CN105037323A - 作为hif羟化酶抑制剂的苯并噻喃衍生物 - Google Patents

作为hif羟化酶抑制剂的苯并噻喃衍生物 Download PDF

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Publication number
CN105037323A
CN105037323A CN201510259787.8A CN201510259787A CN105037323A CN 105037323 A CN105037323 A CN 105037323A CN 201510259787 A CN201510259787 A CN 201510259787A CN 105037323 A CN105037323 A CN 105037323A
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hydroxyl
oxo
amino
carbonyl
substituted
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Chinese (zh)
Inventor
文彬·何
李·R·维特
埃里克·D·图尔托
克雷格·莫斯门
李·A·弗利平
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Fibrogen Inc
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Fibrogen Inc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D335/00Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
    • C07D335/04Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D335/06Benzothiopyrans; Hydrogenated benzothiopyrans
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/382Heterocyclic compounds having sulfur as a ring hetero atom having six-membered rings, e.g. thioxanthenes
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • 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
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201510259787.8A 2008-11-14 2009-11-11 作为hif羟化酶抑制剂的苯并噻喃衍生物 Pending CN105037323A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US11497108P 2008-11-14 2008-11-14
US61/114,971 2008-11-14
CN200980154106.4A CN102272117B (zh) 2008-11-14 2009-11-11 作为hif羟化酶抑制剂的苯并噻喃衍生物

Related Parent Applications (1)

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CN200980154106.4A Division CN102272117B (zh) 2008-11-14 2009-11-11 作为hif羟化酶抑制剂的苯并噻喃衍生物

Publications (1)

Publication Number Publication Date
CN105037323A true CN105037323A (zh) 2015-11-11

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CN201510259787.8A Pending CN105037323A (zh) 2008-11-14 2009-11-11 作为hif羟化酶抑制剂的苯并噻喃衍生物
CN200980154106.4A Expired - Fee Related CN102272117B (zh) 2008-11-14 2009-11-11 作为hif羟化酶抑制剂的苯并噻喃衍生物

