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WO2002014349A3 - Inhibiteurs non covalents de l'urokinase et de la formation de vaisseaux sanguins - Google Patents

Inhibiteurs non covalents de l'urokinase et de la formation de vaisseaux sanguins Download PDF

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Publication number
WO2002014349A3
WO2002014349A3 PCT/US2001/025337 US0125337W WO0214349A3 WO 2002014349 A3 WO2002014349 A3 WO 2002014349A3 US 0125337 W US0125337 W US 0125337W WO 0214349 A3 WO0214349 A3 WO 0214349A3
Authority
WO
WIPO (PCT)
Prior art keywords
urokinase
blood vessel
vessel formation
covalent inhibitors
activity
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/US2001/025337
Other languages
English (en)
Other versions
WO2002014349A2 (fr
Inventor
Odile Esther Levy
Edwin L Madison
Joseph Edward Semple
Amir P Tamiz
Michael I Weinhouse
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
Priority claimed from US09/733,645 external-priority patent/US6586405B2/en
Priority to IL14904201A priority Critical patent/IL149042A0/xx
Priority to JP2002519486A priority patent/JP2004506648A/ja
Priority to CA002387002A priority patent/CA2387002A1/fr
Priority to NZ518195A priority patent/NZ518195A/en
Priority to AU83347/01A priority patent/AU785260B2/en
Application filed by Corvas International Inc filed Critical Corvas International Inc
Publication of WO2002014349A2 publication Critical patent/WO2002014349A2/fr
Priority to IL149042A priority patent/IL149042A/en
Publication of WO2002014349A3 publication Critical patent/WO2002014349A3/fr
Anticipated expiration legal-status Critical
Priority to AU2006235835A priority patent/AU2006235835B2/en
Ceased legal-status Critical Current

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    • 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
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • A61P31/10—Antimycotics
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • 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
    • 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
    • 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
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • 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
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Biochemistry (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

L'invention concerne de nouveaux composés présentant une activité d'inhibiteurs non covalents de l'urokinase ainsi qu'une activité de réduction ou d'inhibition de la formation de vaisseaux sanguins. Ces composés comportent en P1 un groupe portant un fragment amidino ou guanidino ou un dérivé de ce fragment. Ces composés servent au contrôle in vivo de niveaux d'activateurs de plasminogène, au traitement in vivo d'affections pouvant être traitées par inhibition ou réduction de l'activité de l'urokinase, ainsi qu'au traitement d'affections pathologiques dans lesquelles la formation de vaisseaux sanguins est liée à une affection pathologique.
PCT/US2001/025337 2000-08-11 2001-08-10 Inhibiteurs non covalents de l'urokinase et de la formation de vaisseaux sanguins Ceased WO2002014349A2 (fr)

Priority Applications (7)

Application Number Priority Date Filing Date Title
IL14904201A IL149042A0 (en) 2000-08-11 2001-08-10 Non-covalent inhibitors of urokinase and blood vessel formation
JP2002519486A JP2004506648A (ja) 2000-08-11 2001-08-10 ウロキナーゼおよび血管形成の非共有結合性インヒビター
CA002387002A CA2387002A1 (fr) 2000-08-11 2001-08-10 Inhibiteurs non covalents de l'urokinase et de la formation de vaisseaux sanguins
NZ518195A NZ518195A (en) 2000-08-11 2001-08-10 Non-covalent inhibitors of urokinase and blood vessel formation
AU83347/01A AU785260B2 (en) 2000-08-11 2001-08-10 Non-covalent inhibitors of urokinase and blood vessel formation
IL149042A IL149042A (en) 2000-08-11 2002-04-09 Non-covalent inhibitors of urokinase and vascular formation
AU2006235835A AU2006235835B2 (en) 2000-08-11 2006-11-03 Non-covalent inhibitors of urokinase and blood vessel formation

