CA2264227A1 - Promedicaments hydrolysables pour la liberation de medicaments anticancereux dans des cellules metastatiques - Google Patents

Promedicaments hydrolysables pour la liberation de medicaments anticancereux dans des cellules metastatiques Download PDF

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Publication number
CA2264227A1
CA2264227A1 CA002264227A CA2264227A CA2264227A1 CA 2264227 A1 CA2264227 A1 CA 2264227A1 CA 002264227 A CA002264227 A CA 002264227A CA 2264227 A CA2264227 A CA 2264227A CA 2264227 A1 CA2264227 A1 CA 2264227A1
Authority
CA
Canada
Prior art keywords
peptide
aminobenzyl
amino
hydrolyzable
prodrug
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.)
Abandoned
Application number
CA002264227A
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English (en)
Inventor
Raymond A. Firestone
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.)
Bristol Myers Squibb Co
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Individual
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 Individual filed Critical Individual
Publication of CA2264227A1 publication Critical patent/CA2264227A1/fr
Abandoned legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/78—Connective tissue peptides, e.g. collagen, elastin, laminin, fibronectin, vitronectin or cold insoluble globulin [CIG]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • 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
    • C07K5/06052—Val-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
    • C07K5/06078—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
    • C07K5/08—Tripeptides
    • C07K5/0815—Tripeptides with the first amino acid being basic
    • 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)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Toxicology (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Les promédicaments hydrolysables selon l'invention sont activés par des protéases situées dans les membranes cellulaires de cellules métastatiques, de sorte que soient produits des médicaments anticancéreux actifs pouvant être absorbés par les cellules métastatiques. En général, un promédicament hydrolysable selon l'invention, comprend un peptide coiffé d'un N-terminal et qui constitue un substrat pour une peptidohydrolase située à la surface d'une cellule métastatique liée de manière covalente à un médicament thérapeutique par l'intermédiaire d'un espaceur à auto-immolation présentant une longueur suffisante pour empêcher l'apparition d'un empêchement stérique. Le médicament thérapeutique est généralement un médicament anti-cancéreux, généralement de la doxorubicine, du taxol, de la camptothécine, de la mitomycine C ou de l'espéramycine. Généralement, la peptidohydrolase qui hydrolyse le substrat du promédicament hydrolysable est de la cathepsine B.
CA002264227A 1996-09-27 1997-09-25 Promedicaments hydrolysables pour la liberation de medicaments anticancereux dans des cellules metastatiques Abandoned CA2264227A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US4433496P 1996-09-27 1996-09-27
US60/044,334 1996-09-27
PCT/US1997/017410 WO1998013059A1 (fr) 1996-09-27 1997-09-25 Promedicaments hydrolysables pour la liberation de medicaments anticancereux dans des cellules metastatiques

Publications (1)

Publication Number Publication Date
CA2264227A1 true CA2264227A1 (fr) 1998-04-02

Family

ID=21931799

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002264227A Abandoned CA2264227A1 (fr) 1996-09-27 1997-09-25 Promedicaments hydrolysables pour la liberation de medicaments anticancereux dans des cellules metastatiques

Country Status (4)

Country Link
EP (1) EP0961619A4 (fr)
AU (1) AU739028B2 (fr)
CA (1) CA2264227A1 (fr)
WO (1) WO1998013059A1 (fr)

Families Citing this family (135)

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EP0961619A1 (fr) 1999-12-08
AU739028B2 (en) 2001-10-04

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