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US (2) US8927591B2 (enExample)
EP (1) EP2370422B1 (enExample)
JP (1) JP5649584B2 (enExample)
CN (2) CN105037323A (enExample)
AU (1) AU2009314155B2 (enExample)
IL (1) IL212762A (enExample)
NZ (1) NZ592741A (enExample)
WO (1) WO2010056767A1 (enExample)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102718708A (zh) 2003-06-06 2012-10-10 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
US8614204B2 (en) 2003-06-06 2013-12-24 Fibrogen, Inc. Enhanced erythropoiesis and iron metabolism
US8269008B2 (en) 2007-12-03 2012-09-18 Fibrogen, Inc. Oxazolopyridine and isoxazolopyridine derivatives for use in the treatment of HIF-mediated conditions
US8952160B2 (en) 2008-01-11 2015-02-10 Fibrogen, Inc. Isothiazole-pyridine derivatives as modulators of HIF (hypoxia inducible factor) activity
US8324405B2 (en) 2008-02-05 2012-12-04 Fibrogen, Inc. Chromene derivatives and use thereof as HIF hydroxylase activity inhibitors
EP2334682B1 (en) 2008-08-20 2017-10-04 Fibrogen, Inc. Pyrrolo [ 1, 2 -b] pyridazine derivatives and their use as hif modulators
CN105037323A (zh) 2008-11-14 2015-11-11 菲布罗根有限公司 作为hif羟化酶抑制剂的苯并噻喃衍生物
AU2011235212B2 (en) 2010-03-31 2014-07-31 The Scripps Research Institute Reprogramming cells
EP2465841A1 (en) * 2010-11-19 2012-06-20 Lonza Ltd. Preparation of esters of mono- or dicarboxylic non-aromatic and aromatic acids
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
GB201102659D0 (en) 2011-02-15 2011-03-30 Isis Innovation Assay
NO2686520T3 (enExample) 2011-06-06 2018-03-17
GB201113101D0 (en) 2011-07-28 2011-09-14 Isis Innovation Assay
JP6129217B2 (ja) 2012-03-09 2017-05-17 フィブロジェン インコーポレイテッド Hifヒドロキシラーゼインヒビターとしての4−ヒドロキシ−イソキノリン化合物
ES2631655T3 (es) 2012-07-16 2017-09-01 Fibrogen, Inc. Procedimiento para fabricar compuestos de isoquinolina
US8883823B2 (en) 2012-07-16 2014-11-11 Fibrogen, Inc. Crystalline forms of a prolyl hydroxylase inhibitor
KR20220164068A (ko) 2012-07-16 2022-12-12 피브로겐, 인크. 프롤릴 하이드록실라제 억제제 [(4-하이드록시-1-메틸-7-페녹시-아이소퀴놀린-3-카보닐)-아미노]-아세트산의 결정형
LT3003284T (lt) 2013-06-06 2020-04-27 Fibrogen, Inc. Hif hidroksilazės inhibitoriaus farmacinės kompozicijos
DK3007695T3 (da) 2013-06-13 2024-03-18 Akebia Therapeutics Inc Sammensætninger og fremgangsmåder til behandling af anæmi
WO2016034108A1 (zh) 2014-09-02 2016-03-10 广东东阳光药业有限公司 喹啉酮类化合物及其应用
MX2017009417A (es) 2015-01-23 2017-12-07 Akebia Therapeutics Inc Formas solidas de acido 2-(5-(3-fluorofenil)-3-hidroxipicolinamido )acetico, composiciones y usos de las mismas.
AU2016235534A1 (en) * 2015-03-20 2017-10-12 Akebia Therapeutics, Inc. Deuterium-enriched hypoxia-inducible factor prolyl hydroxylase enzyme inhibitors
PT3277270T (pt) 2015-04-01 2021-12-07 Akebia Therapeutics Inc Composições e métodos de tratamento de anemia
CN113004271A (zh) 2017-05-09 2021-06-22 杭州安道药业有限公司 吲哚嗪衍生物及其在医药上的应用
MX2020011845A (es) 2018-05-09 2021-01-15 Akebia Therapeutics Inc Proceso para preparar acido 2-[[5-(3-clorofenil)-3-hidroxipiridina -2-carbonil]amino]acetico.
US20230218592A1 (en) 2020-04-20 2023-07-13 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
WO2022150623A1 (en) 2021-01-08 2022-07-14 Akebia Therapeutics, Inc. Compounds and composition for the treatment of anemia
TW202313072A (zh) 2021-05-27 2023-04-01 美商凱立克斯生物製藥股份有限公司 檸檬酸鐵之兒科調配物
CN115944626B (zh) * 2022-12-08 2024-04-19 桂林医学院附属医院 小分子化合物在制备抗缺氧或缺血再灌注损伤药物中的应用

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN85103105A (zh) * 1984-04-12 1986-10-22 里昂利发制药厂 羟基-4-2h-1-苯并噻喃-2-酮衍生物的制备方法
JPH10279575A (ja) * 1997-03-31 1998-10-20 Fuji Photo Film Co Ltd ベンゾピラン化合物の製造方法
WO2007038571A2 (en) * 2005-09-26 2007-04-05 Smithkline Beecham Corporation Prolyl hydroxylase antagonists
WO2007103905A2 (en) * 2006-03-07 2007-09-13 Smithkline Beecham Corporation Prolyl hydroxylase inhibitors
US20070249605A1 (en) * 2005-12-09 2007-10-25 Allen Jennifer R Quinolone based compounds exhibiting prolyl hydroxylase inhibitory activity, and compositions, and uses thereof
WO2009075826A1 (en) * 2007-12-07 2009-06-18 Fibrogen, Inc. Methods for increasing white blood cells

