WO2011054837A3 - Bifunktionale prodrugs und drugs - Google Patents

Bifunktionale prodrugs und drugs Download PDF

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Publication number
WO2011054837A3
WO2011054837A3 PCT/EP2010/066688 EP2010066688W WO2011054837A3 WO 2011054837 A3 WO2011054837 A3 WO 2011054837A3 EP 2010066688 W EP2010066688 W EP 2010066688W WO 2011054837 A3 WO2011054837 A3 WO 2011054837A3
Authority
WO
WIPO (PCT)
Prior art keywords
drugs
prodrugs
bifunctional
bifunctional prodrugs
relates
Prior art date
Application number
PCT/EP2010/066688
Other languages
English (en)
French (fr)
Other versions
WO2011054837A2 (de
Inventor
Lutz Tietze
Jan Marian Von Hof
Original Assignee
Georg-August-Universität Göttingen Stiftung Öffenlichen Rechts
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 Georg-August-Universität Göttingen Stiftung Öffenlichen Rechts filed Critical Georg-August-Universität Göttingen Stiftung Öffenlichen Rechts
Publication of WO2011054837A2 publication Critical patent/WO2011054837A2/de
Publication of WO2011054837A3 publication Critical patent/WO2011054837A3/de

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/02Heterocyclic radicals containing only nitrogen as ring hetero atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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 an organic compound
    • A61K47/55Medicinal 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 an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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 an organic compound
    • A61K47/555Medicinal 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 an organic compound pre-targeting systems involving an organic compound, other than a peptide, protein or antibody, for targeting specific cells
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56Ring systems containing three or more rings
    • C07D209/58[b]- or [c]-condensed
    • C07D209/60Naphtho [b] pyrroles; Hydrogenated naphtho [b] pyrroles

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Die vorliegende Erfindung richtet sich auf neue Verbindungen, genauer auf neue bifunktionale Prodrugs und Drugs. In einem weiteren Aspekt richtet sich die vorliegende Erfindung auf pharmazeutische Zusammensetzungen enthaltend diese Prodrugs und Drugs sowie deren Verwendung als Zytostatika in der Tumortherapie. Die erfindungsgemäßen Verbindungen beruhen dabei auf CC-1065 Analoga.
PCT/EP2010/066688 2009-11-03 2010-11-03 Bifunktionale prodrugs und drugs WO2011054837A2 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DEDE102009051799.5 2009-11-03
DE102009051799.5A DE102009051799B4 (de) 2009-11-03 2009-11-03 Bifunktionale Prodrugs und Drugs

Publications (2)

Publication Number Publication Date
WO2011054837A2 WO2011054837A2 (de) 2011-05-12
WO2011054837A3 true WO2011054837A3 (de) 2011-09-15

Family

ID=43569318

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2010/066688 WO2011054837A2 (de) 2009-11-03 2010-11-03 Bifunktionale prodrugs und drugs

Country Status (2)

Country Link
DE (1) DE102009051799B4 (de)
WO (1) WO2011054837A2 (de)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2857649T3 (es) 2012-03-01 2021-09-29 Array Biopharma Inc Inhibidores de serina/treonina cinasa
SG11201601005XA (en) * 2013-08-12 2016-03-30 Genentech Inc 1-(chloromethyl)-2,3-dihydro-1h-benzo[e]indole dimer antibody-drug conjugate compounds, and methods of use and treatment
CA2929565A1 (en) * 2013-12-16 2015-06-25 Genentech, Inc. 1-(chloromethyl)-2,3-dihydro-1h-benzo[e]indole dimer antibody-drug conjugate compounds, and methods of use and treatment
BR112016013861A2 (pt) 2013-12-16 2017-10-10 Genentech Inc conjugados de droga e anticorpo, compostos, método de tratamento e composição farmacêutica
CA2937731C (en) 2014-01-27 2019-09-24 Pfizer Inc. Bifunctional cytotoxic agents
ES2785551T3 (es) 2014-06-30 2020-10-07 Glykos Finland Oy Derivado de sacárido de una carga útil tóxica y sus conjugados con anticuerpos
SG11201706991YA (en) 2015-03-20 2017-10-30 Pfizer Bifunctional cytotoxic agents containing the cti pharmacophore
EP3271365B1 (de) * 2015-03-20 2019-12-18 Pfizer Inc Bifunktionelle zytotoxische mittel mit cti-pharmakophor
CN108064246A (zh) 2015-06-15 2018-05-22 基因泰克公司 抗体和免疫结合物
DE102016105449A1 (de) 2015-10-29 2017-05-04 Georg-August-Universität Göttingen Stiftung Öffentlichen Rechts Bifunktionale Prodrugs

