CA2842730C - Polymorphic forms of compounds as prolyl hydroxylase inhibitor, and uses thereof - Google Patents
Polymorphic forms of compounds as prolyl hydroxylase inhibitor, and uses thereof Download PDFInfo
- Publication number
- CA2842730C CA2842730C CA2842730A CA2842730A CA2842730C CA 2842730 C CA2842730 C CA 2842730C CA 2842730 A CA2842730 A CA 2842730A CA 2842730 A CA2842730 A CA 2842730A CA 2842730 C CA2842730 C CA 2842730C
- Authority
- CA
- Canada
- Prior art keywords
- crystalline polymorph
- compound
- formula
- ray powder
- diffraction pattern
- 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.)
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
- C07D217/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- 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)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Transplantation (AREA)
- Emergency Medicine (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201110207175.6 | 2011-07-22 | ||
| CN201110207175 | 2011-07-22 | ||
| CN201110209657.5 | 2011-07-25 | ||
| CN201110209657 | 2011-07-25 | ||
| CN201110211297 | 2011-07-26 | ||
| CN201110211297.2 | 2011-07-26 | ||
| PCT/CN2012/079058 WO2013013609A1 (en) | 2011-07-22 | 2012-07-23 | Polymorphic forms of compounds as prolyl hydroxylase inhibitor, and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2842730A1 CA2842730A1 (en) | 2013-01-31 |
| CA2842730C true CA2842730C (en) | 2018-08-21 |
Family
ID=47600518
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2842730A Active CA2842730C (en) | 2011-07-22 | 2012-07-23 | Polymorphic forms of compounds as prolyl hydroxylase inhibitor, and uses thereof |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9206134B2 (enExample) |
| EP (1) | EP2734504B1 (enExample) |
| JP (1) | JP6099644B2 (enExample) |
| KR (1) | KR102029951B1 (enExample) |
| CN (1) | CN104024227B8 (enExample) |
| AU (1) | AU2012289429B2 (enExample) |
| CA (1) | CA2842730C (enExample) |
| ES (1) | ES2606631T3 (enExample) |
| IL (1) | IL230580B (enExample) |
| WO (1) | WO2013013609A1 (enExample) |
| ZA (1) | ZA201401310B (enExample) |
Families Citing this family (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103145616B (zh) | 2003-06-06 | 2015-09-30 | 菲布罗根有限公司 | 含氮杂芳基化合物及其在增加内源性促红细胞生成素中的用途 |
| NO2686520T3 (enExample) | 2011-06-06 | 2018-03-17 | ||
| EP3470397B1 (en) * | 2012-07-16 | 2021-12-29 | Fibrogen, Inc. | Crystalline forms of a prolyl hydroxylase inhibitor |
| SG11201500234YA (en) | 2012-07-16 | 2015-02-27 | Fibrogen Inc | Process for making isoquinoline compounds |
| US8883823B2 (en) | 2012-07-16 | 2014-11-11 | Fibrogen, Inc. | Crystalline forms of a prolyl hydroxylase inhibitor |
| IL296484B2 (en) | 2013-06-06 | 2025-03-01 | Fibrogen Inc | Pharmaceutical formulations of HIF hydroxylase inhibitor |
