JP6099644B2 - プロリルヒドロキシラーゼ阻害剤としての化合物の多形体、およびその使用 - Google Patents
プロリルヒドロキシラーゼ阻害剤としての化合物の多形体、およびその使用 Download PDFInfo
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- JP6099644B2 JP6099644B2 JP2014520521A JP2014520521A JP6099644B2 JP 6099644 B2 JP6099644 B2 JP 6099644B2 JP 2014520521 A JP2014520521 A JP 2014520521A JP 2014520521 A JP2014520521 A JP 2014520521A JP 6099644 B2 JP6099644 B2 JP 6099644B2
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- 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)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Emergency Medicine (AREA)
- Transplantation (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Urology & Nephrology (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 | 2011-07-22 | ||
| CN201110207175.6 | 2011-07-22 | ||
| CN201110209657.5 | 2011-07-25 | ||
| CN201110209657 | 2011-07-25 | ||
| CN201110211297.2 | 2011-07-26 | ||
| CN201110211297 | 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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2014524920A JP2014524920A (ja) | 2014-09-25 |
| JP2014524920A5 JP2014524920A5 (OSRAM) | 2015-09-10 |
| JP6099644B2 true JP6099644B2 (ja) | 2017-03-22 |
Family
ID=47600518
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014520521A Expired - Fee Related JP6099644B2 (ja) | 2011-07-22 | 2012-07-23 | プロリルヒドロキシラーゼ阻害剤としての化合物の多形体、およびその使用 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9206134B2 (OSRAM) |
| EP (1) | EP2734504B1 (OSRAM) |
| JP (1) | JP6099644B2 (OSRAM) |
| KR (1) | KR102029951B1 (OSRAM) |
| CN (1) | CN104024227B8 (OSRAM) |
| AU (1) | AU2012289429B2 (OSRAM) |
| CA (1) | CA2842730C (OSRAM) |
| ES (1) | ES2606631T3 (OSRAM) |
| IL (1) | IL230580B (OSRAM) |
| WO (1) | WO2013013609A1 (OSRAM) |
| ZA (1) | ZA201401310B (OSRAM) |
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004108681A1 (en) | 2003-06-06 | 2004-12-16 | Fibrogen, Inc. | Nitrogen-containing heteroaryl compounds and their use in increasing endogenous erythropoietin |
| NO2686520T3 (OSRAM) | 2011-06-06 | 2018-03-17 | ||
| US8883823B2 (en) | 2012-07-16 | 2014-11-11 | Fibrogen, Inc. | Crystalline forms of a prolyl hydroxylase inhibitor |
| HUE034409T2 (en) * | 2012-07-16 | 2018-02-28 | Fibrogen Inc | Process for the preparation of isoquinoline compounds |
| CN109369524A (zh) | 2012-07-16 | 2019-02-22 | 菲布罗根有限公司 | 脯氨酰羟化酶抑制剂的晶体形态 |
| CN105377242A (zh) | 2013-06-06 | 2016-03-02 | 菲布罗根有限公司 | Hif羟化酶抑制剂的药物制剂 |
| NZ714963A (en) | 2013-06-13 | 2020-07-31 | Akebia Therapeutics Inc | Compositions and methods for treating anemia |
| TWI846166B (zh) | 2013-11-15 | 2024-06-21 | 美商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 |
| JP2018502882A (ja) | 2015-01-23 | 2018-02-01 | アケビア セラピューティクス インコーポレイテッドAkebia Therapeutics Inc. | 2−(5−(3−フルオロフェニル)−3−ヒドロキシピコリンアミド)酢酸の固体形態、その組成物及び使用 |
| 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 |
| UA123308C2 (uk) | 2015-04-01 | 2021-03-17 | Екебіа Терапьютікс, Інк. | Композиції і способи для лікування анемії |
| 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 |
| CN113694077A (zh) * | 2015-08-13 | 2021-11-26 | 索马根尼科斯公司 | 用于伤口愈合的短小发夹rna与微rna的组合物以及方法 |
| 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 |
| EP3664805A4 (en) * | 2017-08-11 | 2021-06-30 | Dr. Reddy's Laboratories Limited | POLYMORPHIC AND CO-CRYSTALS OF ROXADUSTAT |
| CA3074529C (en) * | 2017-09-04 | 2022-07-05 | Sandoz Ag | Co-crystal of roxadustat with l-proline and uses thereof |