Family Cites Families (96)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4036964A (en) 1973-10-11 1977-07-19 Beecham Group Limited Isocarbostyril-3-carboxylic acid derivatives for the prophylaxis of asthma, hayfever and rhinitis
US3989704A (en) 1973-10-30 1976-11-02 Sandoz, Inc. 3-Substituted-4-aryl isoquinolines
GB1582217A (en) 1978-02-27 1981-01-07 Teijin Ltd Penicillin derivatives medicines containing the same and process for producing the same
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
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
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
GB8816519D0 (en) 1987-07-23 1988-08-17 Ici Plc Antibiotic compounds
US4966906A (en) 1987-11-27 1990-10-30 Hoechst-Roussel Pharmaceuticals Inc. 1-aryl-3-isoquinolinecarboxamides
US4952588A (en) 1987-11-27 1990-08-28 Hoechst-Roussel Pharmaceuticals Inc. 1-aryl-3-quinoline-and 1-aryl-3-isoquinoline-carboxamides
EP0532466A3 (en) 1991-09-12 1993-06-16 Ciba-Geigy Ag Derivatives of 5-amino-4-hydroxy-hexanoic acid and their therapeutical use
US5378720A (en) 1991-12-19 1995-01-03 Sterling Winthrop Inc. Saccharin derivative proteolytic enzyme inhibitors
EP0626178A1 (de) 1993-05-17 1994-11-30 Ciba-Geigy Ag Verwendung von Hemmstoffen von HIV-Aspartatproteasen zur Bekämpfung von Tumorerkrankungen
ES2101420T3 (es) 1993-11-02 1997-07-01 Hoechst Ag Esteres-amidas de acidos carboxilicos heterociclicos sustituidos, su preparacion y su utilizacion como medicamentos.
ATE149486T1 (de) 1993-11-02 1997-03-15 Hoechst Ag Substituierte heterocyclische carbonsäureamide, ihre herstellung und ihre verwendung als arzneimittel
CA2138929A1 (en) 1993-12-30 1995-07-01 Klaus Weidmann Substituted heterocyclic carboxamides, their preparation and their use as pharmaceuticals
US5563143A (en) 1994-09-21 1996-10-08 Pfizer Inc. Catechol diether compounds as inhibitors of TNF release
AU4515696A (en) 1994-12-12 1996-07-03 Merck & Co., Inc. Substituted 2-aminopyridines as inhibitors of nitric oxide synthase
US5741657A (en) 1995-03-20 1998-04-21 The Regents Of The University Of California Fluorogenic substrates for β-lactamase and methods of use
IL135495A (en) 1995-09-28 2002-12-01 Hoechst Ag Intermediate compounds for the preparation of quinoline-converted amines - 2 - carboxylic acid
US5955604A (en) 1996-10-15 1999-09-21 The Regents Of The University Of California Substrates for β-lactamase and uses thereof
US6130231A (en) 1996-11-27 2000-10-10 Dupont Pharmaceuticals Integrin receptor antagonists
WO1998050346A2 (en) 1997-04-18 1998-11-12 Smithkline Beecham Plc Acetamide and urea derivatives, process for their preparation and their use in the treatment of cns disorders
GB9707830D0 (en) 1997-04-18 1997-06-04 Smithkline Beecham Plc Novel compounds
DE19746287A1 (de) 1997-10-20 1999-04-22 Hoechst Marion Roussel De Gmbh Substituierte Isochinolin-2-Carbonsäureamide, ihre Herstellung und ihre Verwendung als Arzneimittel
FR2779963A1 (fr) 1998-06-22 1999-12-24 Centre Nat Rech Scient Utilisation d'un compose possedant une affinite pour le recepteur mitochondrial des benzodiazepines en therapie du cancer
