TWI305204B - Lactam compounds for inhibiting ß-amyloid p eptide release and/or its synthesis and pharmaceutical compositions comprising the same - Google Patents

Lactam compounds for inhibiting ß-amyloid p eptide release and/or its synthesis and pharmaceutical compositions comprising the same Download PDF

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Publication number
TWI305204B
TWI305204B TW090128005A TW90128005A TWI305204B TW I305204 B TWI305204 B TW I305204B TW 090128005 A TW090128005 A TW 090128005A TW 90128005 A TW90128005 A TW 90128005A TW I305204 B TWI305204 B TW I305204B
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TW
Taiwan
Prior art keywords
compound
formula
tetrahydro
reaction
amino
Prior art date
Application number
TW090128005A
Other languages
English (en)
Chinese (zh)
Inventor
Edmund Audia James
John Varghese
H Latimer Lee
Leigh Mcdaniel Stacey
Scott Nissen Jeffrey
D Thorsett Eugene
S Tung Jay
Original Assignee
Lilly Co Eli
Elan Pharm 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 Lilly Co Eli, Elan Pharm Inc filed Critical Lilly Co Eli
Application granted granted Critical
Publication of TWI305204B publication Critical patent/TWI305204B/zh

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Classifications

    • 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)
  • 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)
TW090128005A 2000-11-17 2001-11-12 Lactam compounds for inhibiting ß-amyloid p eptide release and/or its synthesis and pharmaceutical compositions comprising the same TWI305204B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US24955200P 2000-11-17 2000-11-17

Publications (1)

Publication Number Publication Date
TWI305204B true TWI305204B (en) 2009-01-11

Family

ID=22943982

Family Applications (1)

Application Number Title Priority Date Filing Date
TW090128005A TWI305204B (en) 2000-11-17 2001-11-12 Lactam compounds for inhibiting ß-amyloid p eptide release and/or its synthesis and pharmaceutical compositions comprising the same

Country Status (33)

Country Link
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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UA74849C2 (en) * 2000-11-17 2006-02-15 Lilly Co Eli Lactam
US7468365B2 (en) 2000-11-17 2008-12-23 Eli Lilly And Company Lactam compound
EP1867636B1 (en) 2005-04-08 2013-06-05 Daiichi Sankyo Company, Limited Pyridylmethylsulfone derivative
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
CL2008002060A1 (es) * 2007-07-16 2008-11-21 Wyeth Corp Compuestos derivados de sulfonamida, inhibidores de la produccion de beta amiloide; metodo de preparacion; composicion farmaceutica; kit farmaceutico; y uso en el tratamiento de enfermedades tales como alzheimer, angiopatia amiloide, sindrome de down, entre otras.
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
US20160194368A1 (en) 2013-09-03 2016-07-07 Moderna Therapeutics, Inc. Circular polynucleotides
EP3613418A1 (en) 2014-01-17 2020-02-26 Ligand Pharmaceuticals, Inc. Methods and compositions for modulating hormone levels
EP3212773B1 (en) 2014-10-29 2021-09-15 Massachusetts Eye and Ear Infirmary Efficient delivery of therapeutic molecules to cells of the inner ear
EP3458076A4 (en) 2016-05-16 2020-01-22 The General Hospital Corporation HUMAN RESPIRATORY STEM CELLS IN BREEDING LUNG EPITHEL
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
EP3706747B1 (en) 2017-11-08 2025-09-03 Merck Sharp & Dohme LLC Prmt5 inhibitors
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
WO2021126729A1 (en) 2019-12-17 2021-06-24 Merck Sharp & Dohme Corp. Prmt5 inhibitors
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
CR20250146A (es) 2022-10-25 2025-05-26 Merck Sharp & Dohme Llc Enlazadores-cargas útiles de adc derivados de exatecán, composiciones farmacéuticas, y usos de los mismos
CN120359051A (zh) 2022-12-14 2025-07-22 默沙东有限责任公司 奥瑞他汀接头-载荷、药物组合物及其用途

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2272305A1 (en) * 1996-12-23 1998-07-02 Elan Pharmaceuticals, Inc. Cycloalkyl, lactam, lactone and related compounds as .beta.-amyloid peptide release inhibitors
WO1999067219A1 (en) * 1998-06-22 1999-12-29 Elan Pharmaceuticals, Inc. Compounds for inhibiting beta-amyloid peptide release and/or its synthesis
WO2001034571A1 (en) * 1999-11-09 2001-05-17 Eli Lilly And Company β-AMINOACID COMPOUNDS USEFUL FOR INHIBITING β-AMYLOID PEPTIDE RELEASE AND/OR ITS SYNTHESIS
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
UA74849C2 (en) * 2000-11-17 2006-02-15 Lilly Co Eli Lactam
CA2425558C (en) * 2000-11-17 2012-01-03 Eli Lilly And Company Lactam compound

Also Published As

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
IL155960A0 (en) 2003-12-23
JP4116437B2 (ja) 2008-07-09
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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