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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China
Prior art keywords
crystalline form
indazole
piperidin
carboxamide
phenyl
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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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    • 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
    • C07D401/12Heterocyclic 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
    • 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
    • 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
    • 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

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  • 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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (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

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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 (https=)
JP (1) JP7472115B2 (https=)
KR (1) KR20210071022A (https=)
CN (2) CN113166071B (https=)
ES (1) ES2967517T3 (https=)
TW (2) TW202513550A (https=)
WO (1) WO2020072797A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI905184B (zh) 2020-05-08 2025-11-21 比利時商健生藥品公司 用醋酸阿比特龍和尼拉帕尼之組合治療前列腺癌
JP2024525881A (ja) 2021-07-19 2024-07-12 ヤンセン ファーマシューティカ エヌ.ベー. ニラパリブ(niraparib)による転移性去勢抵抗性前立腺癌の治療
CN121311226A (zh) 2023-05-17 2026-01-09 特沙诺有限公司 聚adp核糖聚合酶(parp)抑制剂在治疗癌症中的新用途

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 (https=) 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
KR101653548B1 (ko) * 2008-01-08 2016-09-02 머크 샤프 앤드 돔 리미티드 2-{4-[(3s)-피페리딘-3-일]페닐}-2h-인다졸-7-카복스아미드의 약제학적으로 허용되는 염
EP2928473B1 (en) 2012-12-07 2017-06-28 Merck Sharp & Dohme Corp. Regioselective n-2 arylation of indazoles
SMT202100065T1 (it) 2013-05-02 2021-03-15 Anaptysbio Inc Anticorpi diretti contro la proteina della morte programmata (pd-1)
MA41463A (fr) 2015-02-03 2017-12-12 Anaptysbio Inc Anticorps dirigés contre le gène d'activation 3 des lymphocytes (lag-3)
FI3277321T3 (fi) 2015-04-01 2024-10-31 Anaptysbio Inc T-soluimmunoglobuliinia ja musiiniproteiini 3:a (tim-3) vastaan suunnattuja vasta-aineita
SG11201811564QA (en) 2016-06-29 2019-01-30 Tesaro Inc Methods of treating ovarian cancer
MX2019005116A (es) 2016-11-01 2019-11-12 Anaptysbio Inc Anticuerpos dirigidos contra la proteina de inmunoglobulina de linfocitos t y de mucina 3 (tim-3).
JP2019533458A (ja) 2016-11-01 2019-11-21 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
AU2018206481B2 (en) 2017-01-09 2025-02-27 Tesaro, Inc. Methods of treating cancer with anti-PD-1 antibodies
WO2018129553A1 (en) 2017-01-09 2018-07-12 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
CN118994103A (zh) 2024-11-22
TW202028181A (zh) 2020-08-01
KR20210071022A (ko) 2021-06-15
TW202513550A (zh) 2025-04-01
EP3860981A1 (en) 2021-08-11
EP3860981B1 (en) 2023-11-29
WO2020072797A1 (en) 2020-04-09
ES2967517T3 (es) 2024-04-30
JP7472115B2 (ja) 2024-04-22
JP2022504236A (ja) 2022-01-13
CN113166071A (zh) 2021-07-23
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.