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US63748300A 2000-08-11 2000-08-11
US09/637,483 2000-08-11
US09/733,645 US6586405B2 (en) 2000-08-11 2000-12-07 Non-covalent inhibitors of urokinase and blood vessel formation
EP00126874.7 2000-12-07
US09/733,645 2000-12-07
EP00126874A EP1182207B1 (fr) 2000-08-11 2000-12-07 Inhibiteurs non-covalents de l'urokinase et de l'angiogenèse

Publications (2)

Publication Number Publication Date
WO2002014349A2 WO2002014349A2 (fr) 2002-02-21
WO2002014349A3 true WO2002014349A3 (fr) 2002-10-03

Family

ID=27223185

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/025337 Ceased WO2002014349A2 (fr) 2000-08-11 2001-08-10 Inhibiteurs non covalents de l'urokinase et de la formation de vaisseaux sanguins

Country Status (6)

Country Link
JP (1) JP2004506648A (fr)
AU (2) AU785260B2 (fr)
CA (1) CA2387002A1 (fr)
IL (1) IL149042A0 (fr)
NZ (3) NZ518195A (fr)
WO (1) WO2002014349A2 (fr)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1364960A4 (fr) * 2001-02-02 2005-05-18 Chugai Pharmaceutical Co Ltd Derives de peptide
US7125703B2 (en) 2001-03-13 2006-10-24 Dendreon Corporation Nucleic acid molecules encoding a transmembrane serine protease 7, the encoded polypeptides and methods based thereon
AU2002254357A1 (en) 2001-03-22 2002-10-08 Dendreon Corporation Nucleic acid molecules encoding serine protease cvsp14, the encoded polypeptides and methods based thereon
JP2005506047A (ja) 2001-03-27 2005-03-03 デンドレオン・サンディエゴ・リミテッド・ライアビリティ・カンパニー 膜貫通型セリンプロテアーゼ９をコード化する核酸分子、コード化されたポリペプチドおよびそれらに基づく方法
KR20040080940A (ko) 2001-05-14 2004-09-20 덴드레온 코포레이션 트랜스막 세린 프로테아제 10을 암호화하는 핵산 분자,암호화된 폴리펩티드 및 이에 근거한 방법
WO2003048127A1 (fr) * 2001-12-04 2003-06-12 Corvas International, Inc. Inhibiteurs non covalents heterocycliques aromatiques de l'urokinase et de la formation de vaisseaux sanguins
WO2003053999A2 (fr) * 2001-12-12 2003-07-03 Wilex Ag Inhibiteurs selectifs d'urokinase
JP4898091B2 (ja) 2002-03-11 2012-03-14 ザ メディシンズ カンパニー （ライプツィヒ） ゲーエムベーハー ウロキナーゼの阻害剤、それらの製造および使用
DE10301300B4 (de) * 2003-01-15 2009-07-16 Curacyte Chemistry Gmbh Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein
DE10323898A1 (de) 2003-05-26 2004-12-23 Wilex Ag Hydroxyamidin- und Hydroxyguanidin-Verbindungen als Urokinase-Hemmstoffe
DE10342108A1 (de) 2003-09-11 2005-04-14 Curacyte Chemistry Gmbh Basisch-substituierte Benzylaminanaloga als Inhibitoren des Gerinnungsfaktors Xa, ihre Herstellung und Verwendung
CA2612262A1 (fr) 2005-06-24 2006-12-28 Wilex Ag Utilisation d'inhibiteurs d'urokinase pour le traitement et/ou la prevention de maladies neuropathologiques
CA2620683A1 (fr) * 2005-08-29 2007-03-08 Wilex Ag Composes d'oxadiazole utilises comme inhibiteurs d'urokinase
DE102005044319A1 (de) 2005-09-16 2007-03-22 Curacyte Chemistry Gmbh 2-(Aminomethyl)-5-Chlor-Benzylamid-Derivate und ihre Verwendung als Hemmstoffe des Gerinnungsfaktors Xa
DE102006050672A1 (de) 2006-10-24 2008-04-30 Curacyte Discovery Gmbh Hemmstoffe des Plasmins und des Plasmakallikreins
GB0807828D0 (en) * 2008-04-29 2008-06-04 Vantia Ltd Aminopyridine derivatives
ES2483802T3 (es) 2010-07-07 2014-08-07 The Medicines Company (Leipzig) Gmbh Inhibidores de serina proteasa
WO2021032933A1 (fr) * 2019-08-21 2021-02-25 Kalvista Pharmaceuticals Limited Inhibiteurs d'enzymes
CN114957087A (zh) * 2022-04-13 2022-08-30 湖南复瑞生物医药技术有限责任公司 一种帕罗韦德中间体制备方法

