JP5755741B2 - プロリルヒドロキシラーゼインヒビタとしての４−アミノキナゾリン−２−イル−１−ピラゾール−４−カルボン酸化合物 - Google Patents

プロリルヒドロキシラーゼインヒビタとしての４−アミノキナゾリン−２−イル−１−ピラゾール−４−カルボン酸化合物 Download PDF

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JP5755741B2
JP5755741B2 JP2013524250A JP2013524250A JP5755741B2 JP 5755741 B2 JP5755741 B2 JP 5755741B2 JP 2013524250 A JP2013524250 A JP 2013524250A JP 2013524250 A JP2013524250 A JP 2013524250A JP 5755741 B2 JP5755741 B2 JP 5755741B2
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pyrazole
carboxylic acid
quinazolin
amino
fluoro
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JP2013536194A (ja
JP2013536194A5 (https=
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ラビノウィッツ，マイケル，エイチ．
ローゼン，マーク，ディー．
タランティーノ，カイル，ティー．
ヴェンカテサン，ハリハラン
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ヤンセン ファーマシューティカ エヌ．ベー．
ヤンセン ファーマシューティカ エヌ．ベー．
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
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    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
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    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2013524250A 2010-08-13 2011-08-12 プロリルヒドロキシラーゼインヒビタとしての４−アミノキナゾリン−２−イル−１−ピラゾール−４−カルボン酸化合物 Expired - Fee Related JP5755741B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US37366410P 2010-08-13 2010-08-13
US61/373,664 2010-08-13
PCT/US2011/047626 WO2012021830A1 (en) 2010-08-13 2011-08-12 4 - aminoquinazolin- 2 - yl - 1 - pyrrazole - 4 - carboxylic acid compounds as prolyl hydroxylase inhibitors

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JP2013536194A JP2013536194A (ja) 2013-09-19
JP2013536194A5 JP2013536194A5 (https=) 2014-09-25
JP5755741B2 true JP5755741B2 (ja) 2015-07-29

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JP2013524250A Expired - Fee Related JP5755741B2 (ja) 2010-08-13 2011-08-12 プロリルヒドロキシラーゼインヒビタとしての４−アミノキナゾリン−２−イル−１−ピラゾール−４−カルボン酸化合物

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US (5) US8796263B2 (https=)
EP (1) EP2603502B1 (https=)
JP (1) JP5755741B2 (https=)
CN (1) CN103068821B (https=)
AU (1) AU2011289230B2 (https=)
WO (1) WO2012021830A1 (https=)

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WO2011035540A1 (zh) 2009-09-28 2011-03-31 齐鲁制药有限公司 作为酪氨酸激酶抑制剂的4-（取代苯胺基）喹唑啉衍生物
AU2011289230B2 (en) * 2010-08-13 2014-09-04 Janssen Pharmaceutica Nv 4 - aminoquinazolin- 2 - yl - 1 - pyrrazole - 4 - carboxylic acid compounds as prolyl hydroxylase inhibitors
WO2013063221A1 (en) 2011-10-25 2013-05-02 Janssen Pharmaceutica Nv Meglumine salt formulations of 1-(5,6-dichloro-1h-benzo[d]imidazol-2-yl)-1h-pyrazole-4-carboxylic acid
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
JP6882289B2 (ja) * 2015-11-25 2021-06-02 コンバージーン・リミテッド・ライアビリティ・カンパニーＣｏｎｖｅｒｇｅｎｅ Ｌｌｃ 二環式ｂｅｔブロモドメイン阻害剤及びその使用
BR112022007680A2 (pt) * 2019-10-25 2022-08-09 Merck Sharp & Dohme Derivados de n-(heteroaril)quinazolin-2-amina como inibidores de lrrk2, composições farmacêuticas, e usos dos mesmos
WO2021216530A1 (en) 2020-04-20 2021-10-28 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
EP4142721A1 (en) * 2020-04-29 2023-03-08 Bioage Labs, Inc. Hypoxia-inducible factor prolyl hydroxylase inhibitors for treating aging-related conditions
CN114075175A (zh) * 2020-08-14 2022-02-22 成都海博为药业有限公司 一种作为pak4激酶抑制剂的化合物及其制备方法和应用
CN115943144B (zh) * 2020-08-14 2025-05-13 成都海博为药业有限公司 一种作为pak4激酶抑制剂的化合物及其制备方法和应用
TWI896831B (zh) * 2020-12-31 2025-09-11 大陸商成都海博為藥業有限公司 一種作為ｐａｋ４激酶抑制劑的化合物及其製備方法和應用
WO2022150623A1 (en) 2021-01-08 2022-07-14 Akebia Therapeutics, Inc. Compounds and composition for the treatment of anemia
EP4347022A1 (en) 2021-05-27 2024-04-10 Keryx Biopharmaceuticals, Inc. Pediatric formulations of ferric citrate
US20240415878A1 (en) * 2021-10-13 2024-12-19 Board Of Regents, The University Of Texas System Compositions and Methods for Modulating Mitochondrial Function
US20230183356A1 (en) * 2021-12-14 2023-06-15 Brown University HIF-1a MODULATORS AND USES THEREOF
WO2026015819A1 (en) * 2024-07-12 2026-01-15 The General Hospital Corporation Trdmt1 inhibitors

