JP4116437B2 - β−アミロイドペプチドの放出および/または合成を阻害するラクタム化合物 - Google Patents

β−アミロイドペプチドの放出および/または合成を阻害するラクタム化合物 Download PDF

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JP4116437B2
JP4116437B2 JP2002549245A JP2002549245A JP4116437B2 JP 4116437 B2 JP4116437 B2 JP 4116437B2 JP 2002549245 A JP2002549245 A JP 2002549245A JP 2002549245 A JP2002549245 A JP 2002549245A JP 4116437 B2 JP4116437 B2 JP 4116437B2
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methyl
tetrahydro
amino
reaction
formula
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JP2004517090A5 (enExample
JP2004517090A (ja
Inventor
ジェイムズ・エドモンド・オーディア
バーゲス・ジョン
リー・エイチ・ラティマー
ステイシー・リー・マクダニエル
ジェフリー・スコット・ニッセン
ユージーン・ディ・ソーセット
ジェイ・エス・トゥン
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イーライ リリー アンド カンパニー
エラン ファーマシューティカルズ,インコーポレイテッド
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D223/00Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16Benzazepines; Hydrogenated benzazepines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Animal Behavior & Ethology (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Hydrogenated Pyridines (AREA)
JP2002549245A 2000-11-17 2001-11-05 β−アミロイドペプチドの放出および/または合成を阻害するラクタム化合物 Expired - Fee Related JP4116437B2 (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24955200P 2000-11-17 2000-11-17
PCT/US2001/027799 WO2002047671A2 (en) 2000-11-17 2001-11-05 Lactam compound to inhibit beta-amyloid peptide release or synthesis

Publications (3)

Publication Number Publication Date
JP2004517090A JP2004517090A (ja) 2004-06-10
JP2004517090A5 JP2004517090A5 (enExample) 2006-08-17
JP4116437B2 true JP4116437B2 (ja) 2008-07-09

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JP2002549245A Expired - Fee Related JP4116437B2 (ja) 2000-11-17 2001-11-05 β−アミロイドペプチドの放出および/または合成を阻害するラクタム化合物

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US (1) US20050261495A1 (enExample)
EP (1) EP1341531B1 (enExample)
JP (1) JP4116437B2 (enExample)
KR (1) KR100819679B1 (enExample)
CN (1) CN1486184A (enExample)
AR (1) AR035927A1 (enExample)
AU (2) AU2002243192B2 (enExample)
BR (1) BR0115427A (enExample)
CA (1) CA2427227C (enExample)
CY (1) CY1106366T1 (enExample)
CZ (1) CZ20031351A3 (enExample)
DE (1) DE60126132T2 (enExample)
DK (1) DK1341531T3 (enExample)
DZ (1) DZ3453A1 (enExample)
EA (1) EA005954B1 (enExample)
EC (1) ECSP034600A (enExample)
ES (1) ES2278804T3 (enExample)
HR (1) HRP20030383B1 (enExample)
HU (1) HU228117B1 (enExample)
IL (2) IL155960A0 (enExample)
MX (1) MXPA03004292A (enExample)
MY (1) MY134559A (enExample)
NO (1) NO324324B1 (enExample)
NZ (1) NZ525854A (enExample)
PE (1) PE20020802A1 (enExample)
PL (1) PL212199B1 (enExample)
PT (1) PT1341531E (enExample)
SI (1) SI1341531T1 (enExample)
SK (1) SK288065B6 (enExample)
TW (1) TWI305204B (enExample)
UA (1) UA74849C2 (enExample)
WO (1) WO2002047671A2 (enExample)
ZA (1) ZA200303789B (enExample)

