WO2001097794A8 - Inhibitors of matriptase for the treatment of cancer - Google Patents

Inhibitors of matriptase for the treatment of cancer

Info

Publication number
WO2001097794A8
WO2001097794A8 PCT/US2001/018773 US0118773W WO0197794A8 WO 2001097794 A8 WO2001097794 A8 WO 2001097794A8 US 0118773 W US0118773 W US 0118773W WO 0197794 A8 WO0197794 A8 WO 0197794A8
Authority
WO
WIPO (PCT)
Prior art keywords
matriptase
subject
inhibitors
cancer
treatment
Prior art date
Application number
PCT/US2001/018773
Other languages
French (fr)
Other versions
WO2001097794A2 (en
WO2001097794A3 (en
Inventor
Chen-Yong Lin
Robert B Dickson
Shaomeng Wang
Istvan Enyedy
Sheau-Ling Lee
Original Assignee
Univ Georgetown
Chen-Yong Lin
Robert B Dickson
Shaomeng Wang
Istvan Enyedy
Sheau-Ling Lee
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 Univ Georgetown, Chen-Yong Lin, Robert B Dickson, Shaomeng Wang, Istvan Enyedy, Sheau-Ling Lee filed Critical Univ Georgetown
Priority to AU2001266838A priority Critical patent/AU2001266838A1/en
Priority to EP01944426A priority patent/EP1355637A2/en
Publication of WO2001097794A2 publication Critical patent/WO2001097794A2/en
Publication of WO2001097794A3 publication Critical patent/WO2001097794A3/en
Publication of WO2001097794A8 publication Critical patent/WO2001097794A8/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/655Azo (—N=N—), diazo (=N2), azoxy (>N—O—N< or N(=O)—N<), azido (—N3) or diazoamino (—N=N—N<) compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/155Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00Preparations for testing in vivo
    • A61K49/0002General or multifunctional contrast agents, e.g. chelated agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/574Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/90Enzymes; Proenzymes
    • G01N2333/914Hydrolases (3)
    • G01N2333/948Hydrolases (3) acting on peptide bonds (3.4)
    • G01N2333/95Proteinases, i.e. endopeptidases (3.4.21-3.4.99)
    • G01N2333/964Proteinases, i.e. endopeptidases (3.4.21-3.4.99) derived from animal tissue
    • G01N2333/96425Proteinases, i.e. endopeptidases (3.4.21-3.4.99) derived from animal tissue from mammals
    • G01N2333/96427Proteinases, i.e. endopeptidases (3.4.21-3.4.99) derived from animal tissue from mammals in general
    • G01N2333/9643Proteinases, i.e. endopeptidases (3.4.21-3.4.99) derived from animal tissue from mammals in general with EC number
    • G01N2333/96486Metalloendopeptidases (3.4.24)

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Microbiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Biotechnology (AREA)
  • Cell Biology (AREA)
  • Hospice & Palliative Care (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention relates to a method of inhibiting carcinoma progression wherein matriptase plays a role in a subject in need of such inhibition including administering to a subject an effective amount of a compound comprising two positively charged groups, which are the same or different. The groups are linked by a chemical group having a length of between 5 and 30 A, and preferably between 15 and 24 A. Diagnostic methods based on matriptase action and therapeutic methods involving inhibition of matriptase activity are provided. Exemplary compounds are pentamidine and analogs thereof.
PCT/US2001/018773 2000-06-21 2001-06-12 Inhibitors of matriptase for the treatment of cancer WO2001097794A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2001266838A AU2001266838A1 (en) 2000-06-21 2001-06-12 Inhibitors of matriptase for the treatment of cancer
EP01944426A EP1355637A2 (en) 2000-06-21 2001-06-12 Inhibitors of matriptase for the treatment of cancer

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US21307300P 2000-06-21 2000-06-21
US60/213,073 2000-06-21

Publications (3)

Publication Number Publication Date
WO2001097794A2 WO2001097794A2 (en) 2001-12-27
WO2001097794A3 WO2001097794A3 (en) 2003-08-21
WO2001097794A8 true WO2001097794A8 (en) 2003-10-30

Family

ID=22793641

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/018773 WO2001097794A2 (en) 2000-06-21 2001-06-12 Inhibitors of matriptase for the treatment of cancer