| HUE066123T2 (hu) | 2013-06-13 | 2024-07-28 | Akebia Therapeutics Inc | Készítmények és módszerek anémia kezelésére |
| TWI665190B (zh) | 2013-11-15 | 2019-07-11 | 阿克比治療有限公司 | {[5-(3-氯苯基)-3-羥基吡啶-2-羰基]胺基}乙酸之固體型式,其組合物及用途 |
| CN103694172A (zh) * | 2013-12-26 | 2014-04-02 | 辽宁亿灵科创生物医药科技有限公司 | 含氮杂芳基化合物的衍生物 |
| CA2974691A1 (en) | 2015-01-23 | 2016-07-28 | Akebia Therapeutics, Inc. | Solid forms of 2-(5-(3-fluorophenyl)-3-hydroxypicolinamido)acetic acid, compositions, and uses thereof |
| CN106146490B (zh) * | 2015-03-27 | 2018-10-23 | 沈阳三生制药有限责任公司 | 被芳氧基或杂芳氧基取代的5-羟基-1,7-萘啶化合物、其制备方法及其制药用途 |
| NZ735973A (en) | 2015-04-01 | 2023-06-30 | Akebia Therapeutics Inc | Compositions and methods for treating anemia |
| CN104910113B (zh) * | 2015-05-21 | 2017-05-10 | 中国科学院宁波材料技术与工程研究所 | 一种羟基苯酐的制备方法 |
| CN104892509B (zh) * | 2015-06-04 | 2018-03-09 | 苏州明锐医药科技有限公司 | 诺得司他的制备方法 |
| US10450569B2 (en) | 2015-08-13 | 2019-10-22 | Somagenics, Inc. | Methods and compositions of short small hairpin RNAS and microRNAS for wound healing |
| CN105130888A (zh) * | 2015-10-09 | 2015-12-09 | 中国药科大学 | 炔基吡啶类脯氨酰羟化酶抑制剂、其制备方法和医药用途 |
| CN106916105A (zh) * | 2015-12-28 | 2017-07-04 | 徐州万邦金桥制药有限公司 | 一种纯化可博美的方法 |
| CN106187888A (zh) * | 2016-07-18 | 2016-12-07 | 江苏德源药业股份有限公司 | Fg‑4592单晶及其制备方法 |
| CZ2016627A3 (cs) | 2016-10-07 | 2018-04-18 | Zentiva, K.S. | Způsob přípravy (7-fenoxy-4-hydroxy-1-methylisochinolin-3-karbonyl)glycinu (roxadustatu) a jeho intermediátů založený na souběžném otevírání oxazolového kruhu, štěpení etheru a tvorbě iminu |
| CN107954931B (zh) * | 2016-10-17 | 2021-06-22 | 上海医药集团青岛国风药业股份有限公司 | 一种诺得司他的制备方法 |
| CN108017583B (zh) * | 2016-11-01 | 2021-04-06 | 徐州万邦金桥制药有限公司 | 一种可博美的制备方法 |
| US11168057B2 (en) | 2017-08-11 | 2021-11-09 | Dr. Reddy's Laboratories Limited | Polymorphs and co-crystals of roxadustat |
| ES2898878T3 (es) * | 2017-09-04 | 2022-03-09 | Sandoz Ag | Cocristal de un inhibidor de la prolil·hidroxilasa de HIF disponible por vía oral |
| CN111566090A (zh) * | 2017-12-01 | 2020-08-21 | 雷迪博士实验室有限公司 | 罗沙司他及其中间体的制备方法 |
| CN109956870A (zh) | 2017-12-14 | 2019-07-02 | 南京卡文迪许生物工程技术有限公司 | 一种罗沙司他的合成方法及其中间体化合物 |
| CN108059679B (zh) * | 2017-12-27 | 2020-03-24 | 吉林大学 | 一种人源单链抗体及其应用 |
| CN110218184B (zh) * | 2018-03-01 | 2022-09-27 | 广东东阳光药业有限公司 | 诺德司他共晶及其制备方法 |
| CN110272386B (zh) * | 2018-03-16 | 2022-09-09 | 上海医药集团青岛国风药业股份有限公司 | 一种诺得司他的制备方法 |
| CN108424388B (zh) * | 2018-04-19 | 2020-08-21 | 杭州科巢生物科技有限公司 | 一种慢性贫血药物的制备方法 |
| US11713298B2 (en) | 2018-05-09 | 2023-08-01 | Akebia Therapeutics, Inc. | Process for preparing 2-[[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino]acetic acid |
| CN110903242B (zh) * | 2018-09-14 | 2023-05-12 | 四川科伦药物研究院有限公司 | 罗沙司他中间体的制备方法 |
| CN109369525A (zh) * | 2018-12-29 | 2019-02-22 | 安礼特(上海)医药科技有限公司 | 罗沙司它的新晶型及其制备方法 |
