TWI825191B - 尼拉帕尼（niraparib）游離鹼之結晶形 - Google Patents
尼拉帕尼（niraparib）游離鹼之結晶形 Download PDFInfo
- Publication number
- TWI825191B TWI825191B TW108135910A TW108135910A TWI825191B TW I825191 B TWI825191 B TW I825191B TW 108135910 A TW108135910 A TW 108135910A TW 108135910 A TW108135910 A TW 108135910A TW I825191 B TWI825191 B TW I825191B
- Authority
- TW
- Taiwan
- Prior art keywords
- niraparib
- free base
- crystalline
- xrpd
- crystalline form
- Prior art date
Links
Classifications
-
- 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
- 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
-
- 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)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Vascular Medicine (AREA)
- Transplantation (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862740869P | 2018-10-03 | 2018-10-03 | |
| US62/740,869 | 2018-10-03 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW202028185A TW202028185A (zh) | 2020-08-01 |
| TWI825191B true TWI825191B (zh) | 2023-12-11 |
Family
ID=68425251
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW108135910A TWI825191B (zh) | 2018-10-03 | 2019-10-03 | 尼拉帕尼（niraparib）游離鹼之結晶形 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US12297184B2 (cg-RX-API-DMAC10.html) |
| EP (1) | EP3860988A1 (cg-RX-API-DMAC10.html) |
| JP (1) | JP2022504228A (cg-RX-API-DMAC10.html) |
| KR (1) | KR20210069678A (cg-RX-API-DMAC10.html) |
| CN (1) | CN113330007A (cg-RX-API-DMAC10.html) |
| TW (1) | TWI825191B (cg-RX-API-DMAC10.html) |
| WO (1) | WO2020072796A1 (cg-RX-API-DMAC10.html) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2018246214B2 (en) * | 2017-03-27 | 2021-07-08 | Merck Sharp & Dohme Llc | Niraparib compositions |
| US12297184B2 (en) | 2018-10-03 | 2025-05-13 | Tesaro, Inc. | Niraparib salts |
| 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 (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009087381A1 (en) * | 2008-01-08 | 2009-07-16 | Merck Sharp & Dohme Ltd | Pharmaceutically acceptable salts of 2-{4-[(3s)-piperidin-3- yl]phenyl} -2h-indazole-7-carboxamide |
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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 |
| GB9404485D0 (en) | 1994-03-09 | 1994-04-20 | Cancer Res Campaign Tech | Benzamide analogues |
| AT401651B (de) | 1994-06-14 | 1996-11-25 | Biochemie Gmbh | 7-(2-(2-aminothiazol-4-yl)-2-(z)- hydroximinoacetamido)-3-n,n- dimethylcarbamoyloxymethyl-3-cephem-4- |
| DK0841924T3 (da) | 1995-08-02 | 2003-02-10 | Univ Newcastle Ventures Ltd | Benzimidazolforbindelser |
| JP2002515488A (ja) | 1998-05-15 | 2002-05-28 | ギルフォード ファーマシューティカルズ インコーポレイテッド | カルボキサミド化合物、組成物、及びｐａｒｐ活性の抑制方法 |
| WO2000026193A1 (de) | 1998-10-30 | 2000-05-11 | Lonza Ag | Verfahren zur herstellung von 4-[(2',5'-diamino-6'-halogenpyrimidin-4'-yl)amino]-cyclopent-2-enylmethanolen |
| TR200101239T2 (tr) | 1998-11-03 | 2001-11-21 | Basf Aktiengesellschaft | İkameli-2-fenilbenzimidazoller, üretimleri ve kullanımları |
| JP2002529537A (ja) | 1998-11-17 | 2002-09-10 | ビーエーエスエフ アクチェンゲゼルシャフト | ２−フェニルベンズイミダゾールおよび２−フェニルインドール、その製造方法ならびに使用 |
| DK1133477T3 (da) | 1998-11-27 | 2004-06-21 | Abbott Gmbh & Co Kg | Substituerede benzimidazoler og deres anvendelse som parpinhibitorer |
| DE19918211A1 (de) | 1999-04-22 | 2000-10-26 | Basf Ag | Cycloalkylsubstituierte Benzimidazole, deren Herstellung und Anwendung |
| DE19920936A1 (de) | 1999-05-07 | 2000-11-09 | Basf Ag | Heterozyklisch substituierte Benzimidazole, deren Herstellung und Anwendung |
| AU7314200A (en) | 1999-09-17 | 2001-04-24 | Yamanouchi Pharmaceutical Co., Ltd. | Benzimidazole derivatives |
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| DE10022925A1 (de) | 2000-05-11 | 2001-11-15 | Basf Ag | Substituierte Indole als PARP-Inhibitoren |
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| US20090275619A1 (en) | 2006-04-03 | 2009-11-05 | BOUERES Julia | Amide Substituted Indazole and Benzotriazole Derivatives as Poly(ADP-Ribose)Polymerase (PARP) Inhibitors |
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| MA41463A (fr) | 2015-02-03 | 2017-12-12 | Anaptysbio Inc | Anticorps dirigés contre le gène d'activation 3 des lymphocytes (lag-3) |
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| CN106496187A (zh) | 2016-09-14 | 2017-03-15 | 陕西科技大学 | 一种制备PARP抑制剂Niraparib的合成方法 |
| 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 |
| 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 |
| TWI791519B (zh) | 2017-04-27 | 2023-02-11 | 美商提薩羅有限公司 | 針對淋巴細胞活化基因-3（lag-3）之抗體藥劑及其用途 |
| 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 |
| CN108530425A (zh) * | 2017-05-27 | 2018-09-14 | 广州科锐特生物科技有限公司 | 一种尼拉帕尼对甲苯磺酸盐水合物晶型及其制备方法 |
| 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 |
| US12297184B2 (en) | 2018-10-03 | 2025-05-13 | Tesaro, Inc. | Niraparib salts |
-
2019
- 2019-10-03 US US17/282,344 patent/US12297184B2/en active Active
- 2019-10-03 JP JP2021518546A patent/JP2022504228A/ja not_active Ceased
- 2019-10-03 KR KR1020217012839A patent/KR20210069678A/ko not_active Ceased
- 2019-10-03 CN CN201980078328.6A patent/CN113330007A/zh active Pending
- 2019-10-03 EP EP19797406.6A patent/EP3860988A1/en not_active Withdrawn
- 2019-10-03 TW TW108135910A patent/TWI825191B/zh active
- 2019-10-03 WO PCT/US2019/054533 patent/WO2020072796A1/en not_active Ceased
- 2019-10-03 US US17/282,358 patent/US20210347758A1/en not_active Abandoned
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009087381A1 (en) * | 2008-01-08 | 2009-07-16 | Merck Sharp & Dohme Ltd | Pharmaceutically acceptable salts of 2-{4-[(3s)-piperidin-3- yl]phenyl} -2h-indazole-7-carboxamide |
Also Published As
| Publication number | Publication date |
|---|---|
| US20210347758A1 (en) | 2021-11-11 |
| EP3860988A1 (en) | 2021-08-11 |
| JP2022504228A (ja) | 2022-01-13 |
| WO2020072796A1 (en) | 2020-04-09 |
| TW202028185A (zh) | 2020-08-01 |
| CN113330007A (zh) | 2021-08-31 |
| KR20210069678A (ko) | 2021-06-11 |
| US20210347760A1 (en) | 2021-11-11 |
| US12297184B2 (en) | 2025-05-13 |
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