AU2018258274C1 - Methods of manufacturing of niraparib - Google Patents
Methods of manufacturing of niraparib Download PDFInfo
- Publication number
- AU2018258274C1 AU2018258274C1 AU2018258274A AU2018258274A AU2018258274C1 AU 2018258274 C1 AU2018258274 C1 AU 2018258274C1 AU 2018258274 A AU2018258274 A AU 2018258274A AU 2018258274 A AU2018258274 A AU 2018258274A AU 2018258274 C1 AU2018258274 C1 AU 2018258274C1
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- Prior art keywords
- formula
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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
-
- 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)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicinal Preparation (AREA)
- Saccharide Compounds (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2021215116A AU2021215116B2 (en) | 2017-04-24 | 2021-08-09 | Methods of Manufacturing of Niraparib |
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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2021215116A Division AU2021215116B2 (en) | 2017-04-24 | 2021-08-09 | Methods of Manufacturing of Niraparib |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| AU2018258274A1 AU2018258274A1 (en) | 2019-11-14 |
| AU2018258274B2 AU2018258274B2 (en) | 2021-05-13 |
| AU2018258274C1 true AU2018258274C1 (en) | 2021-12-02 |
Family
ID=63919973
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2018258274A Active AU2018258274C1 (en) | 2017-04-24 | 2018-04-24 | Methods of manufacturing of niraparib |
| AU2021215116A Active AU2021215116B2 (en) | 2017-04-24 | 2021-08-09 | Methods of Manufacturing of Niraparib |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2021215116A Active AU2021215116B2 (en) | 2017-04-24 | 2021-08-09 | Methods of Manufacturing of Niraparib |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US11161834B2 (enExample) |
| EP (1) | EP3615513B1 (enExample) |
| JP (1) | JP7179014B2 (enExample) |
| KR (1) | KR102582624B1 (enExample) |
| CN (2) | CN110753684A (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 |
|---|---|---|---|---|
| DK3478286T3 (da) | 2016-06-29 | 2024-01-29 | Tesaro Inc | Fremgangsmåder til behandling af ovariecancer |
| CN110944638A (zh) | 2017-03-27 | 2020-03-31 | 特沙诺有限公司 | 尼拉帕尼组合物 |
| CN110753684A (zh) | 2017-04-24 | 2020-02-04 | 特沙诺有限公司 | 尼拉帕利的制造方法 |
| TWI879716B (zh) | 2017-05-09 | 2025-04-11 | 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 |
| BR112020006039A2 (pt) | 2017-09-26 | 2020-10-06 | Tesaro, Inc. | formulações de niraparibe |
| SG11202002862RA (en) | 2017-09-30 | 2020-04-29 | Tesaro Inc | Combination therapies for treating cancer |
| KR20200067164A (ko) | 2017-10-06 | 2020-06-11 | 테사로, 인코포레이티드 | 조합 요법 및 그의 용도 |
| 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 (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20150299167A1 (en) * | 2012-12-07 | 2015-10-22 | 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 |
| US5837458A (en) | 1994-02-17 | 1998-11-17 | Maxygen, Inc. | Methods and compositions for cellular and metabolic engineering |
| US6335160B1 (en) | 1995-02-17 | 2002-01-01 | Maxygen, Inc. | Methods and compositions for polypeptide 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 |
| IL136574A0 (en) | 1997-12-08 | 2001-06-14 | California Inst Of Techn | A method for forming a polynucleotide of desired properties |
| JP4221100B2 (ja) | 1999-01-13 | 2009-02-12 | エルピーダメモリ株式会社 | 半導体装置 |
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| CN102405281B (zh) | 2009-02-26 | 2015-05-13 | 科德克希思公司 | 转氨酶生物催化剂 |
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| DK3478286T3 (da) | 2016-06-29 | 2024-01-29 | Tesaro Inc | Fremgangsmåder til behandling af ovariecancer |
