WO2003094972A3 - Fap-activated anti-tumor prodrugs - Google Patents

Fap-activated anti-tumor prodrugs Download PDF

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Publication number
WO2003094972A3
WO2003094972A3 PCT/EP2003/004713 EP0304713W WO03094972A3 WO 2003094972 A3 WO2003094972 A3 WO 2003094972A3 EP 0304713 W EP0304713 W EP 0304713W WO 03094972 A3 WO03094972 A3 WO 03094972A3
Authority
WO
WIPO (PCT)
Prior art keywords
prodrugs
fap
fapα
cytotoxic
carboxylic acid
Prior art date
Application number
PCT/EP2003/004713
Other languages
French (fr)
Other versions
WO2003094972A2 (en
Inventor
Erik Patzelt
John Edward Park
Stefan Peters
Original Assignee
Boehringer Ingelheim Pharma
Erik Patzelt
John Edward Park
Stefan Peters
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 Boehringer Ingelheim Pharma, Erik Patzelt, John Edward Park, Stefan Peters filed Critical Boehringer Ingelheim Pharma
Priority to EP03727438A priority Critical patent/EP1506221A2/en
Priority to AU2003233238A priority patent/AU2003233238A1/en
Publication of WO2003094972A2 publication Critical patent/WO2003094972A2/en
Publication of WO2003094972A3 publication Critical patent/WO2003094972A3/en

Links

Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

The present invention relates to prodrugs which are capable of being converted into prodrug intermediates of a cytotoxic or cytostatic drug, by the catalytic action of FAPα, said prodrugs exhibit- an oligomeric part comprising up to (9) amino carboxylic acid residues, the amide bond between the C-terminal amino carboxylic acid and the preceding amino acid thereof is recognized and cleaved by FAPα in the immediate environment of a target cell, and- a cytotoxic or cytostatic part, wherein the N-terminal amino function of the oligomeric part is attached to a capping group (Cg).
PCT/EP2003/004713 2002-05-10 2003-05-06 Fap-activated anti-tumor prodrugs WO2003094972A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP03727438A EP1506221A2 (en) 2002-05-10 2003-05-06 Fap-activated anti-tumor prodrugs
AU2003233238A AU2003233238A1 (en) 2002-05-10 2003-05-06 Fap-activated anti-tumor prodrugs

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP02010552 2002-05-10
EP02010552.4 2002-05-10

Publications (2)

Publication Number Publication Date
WO2003094972A2 WO2003094972A2 (en) 2003-11-20
WO2003094972A3 true WO2003094972A3 (en) 2004-03-18

Family

ID=29414680

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2003/004713 WO2003094972A2 (en) 2002-05-10 2003-05-06 Fap-activated anti-tumor prodrugs

Country Status (3)

Country Link
EP (1) EP1506221A2 (en)
AU (1) AU2003233238A1 (en)
WO (1) WO2003094972A2 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100047170A1 (en) * 2006-01-05 2010-02-25 Denmeade Samuel R Peptide Prodrugs
WO2015192124A1 (en) 2014-06-13 2015-12-17 Trustees Of Tufts College Fap-activated therapeutic agents, and uses related thereto
CN116635054A (en) 2020-12-22 2023-08-22 科比欧尔斯公司 Compounds comprising tetrapeptide moieties
WO2022167664A1 (en) 2021-02-07 2022-08-11 Cobiores Nv Compounds comprising a tetrapeptidic moiety

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997014416A1 (en) * 1995-10-18 1997-04-24 Merck & Co., Inc. Conjugates useful in the treatment of benign prostatic hyperplasia
WO2000033888A2 (en) * 1998-12-11 2000-06-15 Coulter Pharmaceutical, Inc. Prodrug compounds and process for preparation thereof
WO2000071571A2 (en) * 1999-05-14 2000-11-30 Boehringer Ingelheim Pharma Kg Fap-activated anti-tumor compounds
WO2002100353A2 (en) * 2001-06-11 2002-12-19 Medarex, Inc. Cd10-activated prodrug compounds

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997014416A1 (en) * 1995-10-18 1997-04-24 Merck & Co., Inc. Conjugates useful in the treatment of benign prostatic hyperplasia
WO2000033888A2 (en) * 1998-12-11 2000-06-15 Coulter Pharmaceutical, Inc. Prodrug compounds and process for preparation thereof
WO2000071571A2 (en) * 1999-05-14 2000-11-30 Boehringer Ingelheim Pharma Kg Fap-activated anti-tumor compounds
WO2002100353A2 (en) * 2001-06-11 2002-12-19 Medarex, Inc. Cd10-activated prodrug compounds

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
BREISTOL K ET AL: "The antitumour activity of the prodrug N-l-leucyl-doxorubicin and its parent compound doxorubicin in human tumour xenografts", EUROPEAN JOURNAL OF CANCER, PERGAMON PRESS, OXFORD, GB, vol. 34, no. 10, September 1998 (1998-09-01), pages 1602 - 1606, XP004285055, ISSN: 0959-8049 *

Also Published As

Publication number Publication date
WO2003094972A2 (en) 2003-11-20
AU2003233238A1 (en) 2003-11-11
AU2003233238A8 (en) 2003-11-11
EP1506221A2 (en) 2005-02-16

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