Country Status (3)

Country Link
EP (1) EP1355637A2 (en)
AU (1) AU2001266838A1 (en)
WO (1) WO2001097794A2 (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9290757B2 (en) 2006-07-05 2016-03-22 Catalyst Biosciences, Inc. Protease screening methods and proteases identified thereby
US9359598B2 (en) 2004-04-12 2016-06-07 Catalyst Biosciences, Inc. Mutant MT-SP1 proteases with altered substrate specificity or activity

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6797504B1 (en) 2000-09-08 2004-09-28 Dendreon San Diego Llc Inhibitors of serine protease activity of matriptase or MTSP1
US7157596B2 (en) 2000-09-08 2007-01-02 Dendreon Corporation Inhibitors of serine protease activity of matriptase or MTSP1
WO2003076391A2 (en) 2002-03-11 2003-09-18 Curacyte Ag Urokinase inhibitors, production and use thereof
US7939304B2 (en) 2002-10-02 2011-05-10 Catalyst Biosciences, Inc. Mutant MT-SP1 proteases with altered substrate specificity or activity
US7019019B2 (en) 2002-12-23 2006-03-28 Dendreon Corporation Matriptase inhibitors and methods of use
DE10301300B4 (en) 2003-01-15 2009-07-16 Curacyte Chemistry Gmbh Use of acylated 4-amidino- and 4-guanidinobenzylamines for the inhibition of plasma kallikrein
DE10322191B4 (en) 2003-05-16 2014-02-27 The Medicines Company (Leipzig) Gmbh N-sulfonylated amino acid derivatives, process for their preparation and their use
DE10342108A1 (en) 2003-09-11 2005-04-14 Curacyte Chemistry Gmbh Basic substituted benzylamine analogs as coagulation factor Xa inhibitors, their preparation and use
US7439226B2 (en) 2003-09-30 2008-10-21 The United States Of America As Represented By The Department Of Health And Human Services Serine protease inhibitors
DE102006050672A1 (en) 2006-10-24 2008-04-30 Curacyte Discovery Gmbh New glycylglycine derivatives with a benzylsulfonylamido group and an amidino-organylamido group at the opposite chain ends, used in drugs for reducing loss of blood, e.g. in operations
DE102008007440A1 (en) * 2008-02-01 2009-08-13 Dritte Patentportfolio Beteiligungsgesellschaft Mbh & Co.Kg Amino acid derivatives as drugs
SG175711A1 (en) 2009-05-18 2011-12-29 Orion Corp Protease inhibitors
US10175238B2 (en) * 2014-05-13 2019-01-08 Georgetown University Markers for abnormal cells
MX2019007522A (en) * 2016-12-22 2019-11-08 Verlyx Pharma Inc Amidine substituted analogues and uses thereof.

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH525897A (en) * 1961-09-11 1972-07-31 Wander Ag Dr A Cyclic bis-amidine cpds - esp useful as tuberculostats
AU4432597A (en) * 1996-09-25 1998-04-17 Regents Of The University Of California, The Methods of using agmatine to reduce intracellular polyamine levels and to inhibit inducible nitric oxide synthase
MXPA01011000A (en) * 1999-04-30 2003-06-30 Slil Biomedical Corp Conformationally restricted polyamine analogs as disease therapies.
AU780538B2 (en) * 1999-11-16 2005-03-24 Oncozyme Pharma Inc. Inhibitors of endo-exonuclease activity for treating cancer
DE19955476A1 (en) * 1999-11-18 2001-05-23 Boehringer Ingelheim Pharma Bis-basic compounds as tryptase inhibitors, process for their preparation and their use as medicaments

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9359598B2 (en) 2004-04-12 2016-06-07 Catalyst Biosciences, Inc. Mutant MT-SP1 proteases with altered substrate specificity or activity
US9290757B2 (en) 2006-07-05 2016-03-22 Catalyst Biosciences, Inc. Protease screening methods and proteases identified thereby

Also Published As

Publication number Publication date
WO2001097794A2 (en) 2001-12-27
WO2001097794A3 (en) 2003-08-21
EP1355637A2 (en) 2003-10-29
AU2001266838A1 (en) 2002-01-02

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