IT1302677B1 (it) 1998-10-15 2000-09-29 Zambon Spa Derivati benzazinici inibitori della fosfodiesterasi 4
AU4802500A (en) 1999-04-26 2000-11-10 Neurogen Corporation 2-aminoquinolinecarboxamides: neurokinin receptor ligands
IT1320162B1 (it) 2000-02-09 2003-11-18 Rotta Research Lab Derivati della tirosina ad attivita' anti leucotrienica, procedimentoper la loro preparazione e loro uso farmaceutico.
US7622503B2 (en) 2000-08-24 2009-11-24 University Of Tennessee Research Foundation Selective androgen receptor modulators and methods of use thereof
FI20002044A0 (fi) 2000-09-15 2000-09-15 Orion Yhtymae Oyj Comt-entsyymiä estäviä naftaleenijohdannaisia
DE10110750A1 (de) 2001-03-07 2002-09-12 Bayer Ag Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften
AU2002241154A1 (en) 2001-03-21 2002-10-03 Isis Innovation Ltd. Assays, methods and means relating to hypoxia inducible factor (hif) hydroxylase
US6716866B2 (en) 2001-06-13 2004-04-06 Genesoft Pharmaceuticals, Inc. Aryl-benzimidazole compounds having antiinfective activity
JP2005505507A (ja) 2001-06-13 2005-02-24 ジーンソフト ファーマシューティカルズ インコーポレイテッド 抗感染活性を有するイソキノリン化合物
CA2448737C (en) 2001-07-20 2010-06-01 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
EP2335700A1 (en) 2001-07-25 2011-06-22 Boehringer Ingelheim (Canada) Ltd. Hepatitis C virus polymerase inhibitors with a heterobicylic structure
US7294457B2 (en) 2001-08-07 2007-11-13 Boehringer Ingelheim (Canada) Ltd. Direct binding assay for identifying inhibitors of HCV polymerase
US6762318B2 (en) 2001-12-03 2004-07-13 Novo Nordisk A/S Glucagon antagonists
JP2005524612A (ja) 2001-12-06 2005-08-18 ファイブローゲン、インコーポレーテッド 内因性エリスロポエチン(epo)を増加させる方法
GB0206711D0 (en) 2002-03-21 2002-05-01 Isis Innovation HIF Inhibitor
CN1506359A (zh) 2002-12-05 2004-06-23 �й�ҽѧ��ѧԺҩ���о��� 新的香豆素酰胺衍生物及其制法和其药物组合物与用途
US7618940B2 (en) 2002-12-06 2009-11-17 Fibrogen, Inc. Fat regulation
US8124582B2 (en) 2002-12-06 2012-02-28 Fibrogen, Inc. Treatment of diabetes
US8614204B2 (en) 2003-06-06 2013-12-24 Fibrogen, Inc. Enhanced erythropoiesis and iron metabolism
CN102718708A (zh) 2003-06-06 2012-10-10 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
US20060251638A1 (en) 2003-06-06 2006-11-09 Volkmar Guenzler-Pukall Cytoprotection through the use of hif hydroxylase inhibitors
CA2532064A1 (en) 2003-07-15 2005-02-03 Merck & Co., Inc. Hydroxypyridine cgrp receptor antagonists
WO2005011696A1 (en) 2003-08-01 2005-02-10 Fibrogen, Inc. Inhibitors of 2-oxoglutarate dioxygenase as gamma globin inducers
US7208601B2 (en) 2003-08-08 2007-04-24 Mjalli Adnan M M Aryl and heteroaryl compounds, compositions, and methods of use
JP2007501844A (ja) 2003-08-08 2007-02-01 トランス テック ファーマ,インコーポレイテッド アリール及びヘテロアリール化合物、組成物並びに使用方法
US7304168B2 (en) 2003-08-14 2007-12-04 Board Of Regents, University Of Texas System Photo-caged fluorescent molecules
EP1720839A1 (en) 2004-02-10 2006-11-15 Janssen Pharmaceutica N.V. Pyridazinones as antagonists of a4 integrins
