CN113330007A - 尼拉帕利游离碱的晶体形式 - Google Patents
尼拉帕利游离碱的晶体形式 Download PDFInfo
- Publication number
- CN113330007A CN113330007A CN201980078328.6A CN201980078328A CN113330007A CN 113330007 A CN113330007 A CN 113330007A CN 201980078328 A CN201980078328 A CN 201980078328A CN 113330007 A CN113330007 A CN 113330007A
- Authority
- CN
- China
- Prior art keywords
- nilapali
- free base
- crystalline
- cancer
- crystalline form
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
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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 (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862740869P | 2018-10-03 | 2018-10-03 | |
| US62/740,869 | 2018-10-03 | ||
| PCT/US2019/054533 WO2020072796A1 (en) | 2018-10-03 | 2019-10-03 | Crystalline forms of niraparib freebase |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN113330007A true CN113330007A (zh) | 2021-08-31 |
Family
ID=68425251
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201980078328.6A Pending CN113330007A (zh) | 2018-10-03 | 2019-10-03 | 尼拉帕利游离碱的晶体形式 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US20210347758A1 (https=) |
| EP (1) | EP3860988A1 (https=) |
| JP (1) | JP2022504228A (https=) |
| KR (1) | KR20210069678A (https=) |
| CN (1) | CN113330007A (https=) |
| TW (1) | TWI825191B (https=) |
| WO (1) | WO2020072796A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110944638A (zh) * | 2017-03-27 | 2020-03-31 | 特沙诺有限公司 | 尼拉帕尼组合物 |
| JP2022504228A (ja) | 2018-10-03 | 2022-01-13 | テサロ, インコーポレイテッド | ニラパリブ遊離塩基の結晶形態 |
| 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 (3)
| 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 |
| WO2017218365A1 (en) * | 2016-06-16 | 2017-12-21 | Sunshine Lake Pharma Co., Ltd. | Crystalline form of a substituted quinoline compound and pharmaceutical compositions thereof |
| 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 |
Family Cites Families (62)
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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 |
| 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- |
| EP0841924B1 (en) | 1995-08-02 | 2002-10-02 | Newcastle University Ventures Limited | Benzimidazole compounds |
| CA2332279A1 (en) | 1998-05-15 | 1999-11-25 | Jia-He Li | Carboxamide compounds, compositions, and methods for inhibiting parp activity |
| EP1124805B1 (de) | 1998-10-30 | 2003-05-21 | Lonza AG | Verfahren zur herstellung von 4-[(2',5'-diamino-6'-halogenpyrimidin-4'-yl)amino]-cyclopent-2-enylmethanolen |
| IL142917A0 (en) | 1998-11-03 | 2002-04-21 | Basf Ag | Substituted 2-phenylbenzimidazoles, the production thereof and their use |
| HRP20010451A2 (en) | 1998-11-17 | 2003-04-30 | Basf Ag | 2-phenylbenzimidazoles and 2-phenylindoles, and production and use thereof |
| TR200101498T2 (tr) | 1998-11-27 | 2001-11-21 | Basf Aktiengesellschaft | İkameli benzimidazoller ve parp inhibitörleri olarak kullanımları |
| 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 |
| DE50112961D1 (de) | 2000-02-01 | 2007-10-18 | Abbott Gmbh & Co Kg | Heterozyklische verbindungen und deren anwendung als parp-inhibitoren |
| DE10022925A1 (de) | 2000-05-11 | 2001-11-15 | Basf Ag | Substituierte Indole als PARP-Inhibitoren |
| JPWO2002068407A1 (ja) | 2001-02-28 | 2004-06-24 | 山之内製薬株式会社 | ベンゾイミダゾール化合物 |
| JP2003005323A (ja) | 2001-06-20 | 2003-01-08 | Konica Corp | 熱現像写真感光材料及び画像形成方法 |
| WO2003007959A1 (en) | 2001-07-16 | 2003-01-30 | Fujisawa Pharmaceutical Co., Ltd. | Quinoxaline derivatives which have parp inhibitory action |
| BR0212841A (pt) | 2001-09-26 | 2004-08-03 | Pharmacia Italia Spa | Derivado ativo de aminoindazole como inibidores de cinase, processo para sua preparação e composições farmacêuticas que os contém |
| WO2003062234A1 (en) | 2002-01-23 | 2003-07-31 | Yamanouchi Pharmaceutical Co., Ltd. | Quinoxaline compounds |
| US20040034078A1 (en) | 2002-06-14 | 2004-02-19 | Agouron Pharmaceuticals, Inc. | Benzimidazole inhibitors of poly(ADP-ribosyl) polymerase |
| JPWO2004014861A1 (ja) | 2002-08-09 | 2005-12-02 | 杏林製薬株式会社 | 4−置換キノリン−8−カルボン酸アミド誘導体とその薬理上許容される付加塩 |
| AU2003296405A1 (en) | 2003-01-06 | 2004-08-10 | Eli Lilly And Company | Fused heterocyclic derivatives as ppar modulators |