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE279390T1 (de) 2000-05-02 2004-10-15 Tietze Lutz F Prof Dr Neue prodrugs von 6-hydroxy-2,3-dihydro-1h- indolen, 5-hydroxy-1,2-dihydro-3h-pyrrolo 3,2- e)indolen und 5-hydroxy-1,2-dihydro-3h-benzo e)indolen sowie von 6-hydroxy-1,2,3,4-tetrahydro- benzo f)chinolin-derivaten für eine selektive krebstherapie
MX2008009956A (es) 2006-02-02 2008-12-12 Syntarga Bv Analogos de cc-1065 solubles en agua y sus conjugados.

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
FUKUDA Y ET AL: "The novel cyclopropapyrroloindole(CPI) bisalkylators bearing 3,3'-(1,4-phenylene)diacryloyl group as a linker", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, ELSEVIER SCIENCE, GB, vol. 8, no. 15, 4 August 1998 (1998-08-04), pages 2003 - 2004, XP004137175, ISSN: 0960-894X, DOI: DOI:10.1016/S0960-894X(98)00346-1 *
JIA G ET AL: "Design, synthesis and cytotoxicity evaluation of 1-chloromethyl-5-hydroxy-1,2-dihydro-3H-benz[e]indole (seco-CBI) dimers", BIOORGANIC AND MEDICINAL CHEMISTRY 200007 GB LNKD- DOI:10.1016/S0968-0896(00)00088-2, vol. 8, no. 7, July 2000 (2000-07-01), pages 1607 - 1617, XP002624235, ISSN: 0968-0896 *
KUMAR ROHTASH ET AL: "Synthesis and cytotoxicity evaluation of novel C7-c7, C7-N3 and N3-N3 dimers of 1-chloromethyl-5-hydroxy-1,2-dihydro-3H-benzo[e]indole (seco-CBI) with pyrrole and imidazole polyamide conjugates.", ORGANIC & BIOMOLECULAR CHEMISTRY 7 AUG 2003 LNKD- PUBMED:12948187, vol. 1, no. 15, 7 August 2003 (2003-08-07), pages 2630 - 2647, XP002624236, ISSN: 1477-0520 *
MITCHELL M A ET AL: "Synthesis and DNA cross-linking by a rigid CPI dimer", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY 1991 US, vol. 113, no. 23, 1991, pages 8994 - 8995, XP002624234, ISSN: 0002-7863 *
SCHWARTZ G H ET AL: "A phase I study of bizelesin, a highly potent and selective DNA-interactive agent, in patients with advanced solid malignancies", ANNALS OF ONCOLOGY 20030501 GB LNKD- DOI:10.1093/ANNONC/MDG215, vol. 14, no. 5, 1 May 2003 (2003-05-01), pages 775 - 782, XP002624233, ISSN: 0923-7534 *
TIETZE L F ET AL: "ENZYME AND PROTON-ACTIVATED PRODRUGS FOR A SELECTIVE CANCER THERAPY", CURRENT PHARMACEUTICAL DESIGN, BENTHAM SCIENCE PUBLISHERS, NL, vol. 9, no. 26, 1 January 2003 (2003-01-01), pages 2155 - 2175, XP008028312, ISSN: 1381-6128, DOI: DOI:10.2174/1381612033454072 *

Also Published As

Publication number Publication date
DE102009051799B4 (de) 2021-07-01
DE102009051799A1 (de) 2011-05-05
WO2011054837A2 (de) 2011-05-12

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