WO2006020133A2 (en) 2004-07-15 2006-02-23 Powerprecise Solutions, Inc. One time operating state detecting method and apparatus
EP1676834A1 (en) 2004-12-30 2006-07-05 Sanofi-Aventis Deutschland GmbH Fused bicyclic carboxamide derivates for use as CXCR2 inhibitors in the treatment of inflammation
JP4792048B2 (ja) 2005-03-02 2011-10-12 ファイブロゲン インコーポレイティッド チエノピリジン化合物およびその使用方法
US20060276477A1 (en) 2005-06-06 2006-12-07 Fibrogen, Inc. Treatment method for anemia
CN101242817B (zh) 2005-06-15 2016-08-31 菲布罗根公司 HIF1α调节剂在治疗癌症中的用途
AU2006282888A1 (en) 2005-08-25 2007-03-01 Emory University HIF inhibitors
EP2341140B1 (en) 2005-12-01 2017-07-19 Nuevolution A/S Enzymatic encoding methods for efficient synthesis of large libraries
RU2457204C2 (ru) 2006-01-27 2012-07-27 Файброджен, Инк. Цианоизохинолиновые соединения (варианты), фармацевтическая композиция на их основе, способ ингибирования активности гидроксилазы гипоксия-индуцибельного фактора (hif) и способ лечения и/или профилактики состояния, связанного с hif, и/или состояния, связанного с эритропоэтином, и/или анемии
AU2007234408B2 (en) * 2006-04-04 2011-05-19 Fibrogen, Inc. Pyrrolo- and thiazolo-pyridine compounds as HIF modulators
JP2009537558A (ja) 2006-05-16 2009-10-29 スミスクライン・ビーチャム・コーポレイション プロリルヒドロキシラーゼ阻害剤
US20070293575A1 (en) 2006-06-15 2007-12-20 Fibrogen, Inc. Compounds and methods for treatment of cancer-related anemia
US7713986B2 (en) 2006-06-15 2010-05-11 Fibrogen, Inc. Compounds and methods for treatment of chemotherapy-induced anemia
AR061570A1 (es) 2006-06-23 2008-09-03 Smithkline Beecham Corp Compuesto de glicina sustituido en el n heteroaromatico composicion farmaceutica que lo comprende, su uso para preparar un medicamento, procedimientos para preparar dicha composicion farmaceutica y para preparar el compuesto
CA2672656C (en) * 2006-12-18 2012-03-20 Amgen Inc. Naphthalenone compounds exhibiting prolyl hydroxylase inhibitory activity, compositions, and uses thereof
ES2393326T3 (es) 2006-12-18 2012-12-20 Amgen, Inc Compuestos basados en azaquinolona que presentan actividad inhibidora de prolil hidroxilasas, composiciones y usos de los mismos
CL2008000065A1 (es) 2007-01-12 2008-09-22 Smithkline Beecham Corp Compuestos derivados de glicina n-sustituida, inhibidores de hif prolil hidroxilasas; su proceso de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso en el tratamiento de la anemia.
TW200845991A (en) 2007-01-12 2008-12-01 Smithkline Beecham Corp N-substituted glycine derivatives: hydroxylase inhibitors
CN101663037A (zh) * 2007-04-18 2010-03-03 默克公司 新的1,8-二氮杂萘化合物
EP2155680B1 (en) 2007-04-18 2013-12-04 Amgen, Inc Indanone derivatives that inhibit prolyl hydroxylase
CA2683956C (en) * 2007-04-18 2012-12-18 Amgen Inc. Quinolones and azaquinolones that inhibit prolyl hydroxylase
EP2150251B9 (en) 2007-05-04 2013-02-27 Amgen, Inc Thienopyridine and thiazolopyridine derivatives that inhibit prolyl hydroxylase activity
AU2008248165B2 (en) 2007-05-04 2011-12-08 Amgen Inc. Diazaquinolones that inhibit prolyl hydroxylase activity