| ATE411980T1 (de) | 2003-07-21 | 2008-11-15 | Smithkline Beecham Corp | (2s,4s)-4-fluor-1-ä4-fluor-beta-(4-fluorphenyl) l-phenylalanylü-2-pyrrolidincarbonitril-p- toluolsulfonsäuresalz und wasserfreie kristalline formen davon |
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| PT1794163E (pt) | 2004-09-22 | 2010-03-01 | Pfizer | Método para a preparação de inibidores de poli(adpribose)- polimerases |
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| US7728026B2 (en) | 2005-04-11 | 2010-06-01 | Abbott Laboratories, Inc. | 2-substituted-1 h-benzimidazile-4-carboxamides are PARP inhibitors |
| JP5227796B2 (ja) | 2005-09-29 | 2013-07-03 | アボット・ラボラトリーズ | 2位においてフェニルによって置換された1h−ベンズイミダゾール−4−カルボキサミドは強力なparp阻害薬である |
| JP5162465B2 (ja) | 2005-11-15 | 2013-03-13 | アボット・ラボラトリーズ | 置換1h−ベンズイミダゾール−4−カルボキサミド類は強力なparp阻害薬である |
| CA2647545C (en) | 2006-04-03 | 2016-02-23 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | Amide substituted indazole and benzotriazole derivatives as poly(adp-ribose)polymerase (parp) inhibitors |
| MX2008014004A (es) | 2006-05-02 | 2008-11-12 | Abbott Lab | 1h-benzimidazol-4-carboxamidas sustituidas son inhibidores de parp potentes. |
| JP4611444B2 (ja) | 2007-01-10 | 2011-01-12 | イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・ピー・アー | ポリ(adp−リボース)ポリメラーゼ(parp)阻害剤としてのアミド置換インダゾール |
| US20090062268A1 (en) | 2007-08-27 | 2009-03-05 | Lead Therapeutics, Inc. | Novel inhibitors of poly(adp-ribose)polymerase (parp) |
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| 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 |
| WO2018018354A1 (zh) | 2016-07-25 | 2018-02-01 | 刘文婷 | 超市智能结算购物车及其使用方法 |
| 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 |
| 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 |
| 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). |
| 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 |
| WO2018129553A1 (en) | 2017-01-09 | 2018-07-12 | Tesaro, Inc. | Methods of treating cancer with anti-tim-3 antibodies |
| AU2018206481B2 (en) | 2017-01-09 | 2025-02-27 | Tesaro, Inc. | Methods of treating cancer with anti-PD-1 antibodies |
| CN110944638A (zh) | 2017-03-27 | 2020-03-31 | 特沙诺有限公司 | 尼拉帕尼组合物 |
| MA48475A (fr) | 2017-04-24 | 2020-03-04 | Tesaro Inc | Procédés de fabrication de niraparib |
| SG11201909395TA (en) | 2017-04-27 | 2019-11-28 | Tesaro Inc | Antibody agents directed against lymphocyte activation gene-3 (lag-3) and uses thereof |
| KR20200005662A (ko) | 2017-05-18 | 2020-01-15 | 테사로, 인코포레이티드 | 암을 치료하기 위한 조합 요법 |
| 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 |
| JP2022504228A (ja) | 2018-10-03 | 2022-01-13 | テサロ, インコーポレイテッド | ニラパリブ遊離塩基の結晶形態 |
-
2019
- 2019-10-03 JP JP2021518546A patent/JP2022504228A/ja not_active Ceased
- 2019-10-03 TW TW108135910A patent/TWI825191B/zh active
- 2019-10-03 KR KR1020217012839A patent/KR20210069678A/ko not_active Ceased
- 2019-10-03 US US17/282,358 patent/US20210347758A1/en not_active Abandoned
- 2019-10-03 EP EP19797406.6A patent/EP3860988A1/en not_active Withdrawn
- 2019-10-03 US US17/282,344 patent/US12297184B2/en active Active
- 2019-10-03 CN CN201980078328.6A patent/CN113330007A/zh active Pending
- 2019-10-03 WO PCT/US2019/054533 patent/WO2020072796A1/en not_active Ceased
Patent Citations (3)
| 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 |
| WO2017218365A1 (en) * | 2016-06-16 | 2017-12-21 | Sunshine Lake Pharma Co., Ltd. | Crystalline form of a substituted quinoline compound and pharmaceutical compositions thereof |
| 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 |
Non-Patent Citations (3)
| Title |
|---|
| J.GRAS ET AL.: "NIRAPARIB HYDROCHLORIDE", 《DRUGS OF THE FUTURE》, vol. 38, no. 10, pages 679 - 685, XP009195509, DOI: 10.1358/dof.2013.38.10.2059820 * |
| JIANG PEI ET AL.: "CRYSTALLINE FORM OF NIRAPARIB TOSYLATE", 《IP.COM》, pages 1 - 8 * |
| 吕扬 等: "《晶型药物》", vol. 1, 人民卫生出版社, pages: 24 - 25 * |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3860988A1 (en) | 2021-08-11 |
| KR20210069678A (ko) | 2021-06-11 |
| TWI825191B (zh) | 2023-12-11 |
| US12297184B2 (en) | 2025-05-13 |
| JP2022504228A (ja) | 2022-01-13 |
| TW202028185A (zh) | 2020-08-01 |
| US20210347760A1 (en) | 2021-11-11 |
| US20210347758A1 (en) | 2021-11-11 |
| WO2020072796A1 (en) | 2020-04-09 |
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