WO2000005245A3 - Inhibitors of urokinase and blood vessel formation - Google Patents

Inhibitors of urokinase and blood vessel formation Download PDF

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Publication number
WO2000005245A3
WO2000005245A3 PCT/US1999/016577 US9916577W WO0005245A3 WO 2000005245 A3 WO2000005245 A3 WO 2000005245A3 US 9916577 W US9916577 W US 9916577W WO 0005245 A3 WO0005245 A3 WO 0005245A3
Authority
WO
WIPO (PCT)
Prior art keywords
urokinase
blood vessel
vessel formation
inhibitors
arginine
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.)
Ceased
Application number
PCT/US1999/016577
Other languages
French (fr)
Other versions
WO2000005245A2 (en
Inventor
Terence K Brunck
Susan Y Tamura
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.)
Dendreon Pharmaceuticals LLC
Original Assignee
Corvas International Inc
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 Corvas International Inc filed Critical Corvas International Inc
Priority to JP2000561201A priority Critical patent/JP2002521386A/en
Priority to IL14093999A priority patent/IL140939A0/en
Priority to KR1020017000985A priority patent/KR20010083140A/en
Priority to CA2338524A priority patent/CA2338524C/en
Priority to AU50058/99A priority patent/AU772024B2/en
Priority to NZ509400A priority patent/NZ509400A/en
Priority to EP99934173A priority patent/EP1100814A2/en
Priority to PL99345960A priority patent/PL345960A1/en
Publication of WO2000005245A2 publication Critical patent/WO2000005245A2/en
Publication of WO2000005245A3 publication Critical patent/WO2000005245A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • 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
    • C07K5/0606—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
    • C07K5/06069—Ser-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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/12—Keratolytics, e.g. wart or anti-corn preparations
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Novel compounds having activity inhibitors of urokinase and in reducing or inhibiting blood vessel formation are provided. These compounds have an arginine or arginine mimic aldehyde or an arginine ketoamide group at P1. These compounds are useful in vitro for monitoring plasminogen activator levels and in vivo in treatment of conditions which are ameliorated by inhibition of or decreased activity of urokinase and in treating pathologic conditions wherein blood vessel formation is related to a pathologic condition.
PCT/US1999/016577 1998-07-24 1999-07-22 Inhibitors of urokinase and blood vessel formation Ceased WO2000005245A2 (en)

Priority Applications (8)

Application Number Priority Date Filing Date Title
JP2000561201A JP2002521386A (en) 1998-07-24 1999-07-22 Urokinase and angiogenesis inhibitors
IL14093999A IL140939A0 (en) 1998-07-24 1999-07-22 Inhibitors of urokinase and blood vessel formation
KR1020017000985A KR20010083140A (en) 1998-07-24 1999-07-22 Inhibitors of Urokinase and Blood Vessel Formation
CA2338524A CA2338524C (en) 1998-07-24 1999-07-22 Inhibitors of urokinase and blood vessel formation
AU50058/99A AU772024B2 (en) 1998-07-24 1999-07-22 Inhibitors of urokinase and blood vessel formation
NZ509400A NZ509400A (en) 1998-07-24 1999-07-22 Inhibitors of urokinase and blood vessel formation
EP99934173A EP1100814A2 (en) 1998-07-24 1999-07-22 Inhibitors of urokinase and blood vessel formation
PL99345960A PL345960A1 (en) 1998-07-24 1999-07-22 Inhibitors of urokinase and blood vessel formation

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US09/121,921 US6576613B1 (en) 1998-07-24 1998-07-24 Title inhibitors of urokinase
US09/121,921 1998-07-24

Publications (2)

Publication Number Publication Date
WO2000005245A2 WO2000005245A2 (en) 2000-02-03
WO2000005245A3 true WO2000005245A3 (en) 2000-04-20

Family

ID=22399547

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1999/016577 Ceased WO2000005245A2 (en) 1998-07-24 1999-07-22 Inhibitors of urokinase and blood vessel formation

