JP2007530696A - アスパラギン酸プロテアーゼ阻害剤として有用な２−アミノチアゾール化合物 - Google Patents

アスパラギン酸プロテアーゼ阻害剤として有用な２−アミノチアゾール化合物 Download PDF

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Publication number
JP2007530696A
JP2007530696A JP2007506409A JP2007506409A JP2007530696A JP 2007530696 A JP2007530696 A JP 2007530696A JP 2007506409 A JP2007506409 A JP 2007506409A JP 2007506409 A JP2007506409 A JP 2007506409A JP 2007530696 A JP2007530696 A JP 2007530696A
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JP
Japan
Prior art keywords
alkyl
group
hydrogen
cyano
alkoxy
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JP2007506409A
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English (en)
Japanese (ja)
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JP2007530696A5 (enExample
Inventor
コバーン，クレイグ・エイ
エスペセス，エイミー・エス
ステイチエル，シヨーン・ジエイ
オルセン，デイビツド・ビー
ハズダ，ダリア・ジエイ
ホロウエイ，エム・キヤサリン
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Merck and Co Inc
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Merck and Co Inc
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Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of JP2007530696A publication Critical patent/JP2007530696A/ja
Publication of JP2007530696A5 publication Critical patent/JP2007530696A5/ja
Withdrawn legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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 three or more hetero rings
    • 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
    • A61P25/28—Drugs 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/40—Unsubstituted amino or imino radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles 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 in position 2
    • C07D277/82—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/84—Naphthothiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/06—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/08—Heterocyclic 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 alicyclic rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Virology (AREA)
  • Hospice & Palliative Care (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2007506409A 2004-03-30 2005-03-25 アスパラギン酸プロテアーゼ阻害剤として有用な２−アミノチアゾール化合物 Withdrawn JP2007530696A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US55776904P 2004-03-30 2004-03-30
US59138604P 2004-07-27 2004-07-27
PCT/US2005/010224 WO2005097767A1 (en) 2004-03-30 2005-03-25 2-aminothiazole compounds useful as aspartyl protease inhibitors

Publications (2)

Publication Number Publication Date
JP2007530696A true JP2007530696A (ja) 2007-11-01
JP2007530696A5 JP2007530696A5 (enExample) 2008-05-08

Family

ID=35124991

Family Applications (1)

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JP2007506409A Withdrawn JP2007530696A (ja) 2004-03-30 2005-03-25 アスパラギン酸プロテアーゼ阻害剤として有用な２−アミノチアゾール化合物

Country Status (6)

Country Link
US (1) US20070203147A1 (enExample)
EP (1) EP1732906A4 (enExample)
JP (1) JP2007530696A (enExample)
AU (1) AU2005230878A1 (enExample)
CA (1) CA2561267A1 (enExample)
WO (1) WO2005097767A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
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WO2010013302A1 (ja) * 2008-07-28 2010-02-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 スピロアミノジヒドロチアジン誘導体