| 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 |
| CN110944638A (zh) | 2017-03-27 | 2020-03-31 | 特沙诺有限公司 | 尼拉帕尼组合物 |
| TW201842908A (zh) | 2017-03-27 | 2018-12-16 | 美商提薩羅有限公司 | 尼拉帕尼(niraparib)調配物 |
| CN110753684A (zh) | 2017-04-24 | 2020-02-04 | 特沙诺有限公司 | 尼拉帕利的制造方法 |
| TWI879716B (zh) | 2017-05-09 | 2025-04-11 | 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 |
| BR112020006039A2 (pt) | 2017-09-26 | 2020-10-06 | Tesaro, Inc. | formulações de niraparibe |
| SG11202002862RA (en) | 2017-09-30 | 2020-04-29 | Tesaro Inc | Combination therapies for treating cancer |
| KR20200067164A (ko) | 2017-10-06 | 2020-06-11 | 테사로, 인코포레이티드 | 조합 요법 및 그의 용도 |
| CN111801117A (zh) | 2017-12-27 | 2020-10-20 | 特沙诺有限公司 | 治疗癌症的方法 |
| US20210030735A1 (en) | 2018-02-05 | 2021-02-04 | Tesaro, Inc. | Pediatric niraparib formulations and pediatric treatment methods |
-
2018
- 2018-04-24 CN CN201880040321.0A patent/CN110753684A/zh active Pending
- 2018-04-24 TW TW107113922A patent/TWI783993B/zh active
- 2018-04-24 CN CN202410234039.3A patent/CN118271233A/zh active Pending
- 2018-04-24 SG SG11201909807T patent/SG11201909807TA/en unknown
- 2018-04-24 CA CA3060715A patent/CA3060715C/en active Active
- 2018-04-24 ES ES18790167T patent/ES2926255T3/es active Active
- 2018-04-24 EP EP18790167.3A patent/EP3615513B1/en active Active
- 2018-04-24 JP JP2019557567A patent/JP7179014B2/ja active Active
- 2018-04-24 WO PCT/US2018/029131 patent/WO2018200517A1/en not_active Ceased
- 2018-04-24 KR KR1020197034673A patent/KR102582624B1/ko active Active
- 2018-04-24 US US16/608,059 patent/US11161834B2/en active Active
- 2018-04-24 AU AU2018258274A patent/AU2018258274C1/en active Active
- 2018-04-24 MA MA048475A patent/MA48475A/fr unknown
- 2018-04-24 MX MX2019012658A patent/MX393879B/es unknown
- 2018-04-24 IL IL270068A patent/IL270068B/en unknown
-
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 (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20150299167A1 (en) * | 2012-12-07 | 2015-10-22 | Merck Sharp & Dohme Corp. | Regioselective N-2 Arylation of Indazoles |
Non-Patent Citations (2)
| Title |
|---|
| Chung, C.K. et al. 'Process Development of C−N Cross-Coupling and Enantioselective Biocatalytic Reactions for the Asymmetric Synthesis of Niraparib', Org. Process Res. Dev., 2014, vol. 18, pages 215-227. * |
| Wallace, D.J. et al. 'Development of a Fit-for-Purpose Large-Scale Synthesis of an Oral PARP Inhibitor', Org. Process Res. Dev., 2011, vol. 15, pages 831–840. * |
Also Published As
| Publication number | Publication date |
|---|---|
| KR20200021456A (ko) | 2020-02-28 |
| JP2020517668A (ja) | 2020-06-18 |
| US20200055837A1 (en) | 2020-02-20 |
| BR112019022320A2 (pt) | 2020-05-26 |
| IL270068B (en) | 2022-06-01 |
| EP3615513A1 (en) | 2020-03-04 |
| MA48475A (fr) | 2020-03-04 |
| SG11201909807TA (en) | 2019-11-28 |
| ES2926255T3 (es) | 2022-10-24 |
| EP3615513B1 (en) | 2022-07-20 |
| AU2021215116B2 (en) | 2022-12-01 |
| CN110753684A (zh) | 2020-02-04 |
| KR102582624B1 (ko) | 2023-09-22 |
| AU2018258274A1 (en) | 2019-11-14 |
| CA3060715A1 (en) | 2018-11-01 |
| TW201841889A (zh) | 2018-12-01 |
| US11629137B2 (en) | 2023-04-18 |
| MX393879B (es) | 2025-03-24 |
| CA3060715C (en) | 2024-10-01 |
| JP7179014B2 (ja) | 2022-11-28 |
| NZ758948A (en) | 2024-04-26 |
| AU2021215116A1 (en) | 2021-08-26 |
| EP3615513A4 (en) | 2020-12-09 |
| AU2018258274B2 (en) | 2021-05-13 |
| CN118271233A (zh) | 2024-07-02 |
| US20220041575A1 (en) | 2022-02-10 |
| WO2018200517A1 (en) | 2018-11-01 |
| TWI783993B (zh) | 2022-11-21 |
| ZA201906944B (en) | 2023-03-29 |
| US11161834B2 (en) | 2021-11-02 |
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