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

Info

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
Authority
JP
Japan
Prior art keywords
alkyl
group
hydrogen
cyano
alkoxy
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.)
Withdrawn
Application number
JP2007506409A
Other languages
English (en)
Japanese (ja)
Other versions
JP2007530696A5 (https=
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
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 and Co Inc
Original Assignee
Merck and Co Inc
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 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Withdrawn legal-status Critical Current

Links

Classifications

    • 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

Landscapes

  • 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)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole 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 (https=) 2008-05-08

Family

ID=35124991

Family Applications (1)

Application Number Title Priority Date Filing Date
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 (https=)
EP (1) EP1732906A4 (https=)
JP (1) JP2007530696A (https=)
AU (1) AU2005230878A1 (https=)
CA (1) CA2561267A1 (https=)
WO (1) WO2005097767A1 (https=)

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

Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
WO2005103020A1 (en) 2004-04-20 2005-11-03 Merck & Co., Inc. 1,3,5-substituted phenyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease
JP2008520718A (ja) 2004-11-23 2008-06-19 メルク エンド カムパニー インコーポレーテッド アルツハイマー病の治療のためのβ−セクレターゼ阻害剤として有用な２，３，４，６−置換ピリジル誘導体化合物
WO2006080406A1 (ja) * 2005-01-28 2006-08-03 Taisho Pharmaceutical Co., Ltd. 三環性化合物
RU2416603C9 (ru) 2005-10-25 2012-06-20 Сионоги Энд Ко., Лтд. Производные аминодигидротиазина
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
RU2476431C2 (ru) 2008-01-18 2013-02-27 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Конденсированное производное аминодигидротиазина
AU2009217518A1 (en) 2008-02-28 2009-09-03 Merck Sharp & Dohme Corp. 2-aminoimidazole beta-secretase inhibitors for the treatment of Alzheimer's disease
WO2009151098A1 (ja) 2008-06-13 2009-12-17 塩野義製薬株式会社 βセクレターゼ阻害作用を有する含硫黄複素環誘導体
EP2318416B1 (en) 2008-07-28 2013-09-04 Eisai R&D Management Co., Ltd. Spiroaminodihydrothiazine derivatives
CA2736130C (en) 2008-09-11 2014-01-14 Amgen Inc. Spiro-tetracyclic ring compounds as beta-secretase modulators and methods of use
KR20110076965A (ko) 2008-09-30 2011-07-06 에자이 알앤드디 매니지먼트 가부시키가이샤 신규한 축합 아미노 디하이드로티아진 유도체
CN102186841A (zh) 2008-10-22 2011-09-14 盐野义制药株式会社 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物
TW201020244A (en) 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
WO2010113848A1 (ja) 2009-03-31 2010-10-07 塩野義製薬株式会社 Ｂａｃｅ１阻害作用を有するイソチオウレア誘導体またはイソウレア誘導体
GB0912777D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydropyrimidone derivatives
GB0912778D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine 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
EP2514747A4 (en) 2009-12-09 2013-05-08 Shionogi & Co SUBSTITUTED AMINOTHIAZINE DERIVATIVE
TWI488852B (zh) 2009-12-11 2015-06-21 Shionogi & Co 衍生物
MX2012010657A (es) 2010-03-15 2013-02-07 Amgen Inc Compuestos de espiro amino-dihidrooxazina y amino-dihidrotiazina como moduladores de beta-secretasa y su uso medico.
EP2547685A1 (en) 2010-03-15 2013-01-23 Amgen Inc. Spiro-tetracyclic ring compounds as beta - secretase modulators
WO2012019056A1 (en) 2010-08-05 2012-02-09 Amgen Inc. Amino-iso-indole, amino-aza-iso-indole, amino-dihydroisoquinoline and amino-benzoxazine compounds as beta-secretase modulators and methods of use
JP5816630B2 (ja) 2010-10-29 2015-11-18 塩野義製薬株式会社 ナフチリジン誘導体
JP5766198B2 (ja) 2010-10-29 2015-08-19 塩野義製薬株式会社 縮合アミノジヒドロピリミジン誘導体
EP2643299B1 (en) 2010-11-22 2016-06-22 Noscira, S.A. Bipyridine sulfonamide derivatives for the treatment of neurodegenerative diseases or conditions
EP2643325A1 (en) 2010-11-23 2013-10-02 Amgen Inc. Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use
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
US8426584B2 (en) 2011-01-21 2013-04-23 Eisai R&D Management Co., Ltd. Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives
GB201101139D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
EP2673279A1 (en) 2011-02-07 2013-12-18 Amgen Inc. 5-amino-oxazepine and 5-amino-thiazepane compounds as beta-secretase antagonists and methods of use
EP2675810A1 (en) 2011-02-15 2013-12-25 Amgen Inc. Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use
TW201247635A (en) 2011-04-26 2012-12-01 Shionogi & Co Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them
JP6010118B2 (ja) * 2011-06-30 2016-10-19 ゴーダーヴァリ バイオリファイナリーズ リミテッド クレイスタンチンａおよびその誘導体の合成
WO2013044092A1 (en) 2011-09-21 2013-03-28 Amgen Inc. Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
KR20140071472A (ko) 2011-10-04 2014-06-11 인스티튜트 포 헤퍼타이티스 앤드 바이러스 리서치 간세포 암종을 포함하는 암의 저해제로서 그리고 간염 바이러스 복제의 저해제로서의 치환된 아미노티아졸
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
WO2014078314A1 (en) 2012-11-15 2014-05-22 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
US12083099B2 (en) * 2020-10-28 2024-09-10 Accencio LLC Methods of treating symptoms of coronavirus infection with viral protease inhibitors

