CA2783209C - Amino-heteroaryl derivatives as hcn blockers - Google Patents

Amino-heteroaryl derivatives as hcn blockers Download PDF

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Publication number
CA2783209C
CA2783209C CA2783209A CA2783209A CA2783209C CA 2783209 C CA2783209 C CA 2783209C CA 2783209 A CA2783209 A CA 2783209A CA 2783209 A CA2783209 A CA 2783209A CA 2783209 C CA2783209 C CA 2783209C
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CA
Canada
Prior art keywords
formula
alkyl
pyrimidin
ethyl
amine
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CA2783209A
Other languages
English (en)
French (fr)
Other versions
CA2783209A1 (en
Inventor
Simon James Anthony Grove
Angus John Morrison
Craig Jamieson
Ronald Palin
John Kinnaird Ferguson Maclean
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme BV
Original Assignee
Merck Sharp and Dohme BV
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
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Publication of CA2783209A1 publication Critical patent/CA2783209A1/en
Application granted granted Critical
Publication of CA2783209C publication Critical patent/CA2783209C/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61P25/04Centrally 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
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/73Unsubstituted amino or imino radicals
    • 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Addiction (AREA)
  • Molecular Biology (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CA2783209A 2009-12-22 2010-12-20 Amino-heteroaryl derivatives as hcn blockers Expired - Fee Related CA2783209C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US28918209P 2009-12-22 2009-12-22
EP09180321 2009-12-22
US61/289,182 2009-12-22
EP09180321.3 2009-12-22
PCT/EP2010/070213 WO2011076723A1 (en) 2009-12-22 2010-12-20 Amino-heteroaryl derivatives as hcn blockers

Publications (2)

Publication Number Publication Date
CA2783209A1 CA2783209A1 (en) 2011-06-30
CA2783209C true CA2783209C (en) 2017-03-14

Family

ID=42045216

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2783209A Expired - Fee Related CA2783209C (en) 2009-12-22 2010-12-20 Amino-heteroaryl derivatives as hcn blockers

Country Status (12)

Country Link
US (1) US8952001B2 (enExample)
EP (1) EP2516397B1 (enExample)
JP (1) JP5728024B2 (enExample)
KR (1) KR20120095481A (enExample)
CN (1) CN102884048B (enExample)
AR (1) AR079543A1 (enExample)
AU (1) AU2010335231C1 (enExample)
BR (1) BR112012015170A8 (enExample)
CA (1) CA2783209C (enExample)
MX (1) MX2012007426A (enExample)
RU (1) RU2549546C2 (enExample)
WO (1) WO2011076723A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103442829B (zh) * 2011-05-19 2016-11-16 株式会社东芝 钼造粒粉的制造方法及钼造粒粉
PT2753606T (pt) 2011-09-02 2017-10-02 Purdue Pharma Lp Pirimidinas como bloqueadoras dos canais de sódio
WO2013072758A1 (en) 2011-11-15 2013-05-23 Purdue Pharma L.P. Pyrimidine diol amides as sodium channel blockers
BR112014028006A2 (pt) * 2012-05-30 2017-06-27 Hoffmann La Roche heterociclos de pirrolidino
CN106588803A (zh) * 2016-11-16 2017-04-26 西南科技大学 一种制备5‑乙酰基异噁唑的新方法

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4606757A (en) * 1982-12-23 1986-08-19 The Dow Chemical Company Diphenoxymethylpyridines having herbicidal properties
KR100197583B1 (ko) 1997-02-04 1999-06-15 이민화 환자용모니터를 구비한 초음파진단장치
EP1297136A2 (en) 2000-05-24 2003-04-02 Akzo Nobel N.V. Full length human hcn1 ih channel subunit and variants
EP1378237A4 (en) * 2001-04-10 2009-03-25 Nippon Shinyaku Co Ltd THERAPEUTIC AGENT FOR CHRONIC JOINT RHEUMATISM
US6980419B2 (en) 2003-03-12 2005-12-27 Zonare Medical Systems, Inc. Portable ultrasound unit and docking station
WO2006030378A1 (en) 2004-09-17 2006-03-23 Koninklijke Philips Electronics, N.V. Wireless ultrasound system display
US20070135437A1 (en) * 2005-03-04 2007-06-14 Alsgen, Inc. Modulation of neurodegenerative diseases
WO2008058341A1 (en) * 2006-11-15 2008-05-22 Cytopia Research Pty Ltd Inhibitors of kinase activity
WO2009077608A1 (en) * 2007-12-19 2009-06-25 Palau Pharma, S. A. 2 -aminopyrimidine derivatives as histamine h4 antagonists
CN102245573B (zh) * 2008-02-28 2013-11-20 沃泰克斯药物股份有限公司 作为cftr调节剂的杂芳基衍生物
TW201022233A (en) 2008-11-04 2010-06-16 Organon Nv (Pyrrolidin-2-yl)phenyl derivatives

Also Published As

Publication number Publication date
US20120264728A1 (en) 2012-10-18
CA2783209A1 (en) 2011-06-30
AU2010335231A1 (en) 2012-06-21
BR112012015170A8 (pt) 2017-12-26
CN102884048B (zh) 2014-07-23
KR20120095481A (ko) 2012-08-28
AU2010335231C1 (en) 2015-04-16
RU2012131279A (ru) 2014-01-27
CN102884048A (zh) 2013-01-16
EP2516397A1 (en) 2012-10-31
MX2012007426A (es) 2012-07-23
AU2010335231B2 (en) 2014-09-11
BR112012015170A2 (pt) 2016-03-29
WO2011076723A1 (en) 2011-06-30
RU2549546C2 (ru) 2015-04-27
JP2013515031A (ja) 2013-05-02
JP5728024B2 (ja) 2015-06-03
EP2516397B1 (en) 2016-07-13
AR079543A1 (es) 2012-02-01
US8952001B2 (en) 2015-02-10

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Effective date: 20151211

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Effective date: 20210831

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Effective date: 20191220