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0601459A2 (fr) * 1992-12-02 1994-06-15 Bristol-Myers Squibb Company Inhibiteurs hétérocycliques de thrombine contenant un groupe sulfonamid
EP0669317A1 (fr) * 1994-01-27 1995-08-30 Mitsubishi Chemical Corporation Dérivés de la prolinamide
WO1996017860A1 (fr) * 1994-12-06 1996-06-13 Basf Aktiengesellschaft Nouveaux p-amidinobenzylamides dipeptidiques a restes n-terminaux sulfonyle ou aminosulfonyle
US5932567A (en) * 1995-02-10 1999-08-03 Basf Aktiengesellschaft Thrombin inhibitors
WO2000005245A2 (fr) * 1998-07-24 2000-02-03 Corvas International, Inc. Inhibiteurs d'urokinase et de la formation de vaisseaux sanguins
WO2000061608A2 (fr) * 1999-04-09 2000-10-19 Basf Aktiengesellschaft Inhibiteurs de faible poids moleculaire des proteases du complement
WO2001096286A2 (fr) * 2000-06-15 2001-12-20 Curacyte Ag Inhibiteurs de l'urokinase
WO2001096366A2 (fr) * 2000-06-15 2001-12-20 Curacyte Ag Inhibiteurs du facteur de coagulation xa

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0601459A2 (fr) * 1992-12-02 1994-06-15 Bristol-Myers Squibb Company Inhibiteurs hétérocycliques de thrombine contenant un groupe sulfonamid
EP0669317A1 (fr) * 1994-01-27 1995-08-30 Mitsubishi Chemical Corporation Dérivés de la prolinamide
WO1996017860A1 (fr) * 1994-12-06 1996-06-13 Basf Aktiengesellschaft Nouveaux p-amidinobenzylamides dipeptidiques a restes n-terminaux sulfonyle ou aminosulfonyle
US5932567A (en) * 1995-02-10 1999-08-03 Basf Aktiengesellschaft Thrombin inhibitors
WO2000005245A2 (fr) * 1998-07-24 2000-02-03 Corvas International, Inc. Inhibiteurs d'urokinase et de la formation de vaisseaux sanguins
WO2000061608A2 (fr) * 1999-04-09 2000-10-19 Basf Aktiengesellschaft Inhibiteurs de faible poids moleculaire des proteases du complement
WO2001096286A2 (fr) * 2000-06-15 2001-12-20 Curacyte Ag Inhibiteurs de l'urokinase
WO2001096366A2 (fr) * 2000-06-15 2001-12-20 Curacyte Ag Inhibiteurs du facteur de coagulation xa

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
TAMURA^@? S Y ET AL: "Synthesis and biological activity of peptidyl aldehyde urokinase inhibitors", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 10, no. 9, May 2000 (2000-05-01), pages 983 - 987, XP004199057, ISSN: 0960-894X *

Also Published As

Publication number Publication date
NZ518195A (en) 2005-04-29
AU2006235835B2 (en) 2009-06-25
AU2006235835A1 (en) 2006-11-30
NZ547626A (en) 2007-10-26
AU8334701A (en) 2002-02-25
CA2387002A1 (fr) 2002-02-21
NZ538572A (en) 2006-09-29
IL149042A0 (en) 2002-11-10
WO2002014349A2 (fr) 2002-02-21
AU785260B2 (en) 2006-12-07
JP2004506648A (ja) 2004-03-04

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