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)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (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)

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

Family

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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

Country Status (6)

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)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2535176T3 (es) 2009-09-28 2015-05-06 Qilu Pharmaceutical Co., Ltd Derivados de 4-(anilino sustituido)quinazolina como inhibidores de la tirosina quinasa
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
EP2776023B1 (en) 2011-10-25 2016-03-09 Janssen Pharmaceutica, N.V. Meglumine salt formulations of 1-(5,6-dichloro-1h-benzo[d]imidazol-2-yl)-1h-pyrazole-4-carboxylic acid
CN105384687B (zh) 2014-09-02 2018-05-01 广东东阳光药业有限公司 喹啉酮类化合物及其在药物中应用
EP4050005B1 (en) * 2015-11-25 2024-12-25 Convergene Llc Bicyclic bet bromodomain inhibitors and uses thereof
EP4048261A4 (en) * 2019-10-25 2023-11-22 Merck Sharp & Dohme LLC N-(HETEROARYL)-QUINAZOLINE-2-AMINE DERIVATIVES AS LRRK2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
EP4138825A1 (en) 2020-04-20 2023-03-01 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
WO2021222424A1 (en) * 2020-04-29 2021-11-04 BioAge Labs, Inc. Hypoxia-inducible factor prolyl hydroxylase inhibitors for treating aging-related conditions
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
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
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
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
WO2023064512A1 (en) * 2021-10-13 2023-04-20 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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010020422A1 (de) * 2008-08-22 2010-02-25 Inventus Engineering Gmbh Bewegung dämpfende vorrichtung

Family Cites Families (11)

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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
EP1893186A2 (en) 2005-06-06 2008-03-05 Fibrogen, Inc. Improved treatment for anemia using a hif-alpha stabilising agent
US7728130B2 (en) 2005-12-09 2010-06-01 Amgen Inc. Quinolone based compounds exhibiting prolyl hydroxylase inhibitory activity
TW200808793A (en) 2006-03-07 2008-02-16 Smithkline Beecham Corp Prolyl hydroxylase inhibitors
TWI394747B (zh) 2006-06-23 2013-05-01 Smithkline Beecham Corp 脯胺醯基羥化酶抑制劑
BRPI0713350B1 (pt) 2006-06-26 2022-04-12 Akebia Therapeutics Inc Composto, e, composição
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
AU2010213814B2 (en) 2009-02-10 2015-07-30 Janssen Pharmaceutica Nv Quinazolinones as prolyl hydroxylase 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

Patent Citations (1)

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

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