JP2008526999A - アルツハイマー病治療用ベータ−セクレターゼインヒビターとして活性な置換へテロ環含有三級カルビナミン - Google Patents

アルツハイマー病治療用ベータ−セクレターゼインヒビターとして活性な置換へテロ環含有三級カルビナミン Download PDF

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JP2008526999A
JP2008526999A JP2007551435A JP2007551435A JP2008526999A JP 2008526999 A JP2008526999 A JP 2008526999A JP 2007551435 A JP2007551435 A JP 2007551435A JP 2007551435 A JP2007551435 A JP 2007551435A JP 2008526999 A JP2008526999 A JP 2008526999A
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alkylene
alkyl
group
aryl
heteroaryl
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JP2008526999A5 (enExample
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マクゴギー,ジョージア,ビー
ナンテルメット,フィリップ,ジー
ラジャパクセ,ヘマカ,エイ
シュタウファー,ショーン,アール
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Merck and Co Inc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D271/00Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/101,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
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    • C07D271/00Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/101,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • C07D271/1071,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles with two aryl or substituted aryl radicals attached in positions 2 and 5
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    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07ORGANIC CHEMISTRY
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    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D453/00Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
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    • 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
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    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Medicinal Chemistry (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
JP2007551435A 2005-01-19 2006-01-13 アルツハイマー病治療用ベータ−セクレターゼインヒビターとして活性な置換へテロ環含有三級カルビナミン Pending JP2008526999A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US64492405P 2005-01-19 2005-01-19
US65242105P 2005-02-11 2005-02-11
PCT/US2006/001367 WO2006078577A1 (en) 2005-01-19 2006-01-13 Tertiary carbinamines having substituted heterocycles, which are active as inhibitors of beta-secretase, for the treatment of alzheimer's disease

Publications (2)

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JP2008526999A true JP2008526999A (ja) 2008-07-24
JP2008526999A5 JP2008526999A5 (enExample) 2009-02-19

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US (1) US8338614B2 (enExample)
EP (1) EP1841426B1 (enExample)
JP (1) JP2008526999A (enExample)
AT (1) ATE506951T1 (enExample)
AU (1) AU2006206654A1 (enExample)
CA (1) CA2594946A1 (enExample)
DE (1) DE602006021535D1 (enExample)
WO (1) WO2006078577A1 (enExample)

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WO2010038686A1 (ja) * 2008-09-30 2010-04-08 エーザイ・アール・アンド・ディー・マネジメント株式会社 新規な縮合アミノジヒドロチアジン誘導体
WO2016153023A1 (ja) * 2015-03-25 2016-09-29 国立研究開発法人国立長寿医療研究センター 新規オキサジアゾール誘導体及びこれを含有する医薬

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US8383637B2 (en) 2004-08-06 2013-02-26 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
US8436006B2 (en) 2004-08-06 2013-05-07 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
WO2006078576A2 (en) 2005-01-19 2006-07-27 Merck & Co., Inc. Aminomethyl beta-secretase inhibitors for the treatment of alzheimer's disease
CA2594946A1 (en) 2005-01-19 2006-07-27 Merck & Co., Inc Tertiary carbinamines having substituted heterocycles, which are active as inhibitors of beta-secretase, for the treatment of alzheimer's disease
WO2007092854A2 (en) 2006-02-06 2007-08-16 Janssen Pharmaceutica N.V. 2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
WO2007092839A2 (en) 2006-02-06 2007-08-16 Janssen Pharmaceutica N.V. Macrocycle derivatives useful as inhibitors of beta-secretase (bace)
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JP2010534206A (ja) * 2007-07-20 2010-11-04 メルク・シャープ・エンド・ドーム・コーポレイション ピラゾロ[1,5−a]ピリミジン誘導体
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JP4520533B2 (ja) * 2008-01-18 2010-08-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 縮合アミノジヒドロチアジン誘導体
US8076358B2 (en) 2008-01-28 2011-12-13 Janssen Pharmaceutica Nv 6-substituted-thio-2-amino-quinoline derivatives useful as inhibitors of β-secretase (BACE)
JP2011510993A (ja) 2008-01-29 2011-04-07 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ β−セクレターゼ(BACE)阻害剤として有用な2−アミノ−キノリン誘導体
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RU2503681C2 (ru) * 2008-09-30 2014-01-10 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Новое конденсированное производное аминодигидротиазина
GB0912778D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
GB0912777D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydropyrimidone derivatives
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
CN102753545A (zh) * 2009-12-15 2012-10-24 盐野义制药株式会社 具有血管内皮脂酶抑制活性的噁二唑衍生物
TW201300380A (zh) * 2010-10-19 2013-01-01 Comentis Inc 抑制β-分泌酶活性之噁二唑化合物及其使用方法
GB201100181D0 (en) 2011-01-06 2011-02-23 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101140D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101139D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
CN103502231A (zh) 2011-01-21 2014-01-08 卫材R&D管理有限公司 用于稠合氨基二氢噻嗪衍生物的合成的方法和化合物
CA2887699A1 (en) * 2012-10-12 2014-04-17 Children's Medical Center Corporation Compounds for treating rac-gtpase mediated disorder
CN103848827A (zh) * 2012-11-30 2014-06-11 南京大学 一种含苯并三氮唑类衍生物在抗癌药物中的应用
CN103848826A (zh) * 2012-11-30 2014-06-11 南京大学 一类含苯并三氮唑结构的1,3,4-恶二唑类衍生物的制法与用途
US10774075B2 (en) 2015-04-24 2020-09-15 Children's Medical Center Corporation Compounds for treating rac-GTPase mediated disorder
CN111655260A (zh) * 2017-10-26 2020-09-11 南方研究院 作为TGF-β抑制剂的噁二唑和噻二唑

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Cited By (4)

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Publication number Priority date Publication date Assignee Title
WO2010038686A1 (ja) * 2008-09-30 2010-04-08 エーザイ・アール・アンド・ディー・マネジメント株式会社 新規な縮合アミノジヒドロチアジン誘導体
CN102171221B (zh) * 2008-09-30 2013-11-06 卫材R&D管理有限公司 新的稠合的氨基二氢噻嗪衍生物
JP5666304B2 (ja) * 2008-09-30 2015-02-12 エーザイ・アール・アンド・ディー・マネジメント株式会社 新規な縮合アミノジヒドロチアジン誘導体
WO2016153023A1 (ja) * 2015-03-25 2016-09-29 国立研究開発法人国立長寿医療研究センター 新規オキサジアゾール誘導体及びこれを含有する医薬

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AU2006206654A1 (en) 2006-07-27
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CA2594946A1 (en) 2006-07-27
US8338614B2 (en) 2012-12-25
WO2006078577A1 (en) 2006-07-27
US20080139538A1 (en) 2008-06-12
DE602006021535D1 (de) 2011-06-09
ATE506951T1 (de) 2011-05-15
EP1841426B1 (en) 2011-04-27

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