IL236626B - Crystal forms of prolyl hydroxylase inhibitor [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid - Google Patents
Crystal forms of prolyl hydroxylase inhibitor [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acidInfo
- Publication number
- IL236626B IL236626B IL236626A IL23662615A IL236626B IL 236626 B IL236626 B IL 236626B IL 236626 A IL236626 A IL 236626A IL 23662615 A IL23662615 A IL 23662615A IL 236626 B IL236626 B IL 236626B
- Authority
- IL
- Israel
- Prior art keywords
- isoquinoline
- phenoxy
- carbonyl
- hydroxy
- amino
- Prior art date
Links
Classifications
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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
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- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A61P17/00—Drugs for dermatological disorders
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- 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
- A61P25/08—Antiepileptics; Anticonvulsants
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A61P27/00—Drugs for disorders of the senses
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- A—HUMAN NECESSITIES
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- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- 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
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- A61P39/00—General protective or antinoxious agents
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- A—HUMAN NECESSITIES
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
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- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- 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
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Vascular Medicine (AREA)
- Tropical Medicine & Parasitology (AREA)
- Dermatology (AREA)
- Hospice & Palliative Care (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Virology (AREA)
- Gastroenterology & Hepatology (AREA)
- Rheumatology (AREA)
- Toxicology (AREA)
- Emergency Medicine (AREA)
- Pulmonology (AREA)
- Ophthalmology & Optometry (AREA)
- Psychiatry (AREA)
- Endocrinology (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261672191P | 2012-07-16 | 2012-07-16 | |
| US201361768297P | 2013-02-22 | 2013-02-22 | |
| US201361832566P | 2013-06-07 | 2013-06-07 | |
| PCT/US2013/050539 WO2014014835A2 (en) | 2012-07-16 | 2013-07-15 | Crystalline forms of a prolyl hydroxylase inhibitor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IL236626A0 IL236626A0 (en) | 2015-02-26 |
| IL236626B true IL236626B (en) | 2020-03-31 |
Family
ID=48857025
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL236626A IL236626B (en) | 2012-07-16 | 2015-01-11 | Crystal forms of prolyl hydroxylase inhibitor [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid |
Country Status (29)
| Country | Link |
|---|---|
| US (5) | US9115085B2 (show.php) |
| EP (3) | EP4029854A1 (show.php) |
| JP (2) | JP6491093B2 (show.php) |
| KR (4) | KR20220164068A (show.php) |
| CN (9) | CN104684897A (show.php) |
| AU (1) | AU2013290438C1 (show.php) |
| BR (1) | BR112015001101A2 (show.php) |
| CA (1) | CA2879242C (show.php) |
| CY (2) | CY1120805T1 (show.php) |
| DK (2) | DK3470397T3 (show.php) |
| ES (2) | ES2689430T3 (show.php) |
| FR (1) | FR22C1030I2 (show.php) |
| HK (1) | HK1243409A1 (show.php) |
| HR (2) | HRP20181751T1 (show.php) |
| HU (2) | HUE057925T2 (show.php) |
| IL (1) | IL236626B (show.php) |
| IN (1) | IN2015KN00262A (show.php) |
| LT (3) | LT3470397T (show.php) |
| MX (1) | MX355428B (show.php) |
| MY (1) | MY182428A (show.php) |
| NO (1) | NO2022024I1 (show.php) |
| NZ (1) | NZ704662A (show.php) |
| PL (2) | PL2872488T3 (show.php) |
| PT (2) | PT3470397T (show.php) |
| RS (2) | RS57795B1 (show.php) |
| SG (3) | SG11201500236SA (show.php) |
| SI (2) | SI3470397T1 (show.php) |
| SM (2) | SMT201800565T1 (show.php) |
| WO (1) | WO2014014835A2 (show.php) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100932169B1 (ko) | 2003-06-06 | 2009-12-16 | 피브로겐, 인크. | 질소-함유 헤테로아릴 화합물 및 내인성 적혈구생성소의증가에서의 그들의 사용 |
| AU2009314155B2 (en) | 2008-11-14 | 2015-10-08 | Fibrogen, Inc. | Thiochromene derivatives as HIF hydroxylase inhibitors |
| CN103608346B (zh) | 2011-02-02 | 2016-06-15 | 菲布罗根有限公司 | 作为缺氧诱导因子(hif)羟化酶抑制剂的萘啶衍生物 |
