AU2006226084B2 - 2,3-substituted fused pyrimidin-4(3H)-ones as VR1 antagonists - Google Patents

2,3-substituted fused pyrimidin-4(3H)-ones as VR1 antagonists Download PDF

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Publication number
AU2006226084B2
AU2006226084B2 AU2006226084A AU2006226084A AU2006226084B2 AU 2006226084 B2 AU2006226084 B2 AU 2006226084B2 AU 2006226084 A AU2006226084 A AU 2006226084A AU 2006226084 A AU2006226084 A AU 2006226084A AU 2006226084 B2 AU2006226084 B2 AU 2006226084B2
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Prior art keywords
pain
alkyl
membered heteroaromatic
alkoxy
heteroaromatic ring
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Ceased
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AU2006226084A
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AU2006226084A1 (en
Inventor
Tracy Bayliss
Rebecca Elizabeth Brown
Gregory John Hollingworth
A. Brian Jones
Christopher Richard Moyes
Lauren Rogers
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Organon Pharma UK Ltd
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Merck Sharp and Dohme Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/18Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
    • 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
    • A61P1/04Drugs 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
    • 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
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary 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
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
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    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
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    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P27/00Drugs for disorders of the senses
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    • A61P27/16Otologicals
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
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    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Nutrition Science (AREA)
  • Ophthalmology & Optometry (AREA)
  • Transplantation (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU2006226084A 2005-03-24 2006-03-21 2,3-substituted fused pyrimidin-4(3H)-ones as VR1 antagonists Ceased AU2006226084B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB0506147.8A GB0506147D0 (en) 2005-03-24 2005-03-24 Therapeutic agents
GB0506147.8 2005-03-24
PCT/GB2006/050060 WO2006100520A1 (en) 2005-03-24 2006-03-21 2,3-substituted fused pyrimidin-4(3h)-ones as vr1 antagonists

Publications (2)

Publication Number Publication Date
AU2006226084A1 AU2006226084A1 (en) 2006-09-28
AU2006226084B2 true AU2006226084B2 (en) 2011-09-08

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AU2006226084A Ceased AU2006226084B2 (en) 2005-03-24 2006-03-21 2,3-substituted fused pyrimidin-4(3H)-ones as VR1 antagonists

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US (1) US20110152242A1 (enExample)
EP (1) EP1866310B1 (enExample)
JP (1) JP5097696B2 (enExample)
AU (1) AU2006226084B2 (enExample)
CA (1) CA2602395A1 (enExample)
GB (1) GB0506147D0 (enExample)
WO (1) WO2006100520A1 (enExample)

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LT2420498T (lt) 2006-09-26 2017-10-25 Celgene Corporation 5-pakeistieji chinazolinono dariniai, kaip priešvėžiniai agentai
AU2007325940A1 (en) * 2006-11-06 2008-06-05 Neurogen Corporation Cis-cyclohexyl substituted pyrimidinone derivatives
JP5313909B2 (ja) * 2006-11-13 2013-10-09 アイコス コーポレイション 炎症性疾患および癌の処置のためのチエノピリミジノン
US7803940B2 (en) 2006-11-24 2010-09-28 Takeda Pharmaceutical Company Limited Heteromonocyclic compound or a salt thereof having strong antihypertensive action, insulin sensitizing activity and the like production thereof and use thereof for prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases
CN101925575B (zh) 2008-01-28 2014-06-18 株式会社爱茉莉太平洋 作为香草酸受体拮抗剂的化合物、其异构体或其药物学可接受的盐、及包含这些化合物的药物组合物
EP2307394B1 (en) 2008-07-02 2012-09-26 Amorepacific Corporation Sulphonamides as vanilloid receptor antagonist
US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
EP2435046B1 (en) * 2009-05-28 2013-09-04 Otsuka Pharmaceutical Co., Ltd. Heterocyclic compounds for the treatment of stress-related conditions
AR080055A1 (es) 2010-02-01 2012-03-07 Novartis Ag Derivados de pirazolo-[5,1-b]-oxazol como antagonistas de los receptores de crf -1
WO2011092293A2 (en) 2010-02-01 2011-08-04 Novartis Ag Cyclohexyl amide derivatives as crf receptor antagonists
ES2527849T3 (es) 2010-02-02 2015-01-30 Novartis Ag Derivados de ciclohexilamida como antagonistas del receptor de CRF
US11466017B2 (en) 2011-03-10 2022-10-11 Board Of Regents, The University Of Texas System Heterocyclic inhibitors of PTPN11
RS56770B1 (sr) 2011-03-11 2018-04-30 Celgene Corp Čvrste forme 3-(5-amino-2-metil-4-okso-4h-hinazolin-3-il)-piperidin-2,6-diona i njihove farmaceutske smeše i upotrebe
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
CN104755472A (zh) 2012-09-04 2015-07-01 细胞基因公司 3-(5-氨基-2-甲基-4-氧代喹唑啉-3(4h)-基)哌啶-2,6-二酮的同位素体及其制备方法
PE20160685A1 (es) 2013-10-04 2016-07-23 Infinity Pharmaceuticals Inc Compuestos heterociclicos y usos de los mismos
US9751888B2 (en) 2013-10-04 2017-09-05 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
SG10201808053XA (en) 2014-03-19 2018-10-30 Infinity Pharmaceuticals Inc Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders
US9708348B2 (en) 2014-10-03 2017-07-18 Infinity Pharmaceuticals, Inc. Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof
HK1255034A1 (zh) 2015-07-01 2019-08-02 Crinetics Pharmaceuticals, Inc. 生长抑素调节剂及其用途
US10160761B2 (en) 2015-09-14 2018-12-25 Infinity Pharmaceuticals, Inc. Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same
DE102015012049A1 (de) * 2015-09-15 2017-03-16 Merck Patent Gmbh Verbindungen als ASIC-Inhibitoren und deren Verwendungen
WO2017156397A1 (en) * 2016-03-11 2017-09-14 Board Of Regents, The University Of Texas Sysytem Heterocyclic inhibitors of ptpn11
WO2017161116A1 (en) 2016-03-17 2017-09-21 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as pi3k kinase inhibitors
JP7044375B2 (ja) 2016-05-31 2022-03-30 ボード オブ リージェンツ,ザ ユニバーシティ オブ テキサス システム Ptpn11の複素環式阻害剤
US10919914B2 (en) 2016-06-08 2021-02-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
EP3658560A4 (en) 2017-07-25 2021-01-06 Crinetics Pharmaceuticals, Inc. SOMATOSTAT IN MODULATORS AND USES THEREOF
JP7297871B2 (ja) 2018-05-02 2023-06-26 ナビール ファーマ,インコーポレイティド Ptpn11の置換されたヘテロ環式インヒビター
WO2020033828A1 (en) 2018-08-10 2020-02-13 Board Of Regents, The University Of Texas System 6-(4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-3-(2,3-dichlorophenyl)-2-methylpyrimidin-4(3h)-one derivatives and related compounds as ptpn11 (shp2) inhibitors for treating cancer

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Also Published As

Publication number Publication date
EP1866310B1 (en) 2012-07-11
GB0506147D0 (en) 2005-05-04
WO2006100520A1 (en) 2006-09-28
JP2008534486A (ja) 2008-08-28
EP1866310A1 (en) 2007-12-19
US20110152242A1 (en) 2011-06-23
AU2006226084A1 (en) 2006-09-28
CA2602395A1 (en) 2006-09-28
JP5097696B2 (ja) 2012-12-12

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