| WO2020178847A1 (en) | 2019-03-01 | 2020-09-10 | Mylan Laboratories Limited | Cocrystal of roxadustat and d-proline |
| CN109776415B (zh) * | 2019-03-07 | 2020-11-17 | 福建南方制药股份有限公司 | 一种Roxadustat中间体的制备方法 |
| IL287258B2 (en) * | 2019-04-18 | 2026-01-01 | Nikang Therapeutics Inc | Inhibitors as tetrahydro-1h-cyclopenta[cd] indene derivatives as hypoxia inducible factor -2alpha |
| CN109956901B (zh) * | 2019-04-25 | 2022-09-06 | 南京正大天晴制药有限公司 | 异喹啉酮类化合物的制备方法 |
| EP4010318A1 (en) | 2019-08-07 | 2022-06-15 | Teva Pharmaceuticals International GmbH | Processes for the preparation of roxadustat and intermediates thereof |
| CN112679428A (zh) * | 2019-10-17 | 2021-04-20 | 罗欣药业(上海)有限公司 | 罗沙司他新晶型及其制备方法 |
| CN112679430B (zh) * | 2019-10-18 | 2023-05-05 | 上海迪赛诺化学制药有限公司 | 一种制备异喹啉酮类化合物的方法 |
| US20230112619A1 (en) * | 2019-10-18 | 2023-04-13 | Shanghai Desano Chemical Pharmaceutical Co., Ltd. | Method for preparing isoquinolinone compounds |
| CN112679431B (zh) * | 2019-10-18 | 2023-05-05 | 上海迪赛诺化学制药有限公司 | 一种制备异喹啉酮类化合物的方法 |
| CN112679429B (zh) * | 2019-10-18 | 2023-05-05 | 上海迪赛诺化学制药有限公司 | 一种制备异喹啉酮类化合物的方法 |
| CN114344301B (zh) * | 2019-10-22 | 2023-06-23 | 苏州科睿思制药有限公司 | 一种低氧诱导因子脯氨酰羟化酶抑制剂晶型 |
| US11524939B2 (en) | 2019-11-13 | 2022-12-13 | Akebia Therapeutics, Inc. | Solid forms of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino} acetic acid |
| US12612367B2 (en) | 2019-12-10 | 2026-04-28 | Akebia Therapeutics, Inc. | Method for producing nitrogen-containing heteroarylcarboxamide acetic acid derivative |
| WO2021216530A1 (en) | 2020-04-20 | 2021-10-28 | Akebia Therapeutics, Inc. | Treatment of viral infections, of organ injury, and of related conditions using a hif prolyl hydroxylase inhibitor or a hif-alpha stabilizer |
| CN111205224B (zh) * | 2020-04-22 | 2020-08-25 | 南京佰麦生物技术有限公司 | 一种罗沙司他水合物的晶型及其制备方法和应用 |
| CN113801060B (zh) | 2020-06-13 | 2025-06-27 | 苏州鹏旭医药科技有限公司 | 一种多取代异喹啉化合物的制备方法 |
| CN114539149A (zh) | 2020-06-19 | 2022-05-27 | 济川(上海)医学科技有限公司 | 一种含异喹啉环的化合物、其制备方法及其应用 |
| CN112194624A (zh) * | 2020-11-18 | 2021-01-08 | 江苏豪森药业集团有限公司 | 一种异喹啉类化合物的晶型及其制备方法 |
| CN112500344B (zh) * | 2020-11-18 | 2022-07-01 | 江苏豪森药业集团有限公司 | 罗沙司他晶型及其制备方法 |
| CN115144480B (zh) * | 2021-03-31 | 2023-11-28 | 成都倍特药业股份有限公司 | 一种从罗沙司他中间体中检测吗啉和/或四甲基甲烷二胺的方法 |
| CN115724796A (zh) * | 2021-08-26 | 2023-03-03 | 成都苑东生物制药股份有限公司 | 一种罗沙司他新晶型及其制备方法 |
| WO2023095162A1 (en) | 2021-11-26 | 2023-06-01 | Mylan Laboratories Limited | Cocrystal of roxadustat and nicotinamide |
| WO2026060330A1 (en) * | 2024-09-12 | 2026-03-19 | Elanco Us Inc. | Method of crystallizing narasin |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5470285A (en) * | 1977-11-14 | 1979-06-05 | Tanabe Seiyaku Co Ltd | Production of 4-hydroxyisocarbostyryl-3-carboxylic analog |
