WO1998022494A3 - METHODS AND COMPOUNDS FOR INHIBITING β-AMYLOID PEPTIDE RELEASE AND/OR SYNTHESIS - Google Patents

METHODS AND COMPOUNDS FOR INHIBITING β-AMYLOID PEPTIDE RELEASE AND/OR SYNTHESIS Download PDF

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Publication number
WO1998022494A3
WO1998022494A3 PCT/US1997/020804 US9720804W WO9822494A3 WO 1998022494 A3 WO1998022494 A3 WO 1998022494A3 US 9720804 W US9720804 W US 9720804W WO 9822494 A3 WO9822494 A3 WO 9822494A3
Authority
WO
WIPO (PCT)
Prior art keywords
synthesis
amyloid peptide
compounds
methods
peptide release
Prior art date
Application number
PCT/US1997/020804
Other languages
French (fr)
Other versions
WO1998022494A9 (en
WO1998022494A2 (en
Inventor
James E Audia
Thomas C Britton
James J Droste
Beverly K Folmer
George W Huffman
Varghese John
Lee H Latimer
Thomas E Mabry
Jeffrey S Nissen
Warren J Porter
Jon K Reel
Eugene D Thorsett
Jay S Tung
Jing Wu
Clark Norman Eid
William Leonard Scott
Original Assignee
Athena Neurosciences Inc
Lilly Co Eli
James E Audia
Thomas C Britton
James J Droste
Beverly K Folmer
George W Huffman
Varghese John
Lee H Latimer
Thomas E Mabry
Jeffrey S Nissen
Warren J Porter
Jon K Reel
Eugene D Thorsett
Jay S Tung
Jing Wu
Clark Norman Eid
William Leonard Scott
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
Priority to BR9713400-7A priority Critical patent/BR9713400A/en
Priority to EP97950601A priority patent/EP0942924A2/en
Priority to EA199900490A priority patent/EA199900490A1/en
Priority to CA002267634A priority patent/CA2267634A1/en
Priority to HU0100270A priority patent/HUP0100270A3/en
Priority to JP52375698A priority patent/JP2001503782A/en
Application filed by Athena Neurosciences Inc, Lilly Co Eli, James E Audia, Thomas C Britton, James J Droste, Beverly K Folmer, George W Huffman, Varghese John, Lee H Latimer, Thomas E Mabry, Jeffrey S Nissen, Warren J Porter, Jon K Reel, Eugene D Thorsett, Jay S Tung, Jing Wu, Clark Norman Eid, William Leonard Scott filed Critical Athena Neurosciences Inc
Priority to IL12908397A priority patent/IL129083A0/en
Priority to AU53561/98A priority patent/AU5356198A/en
Publication of WO1998022494A2 publication Critical patent/WO1998022494A2/en
Publication of WO1998022494A9 publication Critical patent/WO1998022494A9/en
Publication of WO1998022494A3 publication Critical patent/WO1998022494A3/en
Priority to NO992368A priority patent/NO992368L/en

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    • 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
    • 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
    • C07K5/08Tripeptides
    • C07K5/0827Tripeptides containing heteroatoms different from O, S, or N
    • 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
    • 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
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • 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
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043Leu-amino acid
    • 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
    • C07K5/0606Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
    • 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
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • C07K5/06191Dipeptides containing heteroatoms different from O, S, or N
    • 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
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • 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
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • 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
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0812Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Psychiatry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Hospice & Palliative Care (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
PCT/US1997/020804 1996-11-22 1997-11-21 METHODS AND COMPOUNDS FOR INHIBITING β-AMYLOID PEPTIDE RELEASE AND/OR SYNTHESIS WO1998022494A2 (en)

Priority Applications (9)

Application Number Priority Date Filing Date Title
EP97950601A EP0942924A2 (en) 1996-11-22 1997-11-21 METHODS AND COMPOUNDS FOR INHIBITING $g(b)-AMYLOID PEPTIDE RELEASE AND/OR ITS SYNTHESIS
EA199900490A EA199900490A1 (en) 1996-11-22 1997-11-21 METHODS AND COMPOUNDS FOR INHIBITING β-AMYLOID PEPTIDE ALLOCATION AND / OR ITS SYNTHESIS
CA002267634A CA2267634A1 (en) 1996-11-22 1997-11-21 Methods and compounds for inhibiting .beta.-amyloid peptide release and/or synthesis
HU0100270A HUP0100270A3 (en) 1996-11-22 1997-11-21 Peptids for inhibiting betha-amyloid peptide release and/or its synthesis, pharmaceutical compositions comprising thereof and their use
JP52375698A JP2001503782A (en) 1996-11-22 1997-11-21 Method and compound for inhibiting release of beta-amyloid peptide and / or its synthesis
BR9713400-7A BR9713400A (en) 1996-11-22 1997-11-21 Processes and compounds to inhibit beta-amyloid peptide release and / or its synthesis.
IL12908397A IL129083A0 (en) 1996-11-22 1997-11-21 Methods and compounds for inhibiting beta-amyloid peptide release and/or its synthesis
AU53561/98A AU5356198A (en) 1996-11-22 1997-11-21 Methods and compounds for inhibiting beta-amyloid peptide release and/or its synthesis
NO992368A NO992368L (en) 1996-11-22 1999-05-14 Methods and Compounds for Inhibiting <beta> -amyloid Release and / or its Synthesis

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US75544296A 1996-11-22 1996-11-22
US08/755,442 1996-11-22
US80852897A 1997-02-28 1997-02-28
US80752897A 1997-02-28 1997-02-28
US80742797A 1997-02-28 1997-02-28
US08/807,427 1997-02-28
US08/807,528 1997-02-28
US08/808,528 1997-02-28

Publications (3)

Publication Number Publication Date
WO1998022494A2 WO1998022494A2 (en) 1998-05-28
WO1998022494A9 WO1998022494A9 (en) 1998-08-20
WO1998022494A3 true WO1998022494A3 (en) 1998-11-26

Family

ID=27505670

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1997/020804 WO1998022494A2 (en) 1996-11-22 1997-11-21 METHODS AND COMPOUNDS FOR INHIBITING β-AMYLOID PEPTIDE RELEASE AND/OR SYNTHESIS

Country Status (21)

Country Link
EP (1) EP0942924A2 (en)
JP (1) JP2001503782A (en)
KR (1) KR20000069064A (en)
CN (1) CN1238779A (en)
AR (1) AR016751A1 (en)
AU (1) AU5356198A (en)
BR (1) BR9713400A (en)
CA (1) CA2267634A1 (en)
CO (1) CO4910156A1 (en)
CZ (1) CZ122899A3 (en)
EA (1) EA199900490A1 (en)
HR (1) HRP970627A2 (en)
HU (1) HUP0100270A3 (en)
ID (1) ID22044A (en)
IL (1) IL129083A0 (en)
NO (1) NO992368L (en)
NZ (1) NZ334690A (en)
PE (1) PE16999A1 (en)
TR (3) TR199901133T2 (en)
WO (1) WO1998022494A2 (en)
YU (1) YU46097A (en)

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KR20000069064A (en) 2000-11-25
NO992368D0 (en) 1999-05-14
YU46097A (en) 2000-10-30
ID22044A (en) 1999-08-26
TR199902938T2 (en) 2002-06-21
PE16999A1 (en) 1999-02-19
CZ122899A3 (en) 1999-10-13
BR9713400A (en) 2000-01-25
CN1238779A (en) 1999-12-15
CO4910156A1 (en) 2000-04-24
EP0942924A2 (en) 1999-09-22
AU5356198A (en) 1998-06-10
IL129083A0 (en) 2000-02-17
HUP0100270A3 (en) 2001-09-28
TR199902937T2 (en) 2001-01-22
NZ334690A (en) 2001-09-28
EA199900490A1 (en) 2000-02-28
AR016751A1 (en) 2001-08-01
NO992368L (en) 1999-06-21
WO1998022494A2 (en) 1998-05-28
JP2001503782A (en) 2001-03-21
CA2267634A1 (en) 1998-05-28
HUP0100270A2 (en) 2001-08-28
TR199901133T2 (en) 1999-07-21
HRP970627A2 (en) 1998-08-31

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