WO2005047279A8 - Substituted nitrogen-containing six-membered amino-heterocycles as vanilloid-1 receptor antagonists for treating pain - Google Patents

Substituted nitrogen-containing six-membered amino-heterocycles as vanilloid-1 receptor antagonists for treating pain

Info

Publication number
WO2005047279A8
WO2005047279A8 PCT/GB2004/004719 GB2004004719W WO2005047279A8 WO 2005047279 A8 WO2005047279 A8 WO 2005047279A8 GB 2004004719 W GB2004004719 W GB 2004004719W WO 2005047279 A8 WO2005047279 A8 WO 2005047279A8
Authority
WO
WIPO (PCT)
Prior art keywords
4alkyl
haloc1
4alkoxy
optionally substituted
nitro
Prior art date
Application number
PCT/GB2004/004719
Other languages
French (fr)
Other versions
WO2005047279A1 (en
Inventor
Gregory John Hollingworth
A Brian Jones
Edward Giles Mciver
Christopher Richard Moyes
Lauren Rogers
Original Assignee
Merck Sharp & Dohme
Gregory John Hollingworth
A Brian Jones
Edward Giles Mciver
Christopher Richard Moyes
Lauren Rogers
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GB0326217A external-priority patent/GB0326217D0/en
Priority claimed from GB0407748A external-priority patent/GB0407748D0/en
Application filed by Merck Sharp & Dohme, Gregory John Hollingworth, A Brian Jones, Edward Giles Mciver, Christopher Richard Moyes, Lauren Rogers filed Critical Merck Sharp & Dohme
Priority to EP04798442A priority Critical patent/EP1685124A1/en
Priority to AU2004289518A priority patent/AU2004289518A1/en
Priority to CA002545384A priority patent/CA2545384A1/en
Priority to JP2006538935A priority patent/JP2007510706A/en
Publication of WO2005047279A1 publication Critical patent/WO2005047279A1/en
Publication of WO2005047279A8 publication Critical patent/WO2005047279A8/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/14Antitussive agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (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)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The present invention provides a compound of formula (I): Y-J-NH-Z wherein: Y is a quinoline or isoquinoline optionally substituted with one or two substituents independently chosen from hydroxy, halogen, haloC1-4alkyl, C1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, nitro and amino; J is pyridine, pyridazine, pyrazine, pyrimidine or triazine optionally substituted with one or two substituents independently chosen from hydroxy, halogen, haloC1-4alkyl, C1-4alkyl, C3-5cycloalkyl, C1-4alkoxy, hydroxyC1- 4alkyl, cyano, hydroxy, C1-4cycloalkoxy, C1-4alkylthio, haloC1-4alkoxy, nitro, Q, (CH2)pQ, NR2R3, -(CH2)pNR2R3 and -O(CH2)pNR2R3; wherein J is substituted at positions meta to each other by NH and Y; and Z is phenyl or pyridyl optionally substituted with one or two substituents independently selected from halogen, haloC1-4alkyl, C1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, nitro and amino; Q is phenyl, a five-membered heterocyclic ring containing one, two, three or four heteroatoms chosen from O, N and S, at most one heteroatom being O or S, or a six-membered heterocyclic ring containing one, two or three nitrogen atoms, optionally substituted by C1-4alkyl; each R2 and R3 is chosen from H and C1-4alkyl, or R2 and R3, together with the nitrogen atom to which they are attached, may form a six-membered ring optionally containing an oxygen atom or a further nitrogen atom, which ring is optionally substituted by C1-4alkyl or Q; p is 1, 2 or 3; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in methods of therapy; use of it for manufacturing medicaments; and methods of using it to treat diseases requiring administration of a VR1 antagonist such as pain, cough, GERD and depression.
PCT/GB2004/004719 2003-11-10 2004-11-09 Substituted nitrogen-containing six-membered amino-heterocycles as vanilloid-1 receptor antagonists for treating pain WO2005047279A1 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
EP04798442A EP1685124A1 (en) 2003-11-10 2004-11-09 Substituted nitrogen-containing six-membered amino-heterocycles as vanilloid-1 receptor antagonists for treating pain
AU2004289518A AU2004289518A1 (en) 2003-11-10 2004-11-09 Substituted nitrogen-containing six-membered amino-heterocycles as vanilloid-1 receptor antagonists for treating pain
CA002545384A CA2545384A1 (en) 2003-11-10 2004-11-09 Substituted nitrogen-containing six-membered amino-heterocycles as vanilloid-1 receptor antagonists for treating pain
JP2006538935A JP2007510706A (en) 2003-11-10 2004-11-09 Substituted nitrogen-containing six-membered amino heterocycles as vanilloid-1 receptor antagonists for the treatment of pain

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
GB0326217.7 2003-11-10
GB0326217A GB0326217D0 (en) 2003-11-10 2003-11-10 Therapeutic agents
GB0407748.3 2004-04-05
GB0407748A GB0407748D0 (en) 2004-04-05 2004-04-05 Therapeutic agents
US61713404P 2004-10-08 2004-10-08
US60/617,134 2004-10-08

Publications (2)

Publication Number Publication Date
WO2005047279A1 WO2005047279A1 (en) 2005-05-26
WO2005047279A8 true WO2005047279A8 (en) 2006-08-10

Family

ID=34595632

Family Applications (2)

Application Number Title Priority Date Filing Date
PCT/GB2004/004719 WO2005047279A1 (en) 2003-11-10 2004-11-09 Substituted nitrogen-containing six-membered amino-heterocycles as vanilloid-1 receptor antagonists for treating pain
PCT/GB2004/004730 WO2005047280A1 (en) 2003-11-10 2004-11-09 Substituted nitrogen-containing six-membered amino-heterocycles as vanilloid-1 receptor antagonists for treating pain

