DK2623113T3 - Forbindelse til enzymhæmning - Google Patents

Forbindelse til enzymhæmning Download PDF

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Publication number
DK2623113T3
DK2623113T3 DK13157801.5T DK13157801T DK2623113T3 DK 2623113 T3 DK2623113 T3 DK 2623113T3 DK 13157801 T DK13157801 T DK 13157801T DK 2623113 T3 DK2623113 T3 DK 2623113T3
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mmol
proteasome
compound
solution
cancer
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DK13157801.5T
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English (en)
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Han-Jie Zhou
Congcong M Sun
Kevin D Shenk
Guy J Laidig
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Onyx Therapeutics Inc
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    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/69—Boron compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/55—Protease inhibitors
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
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    • 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
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
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    • 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
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    • 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
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    • C07—ORGANIC CHEMISTRY
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    • 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
    • C07K5/081—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
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    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
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    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
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    • C07K5/10—Tetrapeptides
    • C07K5/1024—Tetrapeptides with the first amino acid being heterocyclic
    • 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)
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  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
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  • AIDS & HIV (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Claims (11)

1. Forbindelse med formlen:
eller et farmaceutisk acceptabelt salt deraf, til anvendelse ved behandling af inflammation, neurodegenerativ sygdom, muskelsvindssygdomme, cancer, kroniske infektionssygdomme, en hyperproliferativ tilstand, muskelinaktivitet, immunrelaterede tilstande, til anvendelse ved hæmning eller reduktion af HIV-infektion, til anvendelse ved påvirkning af niveauet af viral genekspression hos et individ eller til anvendelse ved ændring i udvalget af antigene peptider, som fremstilles af proteasomet i en organisme.
2. Farmaceutisk sammensætning, som omfatter forbindelsen ifølge krav 1 eller et farmaceutisk acceptabelt salt deraf, og et farmaceutisk acceptabelt fortyndingsmiddel eller en farmaceutisk acceptabel bærer, til anvendelse ved behandling af inflammation, neurodegenerativ sygdom, muskelsvindssygdomme, cancer, kroniske infektionssygdomme, en hyperproliferativ tilstand, muskelinaktivitet, immunrelaterede tilstande, til anvendelse ved hæmning eller reduktion af HIV-infektion, til anvendelse ved påvirkning af niveauet af viral genekspression hos et individ eller til anvendelse ved ændring i udvalget af antigene peptider, som fremstilles af proteasomet i en organisme.
3. Farmaceutisk sammensætning ifølge krav 2 til anvendelse ved behandling af cancer, hvor canceren er en hæmrelateret malignitet.
4. Farmaceutisk sammensætning ifølge krav 2 til anvendelse ved behandling af cancer, hvor canceren er myelomatose.
5. Forbindelse ifølge krav 1 til anvendelse ved behandling af cancer, hvor canceren er en hæmrelateret malignitet.
6. Forbindelse ifølge krav 1 til anvendelse ved behandling af cancer, hvor canceren er myelomatose.
7. Forbindelse ifølge krav 1 til anvendelse ved behandling af cancer, hvor canceren er en solid tumor.
8. Farmaceutisk sammensætning ifølge krav 2 til anvendelse ved behandling af cancer, hvor canceren er en solid tumor.
9. Farmaceutisk sammensætning ifølge et hvilket som helst af kravene 2, 3, 4 eller 8, som er en oralt tilgængelig doseringsform valgt blandt en tablet, en kapsel, et granulat, et pulver og en syrup.
10. Farmaceutisk sammensætning ifølge krav 9, hvor forbindelsen eller det farmaceutisk acceptable salt deraf forefindes i en mængde i intervallet fra 0,01 til 2000 mg.
11. Farmaceutisk sammensætning ifølge krav 9, hvor forbindelsen eller det farmaceutisk acceptable salt deraf forefindes i en mængde i intervallet fra 0,01 til ca. 50 mg/kg.
DK13157801.5T 2005-11-09 2006-11-09 Forbindelse til enzymhæmning DK2623113T3 (da)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US73611805P 2005-11-09 2005-11-09
US84258206P 2006-09-05 2006-09-05
EP06837164.0A EP1948678B1 (en) 2005-11-09 2006-11-09 Compounds for enzyme inhibition

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DK2623113T3 true DK2623113T3 (da) 2017-07-17

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DK13157801.5T DK2623113T3 (da) 2005-11-09 2006-11-09 Forbindelse til enzymhæmning
DK06837164.0T DK1948678T3 (da) 2005-11-09 2006-11-09 Forbindelser til enzyminhibering

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DK06837164.0T DK1948678T3 (da) 2005-11-09 2006-11-09 Forbindelser til enzyminhibering

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US (8) US7687456B2 (da)
EP (2) EP2623113B1 (da)
JP (3) JP5436860B2 (da)
KR (3) KR101434522B1 (da)
CN (2) CN105237621A (da)
AU (1) AU2006311584B2 (da)
BR (1) BRPI0618468A2 (da)
CA (1) CA2629084C (da)
CY (1) CY1119405T1 (da)
DK (2) DK2623113T3 (da)
EC (1) ECSP088460A (da)
ES (2) ES2628620T3 (da)
GT (1) GT200800063A (da)
HK (2) HK1121172A1 (da)
HN (1) HN2008000738A (da)
HU (1) HUE034863T2 (da)
IL (2) IL191344A (da)
LT (1) LT2623113T (da)
MX (1) MX2008006090A (da)
MY (2) MY171061A (da)
NZ (2) NZ595196A (da)
PH (1) PH12013501656A1 (da)
PL (2) PL1948678T3 (da)
PT (2) PT2623113T (da)
RU (2) RU2453556C2 (da)
SI (1) SI2623113T1 (da)
SV (1) SV2009002903A (da)
WO (1) WO2007056464A1 (da)
ZA (1) ZA200804455B (da)

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