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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Japanese (ja)
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JP2004517090A5 (https=
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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16—Benzazepines; Hydrogenated benzazepines
    • 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
    • A61P25/28—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Public Health (AREA)
  • Genetics & Genomics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (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)
  • Hydrogenated Pyridines (AREA)
  • Medicinal Preparation (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 (https=) 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

Country Status (33)

Country Link
US (1) US20050261495A1 (https=)
EP (1) EP1341531B1 (https=)
JP (1) JP4116437B2 (https=)
KR (1) KR100819679B1 (https=)
CN (1) CN1486184A (https=)
AR (1) AR035927A1 (https=)
AU (2) AU4319202A (https=)
BR (1) BR0115427A (https=)
CA (1) CA2427227C (https=)
CY (1) CY1106366T1 (https=)
CZ (1) CZ20031351A3 (https=)
DE (1) DE60126132T2 (https=)
DK (1) DK1341531T3 (https=)
DZ (1) DZ3453A1 (https=)
EA (1) EA005954B1 (https=)
EC (1) ECSP034600A (https=)
ES (1) ES2278804T3 (https=)
HR (1) HRP20030383B1 (https=)
HU (1) HU228117B1 (https=)
IL (2) IL155960A0 (https=)
MX (1) MXPA03004292A (https=)
MY (1) MY134559A (https=)
NO (1) NO324324B1 (https=)
NZ (1) NZ525854A (https=)
PE (1) PE20020802A1 (https=)
PL (1) PL212199B1 (https=)
PT (1) PT1341531E (https=)
SI (1) SI1341531T1 (https=)
SK (1) SK288065B6 (https=)
TW (1) TWI305204B (https=)
UA (1) UA74849C2 (https=)
WO (1) WO2002047671A2 (https=)
ZA (1) ZA200303789B (https=)

Families Citing this family (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7468365B2 (en) 2000-11-17 2008-12-23 Eli Lilly And Company Lactam compound
UA74849C2 (en) * 2000-11-17 2006-02-15 Lilly Co Eli Lactam
AU2006234441B2 (en) 2005-04-08 2011-07-07 Daiichi Sankyo Company, Limited Pyridylmethylsulfone derivative
ES2382814T3 (es) 2005-05-17 2012-06-13 Merck Sharp & Dohme Ltd. Ácido cis-4-[(4-clorofenil)sulfonil]-4-(2,5-difluorofenil)ciclohexanopropanoico para el tratamiento del cáncer
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
JP2010533723A (ja) * 2007-07-16 2010-10-28 ワイス・エルエルシー βアミロイド生成の阻害剤
JP5385904B2 (ja) 2007-08-14 2014-01-08 イーライ リリー アンド カンパニー γ−セクレターゼ阻害剤
TW200920362A (en) 2007-09-11 2009-05-16 Daiichi Sankyo Co Ltd Alkylsulfone derivatives
EP2222636B1 (en) 2007-12-21 2013-04-10 Ligand Pharmaceuticals Inc. Selective androgen receptor modulators (sarms) and uses thereof
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
PE20121172A1 (es) 2009-10-14 2012-09-05 Merck Sharp & Dohme Piperidinas sustituidas con actividad en la hdm2
WO2011163330A1 (en) 2010-06-24 2011-12-29 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
EP3330377A1 (en) 2010-08-02 2018-06-06 Sirna Therapeutics, Inc. Rna interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (ctnnb1) gene expression using short interfering nucleic acid (sina)
US9029341B2 (en) 2010-08-17 2015-05-12 Sirna Therapeutics, Inc. RNA interference mediated inhibition of hepatitis B virus (HBV) gene expression using short interfering nucleic acid (siNA)
EP2613782B1 (en) 2010-09-01 2016-11-02 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
WO2012058210A1 (en) 2010-10-29 2012-05-03 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACIDS (siNA)
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
EP2770987B1 (en) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Novel 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
US20150299696A1 (en) 2012-05-02 2015-10-22 Sirna Therapeutics, Inc. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
US20150209406A1 (en) 2012-09-07 2015-07-30 Massachusetts Eye And Ear Infirmary Methods and compositions for regenerating hair cells and/or supporting cells
US20150209367A1 (en) 2012-09-07 2015-07-30 Massachusetts Eye & Ear Infirmary Treating Hearing Loss
RU2660429C2 (ru) 2012-09-28 2018-07-06 Мерк Шарп И Доум Корп. Новые соединения, которые являются ингибиторами erk
RS56680B1 (sr) 2012-11-28 2018-03-30 Merck Sharp & Dohme Kompozicije i postupci za lečenje kancera
KR102196882B1 (ko) 2012-12-20 2020-12-30 머크 샤프 앤드 돔 코포레이션 Hdm2 억제제로서의 치환된 이미다조피리딘
WO2014120748A1 (en) 2013-01-30 2014-08-07 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
JP6319912B2 (ja) 2013-04-19 2018-05-09 国立大学法人 岡山大学 アミロイドβ蛋白質により誘発される認知障害の治療剤およびアルツハイマー病治療薬、ならびにこれらに関連する治療方法および病態解析方法
WO2015034925A1 (en) 2013-09-03 2015-03-12 Moderna Therapeutics, Inc. Circular polynucleotides
US10441567B2 (en) 2014-01-17 2019-10-15 Ligand Pharmaceuticals Incorporated Methods and compositions for modulating hormone levels
US11370823B2 (en) 2014-10-29 2022-06-28 Massachusetts Eye And Ear Infirmary Efficient delivery of therapeutic molecules to cells of the inner ear
JP6840774B2 (ja) 2016-05-16 2021-03-10 ザ ジェネラル ホスピタル コーポレイション 肺上皮エンジニアリングにおけるヒト気道幹細胞
EP3525785B1 (en) 2016-10-12 2025-08-27 Merck Sharp & Dohme LLC Kdm5 inhibitors
EP3706747B1 (en) 2017-11-08 2025-09-03 Merck Sharp & Dohme LLC Prmt5 inhibitors
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
WO2019148067A1 (en) 2018-01-26 2019-08-01 Massachusetts Eye And Ear Infirmary Treatment of hearing loss
US12173026B2 (en) 2018-08-07 2024-12-24 Merck Sharp & Dohme Llc PRMT5 inhibitors
US11981701B2 (en) 2018-08-07 2024-05-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
US12552826B2 (en) 2018-08-07 2026-02-17 Merck Sharp & Dohme Llc PRMT5 inhibitors
EP3833668B1 (en) 2018-08-07 2025-03-19 Merck Sharp & Dohme LLC Prmt5 inhibitors
WO2020214834A1 (en) 2019-04-19 2020-10-22 Ligand Pharmaceuticals Inc. Crystalline forms and methods of producing crystalline forms of a compound
US12441730B2 (en) 2019-12-17 2025-10-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
US12595248B2 (en) 2019-12-17 2026-04-07 Merck Sharp & Dohme Llc PRMT5 inhibitors
BR112022012015A2 (pt) 2019-12-17 2022-08-30 Merck Sharp & Dohme Llc Inibidores de prmt5
WO2021126731A1 (en) 2019-12-17 2021-06-24 Merck Sharp & Dohme Corp. Prmt5 inhibitors
US20240116945A1 (en) 2022-09-02 2024-04-11 Merck Sharp & Dohme Llc Exatecan-derived topoisomerase-1 inhibitors pharmaceutical compositions, and uses thereof
WO2024091437A1 (en) 2022-10-25 2024-05-02 Merck Sharp & Dohme Llc Exatecan-derived adc linker-payloads, pharmaceutical compositions, and uses thereof
GEAP202516798A (en) 2022-12-14 2025-10-27 Merck Sharp & Dohme Llc Auristatin linker-payloads, pharmaceutical compositions, and uses thereof

