | 1997-04-23 | 2009-10-01 | Kaneka Corp | Deoxynukleinsäure welche ein Polypeptid mit stereoselektiver Transaminase Aktivität kodiert, sowie die Deoxynukleinsäure enthaltende Transformanden |
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| US20160160294A1 (en) | 2014-12-08 | 2016-06-09 | Tesaro | Methods and materials for predicting response to niraparib |
| HRP20240136T1 (hr) | 2016-06-29 | 2024-04-12 | Tesaro, Inc. | Metode liječenja raka jajnika |
| CN106496187A (zh) | 2016-09-14 | 2017-03-15 | 陕西科技大学 | 一种制备PARP抑制剂Niraparib的合成方法 |
| CN106432056A (zh) * | 2016-09-17 | 2017-02-22 | 青岛辰达生物科技有限公司 | 一种尼拉帕布中间体(3s)‑3‑(4‑氨基苯基)哌啶‑1‑甲酸叔丁酯的制备方法 |
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| CN106432055A (zh) * | 2016-09-17 | 2017-02-22 | 青岛辰达生物科技有限公司 | 一种尼拉帕布中间体4‑(哌啶‑3‑基)苯胺的制备方法 |
| EP3606523A1 (en) | 2017-03-27 | 2020-02-12 | Tesaro, Inc. | Niraparib formulations |
| AU2018246214B2 (en) | 2017-03-27 | 2021-07-08 | Merck Sharp & Dohme Llc | Niraparib compositions |
| WO2018200517A1 (en) | 2017-04-24 | 2018-11-01 | Tesaro, Inc. | Methods of manufacturing of niraparib |
| TW202444417A (zh) | 2017-05-09 | 2024-11-16 | 美商提薩羅有限公司 | 治療癌症的組合療法 |
| CN110913911A (zh) | 2017-05-18 | 2020-03-24 | 特沙诺有限公司 | 用于治疗癌症的组合疗法 |
| CN111278433A (zh) | 2017-09-26 | 2020-06-12 | 特沙诺有限公司 | 尼拉帕尼制剂 |
| WO2019067978A1 (en) | 2017-09-30 | 2019-04-04 | Tesaro, Inc. | POLYTHERAPIES FOR THE TREATMENT OF CANCER |
| US11801240B2 (en) | 2017-10-06 | 2023-10-31 | Tesaro, Inc. | Combination therapies and uses thereof |
| TW201929902A (zh) | 2017-12-27 | 2019-08-01 | 美商提薩羅有限公司 | 治療癌症之方法 |
| BR112020015909A2 (pt) | 2018-02-05 | 2020-12-15 | Tesaro, Inc. | Formulações pediátricas de niraparib e métodos de tratamento pediátrico |
-
2018
- 2018-04-24 WO PCT/US2018/029131 patent/WO2018200517A1/en not_active Ceased
- 2018-04-24 MX MX2019012658A patent/MX393879B/es unknown
- 2018-04-24 CN CN202410234039.3A patent/CN118271233A/zh active Pending
- 2018-04-24 TW TW107113922A patent/TWI783993B/zh active
- 2018-04-24 AU AU2018258274A patent/AU2018258274C1/en active Active
- 2018-04-24 JP JP2019557567A patent/JP7179014B2/ja active Active
- 2018-04-24 CA CA3060715A patent/CA3060715C/en active Active
- 2018-04-24 US US16/608,059 patent/US11161834B2/en active Active
- 2018-04-24 MA MA048475A patent/MA48475A/fr unknown
- 2018-04-24 ES ES18790167T patent/ES2926255T3/es active Active
- 2018-04-24 IL IL270068A patent/IL270068B/en unknown
- 2018-04-24 CN CN201880040321.0A patent/CN110753684A/zh active Pending
- 2018-04-24 KR KR1020197034673A patent/KR102582624B1/ko active Active
- 2018-04-24 SG SG11201909807T patent/SG11201909807TA/en unknown
- 2018-04-24 EP EP18790167.3A patent/EP3615513B1/en active Active
-
2019
- 2019-10-22 ZA ZA2019/06944A patent/ZA201906944B/en unknown
-
2021
- 2021-08-09 AU AU2021215116A patent/AU2021215116B2/en active Active
- 2021-10-29 US US17/452,928 patent/US11629137B2/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010515715A (ja) | 2007-01-10 | 2010-05-13 | イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・ピー・アー | ポリ(adp−リボース)ポリメラーゼ(parp)阻害剤としてのアミド置換インダゾール |
| JP2011509252A (ja) | 2008-01-08 | 2011-03-24 | メルク シャープ エンド ドーム リミテッド | 2−{4−[(3s)−ピペリジン−3−イル]フェニル}−2h−インダゾール−7−カルボキサミドの薬学的に許容される塩 |
| WO2014088983A1 (en) | 2012-12-07 | 2014-06-12 | Merck Sharp & Dohme Corp. | Regioselective n-2 arylation of indazoles |
Non-Patent Citations (2)
| Title |
|---|
| Chung, Cheol K.,Process Development of C-N Cross-Coupling and Enantioselective Biocatalytic Reactions for the Asymmetric Synthesis of Niraparib,Organic Process Research & Development ,2014年,18(1),,215-227 |
| Wallace, Debra J.,Development of a Fit-for-Purpose Large-Scale Synthesis of an Oral PARP Inhibitor,Organic Process Research & Development,2011年,15(4),,831-840 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3615513B1 (en) | 2022-07-20 |
| TWI783993B (zh) | 2022-11-21 |
| IL270068B (en) | 2022-06-01 |
| AU2018258274B2 (en) | 2021-05-13 |
| ZA201906944B (en) | 2023-03-29 |
| US11161834B2 (en) | 2021-11-02 |
| CA3060715A1 (en) | 2018-11-01 |
| US11629137B2 (en) | 2023-04-18 |
| CN110753684A (zh) | 2020-02-04 |
| EP3615513A1 (en) | 2020-03-04 |
| MA48475A (fr) | 2020-03-04 |
| AU2021215116A1 (en) | 2021-08-26 |
| US20220041575A1 (en) | 2022-02-10 |
| SG11201909807TA (en) | 2019-11-28 |
| AU2018258274C1 (en) | 2021-12-02 |
| NZ758948A (en) | 2024-04-26 |
| CA3060715C (en) | 2024-10-01 |
| BR112019022320A2 (pt) | 2020-05-26 |
| US20200055837A1 (en) | 2020-02-20 |
| CN118271233A (zh) | 2024-07-02 |
| WO2018200517A1 (en) | 2018-11-01 |
| JP2020517668A (ja) | 2020-06-18 |
| AU2018258274A1 (en) | 2019-11-14 |
| ES2926255T3 (es) | 2022-10-24 |
| MX393879B (es) | 2025-03-24 |
| KR20200021456A (ko) | 2020-02-28 |
| EP3615513A4 (en) | 2020-12-09 |
| KR102582624B1 (ko) | 2023-09-22 |
| TW201841889A (zh) | 2018-12-01 |
| AU2021215116B2 (en) | 2022-12-01 |
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