| SMT201800565T1 (it) * | 2012-07-16 | 2018-11-09 | Fibrogen Inc | Forme cristalline di un inibitore di prolil idrossilasi |
| US8883823B2 (en) | 2012-07-16 | 2014-11-11 | Fibrogen, Inc. | Crystalline forms of a prolyl hydroxylase inhibitor |
| BR112015001106B1 (pt) | 2012-07-16 | 2021-11-09 | Fibrogen, Inc | Métodos para a produção de compostos de isoquinolina |
| RS60464B1 (sr) | 2013-06-06 | 2020-07-31 | Fibrogen Inc | Farmaceutske formulacije inhibitora hif hidroksilaze |
| 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 |
| WO2016045125A1 (en) | 2014-09-28 | 2016-03-31 | Merck Sharp & Dohme Corp. | Inhibitors of hif prolyl hydroxylase |
| 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 |
| 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 |
| WO2017143131A1 (en) * | 2016-02-19 | 2017-08-24 | Cornell University | Hif-stabilization and prevention of hyperoxia-induced neonatal lung disease |
| 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 |
| 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 |
| CN107382986B (zh) * | 2017-08-02 | 2022-09-20 | 江苏艾立康医药科技有限公司 | 4-羟基-1-甲基异喹啉衍生物及其在增加内源性促红细胞生成素中的用途 |
| CN111511371A (zh) * | 2017-08-11 | 2020-08-07 | 雷迪博士实验室有限公司 | 罗沙司他的多晶型物和共晶 |
| WO2019042485A1 (en) | 2017-08-30 | 2019-03-07 | Zentiva, K.S. | FORMS IN THE STRONG STATE OF ROXADUSTAT |
| WO2019042641A1 (en) | 2017-09-04 | 2019-03-07 | Sandoz Ag | CO-CRYSTAL OF A HIF PROLYL HYDROXYLASE INHIBITOR AVAILABLE ORALLY |
| WO2019233321A1 (zh) | 2018-06-05 | 2019-12-12 | 沈阳化工大学 | 一种三氟乙基硫醚(亚砜)取代苯类化合物及其用途 |
| CN111320583A (zh) * | 2018-12-14 | 2020-06-23 | 广东东阳光药业有限公司 | 诺德司他新晶型及其制备方法 |
| 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 |
| WO2020217190A1 (en) * | 2019-04-26 | 2020-10-29 | Dr. Reddy’S Laboratories Limited | Process for the purification of roxadustat |
| 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 |
| JP2022553706A (ja) * | 2019-10-22 | 2022-12-26 | ▲蘇▼州科睿思制▲葯▼有限公司 | 低酸素誘導因子-プロリルヒドロキシラーゼ阻害剤の結晶形 |
| CN110721185B (zh) * | 2019-11-13 | 2022-04-12 | 南京市儿童医院 | 罗沙司他用于心肌保护的用途 |
| CN112961107B (zh) * | 2019-12-13 | 2024-06-25 | 罗欣药业(上海)有限公司 | 罗沙司他的晶型及其制备方法 |
| WO2021186356A1 (en) * | 2020-03-17 | 2021-09-23 | Cadila Healthcare Limited | Formulation comprising hif prolyl hydroxylase inhibitors |
| 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 |
| CN113754569B (zh) * | 2020-06-04 | 2024-07-02 | 四川国为制药有限公司 | 一种中间体化合物及其制备方法和用途 |
| CN111533691A (zh) * | 2020-06-08 | 2020-08-14 | 重庆三圣实业股份有限公司 | 一种罗沙司他的制备方法 |
| CN114057643B (zh) * | 2020-08-04 | 2023-02-28 | 成都苑东生物制药股份有限公司 | 一种罗沙司他共晶及其制备方法 |
| 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 |
| 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 |
| 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 |
| CN113956200A (zh) * | 2021-12-16 | 2022-01-21 | 南京威凯尔生物医药科技有限公司 | 一种粒径控制的罗沙司他原料药的结晶工艺 |
| CN116410134A (zh) * | 2021-12-31 | 2023-07-11 | 北京济美堂医药研究有限公司 | 一种罗沙司他水合物晶体及其制备方法和应用 |
| WO2025111214A1 (en) | 2023-11-22 | 2025-05-30 | Fibrogen, Inc. | [(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3- carbonyl)amino]acetic acid (roxadustat) for the treatment of anemia in subjects with myelodysplastic syndrome (mds) |
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| DE2818423A1 (de) | 1978-04-27 | 1979-11-08 | Hoechst Ag | Neue isochinolinderivate und verfahren zu ihrer herstellung |
| DE3233424A1 (de) | 1982-09-09 | 1984-03-15 | Hoechst Ag, 6230 Frankfurt | Isochinolinderivate, verfahren zu ihrer herstellung, pharmazeutische praeparate auf basis dieser verbindungen und ihre verwendung |
| US4558006A (en) | 1983-02-04 | 1985-12-10 | Kirin-Amgen, Inc. | A.T.C.C. HB8209 and its monoclonal antibody to erythropoietin |
| US4559403A (en) | 1983-05-19 | 1985-12-17 | Hoffmann-La Roche Inc. | Substituted isoquinolines |
| US4584379A (en) | 1985-01-22 | 1986-04-22 | Merrell Dow Pharmaceuticals Inc. | Isoquinoline thromboxane synthetase inhibitors |
| US4667016A (en) | 1985-06-20 | 1987-05-19 | Kirin-Amgen, Inc. | Erythropoietin purification |
| US4822800A (en) | 1986-06-09 | 1989-04-18 | Ortho Pharmaceutical Corporation | Isoquinolinol compounds having cardiotonic and phosphodiesterase fraction III inhibiting properties and/or renal vasodilating properties |
| US4966906A (en) | 1987-11-27 | 1990-10-30 | Hoechst-Roussel Pharmaceuticals Inc. | 1-aryl-3-isoquinolinecarboxamides |
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