Family Applications After (1)

Application Number Title Priority Date Filing Date
PCT/GB2004/004730 WO2005047280A1 (en) 2003-11-10 2004-11-09 Substituted nitrogen-containing six-membered amino-heterocycles as vanilloid-1 receptor antagonists for treating pain

Country Status (6)

Country Link
EP (1) EP1685124A1 (en)
JP (1) JP2007510706A (en)
AU (1) AU2004289518A1 (en)
CA (1) CA2545384A1 (en)
TW (1) TW200526196A (en)
WO (2) WO2005047279A1 (en)

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US20050014753A1 (en) * 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
CA2551944A1 (en) * 2003-12-15 2005-06-30 Almirall Prodesfarma Ag 2, 6 bisheteroaryl-4-aminopyrimidines as adenosine receptor antagonists
WO2006089311A1 (en) * 2005-02-15 2006-08-24 Amgen Inc. Vanilloid receptor ligands and their use in treatments
CA2682504C (en) 2007-04-05 2012-10-30 Amgen Inc. Aurora kinase modulators and method of use
EP2238105B1 (en) 2008-01-28 2014-04-16 Amorepacific Corporation Novel compounds as vanilloid receptor antagonists
JP2011515401A (en) 2008-03-20 2011-05-19 アムジエン・インコーポレーテツド Aurora kinase modulator and methods of use
CA2719515C (en) 2008-04-18 2013-11-05 Daewoong Pharmaceutical Co., Ltd. A novel benzoxazine benzimidazole derivative, a pharmaceutical composition comprising the same, and a use thereof
CA2723961C (en) 2008-05-21 2017-03-21 Ariad Pharmaceuticals, Inc. Phosphorous derivatives as kinase inhibitors
JP5438103B2 (en) 2008-07-02 2014-03-12 アモーレパシフィック コーポレイション Novel compounds as vanilloid receptor antagonists, isomers or pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing the same
US9126935B2 (en) 2008-08-14 2015-09-08 Amgen Inc. Aurora kinase modulators and methods of use
JO2885B1 (en) 2008-12-22 2015-03-15 ايلي ليلي اند كومباني Protein kinase inhibitors
AR075858A1 (en) 2009-03-18 2011-05-04 Schering Corp BICYCLE COMPOUNDS AS INHIBITORS OF DIACILGLICEROL ACILTRANSFERASA
WO2011017296A1 (en) * 2009-08-04 2011-02-10 Schering Corporation 4, 5, 6-trisubstituted pyrimidine derivatives as factor ixa inhibitors
KR101293384B1 (en) 2010-10-13 2013-08-05 주식회사 대웅제약 Novel pyridyl benzoxazine derivatives, pharmaceutical composition comprising the same, and use thereof
EP2518070A1 (en) 2011-04-29 2012-10-31 Almirall, S.A. Pyrrolotriazinone derivatives as PI3K inhibitors
CN102558047B (en) * 2011-12-14 2013-10-30 天津药物研究院药业有限责任公司 Method for preparing 3-methylquinoline
CN102702110A (en) * 2012-05-24 2012-10-03 盛世泰科生物医药技术(苏州)有限公司 Preparation method of 4-amino-5, 6-dichloropyrimidine
UY35421A (en) 2013-03-15 2014-10-31 Nihon Nohyaku Co Ltd CONDENSED HETEROCYCLIC COMPOUND OR ITS SALT, AGRICULTURAL OR HERITAGE INSECTICIDE THAT INCLUDES THE COMPOSITE AND METHOD OF USE OF THE INSECTICIDE
PL3089971T3 (en) * 2014-01-01 2021-01-25 Medivation Technologies Llc Compounds and methods of use
US10202373B2 (en) 2014-01-14 2019-02-12 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
WO2018112843A1 (en) 2016-12-22 2018-06-28 Merck Sharp & Dohme Corp. Heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor
CA3093189A1 (en) 2018-03-07 2019-09-12 Bayer Aktiengesellschaft Identification and use of erk5 inhibitors
US11161838B2 (en) 2018-11-13 2021-11-02 Incyte Corporation Heterocyclic derivatives as PI3K inhibitors
US11396502B2 (en) 2018-11-13 2022-07-26 Incyte Corporation Substituted heterocyclic derivatives as PI3K inhibitors
WO2020102198A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Heterocyclic derivatives as pi3k inhibitors
CN111793022A (en) * 2020-04-27 2020-10-20 滁州拜奥生物科技有限公司 Preparation method of 3-methylquinoline
RU2744470C1 (en) * 2020-09-22 2021-03-09 Федеральное государственное бюджетное образовательное учреждение высшего образования "Волгоградский государственный технический университет" (ВолгГТУ) Method for producing isothiobarbamine

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US2002A (en) 1841-03-12 Tor and planter for plowing
US992374A (en) 1910-07-09 1911-05-16 William Mcguire Automatic block-signal joint.
US4788195A (en) * 1986-01-13 1988-11-29 American Cyanamid Company 4,5,6-substituted-N-(substituted-phenyl)-2-pyrimidinamines
US6723730B2 (en) 2000-07-20 2004-04-20 Neurogen Corporation Capsaicin receptor ligands
CA2486376A1 (en) 2002-05-22 2003-12-04 Amgen Inc. Amino-pyridine, -pyridine and pyridazine derivatives for use as vanilloid receptor ligands for the treatment of pain

Also Published As

Publication number Publication date
JP2007510706A (en) 2007-04-26
WO2005047280A1 (en) 2005-05-26
CA2545384A1 (en) 2005-05-26
EP1685124A1 (en) 2006-08-02
TW200526196A (en) 2005-08-16
AU2004289518A1 (en) 2005-05-26
WO2005047279A1 (en) 2005-05-26

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