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 PDF

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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
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crystalline polymorph
compound
formula
ray powder
diffraction pattern
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CA2842730A1 (en
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Xinshan Kang
Wei LONG
Jianxi ZHANG
Yunyan Hu
Yinxiang Wang
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Beijing Betta Pharmaceuticals Co Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic 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
    • C07D217/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • 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)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
CA2842730A 2011-07-22 2012-07-23 Polymorphic forms of compounds as prolyl hydroxylase inhibitor, and uses thereof Active CA2842730C (en)

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

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Family Applications (1)

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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)

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US8883823B2 (en) 2012-07-16 2014-11-11 Fibrogen, Inc. Crystalline forms of a prolyl hydroxylase inhibitor
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TW201632504A (zh) * 2015-01-23 2016-09-16 阿克比治療有限公司 2-(5-(3-氟苯基)-3-羥吡啶醯胺基)乙酸之固體形式、其組合物及其用途
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
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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
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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
JP2020530473A (ja) * 2017-08-11 2020-10-22 ドクター レディズ ラボラトリーズ リミテッド ロキサデュスタットの多形および共結晶
CN111065625A (zh) * 2017-09-04 2020-04-24 桑多斯股份公司 口服可利用的hif脯氨酰羟化酶抑制剂的共晶
JP2021504440A (ja) * 2017-12-01 2021-02-15 ドクター レディズ ラボラトリーズ リミテッド ロキサデュスタット及びその中間体の調製方法
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
KR20210006967A (ko) 2018-05-09 2021-01-19 아케비아 테라퓨틱스 인코포레이티드 2-[[5-(3-클로로페닐)-3-하이드록시피리딘-2-카르보닐]아미노]아세트산을 제조하는 방법
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
UA128792C2 (uk) * 2019-04-18 2024-10-23 Ніканг Терапьютікс, Інк. ПОХІДНІ ТЕТРАГІДРО-1Н-ЦИКЛОПЕНТА[cd]ІНДЕНУ ЯК ІНГІБІТОРИ ФАКТОРА-2(АЛЬФА), ЩО ІНДУКУЄТЬСЯ ГІПОКСІЄЮ
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
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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
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
CN113015722B (zh) * 2019-10-22 2022-02-11 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
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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
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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
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Publication number Publication date
AU2012289429A1 (en) 2014-03-20
CA2842730A1 (en) 2013-01-31
CN104024227B (zh) 2015-12-02
EP2734504A1 (en) 2014-05-28
EP2734504B1 (en) 2016-09-14
IL230580B (en) 2019-07-31
EP2734504A4 (en) 2014-12-31
WO2013013609A1 (en) 2013-01-31
KR20140049004A (ko) 2014-04-24
CN104024227A (zh) 2014-09-03
KR102029951B1 (ko) 2019-11-08
IL230580A0 (en) 2014-03-31
ZA201401310B (en) 2015-04-29
US20150031721A1 (en) 2015-01-29
CN104024227B8 (zh) 2025-07-29
JP6099644B2 (ja) 2017-03-22
AU2012289429B2 (en) 2016-07-28
JP2014524920A (ja) 2014-09-25
ES2606631T3 (es) 2017-03-24
US9206134B2 (en) 2015-12-08

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