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US7521481B2 (en) 2003-02-27 2009-04-21 Mclaurin Joanne Methods of preventing, treating and diagnosing disorders of protein aggregation
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
JP2007533743A (ja) 2004-04-20 2007-11-22 メルク　エンド　カムパニー　インコーポレーテッド アルツハイマー病治療のためのβ−セクレターゼ阻害薬として有用な１，３，５−置換フェニル誘導体化合物
WO2006057945A2 (en) 2004-11-23 2006-06-01 Merck & Co., Inc. 2,3,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease
WO2006080406A1 (ja) * 2005-01-28 2006-08-03 Taisho Pharmaceutical Co., Ltd. 三環性化合物
KR101052122B1 (ko) 2005-10-25 2011-07-26 시오노기세야쿠 가부시키가이샤 아미노디히드로티아진 유도체
TW200815349A (en) 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
ATE543810T1 (de) * 2006-09-01 2012-02-15 Merck Sharp & Dohme Hemmer des 5-lipoxygenase aktivierenden proteins (flap)
AU2007332754A1 (en) 2006-12-12 2008-06-19 Schering Corporation Aspartyl protease inhibitors
EP2147914B1 (en) 2007-04-24 2014-06-04 Shionogi&Co., Ltd. Aminodihydrothiazine derivatives substituted with cyclic groups
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
EP2546232A1 (en) * 2007-06-20 2013-01-16 Merck Sharp & Dohme Corp. Diphenyl Substituted Alkanes
US20100317850A1 (en) 2008-01-18 2010-12-16 Yuichi Suzuki Condensed aminodihydrothiazine derivative
EP2257167B1 (en) 2008-02-28 2015-07-22 Merck Sharp & Dohme Corp. 2-aminoimidazole beta-secretase inhibitors for the treatment of alzheimer's disease
MX2010013256A (es) 2008-06-13 2010-12-21 Shionogi & Co Derivado heterociclico que contiene azufre que tiene actividad inhibitoria de beta-secretasa.
AU2009277485B2 (en) 2008-07-28 2013-05-02 Eisai R&D Management Co., Ltd. Spiroaminodihydrothiazine derivatives
CN102209721A (zh) 2008-09-11 2011-10-05 安姆根有限公司 作为β-分泌酶调节剂的螺四环化合物及其使用方法
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
JPWO2010047372A1 (ja) 2008-10-22 2012-03-22 塩野義製薬株式会社 Ｂａｃｅ１阻害活性を有する２−アミノピリミジン−４−オンおよび２−アミノピリジン誘導体
TW201020244A (en) 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
TW201040141A (en) 2009-03-31 2010-11-16 Shionogi & Co Isothiourea derivatives or isourea derivatives having BACE1 inhibitory activity
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
EP2281824A1 (en) 2009-08-07 2011-02-09 Noscira, S.A. Furan-imidazolone derivatives, for the treatment of cognitive, neurodegenerative or neuronal diseases or disorders
WO2011070781A1 (ja) 2009-12-09 2011-06-16 塩野義製薬株式会社 置換アミノチアジン誘導体
JPWO2011071135A1 (ja) 2009-12-11 2013-04-22 塩野義製薬株式会社 オキサジン誘導体
EP2547686B1 (en) 2010-03-15 2014-01-22 Amgen Inc. Amino-dihydrooxazine and amino-dihydrothiazine spiro compounds as beta-secretase modulators and their medical use
US8883782B2 (en) 2010-03-15 2014-11-11 Amgen Inc. Spiro-tetracyclic ring compounds as beta-secretase modulators and methods of use
US8921363B2 (en) 2010-08-05 2014-12-30 Amgen Inc. Derivatives of 1 H-isoindol-3-amine, 1 H-iso-aza-indol-3amine, 3,4-dihydroisoquinolin-1-amine, and 1,4-dihydroisoquinolin-3-amine as beta-secretase inhibitors
CA2816285A1 (en) 2010-10-29 2012-05-03 Shionogi & Co., Ltd. Naphthyridine derivative
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JP2013542973A (ja) 2010-11-22 2013-11-28 ノスシラ、ソシエダッド、アノニマ 神経変性疾患または神経変性状態を治療するためのビピリジンスルホンアミド誘導体
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TW201247635A (en) 2011-04-26 2012-12-01 Shionogi & Co Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them
BR112013033755A2 (pt) * 2011-06-30 2016-08-16 Godavari Biorefineries Ltd síntese de cleistantina a e seus derivados
JP2014526560A (ja) 2011-09-21 2014-10-06 アムジエン・インコーポレーテツド β‐セクレターゼ調節因子としてのアミノオキサジン化合物およびアミノジヒドロチアジン化合物および使用方法
WO2013052613A1 (en) * 2011-10-04 2013-04-11 Institute For Hepatitis And Virus Research Substituted aminothiazoles as inhibitors of cancers, including hepatocellular carcinoma, and as inhibitors of hepatitis virus replication
JP2016501827A (ja) 2012-10-24 2016-01-21 塩野義製薬株式会社 Ｂａｃｅ１阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体
US9725469B2 (en) 2012-11-15 2017-08-08 Amgen, Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
CN107892697B (zh) 2016-12-26 2020-11-03 郑州泰基鸿诺医药股份有限公司 一种[1,3]噻嗪-2-胺类化合物及应用，药物组合物
CN110117263B (zh) * 2019-06-11 2020-12-25 湖南中医药大学 2-氨基-5-酰基噻唑衍生物及其合成方法
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JPH07215952A (ja) * 1993-12-06 1995-08-15 Otsuka Pharmaceut Factory Inc カテコール誘導体
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010013302A1 (ja) * 2008-07-28 2010-02-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 スピロアミノジヒドロチアジン誘導体

Also Published As

Publication number Publication date
WO2005097767A1 (en) 2005-10-20
EP1732906A1 (en) 2006-12-20
EP1732906A4 (en) 2007-11-21
AU2005230878A1 (en) 2005-10-20
CA2561267A1 (en) 2005-10-20
US20070203147A1 (en) 2007-08-30

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