Country Status (11)

Country Link
US (2) US6576613B1 (en)
EP (1) EP1100814A2 (en)
JP (1) JP2002521386A (en)
KR (1) KR20010083140A (en)
CN (1) CN1313863A (en)
AU (1) AU772024B2 (en)
CA (1) CA2338524C (en)
IL (1) IL140939A0 (en)
NZ (1) NZ509400A (en)
PL (1) PL345960A1 (en)
WO (1) WO2000005245A2 (en)

Families Citing this family (34)

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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
AR029903A1 (en) * 2000-04-05 2003-07-23 Schering Corp MACROCICLIC INHIBITORS OF THE NS3-SERINA PROTEASA, OF THE VIRUS OF HEPATITIS C, WHICH INCLUDE P2 N-CYCLING PARTS, PHARMACEUTICAL COMPOSITIONS AND USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT
DE10029014A1 (en) 2000-06-15 2001-12-20 Univ Schiller Jena Urokinase inhibitors
DK1385870T3 (en) 2000-07-21 2010-07-05 Schering Corp Peptides as inhibitors of NS3 serine protease from hepatitis C virus
KR20030081297A (en) 2000-07-21 2003-10-17 쉐링 코포레이션 Novel peptides as NS3-serine protease inhibitors of hepatitis C virus
US7244721B2 (en) * 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
DE60034447T2 (en) * 2000-08-11 2008-02-14 Wilex Ag Noncovalent urokinase and angiogenesis inhibitors
AU785260B2 (en) * 2000-08-11 2006-12-07 Wilex Ag Non-covalent inhibitors of urokinase and blood vessel formation
US7157596B2 (en) 2000-09-08 2007-01-02 Dendreon Corporation Inhibitors of serine protease activity of matriptase or MTSP1
US7112430B2 (en) * 2001-05-14 2006-09-26 Dendreon Corporation Nucleic acid molecules encoding a transmembrane serine protease 10, the encoded polypeptides and methods based thereon
SI1453852T1 (en) * 2001-12-12 2007-06-30 Wilex Ag Selective urokinase inhibitors
AU2003219039A1 (en) 2002-03-11 2003-09-22 Curacyte Ag Urokinase inhibitors, production and use thereof
US20030228365A1 (en) * 2002-06-07 2003-12-11 Fortuna Haviv Pharmaceutical formulation
CA2499523C (en) * 2002-09-20 2011-04-19 Medisyn Technologies, Inc. Therapeutic agents and corresponding treatments
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
DE10342108A1 (en) 2003-09-11 2005-04-14 Curacyte Chemistry Gmbh Basic substituted benzylamine analogs as coagulation factor Xa inhibitors, their preparation and use
US7252834B2 (en) 2005-04-25 2007-08-07 Clemson University Research Foundation (Curf) Elastin stabilization of connective tissue
MX2007016439A (en) 2005-06-24 2008-03-04 Wilex Ag Use of urokinase inhibitors for the treatment and/or prevention of neuropathological diseases.
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
WO2009064806A1 (en) * 2007-11-12 2009-05-22 Endologix, Inc. Method and agent for in-situ stabilization of vascular tissue
US20110028397A1 (en) 2007-11-30 2011-02-03 Toezser Jozsef Use of Urokinase Type Plasminogen Activator Inhibitors for the Treatment of Corneal Disorders
US20090214654A1 (en) * 2008-02-21 2009-08-27 Isenburg Jason C Treatment of aneurysm with application of connective tissue stabilization agent in combination with a delivery vehicle
US20100016833A1 (en) * 2008-07-15 2010-01-21 Ogle Matthew F Devices for the Treatment of Vascular Aneurysm
US20100267803A1 (en) * 2008-11-07 2010-10-21 The Research Foundation Of State University Of New York Regulators Of Fat Metabolism As Anti-Cancer Targets
US20100119605A1 (en) * 2008-11-12 2010-05-13 Isenburg Jason C Compositions for tissue stabilization
US20100261662A1 (en) * 2009-04-09 2010-10-14 Endologix, Inc. Utilization of mural thrombus for local drug delivery into vascular tissue
WO2011044455A1 (en) * 2009-10-09 2011-04-14 Vatrix Medical, Inc. In vivo chemical stabilization of vulnerable plaque
US8444624B2 (en) * 2009-10-19 2013-05-21 Vatrix Medical, Inc. Vascular medical devices with sealing elements and procedures for the treatment of isolated vessel sections
KR101228668B1 (en) * 2010-09-17 2013-01-31 가톨릭대학교 산학협력단 Peptides inhibiting angiogenic activity and use thereof
US8911468B2 (en) 2011-01-31 2014-12-16 Vatrix Medical, Inc. Devices, therapeutic compositions and corresponding percutaneous treatment methods for aortic dissection
EP2709711B8 (en) 2011-05-18 2017-03-22 Vatrix Medical, Inc. Coated balloons for blood vessel stabilization
US9283241B2 (en) 2012-07-10 2016-03-15 Clemson University Treatment to render implants resistant to diabetes
IT202100023357A1 (en) 2021-09-09 2023-03-09 Cheirontech S R L Peptides with anti-angiogenic activity

