JP5728024B2 - Ｈｃｎ遮断薬としてのアミノ−ヘテロアリール誘導体 - Google Patents

Ｈｃｎ遮断薬としてのアミノ−ヘテロアリール誘導体 Download PDF

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Publication number
JP5728024B2
JP5728024B2 JP2012545268A JP2012545268A JP5728024B2 JP 5728024 B2 JP5728024 B2 JP 5728024B2 JP 2012545268 A JP2012545268 A JP 2012545268A JP 2012545268 A JP2012545268 A JP 2012545268A JP 5728024 B2 JP5728024 B2 JP 5728024B2
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Prior art keywords
pyrimidin
ethyl
amine
formula
alkyl
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JP2012545268A
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JP2013515031A5 (enExample
JP2013515031A (ja
Inventor
グローブ，シモン・ジエイムス・アンソニー
モリソン，アンガス・ジヨン
ジヤミーソン，クレイグ
パリン，ロナルド
マクリーン，ジヨン・キナード・フエルグソン
Original Assignee
メルク・シャープ・エンド・ドーム・ベー・フェー
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    • 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)
  • 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)
JP2012545268A 2009-12-22 2010-12-20 Ｈｃｎ遮断薬としてのアミノ−ヘテロアリール誘導体 Expired - Fee Related JP5728024B2 (ja)

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 (3)

Publication Number Publication Date
JP2013515031A JP2013515031A (ja) 2013-05-02
JP2013515031A5 JP2013515031A5 (enExample) 2013-09-26
JP5728024B2 true JP5728024B2 (ja) 2015-06-03

Family

ID=42045216

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JP2012545268A Expired - Fee Related JP5728024B2 (ja) 2009-12-22 2010-12-20 Ｈｃｎ遮断薬としてのアミノ−ヘテロアリール誘導体

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
CA2783209C (en) 2017-03-14
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
EP2516397B1 (en) 2016-07-13
AR079543A1 (es) 2012-02-01
US8952001B2 (en) 2015-02-10

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