AU2011289230B2 - 4 - aminoquinazolin- 2 - yl - 1 - pyrrazole - 4 - carboxylic acid compounds as prolyl hydroxylase inhibitors - Google Patents

4 - aminoquinazolin- 2 - yl - 1 - pyrrazole - 4 - carboxylic acid compounds as prolyl hydroxylase inhibitors Download PDF

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Publication number
AU2011289230B2
AU2011289230B2 AU2011289230A AU2011289230A AU2011289230B2 AU 2011289230 B2 AU2011289230 B2 AU 2011289230B2 AU 2011289230 A AU2011289230 A AU 2011289230A AU 2011289230 A AU2011289230 A AU 2011289230A AU 2011289230 B2 AU2011289230 B2 AU 2011289230B2
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Australia
Prior art keywords
pyrazole
carboxylic acid
quinazolin
amino
alkyl
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Ceased
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AU2011289230A
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AU2011289230A1 (en
Inventor
Michael H. Rabinowitz
Mark D. Rosen
Kyle T. Tarantino
Hariharan Venkatesan
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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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
    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2011289230A 2010-08-13 2011-08-12 4 - aminoquinazolin- 2 - yl - 1 - pyrrazole - 4 - carboxylic acid compounds as prolyl hydroxylase inhibitors Ceased AU2011289230B2 (en)

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

Publications (2)

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AU2011289230A1 AU2011289230A1 (en) 2013-02-21
AU2011289230B2 true AU2011289230B2 (en) 2014-09-04

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AU2011289230A Ceased AU2011289230B2 (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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Country Link
US (5) US8796263B2 (enExample)
EP (1) EP2603502B1 (enExample)
JP (1) JP5755741B2 (enExample)
CN (1) CN103068821B (enExample)
AU (1) AU2011289230B2 (enExample)
WO (1) WO2012021830A1 (enExample)

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EP2484678B1 (en) 2009-09-28 2015-01-21 Qilu Pharmaceutical Co., Ltd 4-(substituted anilino)quinazoline derivatives as tyrosine kinase inhibitors
EP2603502B1 (en) * 2010-08-13 2014-07-30 Janssen Pharmaceutica, N.V. 4-aminoquinazolin-2-yl-1-pyrrazole-4-carboxylic acid compounds as prolyl hydroxylase inhibitors
ES2818977T3 (es) 2011-10-25 2021-04-14 Janssen Pharmaceutica Nv Método para obtener cristales de sal de meglumina de ácido 1-(5,6-dicloro-1H-benzo[d]imidazol-2-il)-1H-pirazol-4-carboxílico
CA2959688C (en) 2014-09-02 2024-02-27 Sunshine Lake Pharma Co., Ltd. Quinolone compounds and their use to treat diseases related to hypoxia inducible factor and/or erythropoietin
EP3380469B1 (en) * 2015-11-25 2022-03-16 Convergene Llc Bicyclic bet bromodomain inhibitors and uses thereof
CN115243687A (zh) * 2019-10-25 2022-10-25 默沙东有限责任公司 作为lrrk2抑制剂的n-(杂芳基)喹唑啉-2-胺衍生物、药物组合物及其用途
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
KR20230017204A (ko) * 2020-04-29 2023-02-03 바이오에이지 랩스, 인코포레이티드 노화-관련 질환 치료용 저산소증-유도 인자 프롤릴 히드록실라제 억제제
WO2022033420A1 (zh) * 2020-08-14 2022-02-17 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
CN114075175B (zh) * 2020-08-14 2026-06-26 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

Citations (1)

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WO2010020422A1 (de) * 2008-08-22 2010-02-25 Inventus Engineering Gmbh Bewegung dämpfende vorrichtung

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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
CN101849943A (zh) 2005-06-06 2010-10-06 菲布罗根公司 使用HIFα稳定剂的改进的贫血治疗
AU2006326662B2 (en) 2005-12-09 2011-07-28 Amgen Inc. Quinolone based compounds exhibiting prolyl hydroxylase inhibitory activity, and compositions, and uses thereof
PE20071020A1 (es) 2006-03-07 2007-12-11 Smithkline Beecham Corp Compuestos derivados de glicina n-sustituidos como inhibidores de prolil hidroxilasa
TWI394747B (zh) 2006-06-23 2013-05-01 Smithkline Beecham Corp 脯胺醯基羥化酶抑制劑
NZ623002A (en) 2006-06-26 2015-08-28 Akebia Therapeutics Inc Prolyl hydroxylase inhibitors and methods of use
DE102006050513A1 (de) * 2006-10-26 2008-04-30 Bayer Healthcare Ag Substitiuierte Dihydropyrazolone und ihre Verwendung
AU2009225869B2 (en) 2008-03-18 2014-01-23 Merck Sharp & Dohme Llc Substituted 4-hydroxypyrimidine-5-carboxamides
JP5643233B2 (ja) * 2009-02-10 2014-12-17 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプＪａｎｓｓｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａ Ｎａａｍｌｏｚｅ Ｖｅｎｎｏｏｔｓｃｈａｐ プロリルヒドロキシラーゼ阻害物質としてのキナゾリノン
EP2603502B1 (en) * 2010-08-13 2014-07-30 Janssen Pharmaceutica, N.V. 4-aminoquinazolin-2-yl-1-pyrrazole-4-carboxylic acid compounds as prolyl hydroxylase inhibitors

Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
WO2010020422A1 (de) * 2008-08-22 2010-02-25 Inventus Engineering Gmbh Bewegung dämpfende vorrichtung

Also Published As

Publication number Publication date
US10975062B2 (en) 2021-04-13
US20140309215A1 (en) 2014-10-16
AU2011289230A1 (en) 2013-02-21
JP5755741B2 (ja) 2015-07-29
US20170320859A1 (en) 2017-11-09
EP2603502B1 (en) 2014-07-30
HK1184451A1 (en) 2014-01-24
US8796263B2 (en) 2014-08-05
US9573940B2 (en) 2017-02-21
US20150197507A1 (en) 2015-07-16
CN103068821A (zh) 2013-04-24
US20180148435A9 (en) 2018-05-31
CN103068821B (zh) 2015-02-25
US20130143871A1 (en) 2013-06-06
US10246442B2 (en) 2019-04-02
EP2603502A1 (en) 2013-06-19
US9006251B2 (en) 2015-04-14
US20200095234A1 (en) 2020-03-26
WO2012021830A1 (en) 2012-02-16
JP2013536194A (ja) 2013-09-19

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