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5153176A (en) * 1990-08-01 1992-10-06 Nitto Boseki Co., Ltd. Tripeptide derivatives and protease inhibitor composition comprising the same
WO1994008941A1 (en) * 1992-10-16 1994-04-28 Corvas International, Inc. Arginine keto-amide enzyme inhibitors
US5508385A (en) * 1990-09-05 1996-04-16 Nitto Boseki Co., Ltd. Tripeptide derivatives containing pyroglutamic acid residue

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US3867364A (en) * 1968-11-21 1975-02-18 Microbial Chem Res Found Process for the synthesis of leupeptins and their analogues
EP0451130A3 (en) * 1990-04-05 1992-08-05 Baltimore Biotech, Inc. Use of amiloride and other pyrazine derivatives for preventing or treating ocular neovascularization
US5283293A (en) * 1990-12-14 1994-02-01 Corvas, Inc. Reagents for automated synthesis of peptide analogs
US5629327A (en) * 1993-03-01 1997-05-13 Childrens Hospital Medical Center Corp. Methods and compositions for inhibition of angiogenesis
AU735015B2 (en) 1996-06-10 2001-06-28 Scripps Research Institute, The Use of substrate subtraction libraries to distinguish enzyme specificities

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5153176A (en) * 1990-08-01 1992-10-06 Nitto Boseki Co., Ltd. Tripeptide derivatives and protease inhibitor composition comprising the same
US5508385A (en) * 1990-09-05 1996-04-16 Nitto Boseki Co., Ltd. Tripeptide derivatives containing pyroglutamic acid residue
WO1994008941A1 (en) * 1992-10-16 1994-04-28 Corvas International, Inc. Arginine keto-amide enzyme inhibitors

Non-Patent Citations (3)

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PATEL E.A.: "Transition-state affinity chromatography of trypsin-like proteinases with dipeptidyl argininal ligands", BIOCHIM.BIOPHYS.ACTA, vol. 748, 1983, pages 321 - 330, XP002120735 *

Also Published As

Publication number Publication date
AU772024B2 (en) 2004-04-08
US6432922B1 (en) 2002-08-13
CA2338524A1 (en) 2000-02-03
PL345960A1 (en) 2002-01-14
KR20010083140A (en) 2001-08-31
CN1313863A (en) 2001-09-19
NZ509400A (en) 2003-12-19
CA2338524C (en) 2013-01-22
AU5005899A (en) 2000-02-14
US6576613B1 (en) 2003-06-10
JP2002521386A (en) 2002-07-16
WO2000005245A2 (en) 2000-02-03
EP1100814A2 (en) 2001-05-23
IL140939A0 (en) 2002-02-10

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