WO2009039322A1 (en) 2007-09-19 2009-03-26 Smithkline Beecham Corporation Prolyl hydroxylase inhibitors
WO2009039323A1 (en) 2007-09-19 2009-03-26 Smithkline Beecham Corporation Prolyl hydroxylase inhibitors
WO2009039321A1 (en) 2007-09-19 2009-03-26 Smithkline Beecham Corporation Prolyl hydroxylase inhibitors
WO2009049112A1 (en) 2007-10-10 2009-04-16 Smithkline Beecham Corporation Prolyl hydroxylase inhibitors
CN101932324A (zh) 2007-11-30 2010-12-29 葛兰素史密斯克莱有限责任公司 脯氨酰羟化酶抑制剂
EP2227770A4 (en) 2007-11-30 2011-11-09 Glaxosmithkline Llc PROLYLHYDROXYLASEINHIBITOREN
US8269008B2 (en) 2007-12-03 2012-09-18 Fibrogen, Inc. Oxazolopyridine and isoxazolopyridine derivatives for use in the treatment of HIF-mediated conditions
WO2009075822A1 (en) 2007-12-07 2009-06-18 Fibrogen, Inc. Methods for inhibiting t helper cell differentiation
WO2009086044A1 (en) 2007-12-19 2009-07-09 Smith Kline Beecham Corporation Prolyl hydroxylase inhibitors
US8952160B2 (en) 2008-01-11 2015-02-10 Fibrogen, Inc. Isothiazole-pyridine derivatives as modulators of HIF (hypoxia inducible factor) activity
US8324405B2 (en) 2008-02-05 2012-12-04 Fibrogen, Inc. Chromene derivatives and use thereof as HIF hydroxylase activity inhibitors
EP2334682B1 (en) 2008-08-20 2017-10-04 Fibrogen, Inc. Pyrrolo [ 1, 2 -b] pyridazine derivatives and their use as hif modulators
CN105037323A (zh) 2008-11-14 2015-11-11 菲布罗根有限公司 作为hif羟化酶抑制剂的苯并噻喃衍生物
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
JP6129217B2 (ja) 2012-03-09 2017-05-17 フィブロジェン インコーポレイテッド Hifヒドロキシラーゼインヒビターとしての4−ヒドロキシ−イソキノリン化合物
ES2631655T3 (es) 2012-07-16 2017-09-01 Fibrogen, Inc. Procedimiento para fabricar compuestos de isoquinolina
US8883823B2 (en) 2012-07-16 2014-11-11 Fibrogen, Inc. Crystalline forms of a prolyl hydroxylase inhibitor
KR20220164068A (ko) 2012-07-16 2022-12-12 피브로겐, 인크. 프롤릴 하이드록실라제 억제제 [(4-하이드록시-1-메틸-7-페녹시-아이소퀴놀린-3-카보닐)-아미노]-아세트산의 결정형
DK2951159T3 (en) 2013-01-24 2018-11-19 Fibrogen Inc CRYSTALLIC FORMS OF {[1-CYANO-5- (4-CHLORPHENOXY) -4-HYDROXY-ISOQUINOLIN-3-CARBONYL] -AMINO} ACETIC ACID
LT3003284T (lt) 2013-06-06 2020-04-27 Fibrogen, Inc. Hif hidroksilazės inhibitoriaus farmacinės kompozicijos

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN85103105A (zh) * 1984-04-12 1986-10-22 里昂利发制药厂 羟基-4-2h-1-苯并噻喃-2-酮衍生物的制备方法
JPH10279575A (ja) * 1997-03-31 1998-10-20 Fuji Photo Film Co Ltd ベンゾピラン化合物の製造方法
WO2007038571A2 (en) * 2005-09-26 2007-04-05 Smithkline Beecham Corporation Prolyl hydroxylase antagonists
US20070249605A1 (en) * 2005-12-09 2007-10-25 Allen Jennifer R Quinolone based compounds exhibiting prolyl hydroxylase inhibitory activity, and compositions, and uses thereof
WO2007103905A2 (en) * 2006-03-07 2007-09-13 Smithkline Beecham Corporation Prolyl hydroxylase inhibitors
WO2009075826A1 (en) * 2007-12-07 2009-06-18 Fibrogen, Inc. Methods for increasing white blood cells

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
GEORGE A. PATANI AND EDMOND J. LAVOIE: "Bioisosterism: A Rational Approach in Drug Design", 《CHEM. REV.》 *

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