| US20200299242A1 (en) * | 2017-12-01 | 2020-09-24 | Dr. Reddy's Laboratories Limited | Process for the preparation of roxadustat and its intermediates |
| 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 |
| WO2019174631A1 (zh) * | 2018-03-16 | 2019-09-19 | 上海医药集团股份有限公司 | 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 |
| AU2019265629B2 (en) | 2018-05-09 | 2024-09-12 | 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 |
| CN118993939A (zh) | 2019-04-18 | 2024-11-22 | 尼坎治疗公司 | 作为缺氧可诱导因子-2(α)抑制剂的四氢-1H-环戊二烯并[CD]茚衍生物 |
| 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 |
| US20220340532A1 (en) | 2019-08-07 | 2022-10-27 | 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| EP4169906B1 (en) | 2020-06-19 | 2024-09-04 | Jumpcan (Shanghai) Medical Technology Co., Ltd | Method for synthesis of roxadustat and intermediate thereof, and intermediate thereof |
| 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 |
| 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 |
| 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 |
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 |
| CA2444704C (en) * | 2001-04-23 | 2012-07-10 | University Of Virginia Patent Foundation | Synthesis and evaluation of phthalimide mimics as anti-angiogenic agents |
| WO2004108681A1 (en) * | 2003-06-06 | 2004-12-16 | Fibrogen, Inc. | Nitrogen-containing heteroaryl compounds and their use in increasing endogenous erythropoietin |
| US7189697B2 (en) | 2004-04-13 | 2007-03-13 | Trustees Of Tufts College | Compositions and uses of a galectin for treatment of dry eye syndrome |
| EP1893186A2 (en) * | 2005-06-06 | 2008-03-05 | Fibrogen, Inc. | Improved treatment for anemia using a hif-alpha stabilising agent |
| US7728130B2 (en) | 2005-12-09 | 2010-06-01 | Amgen Inc. | Quinolone based compounds exhibiting prolyl hydroxylase inhibitory activity |
| DK2044028T3 (da) * | 2006-01-27 | 2012-08-20 | Fibrogen Inc | Cyanoisoquinolinforbindelser til stabilisering af den hypoxiinducerende faktor (HIF) |
| 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 |
| US8742138B2 (en) | 2009-07-15 | 2014-06-03 | Betta Pharmaceuticals Co., Ltd. | Compounds as hypoxia mimetics, and compositions and uses thereof |
-
2012
- 2012-07-23 WO PCT/CN2012/079058 patent/WO2013013609A1/en not_active Ceased
- 2012-07-23 CA CA2842730A patent/CA2842730C/en active Active
- 2012-07-23 ES ES12817360.6T patent/ES2606631T3/es active Active
- 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 EP EP12817360.6A patent/EP2734504B1/en not_active Not-in-force
- 2012-07-23 AU AU2012289429A patent/AU2012289429B2/en active Active
- 2012-07-23 JP JP2014520521A patent/JP6099644B2/ja not_active Expired - Fee Related
-
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 |
|---|---|
| KR20140049004A (ko) | 2014-04-24 |
| CN104024227B8 (zh) | 2025-07-29 |
| EP2734504A1 (en) | 2014-05-28 |
| AU2012289429A1 (en) | 2014-03-20 |
| CN104024227B (zh) | 2015-12-02 |
| EP2734504A4 (en) | 2014-12-31 |
| CA2842730A1 (en) | 2013-01-31 |
| KR102029951B1 (ko) | 2019-11-08 |
| AU2012289429B2 (en) | 2016-07-28 |
| CA2842730C (en) | 2018-08-21 |
| EP2734504B1 (en) | 2016-09-14 |
| IL230580B (en) | 2019-07-31 |
| ES2606631T3 (es) | 2017-03-24 |
| US20150031721A1 (en) | 2015-01-29 |
| CN104024227A (zh) | 2014-09-03 |
| WO2013013609A1 (en) | 2013-01-31 |
| JP2014524920A (ja) | 2014-09-25 |
| ZA201401310B (en) | 2015-04-29 |
| US9206134B2 (en) | 2015-12-08 |
| IL230580A0 (en) | 2014-03-31 |
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