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WO2006123182A2 (en) 2005-05-17 2006-11-23 Merck Sharp & Dohme Limited Cyclohexyl sulphones for treatment of cancer
JP5198877B2 (ja) * 2006-01-31 2013-05-15 株式会社エーピーアイ コーポレーション ベンゾアゼピノン類の製造方法
CA2676715A1 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperazine derivatives for treatment of ad and related conditions
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CA2694209C (en) 2007-08-14 2013-09-17 Eli Lilly And Company Azepine derivatives as gamma-secretase inhibitors
TW200920362A (en) 2007-09-11 2009-05-16 Daiichi Sankyo Co Ltd Alkylsulfone derivatives
ES2413504T3 (es) 2007-12-21 2013-07-16 Ligand Pharmaceuticals Inc. Moduladores selectivos del receptor de andrógeno (SARM) y usos de los mismos
EP2291181B9 (en) 2008-04-18 2013-09-11 University College Dublin National University Of Ireland, Dublin Captodiamine for the treatment of depression symptoms
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
MY174452A (en) 2009-10-14 2020-04-19 Schering Corp Substituted piperidines that increase p53 activity and the uses thereof
US8999957B2 (en) 2010-06-24 2015-04-07 Merck Sharp & Dohme Corp. Heterocyclic compounds as ERK inhibitors
US8518907B2 (en) 2010-08-02 2013-08-27 Merck Sharp & Dohme Corp. RNA interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (CTNNB1) gene expression using short interfering nucleic acid (siNA)
EP3587574B1 (en) 2010-08-17 2022-03-16 Sirna Therapeutics, Inc. Rna interference mediated inhibition of hepatitis b virus (hbv) gene expression using short interfering nucleic acid (sina)
US8946216B2 (en) 2010-09-01 2015-02-03 Merck Sharp & Dohme Corp. Indazole derivatives useful as ERK inhibitors
US9242981B2 (en) 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
WO2012040444A2 (en) * 2010-09-24 2012-03-29 Bristol-Myers Squibb Company Treatment of patients with incipient alzheimer's disease
US9260471B2 (en) 2010-10-29 2016-02-16 Sirna Therapeutics, Inc. RNA interference mediated inhibition of gene expression using short interfering nucleic acids (siNA)
EP2654748B1 (en) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
US9023865B2 (en) 2011-10-27 2015-05-05 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
CN102690231B (zh) * 2012-04-11 2014-07-09 南京友杰医药科技有限公司 治疗阿尔茨海默病潜在药物司马西特的合成方法
EP3919620A1 (en) 2012-05-02 2021-12-08 Sirna Therapeutics, Inc. Short interfering nucleic acid (sina) compositions
EP3970725B1 (en) 2012-09-07 2025-08-20 Massachusetts Eye & Ear Infirmary A gamma secretase inhibitor for treating hearing loss
JP6486272B2 (ja) 2012-09-07 2019-03-20 マサチューセッツ・アイ・アンド・イア・インファーマリー 有毛細胞および/または支持細胞再生のための方法および組成物
JP6280554B2 (ja) 2012-09-28 2018-02-14 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. Erk阻害剤である新規化合物
DK2925888T3 (en) 2012-11-28 2017-12-18 Merck Sharp & Dohme COMPOSITIONS AND METHODS OF CANCER TREATMENT
AR094116A1 (es) 2012-12-20 2015-07-08 Merck Sharp & Dohme Imidazopiridinas sustituidas como inhibidores de hdm2
WO2014120748A1 (en) 2013-01-30 2014-08-07 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
US20160067306A1 (en) 2013-04-19 2016-03-10 National University Corporation Hokkaido University Treatment agent for cognitive impairment induced by amyloid beta-protein, therapeutic agent for alzheimer's disease, and treatment method and pathological analysis method related to these
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EP3525785B1 (en) 2016-10-12 2025-08-27 Merck Sharp & Dohme LLC Kdm5 inhibitors
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
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US11590152B2 (en) 2018-01-26 2023-02-28 Massachusetts Eye And Ear Infirmary Treatment of hearing loss
WO2020033284A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
US11993602B2 (en) 2018-08-07 2024-05-28 Merck Sharp & Dohme Llc PRMT5 inhibitors
EP3833355A4 (en) 2018-08-07 2022-05-11 Merck Sharp & Dohme Corp. PRMT5 INHIBITORS
BR112021020864A2 (pt) 2019-04-19 2021-12-14 Ligand Pharm Inc Formas cristalinas e métodos de produção de formas cristalinas de um composto
US20230108114A1 (en) 2019-12-17 2023-04-06 Merck Sharp & Dohme Llc Prmt5 inhibitors
AU2020408148B2 (en) 2019-12-17 2025-04-24 Merck Sharp & Dohme Llc PRMT5 inhibitors
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CN120225528A (zh) 2022-09-02 2025-06-27 默沙东有限责任公司 依喜替康衍生的拓扑异构酶-1抑制剂药物组合物及其用途
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Publication number Publication date
IL155960A (en) 2009-06-15
DE60126132D1 (de) 2007-03-08
EP1341531A2 (en) 2003-09-10
MXPA03004292A (es) 2004-02-12
NO324324B1 (no) 2007-09-24
SI1341531T1 (sl) 2007-06-30
EA005954B1 (ru) 2005-08-25
NZ525854A (en) 2004-06-25
SK288065B6 (sk) 2013-04-03
CN1486184A (zh) 2004-03-31
AU2002243192B2 (en) 2006-07-20
NO20032236L (no) 2003-07-10
US20050261495A1 (en) 2005-11-24
KR20030051846A (ko) 2003-06-25
MY134559A (en) 2007-12-31
PE20020802A1 (es) 2002-09-10
CA2427227A1 (en) 2002-06-20
CY1106366T1 (el) 2011-10-12
PL362688A1 (en) 2004-11-02
NO20032236D0 (no) 2003-05-16
ES2278804T3 (es) 2007-08-16
DE60126132T2 (de) 2007-10-18
HRP20030383B1 (hr) 2007-12-31
ECSP034600A (es) 2003-06-25
DZ3453A1 (fr) 2002-06-20
PL212199B1 (pl) 2012-08-31
AR035927A1 (es) 2004-07-28
KR100819679B1 (ko) 2008-04-04
JP2004517090A (ja) 2004-06-10
CZ20031351A3 (cs) 2003-11-12
PT1341531E (pt) 2007-04-30
UA74849C2 (en) 2006-02-15
TWI305204B (en) 2009-01-11
IL155960A0 (en) 2003-12-23
WO2002047671A2 (en) 2002-06-20
AU4319202A (en) 2002-06-24
HRP20030383A2 (en) 2005-10-31
HK1059731A1 (en) 2004-07-16
DK1341531T3 (da) 2007-05-14
ZA200303789B (en) 2004-08-16
EA200300580A1 (ru) 2003-10-30
WO2002047671A3 (en) 2003-03-06
HU228117B1 (en) 2012-11-28
HUP0301842A2 (hu) 2003-09-29
HUP0301842A3 (en) 2010-03-29
SK5592003A3 (en) 2003-12-02
BR0115427A (pt) 2003-10-07
CA2427227C (en) 2010-08-17
EP1341531B1 (en) 2007-01-17

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