WO2002081415A3 - Methode d'inhibition de la metap2 - Google Patents

Methode d'inhibition de la metap2 Download PDF

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Publication number
WO2002081415A3
WO2002081415A3 PCT/US2002/009458 US0209458W WO02081415A3 WO 2002081415 A3 WO2002081415 A3 WO 2002081415A3 US 0209458 W US0209458 W US 0209458W WO 02081415 A3 WO02081415 A3 WO 02081415A3
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WO
WIPO (PCT)
Prior art keywords
inhibiting
metap2
hmetap2
inhibiting metap2
methods
Prior art date
Application number
PCT/US2002/009458
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English (en)
Other versions
WO2002081415A2 (fr
Inventor
Jr Joseph P Marino
M Dominic Ryan
Ward W Smith
Scott K Thompson
Original Assignee
Smithkline Beecham Corp
Jr Joseph P Marino
M Dominic Ryan
Ward W Smith
Scott K Thompson
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 Smithkline Beecham Corp, Jr Joseph P Marino, M Dominic Ryan, Ward W Smith, Scott K Thompson filed Critical Smithkline Beecham Corp
Priority to JP2002579403A priority Critical patent/JP2004535377A/ja
Priority to AU2002306907A priority patent/AU2002306907A1/en
Priority to EP02763868A priority patent/EP1386279A2/fr
Publication of WO2002081415A2 publication Critical patent/WO2002081415A2/fr
Publication of WO2002081415A3 publication Critical patent/WO2002081415A3/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4192—1,2,3-Triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D249/12—Oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D249/14—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/16—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • C07D249/22—Naphthotriazoles

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La présente invention concerne des méthodes d'identification d'inhibiteurs de l'hMetAP2 et des méthodes d'inhibition de l'hMetAP2 à l'aide d'inhibiteurs présentant certaines caractéristiques structurales, physiques et spatiales.
PCT/US2002/009458 2001-04-03 2002-03-28 Methode d'inhibition de la metap2 WO2002081415A2 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP2002579403A JP2004535377A (ja) 2001-04-03 2002-03-28 Ｍｅｔａｐ２を阻害する方法
AU2002306907A AU2002306907A1 (en) 2001-04-03 2002-03-28 Method for inhibiting metap2
EP02763868A EP1386279A2 (fr) 2001-04-03 2002-03-28 Methode d'inhibition de la metap2

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US28122101P 2001-04-03 2001-04-03
US60/281,221 2001-04-03

Publications (2)

Publication Number Publication Date
WO2002081415A2 WO2002081415A2 (fr) 2002-10-17
WO2002081415A3 true WO2002081415A3 (fr) 2002-12-05

Family

ID=23076434

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2002/009458 WO2002081415A2 (fr) 2001-04-03 2002-03-28 Methode d'inhibition de la metap2

Country Status (4)

Country Link
EP (1) EP1386279A2 (fr)
JP (1) JP2004535377A (fr)
AU (1) AU2002306907A1 (fr)
WO (1) WO2002081415A2 (fr)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU7989400A (en) 1999-10-01 2001-05-10 Smithkline Beecham Corporation Compounds and methods
JP2005506299A (ja) * 2001-03-29 2005-03-03 スミスクライン・ビーチャム・コーポレイション 化合物および方法
EP1921072A1 (fr) * 2006-11-10 2008-05-14 Laboratorios del Dr. Esteve S.A. Dérivés de 1,2,3-triazole comme modulateurs du récepteur cannabinoide
DE102008027574A1 (de) 2008-06-10 2009-12-17 Merck Patent Gmbh Neue Pyrrolidinderivate als MetAP-2 Inhibitoren
DE102009005193A1 (de) 2009-01-20 2010-07-22 Merck Patent Gmbh Neue heterocyclische Verbindungen als MetAP-2 Inhibitoren
DE102010048374A1 (de) 2010-10-13 2012-04-19 Merck Patent Gmbh Pyrrolidinone als MetAP-2 Inhibitoren
DE102012006884A1 (de) 2012-04-04 2013-10-10 Merck Patent Gmbh Cyclische Amide als MetAP-2 Inhibitoren

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6136604A (en) * 1999-10-27 2000-10-24 Isis Pharmaceuticals Inc. Antisense inhibition of methionine aminopeptidase 2 expression
US6261794B1 (en) * 1999-10-14 2001-07-17 Saint Louis University Methods for identifying inhibitors of methionine aminopeptidases

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6261794B1 (en) * 1999-10-14 2001-07-17 Saint Louis University Methods for identifying inhibitors of methionine aminopeptidases
US6136604A (en) * 1999-10-27 2000-10-24 Isis Pharmaceuticals Inc. Antisense inhibition of methionine aminopeptidase 2 expression

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
CARDENAS ET AL.: "Antifungal activities of antineoplastic agents: saccharomyces cerevisiae as a model system to study drug action", CLINICAL MICROBIOLOGY REVIEWS, vol. 12, no. 04, October 1999 (1999-10-01), pages 583 - 611, XP002952701 *
GRIFFITH ET AL.: "Molecular recognition of angiogenesis inhibitors fumagillin and ovalicin by methionine aminopeptidase 2", PROC. NATL. ACAD. SCI. USA, vol. 95, no. 26, 22 December 1998 (1998-12-22), pages 15183 - 15188, XP002952598 *
HAN ET AL.: "Design and synthesis of highly potent fumagallin analogues from homology modeling for a human metAP-2", BIOORGANIC AND MEDICINAL LETTERS, vol. 10, no. 01, 3 January 2000 (2000-01-03), pages 39 - 43, XP002952600 *
LIU ET AL.: "Structure of human methionine aminopeptidase-2 complexed with fumagillin", SCIENCE, vol. 282, 13 November 1998 (1998-11-13), pages 1324 - 1327, XP002952599 *

Also Published As

Publication number Publication date
AU2002306907A1 (en) 2002-10-21
EP1386279A2 (fr) 2004-02-04
JP2004535377A (ja) 2004-11-25
WO2002081415A2 (fr) 2002-10-17

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