CN107501177B - 脯氨酰羟化酶抑制剂的晶体形态 - Google Patents

脯氨酰羟化酶抑制剂的晶体形态 Download PDF

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Publication number
CN107501177B
CN107501177B CN201710546191.5A CN201710546191A CN107501177B CN 107501177 B CN107501177 B CN 107501177B CN 201710546191 A CN201710546191 A CN 201710546191A CN 107501177 B CN107501177 B CN 107501177B
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compound
project
salt
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peak
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CN107501177A (zh
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克劳迪娅·维兹
朴贞玟
迈克尔·道格拉斯·汤普森
迈克尔·约翰·马蒂内利
大卫·A·尤为尔
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Fibrogen China Medical Technology Development Co Ltd
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Fibrogen Inc
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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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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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    • 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
    • A—HUMAN NECESSITIES
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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
    • A—HUMAN NECESSITIES
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    • A61P11/00—Drugs for disorders of the respiratory system
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    • 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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    • 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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    • 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
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    • A61P7/06—Antianaemics
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
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    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • 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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    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pain & Pain Management (AREA)
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  • Communicable Diseases (AREA)
  • Oncology (AREA)
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  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
CN201710546191.5A 2012-07-16 2013-07-15 脯氨酰羟化酶抑制剂的晶体形态 Ceased CN107501177B (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201261672191P 2012-07-16 2012-07-16
US61/672,191 2012-07-16
US201361768297P 2013-02-22 2013-02-22
US61/768,297 2013-02-22
US201361832566P 2013-06-07 2013-06-07
US61/832,566 2013-06-07
CN201310302481.7A CN103539735B (zh) 2012-07-16 2013-07-15 脯氨酰羟化酶抑制剂的晶体形态

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CN107501177A CN107501177A (zh) 2017-12-22
CN107501177B true CN107501177B (zh) 2018-12-07

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CN201710546191.5A Ceased CN107501177B (zh) 2012-07-16 2013-07-15 脯氨酰羟化酶抑制剂的晶体形态
CN201710546643.XA Pending CN107540607A (zh) 2012-07-16 2013-07-15 脯氨酰羟化酶抑制剂的晶体形态
CN201710546354.XA Active CN107382859B (zh) 2012-07-16 2013-07-15 脯氨酰羟化酶抑制剂的晶体形态
CN202210791828.8A Pending CN115093370A (zh) 2012-07-16 2013-07-15 脯氨酰羟化酶抑制剂的晶体形态
CN201380037479.XA Pending CN104684897A (zh) 2012-07-16 2013-07-15 脯氨酰羟化酶抑制剂的晶体形态
CN201710546619.6A Pending CN107382860A (zh) 2012-07-16 2013-07-15 脯氨酰羟化酶抑制剂的晶体形态
CN201310302481.7A Active CN103539735B (zh) 2012-07-16 2013-07-15 脯氨酰羟化酶抑制剂的晶体形态
CN202111361393.5A Pending CN114409596A (zh) 2012-07-16 2013-07-15 脯氨酰羟化酶抑制剂的晶体形态
CN201810750543.3A Pending CN109369524A (zh) 2012-07-16 2013-07-15 脯氨酰羟化酶抑制剂的晶体形态

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CN201710546643.XA Pending CN107540607A (zh) 2012-07-16 2013-07-15 脯氨酰羟化酶抑制剂的晶体形态
CN201710546354.XA Active CN107382859B (zh) 2012-07-16 2013-07-15 脯氨酰羟化酶抑制剂的晶体形态
CN202210791828.8A Pending CN115093370A (zh) 2012-07-16 2013-07-15 脯氨酰羟化酶抑制剂的晶体形态
CN201380037479.XA Pending CN104684897A (zh) 2012-07-16 2013-07-15 脯氨酰羟化酶抑制剂的晶体形态
CN201710546619.6A Pending CN107382860A (zh) 2012-07-16 2013-07-15 脯氨酰羟化酶抑制剂的晶体形态
CN201310302481.7A Active CN103539735B (zh) 2012-07-16 2013-07-15 脯氨酰羟化酶抑制剂的晶体形态
CN202111361393.5A Pending CN114409596A (zh) 2012-07-16 2013-07-15 脯氨酰羟化酶抑制剂的晶体形态
CN201810750543.3A Pending CN109369524A (zh) 2012-07-16 2013-07-15 脯氨酰羟化酶抑制剂的晶体形态

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US (5) US9115085B2 (2)
EP (3) EP4029854A1 (2)
JP (2) JP6491093B2 (2)
KR (4) KR102318720B1 (2)
CN (9) CN107501177B (2)
AU (1) AU2013290438C1 (2)
BR (1) BR112015001101A2 (2)
CA (1) CA2879242C (2)
CY (2) CY1120805T1 (2)
DK (2) DK2872488T3 (2)
ES (2) ES2689430T3 (2)
FR (1) FR22C1030I2 (2)
HK (1) HK1243409A1 (2)
HR (2) HRP20220182T1 (2)
HU (2) HUE041458T2 (2)
IL (1) IL236626B (2)
IN (1) IN2015KN00262A (2)
LT (3) LT2872488T (2)
MX (1) MX355428B (2)
MY (1) MY182428A (2)
NO (1) NO2022024I1 (2)
NZ (1) NZ704662A (2)
PL (2) PL3470397T3 (2)
PT (2) PT2872488T (2)
RS (2) RS57795B1 (2)
SG (3) SG10201700873UA (2)
SI (2) SI2872488T1 (2)
SM (2) SMT201800565T1 (2)
WO (1) WO2014014835A2 (2)

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WO2004108681A1 (en) 2003-06-06 2004-12-16 Fibrogen, Inc. Nitrogen-containing heteroaryl compounds and their use in increasing endogenous erythropoietin
JP5649584B2 (ja) 2008-11-14 2015-01-07 フィブロジェン インコーポレイテッド Ｈｉｆヒドロキシラーゼ阻害剤としてのチオクロメン誘導体
WO2012106472A1 (en) 2011-02-02 2012-08-09 Fibrogen, Inc. Naphthyridine derivatives as inhibitors of hypoxia inducible factor (hif) hydroxylase
EP3219706A1 (en) 2012-07-16 2017-09-20 Fibrogen, Inc. Process for making isoquinoline compounds
US8883823B2 (en) 2012-07-16 2014-11-11 Fibrogen, Inc. Crystalline forms of a prolyl hydroxylase inhibitor
AU2013290438C1 (en) 2012-07-16 2019-01-03 Kyntra Bio, Inc. Crystalline forms of the prolyl hydroxylase inhibitor [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid
HRP20200615T1 (hr) 2013-06-06 2020-07-10 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
US11510917B2 (en) 2016-02-19 2022-11-29 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
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
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
CN111978225B (zh) 2018-06-05 2022-03-04 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
US20230190731A1 (en) * 2020-03-17 2023-06-22 Zydus Lifesciences 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
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