AU2010335231C1 - Amino-heteroaryl derivatives as HCN blockers - Google Patents

Amino-heteroaryl derivatives as HCN blockers Download PDF

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Publication number
AU2010335231C1
AU2010335231C1 AU2010335231A AU2010335231A AU2010335231C1 AU 2010335231 C1 AU2010335231 C1 AU 2010335231C1 AU 2010335231 A AU2010335231 A AU 2010335231A AU 2010335231 A AU2010335231 A AU 2010335231A AU 2010335231 C1 AU2010335231 C1 AU 2010335231C1
Authority
AU
Australia
Prior art keywords
pyrimidin
formula
ethyl
amine
alkyl
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.)
Ceased
Application number
AU2010335231A
Other languages
English (en)
Other versions
AU2010335231A1 (en
AU2010335231B2 (en
Inventor
Simon James Anthony Grove
Craig Jamieson
John Kinnaird Ferguson Maclean
Angus John Morrison
Ronald Palin
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 Ltd
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
Application filed by Merck Sharp and Dohme Ltd, Merck Sharp and Dohme BV filed Critical Merck Sharp and Dohme Ltd
Publication of AU2010335231A1 publication Critical patent/AU2010335231A1/en
Assigned to MERCK SHARP & DOHME B.V. reassignment MERCK SHARP & DOHME B.V. Alteration of Name(s) of Applicant(s) under S113 Assignors: MSD OSS B.V.
Publication of AU2010335231B2 publication Critical patent/AU2010335231B2/en
Application granted granted Critical
Publication of AU2010335231C1 publication Critical patent/AU2010335231C1/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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
    • A61K31/435—Heterocyclic 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
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • A61K31/53—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/12—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 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Addiction (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
  • Molecular Biology (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)
AU2010335231A 2009-12-22 2010-12-20 Amino-heteroaryl derivatives as HCN blockers Ceased AU2010335231C1 (en)

Applications Claiming Priority (5)

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

Publications (3)

Publication Number Publication Date
AU2010335231A1 AU2010335231A1 (en) 2012-06-21
AU2010335231B2 AU2010335231B2 (en) 2014-09-11
AU2010335231C1 true AU2010335231C1 (en) 2015-04-16

Family

ID=42045216

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2010335231A Ceased AU2010335231C1 (en) 2009-12-22 2010-12-20 Amino-heteroaryl derivatives as HCN blockers

Country Status (12)

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

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012157336A1 (ja) * 2011-05-19 2012-11-22 株式会社東芝 モリブデン造粒粉の製造方法およびモリブデン造粒粉
AU2012300567B2 (en) 2011-09-02 2016-03-10 Purdue Pharma L.P. Pyrimidines as sodium channel blockers
WO2013072758A1 (en) 2011-11-15 2013-05-23 Purdue Pharma L.P. Pyrimidine diol amides as sodium channel blockers
MX2014014308A (es) * 2012-05-30 2015-02-12 Hoffmann La Roche Pirrolidino heterociclos.
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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008067389A2 (en) * 2006-11-28 2008-06-05 Alsgen, Inc. Modulation of sod protein synthesis for the treatment of neurodegenerative diseases
US20090221597A1 (en) * 2008-02-28 2009-09-03 Sara Hadida Ruah Heteroaryl derivatives as cftr modulators

Family Cites Families (9)

* 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
WO2001090142A2 (en) 2000-05-24 2001-11-29 Akzo Nobel N.V. FULL LENGTH HUMAN HCN1 Ih CHANNEL SUBUNIT AND VARIANTS
CA2443636C (en) * 2001-04-10 2009-11-17 Nippon Shinyaku Co., Ltd. Remedial agent for chronic articular rheumatism
US6980419B2 (en) 2003-03-12 2005-12-27 Zonare Medical Systems, Inc. Portable ultrasound unit and docking station
US20090182228A1 (en) 2004-09-17 2009-07-16 Koninklijke Philips Electronics, N.V. Wireless ultrasound system display
LT2848610T (lt) * 2006-11-15 2017-11-10 Ym Biosciences Australia Pty Ltd Kinazės aktyvumo inhibitoriai
WO2009077608A1 (en) * 2007-12-19 2009-06-25 Palau Pharma, S. A. 2 -aminopyrimidine derivatives as histamine h4 antagonists
TW201022233A (en) 2008-11-04 2010-06-16 Organon Nv (Pyrrolidin-2-yl)phenyl derivatives

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008067389A2 (en) * 2006-11-28 2008-06-05 Alsgen, Inc. Modulation of sod protein synthesis for the treatment of neurodegenerative diseases
US20090221597A1 (en) * 2008-02-28 2009-09-03 Sara Hadida Ruah Heteroaryl derivatives as cftr modulators

Also Published As

Publication number Publication date
JP5728024B2 (ja) 2015-06-03
RU2549546C2 (ru) 2015-04-27
US20120264728A1 (en) 2012-10-18
MX2012007426A (es) 2012-07-23
RU2012131279A (ru) 2014-01-27
CN102884048B (zh) 2014-07-23
AU2010335231A1 (en) 2012-06-21
EP2516397A1 (en) 2012-10-31
CA2783209A1 (en) 2011-06-30
KR20120095481A (ko) 2012-08-28
WO2011076723A1 (en) 2011-06-30
AU2010335231B2 (en) 2014-09-11
CN102884048A (zh) 2013-01-16
EP2516397B1 (en) 2016-07-13
US8952001B2 (en) 2015-02-10
CA2783209C (en) 2017-03-14
BR112012015170A2 (pt) 2016-03-29
BR112012015170A8 (pt) 2017-12-26
JP2013515031A (ja) 2013-05-02
AR079543A1 (es) 2012-02-01

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DA2 Applications for amendment section 104

Free format text: THE NATURE OF THE AMENDMENT IS AS SHOWN IN THE STATEMENT(S) FILED 15 DEC 2014 .

DA3 Amendments made section 104

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FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired