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PE16999A1 - Compuestos para inhibir la liberacion de peptido �-amiloide y/o su sintesis - Google Patents

Compuestos para inhibir la liberacion de peptido �-amiloide y/o su sintesis

Info

Publication number
PE16999A1
PE16999A1 PE1997001056A PE00105697A PE16999A1 PE 16999 A1 PE16999 A1 PE 16999A1 PE 1997001056 A PE1997001056 A PE 1997001056A PE 00105697 A PE00105697 A PE 00105697A PE 16999 A1 PE16999 A1 PE 16999A1
Authority
PE
Peru
Prior art keywords
cycloalkyl
aryl
alkyl
heterocycle
heteroaryl
Prior art date
Application number
PE1997001056A
Other languages
English (en)
Inventor
James E Audia
Thomas C Britton
Beverly K Folmer
Varghese John
Thomas E Mabry
Warren J Porter
Eugene D Thorsett
Jing Wu
William Leonard Scott
Clark Norman Eid
Jay S Tung
Jon K Reel
Jeffrey S Nissen
Lee H Latimer
George W Huffman
James J Droste
Original Assignee
Athena Neurosciences Inc
Lilly Co Eli
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 Athena Neurosciences Inc, Lilly Co Eli filed Critical Athena Neurosciences Inc
Publication of PE16999A1 publication Critical patent/PE16999A1/es

Links

Classifications

    • 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
    • C07K5/08—Tripeptides
    • C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
    • 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
    • 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
    • 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
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • 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
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043—Leu-amino acid
    • 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
    • C07K5/0606—Dipeptides 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
    • 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
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • 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
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • 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
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • 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
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • 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

SE REFIEREN A COMPUESTOS DE FORMULA (I), EN DONDE: "X" ES C(O)Y, C(S)Y o CR6R6Y`; X' e X" SON INDEPENDIENTEMENTE H, OH, F o AMBOS FORMAN UN GRUPO OXO; "Y" ES OH, ALCOXI, NR'R", EN DONDE R' Y R" SON H, ALQUILO, ENTRE OTROS, o R' Y R" JUNTOS FORMAN UN CICLO C2-C8 QUE CONTIENE OPCIONALMENTE 1-2 HETEROATOMOS; Y' ES OH, NH2, ENTRE OTROS; "Z" ES UN ENLACE QUE UNE COVALENTEMENTE R1 A CX'X", OXIGENO o AZUFRE; R1 ES ALQUILO, ALQUENILO, ALQUINILO, CICLOALQUILO, CICLOALQUENILO, ARILO, HETEROARILO o HETEROCICLO, DE PREFERENCIA ES FENILO o PIRIDILO; R2 ES H, ALQUILO, ALQUENILO, ALQUINILO, CICLOALQUILO, ARILO, HETEROARILO o HETEROCICLO; R3 ES H, METILO o R3 CON R4 FORMA UN CICLO C3-C8 OPCIONALMENTE FUSIONADO CON UN ARILO o HETEROARILO COMO: PIRROLIDIN, 2,3-DIHIDROINDOL, PIPERIDIN o 1,2,3,4-TETRAHIDROISOQUINOLIN; R4 ES H, ALQUILO, ALQUENILO, ALQUINILO, ARILO, CICLOALQUILO, CICLOALQUENILO, HETEROARILO, HETEROCICLO; R5 ES H, METILO o R5 JUNTO CON R4 FORMA UN CICLOALQUILO C4-C6; R6 ES H, ALQUILO, CICLOALQUILO, ARILO, HETEROARILO o HETEROCICLO; n ES 1 o 2. LOS COMPUESTOS DE FORMULA (I) ACTUAN COMO INHIBIDORES DE LA LIBERACION DEL PEPTIDO �-AMILOIDE CELULAR Y/O SU SINTESIS, SIENDO UTILES EN LA PREVENCION O TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMER
PE1997001056A 1996-11-22 1997-11-20 Compuestos para inhibir la liberacion de peptido �-amiloide y/o su sintesis PE16999A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US75544296A 1996-11-22 1996-11-22
US80852897A 1997-02-28 1997-02-28
US80752897A 1997-02-28 1997-02-28
US80742797A 1997-02-28 1997-02-28

Publications (1)

Publication Number Publication Date
PE16999A1 true PE16999A1 (es) 1999-02-19

Family

ID=27505670

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1997001056A PE16999A1 (es) 1996-11-22 1997-11-20 Compuestos para inhibir la liberacion de peptido �-amiloide y/o su sintesis

Country Status (21)

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

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Also Published As

Publication number Publication date
EA199900490A1 (ru) 2000-02-28
YU46097A (sh) 2000-10-30
KR20000069064A (ko) 2000-11-25
EP0942924A2 (en) 1999-09-22
HUP0100270A2 (hu) 2001-08-28
AR016751A1 (es) 2001-08-01
NO992368L (no) 1999-06-21
HRP970627A2 (en) 1998-08-31
TR199901133T2 (xx) 1999-07-21
NO992368D0 (no) 1999-05-14
WO1998022494A2 (en) 1998-05-28
HUP0100270A3 (en) 2001-09-28
AU5356198A (en) 1998-06-10
CO4910156A1 (es) 2000-04-24
IL129083A0 (en) 2000-02-17
CZ122899A3 (cs) 1999-10-13
ID22044A (id) 1999-08-26
CN1238779A (zh) 1999-12-15
NZ334690A (en) 2001-09-28
WO1998022494A3 (en) 1998-11-26
TR199902937T2 (xx) 2001-01-22
BR9713400A (pt) 2000-01-25
CA2267634A1 (en) 1998-05-28
TR199902938T2 (xx) 2002-06-21
JP2001503782A (ja) 2001-03-21

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