CN113166071B - 尼拉帕利盐 - Google Patents

尼拉帕利盐 Download PDF

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Publication number
CN113166071B
CN113166071B CN201980078366.1A CN201980078366A CN113166071B CN 113166071 B CN113166071 B CN 113166071B CN 201980078366 A CN201980078366 A CN 201980078366A CN 113166071 B CN113166071 B CN 113166071B
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CN
China
Prior art keywords
crystalline form
indazole
piperidin
carboxamide
phenyl
Prior art date
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Application number
CN201980078366.1A
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English (en)
Chinese (zh)
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CN113166071A (zh
Inventor
A.J.斯图尔特
Y.王
G.吴
J.尹
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Texano Ltd
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Texano Ltd
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Priority to CN202411070879.7A priority Critical patent/CN118994103A/zh
Publication of CN113166071A publication Critical patent/CN113166071A/zh
Application granted granted Critical
Publication of CN113166071B publication Critical patent/CN113166071B/zh
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    • 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
    • C07D401/12—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
    • 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
    • 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
    • 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)
CN201980078366.1A 2018-10-03 2019-10-03 尼拉帕利盐 Active CN113166071B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202411070879.7A CN118994103A (zh) 2018-10-03 2019-10-03 尼拉帕利盐

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862740872P 2018-10-03 2018-10-03
US62/740,872 2018-10-03
PCT/US2019/054534 WO2020072797A1 (en) 2018-10-03 2019-10-03 Niraparib salts

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN202411070879.7A Division CN118994103A (zh) 2018-10-03 2019-10-03 尼拉帕利盐

Publications (2)

Publication Number Publication Date
CN113166071A CN113166071A (zh) 2021-07-23
CN113166071B true CN113166071B (zh) 2025-03-21

Family

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Family Applications (2)

Application Number Title Priority Date Filing Date
CN201980078366.1A Active CN113166071B (zh) 2018-10-03 2019-10-03 尼拉帕利盐
CN202411070879.7A Pending CN118994103A (zh) 2018-10-03 2019-10-03 尼拉帕利盐

Family Applications After (1)

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CN202411070879.7A Pending CN118994103A (zh) 2018-10-03 2019-10-03 尼拉帕利盐

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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018108160A1 (zh) * 2016-12-16 2018-06-21 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

Family Cites Families (16)

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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)
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018108160A1 (zh) * 2016-12-16 2018-06-21 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

Also Published As

Publication number Publication date
JP2022504236A (ja) 2022-01-13
TW202028181A (zh) 2020-08-01
CN113166071A (zh) 2021-07-23
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
TWI853841B (zh) 2024-09-01

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Address after: Delaware, USA

Patentee after: Texano Ltd.

Country or region after: U.S.A.

Address before: Massachusetts, USA

Patentee before: Texano Ltd.

Country or region before: U.S.A.