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB951885A (en) * 1961-05-13 1964-03-11 Sankyo Co A new process for the preparation of thiazole compounds
JPH07215952A (ja) * 1993-12-06 1995-08-15 Otsuka Pharmaceut Factory Inc カテコール誘導体
JPH1129475A (ja) * 1997-07-07 1999-02-02 Sumitomo Pharmaceut Co Ltd Ｓｔａｔ６活性化阻害剤

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

Similar Documents

Publication Publication Date Title
JP2007530696A (ja) 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
JP7097373B2 (ja) キナーゼ阻害剤としてのアミノトリアゾロピリジン
US7378414B2 (en) Anti-infective agents
CN103561576B (zh) 脂质合成的杂环调节剂
KR20210086674A (ko) Il-12, il-23 및/또는 ifn-알파의 조정과 관련된 상태의 치료를 위한 아미드-치환된 헤테로시클릭 화합물
US20070275990A1 (en) Heterocyclic Spiro Compound
CN110177551B (zh) 脂质合成的杂环调节剂
JP2008526999A (ja) 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
JP2007522088A (ja) アルツハイマー病の治療用フェニルカルボン酸ベータセクレターゼ阻害剤
TW200843752A (en) Novel diamide derivative
JPWO2004026873A1 (ja) トリアザスピロ［５．５］ウンデカン誘導体およびそれらを有効成分とする薬剤
US7932275B2 (en) 2-aminopyridine compounds useful as β-secretase inhibitors for the treatment of alzheimer's disease
KR20050016367A (ko) 디케토히드라진 유도체 화합물 및 그 화합물을유효성분으로서 함유하는 약제
CN1409711A (zh) 用作hiv逆转录酶抑制剂的稠合的二氮萘化合物
JP2021501179A (ja) キナーゼ阻害剤としてのアミノイミダゾピリダジン
JPH08507067A (ja) Ｈｉｖ逆転写酵素阻害剤
CN110248949B (zh) 免疫蛋白酶体抑制剂
JP2015527403A (ja) Ｈｉｖプロテアーゼ阻害剤
WO2005019191A2 (en) 1, 1-dioxido-4h-1,2,4-benzothiadiazine derivate und verwandte verbindungen als inhibitoren der hcv polymerase zur behandlung von hepatitis c
CN1142827A (zh) Hiv蛋白酶抑制剂
JP2008527040A (ja) アルツハイマー病の治療のためのアミノメチルベータセクレターゼ阻害剤
US20220009918A1 (en) Chemical Compounds
JP2017521455A (ja) 抗ＨＩＶ作用を有するフェニル及びｔｅｒｔ−ブチル酢酸置換ピリジノン
JP2008520718A (ja) アルツハイマー病の治療のためのβ−セクレターゼ阻害剤として有用な２，３，４，６−置換ピリジル誘導体化合物
JP2008520727A (ja) アルツハイマー病の治療のための大環状アミノピリジルβ−セクレターゼ阻害剤

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20080318

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20080318

A761 Written withdrawal of application

Free format text: JAPANESE INTERMEDIATE CODE: A761

Effective date: 20091203