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 date
Application filed by 美商提薩羅有限公司 filed Critical 美商提薩羅有限公司
Publication of TW202028181A publication Critical patent/TW202028181A/zh
Application granted granted Critical
Publication of TWI853841B publication Critical patent/TWI853841B/zh

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/10Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline 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)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (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 (enExample)
JP (1) JP7472115B2 (enExample)
KR (1) KR20210071022A (enExample)
CN (2) CN118994103A (enExample)
ES (1) ES2967517T3 (enExample)
TW (2) TWI853841B (enExample)
WO (1) WO2020072797A1 (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2021269115A1 (en) 2020-05-08 2023-01-19 Janssen Pharmaceutica Nv Treatment of prostate cancer with a combination of abiraterone acetate and niraparib
EP4373491A1 (en) 2021-07-19 2024-05-29 JANSSEN Pharmaceutica NV Treatment of metastatic castration-resistant prostate cancer with niraparib
EP4712976A1 (en) 2023-05-17 2026-03-25 Tesaro, Inc. Novel use of an inhibior of the a poly-adp ribose polymerase (parp) in the treatment of cancer

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE640616A (enExample) 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
NZ586675A (en) * 2008-01-08 2012-04-27 Merck Sharp & Dohme Pharmaceutically acceptable salts of 2-{ 4-[(3s)-piperidin-3- yl]phenyl} -2h-indazole-7-carboxamide
US9580407B2 (en) 2012-12-07 2017-02-28 Merck Sharp & Dohme Corp. Regioselective N-2 arylation of indazoles
JP6742903B2 (ja) 2013-05-02 2020-08-19 アナプティスバイオ インコーポレイティッド プログラム死−1(pd−1)に対する抗体
MA41463A (fr) 2015-02-03 2017-12-12 Anaptysbio Inc Anticorps dirigés contre le gène d'activation 3 des lymphocytes (lag-3)
EP3277321B1 (en) 2015-04-01 2024-08-14 AnaptysBio, Inc. Antibodies directed against t cell immunoglobulin and mucin protein 3 (tim-3)
FI3478286T3 (fi) 2016-06-29 2024-03-14 Tesaro Inc Menetelmiä munasarjasyövän hoitamiseksi
SG11201903867YA (en) 2016-11-01 2019-05-30 Anaptysbio Inc Antibodies directed against t cell immunoglobulin and mucin protein 3 (tim-3)
EP3666794A1 (en) 2016-11-01 2020-06-17 AnaptysBio, Inc. Antibodies directed against programmed death- 1 (pd-1)
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
EP3565844B8 (en) 2017-01-09 2023-04-12 Tesaro, Inc. Methods of treating cancer with anti-pd-1 antibodies
JP7118073B2 (ja) 2017-01-09 2022-08-15 テサロ, インコーポレイテッド 抗tim-3抗体を用いてがんを処置する方法
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
TW202513550A (zh) 2025-04-01
WO2020072797A1 (en) 2020-04-09
JP7472115B2 (ja) 2024-04-22
CN118994103A (zh) 2024-11-22
TW202028181A (zh) 2020-08-01
ES2967517T3 (es) 2024-04-30
KR20210071022A (ko) 2021-06-15
CN113166071A (zh) 2021-07-23
EP3860981B1 (en) 2023-11-29
CN113166071B (zh) 2025-03-21
EP3860981A1 (en) 2021-08-11

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