TWI853841B - 尼拉帕尼(niraparib)鹽 - Google Patents

尼拉帕尼(niraparib)鹽 Download PDF

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Publication number
TWI853841B
TWI853841B TW108135909A TW108135909A TWI853841B TW I853841 B TWI853841 B TW I853841B TW 108135909 A TW108135909 A TW 108135909A TW 108135909 A TW108135909 A TW 108135909A TW I853841 B TWI853841 B TW I853841B
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TW
Taiwan
Prior art keywords
niraparib
crystalline form
salt
indazole
piperidin
Prior art date
Application number
TW108135909A
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English (en)
Chinese (zh)
Other versions
TW202028181A (zh
Inventor
艾利斯戴爾 詹姆士 史都華
以 王
光中 吳
建國 殷
Original Assignee
美商提薩羅有限公司
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Publication of TW202028181A publication Critical patent/TW202028181A/zh
Application granted granted Critical
Publication of TWI853841B publication Critical patent/TWI853841B/zh

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    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
TW108135909A 2018-10-03 2019-10-03 尼拉帕尼(niraparib)鹽 TWI853841B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862740872P 2018-10-03 2018-10-03
US62/740,872 2018-10-03

Publications (2)

Publication Number Publication Date
TW202028181A TW202028181A (zh) 2020-08-01
TWI853841B true TWI853841B (zh) 2024-09-01

Family

ID=68345029

Family Applications (2)

Application Number Title Priority Date Filing Date
TW108135909A TWI853841B (zh) 2018-10-03 2019-10-03 尼拉帕尼(niraparib)鹽
TW113130597A TW202513550A (zh) 2018-10-03 2019-10-03 尼拉帕尼(niraparib)鹽

Family Applications After (1)

Application Number Title Priority Date Filing Date
TW113130597A TW202513550A (zh) 2018-10-03 2019-10-03 尼拉帕尼(niraparib)鹽

Country Status (7)

Country Link
EP (1) EP3860981B1 (cg-RX-API-DMAC10.html)
JP (1) JP7472115B2 (cg-RX-API-DMAC10.html)
KR (1) KR20210071022A (cg-RX-API-DMAC10.html)
CN (2) CN113166071B (cg-RX-API-DMAC10.html)
ES (1) ES2967517T3 (cg-RX-API-DMAC10.html)
TW (2) TWI853841B (cg-RX-API-DMAC10.html)
WO (1) WO2020072797A1 (cg-RX-API-DMAC10.html)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023524794A (ja) 2020-05-08 2023-06-13 ヤンセン ファーマシューティカ エヌ.ベー. アビラテロン酢酸エステルとニラパリブの組み合わせによる前立腺癌の処置
US20240325369A1 (en) 2021-07-19 2024-10-03 Janssen Pharmaceutica Nv Treatment of metastatic castration-resistant prostate cancer with niraparib
JP2026517228A (ja) 2023-05-17 2026-05-28 テサロ, インコーポレイテッド がんの治療におけるポリadpリボースポリメラーゼ(parp)阻害剤の新規使用

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE640616A (cg-RX-API-DMAC10.html) 1962-12-19
US3492397A (en) 1967-04-07 1970-01-27 Warner Lambert Pharmaceutical Sustained release dosage in the pellet form and process thereof
US4060598A (en) 1967-06-28 1977-11-29 Boehringer Mannheim G.M.B.H. Tablets coated with aqueous resin dispersions
US3538214A (en) 1969-04-22 1970-11-03 Merck & Co Inc Controlled release medicinal tablets
US4173626A (en) 1978-12-11 1979-11-06 Merck & Co., Inc. Sustained release indomethacin
EP2240466B1 (en) 2008-01-08 2015-07-29 Merck Sharp & Dohme Limited Pharmaceutically acceptable salts of 2-{4-[(3s)-piperidin-3- yl]phenyl} -2h-indazole-7-carboxamide
EP2928473B1 (en) 2012-12-07 2017-06-28 Merck Sharp & Dohme Corp. Regioselective n-2 arylation of indazoles
RS61400B1 (sr) 2013-05-02 2021-02-26 Anaptysbio Inc Antitela usmerena protiv programirane smrti-1 (pd-1)
MA41463A (fr) 2015-02-03 2017-12-12 Anaptysbio Inc Anticorps dirigés contre le gène d'activation 3 des lymphocytes (lag-3)
PL3277321T3 (pl) 2015-04-01 2024-11-18 Anaptysbio, Inc. Przeciwciała skierowane przeciwko białku 3 immunoglobuliny limfocytów t i mucyny (tim-3)
HRP20240136T1 (hr) 2016-06-29 2024-04-12 Tesaro, Inc. Metode liječenja raka jajnika
CN110049777A (zh) 2016-11-01 2019-07-23 安奈普泰斯生物有限公司 针对程序性死亡-1(pd-1)的抗体
MA50677A (fr) 2016-11-01 2021-07-14 Anaptysbio Inc Anticorps dirigés contre la protéine d'immunoglobuline de lymphocytes t et mucine 3 (tim-3)
CN108201537A (zh) 2016-12-16 2018-06-26 苏州苏融生物医药有限公司 一种尼拉帕尼缓控释药物组合物及其用途
WO2018122168A1 (en) * 2016-12-29 2018-07-05 Bayer Pharma Aktiengesellschaft Combinations of bub1 kinase and parp inhibitors
PT3565844T (pt) 2017-01-09 2023-05-02 Tesaro Inc Métodos de tratamento de cancro com anticorpos anti-pd-1
AU2018205401B2 (en) 2017-01-09 2025-01-02 Tesaro, Inc. Methods of treating cancer with anti-TIM-3 antibodies
CN108203404A (zh) * 2018-03-02 2018-06-26 上海博邦医药科技有限公司 (r)-3-苯基哌啶或/和(s)-3-苯基哌啶以及尼拉帕尼的手性中间体的合成方法

Also Published As

Publication number Publication date
JP2022504236A (ja) 2022-01-13
TW202028181A (zh) 2020-08-01
CN113166071A (zh) 2021-07-23
CN113166071B (zh) 2025-03-21
TW202513550A (zh) 2025-04-01
EP3860981A1 (en) 2021-08-11
ES2967517T3 (es) 2024-04-30
EP3860981B1 (en) 2023-11-29
CN118994103A (zh) 2024-11-22
WO2020072797A1 (en) 2020-04-09
KR20210071022A (ko) 2021-06-15
JP7472115B2 (ja) 2024-04-22

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