AU2018258274C1 - Methods of manufacturing of niraparib - Google Patents

Methods of manufacturing of niraparib Download PDF

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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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AU
Australia
Prior art keywords
formula
salt
acid
compound
boc
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AU2018258274A
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AU2018258274B2 (en
AU2018258274A1 (en
Inventor
Frank Xing Chen
Alistair Stewart
Anthony Joseph TOTO
George Wu
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Tesaro Inc
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Tesaro Inc
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Publication of AU2018258274A1 publication Critical patent/AU2018258274A1/en
Publication of AU2018258274B2 publication Critical patent/AU2018258274B2/en
Priority to AU2021215116A priority Critical patent/AU2021215116B2/en
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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)
  • 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)
AU2018258274A 2017-04-24 2018-04-24 Methods of manufacturing of niraparib Active AU2018258274C1 (en)

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

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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)

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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)

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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

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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
JP7179014B2 (ja) 2022-11-28
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
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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