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUP0001232A3 (en) * 1996-12-23 2001-02-28 Elan Pharmaceuticals Inc San F Cycloalkyl, lactam, lactone derivatives and their thio analogues inhibiting betha-amyloid peptide release and/or its synthesis and pharmaceutical compositions containing the compounds
JP2002518481A (ja) * 1998-06-22 2002-06-25 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 β−アミロイドペプチドの放出および／またはその合成を阻害するための化合物
JP2003513958A (ja) * 1999-11-09 2003-04-15 イーライ・リリー・アンド・カンパニー β−アミロイドペプチド放出および／またはその合成を阻害するために有用なβ−アミノ酸化合物
EP1345955B1 (en) * 2000-11-17 2008-08-20 Eli Lilly And Company Lactam dipeptide and its use in inhibiting beta-amyloid peptide release
UA74849C2 (en) * 2000-11-17 2006-02-15 Lilly Co Eli Lactam
UA77165C2 (en) * 2000-11-17 2006-11-15 Lilly Co Eli (n)-((s)-2-hydroxy-3-methyl-butyryl)-1-(l-alaninyl)-(s)-1-amino-3-methyl-4,5,6,7-tetrahydro-2h-3-benzazepin-2-one dihydrate, processes for manufacturing and pharmaceutical composition

Also Published As

Publication number Publication date
PT1341531E (pt) 2007-04-30
BR0115427A (pt) 2003-10-07
CA2427227C (en) 2010-08-17
ECSP034600A (es) 2003-06-25
HU228117B1 (en) 2012-11-28
KR100819679B1 (ko) 2008-04-04
NZ525854A (en) 2004-06-25
ES2278804T3 (es) 2007-08-16
PL212199B1 (pl) 2012-08-31
EP1341531A2 (en) 2003-09-10
PE20020802A1 (es) 2002-09-10
WO2002047671A2 (en) 2002-06-20
UA74849C2 (en) 2006-02-15
DE60126132T2 (de) 2007-10-18
DZ3453A1 (fr) 2002-06-20
CY1106366T1 (el) 2011-10-12
HRP20030383B1 (hr) 2007-12-31
EA005954B1 (ru) 2005-08-25
SK288065B6 (sk) 2013-04-03
AU4319202A (en) 2002-06-24
MY134559A (en) 2007-12-31
WO2002047671A3 (en) 2003-03-06
NO20032236L (no) 2003-07-10
HK1059731A1 (en) 2004-07-16
DE60126132D1 (de) 2007-03-08
JP2004517090A (ja) 2004-06-10
SK5592003A3 (en) 2003-12-02
DK1341531T3 (da) 2007-05-14
KR20030051846A (ko) 2003-06-25
AR035927A1 (es) 2004-07-28
CZ20031351A3 (cs) 2003-11-12
IL155960A0 (en) 2003-12-23
EA200300580A1 (ru) 2003-10-30
AU2002243192B2 (en) 2006-07-20
SI1341531T1 (sl) 2007-06-30
HUP0301842A3 (en) 2010-03-29
MXPA03004292A (es) 2004-02-12
CA2427227A1 (en) 2002-06-20
HUP0301842A2 (hu) 2003-09-29
US20050261495A1 (en) 2005-11-24
NO324324B1 (no) 2007-09-24
PL362688A1 (en) 2004-11-02
CN1486184A (zh) 2004-03-31
EP1341531B1 (en) 2007-01-17
HRP20030383A2 (en) 2005-10-31
TWI305204B (en) 2009-01-11
NO20032236D0 (no) 2003-05-16
ZA200303789B (en) 2004-08-16
IL155960A (en) 2009-06-15

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