| DE19746287A1 (de) * | 1997-10-20 | 1999-04-22 | Hoechst Marion Roussel De Gmbh | Substituierte Isochinolin-2-Carbonsäureamide, ihre Herstellung und ihre Verwendung als Arzneimittel |
| US7893071B2 (en) * | 2001-04-23 | 2011-02-22 | University Of Virginia Patent Foundation | Synthesis and evaluation of novel phthalimide mimics as anti-angiogenic |
| CN103145616B (zh) * | 2003-06-06 | 2015-09-30 | 菲布罗根有限公司 | 含氮杂芳基化合物及其在增加内源性促红细胞生成素中的用途 |
| US7189697B2 (en) | 2004-04-13 | 2007-03-13 | Trustees Of Tufts College | Compositions and uses of a galectin for treatment of dry eye syndrome |
| CN101849943A (zh) * | 2005-06-06 | 2010-10-06 | 菲布罗根公司 | 使用HIFα稳定剂的改进的贫血治疗 |
| AU2006326662B2 (en) | 2005-12-09 | 2011-07-28 | Amgen Inc. | Quinolone based compounds exhibiting prolyl hydroxylase inhibitory activity, and compositions, and uses thereof |
| CN102351791B (zh) * | 2006-01-27 | 2014-10-29 | 菲布罗根有限公司 | 使低氧诱导因子(hif)稳定的氰基异喹啉化合物 |
| US20070293575A1 (en) | 2006-06-15 | 2007-12-20 | Fibrogen, Inc. | Compounds and methods for treatment of cancer-related anemia |
| JP4311416B2 (ja) | 2006-06-30 | 2009-08-12 | 株式会社日立製作所 | 渦電流探傷法による表面欠陥長さ評価方法 |
| IN2012DN00549A (enExample) | 2009-07-15 | 2015-06-12 | Zhejiang Beta Pharma Inc |
-
2012
- 2012-07-23 CA CA2842730A patent/CA2842730C/en active Active
- 2012-07-23 ES ES12817360.6T patent/ES2606631T3/es active Active
- 2012-07-23 EP EP12817360.6A patent/EP2734504B1/en not_active Not-in-force
- 2012-07-23 WO PCT/CN2012/079058 patent/WO2013013609A1/en not_active Ceased
- 2012-07-23 JP JP2014520521A patent/JP6099644B2/ja not_active Expired - Fee Related
- 2012-07-23 CN CN201280036322.0A patent/CN104024227B8/zh active Active
- 2012-07-23 KR KR1020147004452A patent/KR102029951B1/ko not_active Expired - Fee Related
- 2012-07-23 US US14/233,902 patent/US9206134B2/en active Active
- 2012-07-23 AU AU2012289429A patent/AU2012289429B2/en active Active
-
2014
- 2014-01-22 IL IL230580A patent/IL230580B/en active IP Right Grant
- 2014-02-20 ZA ZA2014/01310A patent/ZA201401310B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN104024227B8 (zh) | 2025-07-29 |
| AU2012289429B2 (en) | 2016-07-28 |
| US9206134B2 (en) | 2015-12-08 |
| EP2734504A1 (en) | 2014-05-28 |
| EP2734504A4 (en) | 2014-12-31 |
| CA2842730A1 (en) | 2013-01-31 |
| JP2014524920A (ja) | 2014-09-25 |
| AU2012289429A1 (en) | 2014-03-20 |
| CN104024227B (zh) | 2015-12-02 |
| ES2606631T3 (es) | 2017-03-24 |
| KR20140049004A (ko) | 2014-04-24 |
| WO2013013609A1 (en) | 2013-01-31 |
| JP6099644B2 (ja) | 2017-03-22 |
| US20150031721A1 (en) | 2015-01-29 |
| IL230580A0 (en) | 2014-03-31 |
| ZA201401310B (en) | 2015-04-29 |
| KR102029951B1 (ko) | 2019-11-08 |
| IL230580B (en) | 2019-07-31 |
| CN104024227A (zh) | 2014-09-03 |
| EP2734504B1 (en) | 2016-09-14 |
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