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US8124582B2 (en) 2002-12-06 2012-02-28 Fibrogen, Inc. Treatment of diabetes
US7618940B2 (en) 2002-12-06 2009-11-17 Fibrogen, Inc. Fat regulation
AU2006254897A1 (en) 2005-06-06 2006-12-14 Fibrogen, Inc. Improved treatment for anemia using a HIF-alpha stabilising agent
EP1960363B1 (en) 2005-12-09 2014-01-22 Amgen, Inc. Quinolone based compounds exhibiting prolyl hydroxylase inhibitory activity, compositions and uses thereof
AR059733A1 (es) 2006-03-07 2008-04-23 Smithkline Beecham Corp Compuesto derivado de glicina n- sustituida con heteroaromaticos bicicicos, composicion farmaceutica que lo comprende, uso para preparar un medicamento para tratar la anemia y proceso para su preparacion
JO2934B1 (en) 2006-06-23 2015-09-15 سميث كلاين بيتشام كوربوريشن Prolyl hydroxylase inhibitors
PL3357911T3 (pl) 2006-06-26 2022-09-05 Akebia Therapeutics Inc. Inhibitory prolilohydroksylazy i sposoby ich użycia
DE102006050513A1 (de) * 2006-10-26 2008-04-30 Bayer Healthcare Ag Substitiuierte Dihydropyrazolone und ihre Verwendung
ES2524883T3 (es) 2008-03-18 2014-12-15 Merck Sharp & Dohme Corp. 4-Hidroxipirimidina-5-carboxamidas sustituidas
CN102171481B (zh) * 2008-08-22 2015-04-08 因文图斯工程有限公司 运动阻尼装置
RU2528412C2 (ru) 2009-02-10 2014-09-20 Янссен Фармацевтика Нв Хиназолиноны как ингибиторы пролилгидроксилазы
AU2011289230B2 (en) * 2010-08-13 2014-09-04 Janssen Pharmaceutica Nv 4 - aminoquinazolin- 2 - yl - 1 - pyrrazole - 4 - carboxylic acid compounds as prolyl hydroxylase inhibitors

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Publication number Publication date
HK1184451A1 (en) 2014-01-24
EP2603502B1 (en) 2014-07-30
US8796263B2 (en) 2014-08-05
CN103068821A (zh) 2013-04-24
JP2013536194A (ja) 2013-09-19
EP2603502A1 (en) 2013-06-19
US20170320859A1 (en) 2017-11-09
US10246442B2 (en) 2019-04-02
US20140309215A1 (en) 2014-10-16
US20130143871A1 (en) 2013-06-06
US20150197507A1 (en) 2015-07-16
AU2011289230B2 (en) 2014-09-04
WO2012021830A1 (en) 2012-02-16
AU2011289230A1 (en) 2013-02-21
US20180148435A9 (en) 2018-05-31
US20200095234A1 (en) 2020-03-26
CN103068821B (zh) 2015-02-25
US9006251B2 (en) 2015-04-14
US9573940B2 (en) 2017-02-21
US10975062B2 (en) 2021-04-13

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