DE60126132T2 - Lactamverbindung zur hemmung der freisetzung oder der synthese von beta-amyloidpeptid - Google Patents

Lactamverbindung zur hemmung der freisetzung oder der synthese von beta-amyloidpeptid Download PDF

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Publication number
DE60126132T2
DE60126132T2 DE60126132T DE60126132T DE60126132T2 DE 60126132 T2 DE60126132 T2 DE 60126132T2 DE 60126132 T DE60126132 T DE 60126132T DE 60126132 T DE60126132 T DE 60126132T DE 60126132 T2 DE60126132 T2 DE 60126132T2
Authority
DE
Germany
Prior art keywords
methyl
benzazepin
amino
tetrahydro
formula
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.)
Expired - Lifetime
Application number
DE60126132T
Other languages
German (de)
English (en)
Other versions
DE60126132D1 (de
Inventor
Edmund James Zionsville AUDIA
Varghese South San Francisco JOHN
H. Lee Oakland LATIMER
Leigh Stacey Martinsville MCDANIEL
Scott Jeffrey Indianapolis NISSEN
D. Eugene Moss Beach THORSETT
S. Jay Belmont TUNG
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.)
Elan Pharmaceuticals LLC
Eli Lilly and Co
Original Assignee
Elan Pharmaceuticals LLC
Eli Lilly and Co
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 Elan Pharmaceuticals LLC, Eli Lilly and Co filed Critical Elan Pharmaceuticals LLC
Publication of DE60126132D1 publication Critical patent/DE60126132D1/de
Application granted granted Critical
Publication of DE60126132T2 publication Critical patent/DE60126132T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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Classifications

    • 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)
DE60126132T 2000-11-17 2001-11-05 Lactamverbindung zur hemmung der freisetzung oder der synthese von beta-amyloidpeptid Expired - Lifetime DE60126132T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US24955200P 2000-11-17 2000-11-17
US249552P 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 (2)

Publication Number Publication Date
DE60126132D1 DE60126132D1 (de) 2007-03-08
DE60126132T2 true DE60126132T2 (de) 2007-10-18

Family

ID=22943982

Family Applications (1)

Application Number Title Priority Date Filing Date
DE60126132T Expired - Lifetime DE60126132T2 (de) 2000-11-17 2001-11-05 Lactamverbindung zur hemmung der freisetzung oder der synthese von beta-amyloidpeptid

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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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
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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
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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
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
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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Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8328 Change in the person/name/address of the agent

Representative=s name: KROHER, STROBEL RECHTS- UND PATENTANWAELTE, 80336

8328 Change in the person/name/address of the agent

Representative=s name: DR. SCHOEN & PARTNER, 80336 MUENCHEN