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WO2003033437A3 - Procede de fabrication d'inhibiteurs de la neuraminidase au moyen de la chimie combinatoire dynamique et composes ainsi obtenus - Google Patents

Procede de fabrication d'inhibiteurs de la neuraminidase au moyen de la chimie combinatoire dynamique et composes ainsi obtenus Download PDF

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Publication number
WO2003033437A3
WO2003033437A3 PCT/EP2002/011526 EP0211526W WO03033437A3 WO 2003033437 A3 WO2003033437 A3 WO 2003033437A3 EP 0211526 W EP0211526 W EP 0211526W WO 03033437 A3 WO03033437 A3 WO 03033437A3
Authority
WO
WIPO (PCT)
Prior art keywords
forming
neuraminidase
compounds obtained
combinatorial chemistry
functionality
Prior art date
Application number
PCT/EP2002/011526
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English (en)
Other versions
WO2003033437A2 (fr
Inventor
Christoph Steeneck
Alexey V Eliseev
Matthias Hochguertel
Heiko Kroth
Original Assignee
Therascope Ag
Christoph Steeneck
Alexey V Eliseev
Matthias Hochguertel
Heiko Kroth
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 Therascope Ag, Christoph Steeneck, Alexey V Eliseev, Matthias Hochguertel, Heiko Kroth filed Critical Therascope Ag
Publication of WO2003033437A2 publication Critical patent/WO2003033437A2/fr
Publication of WO2003033437A3 publication Critical patent/WO2003033437A3/fr

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C40—COMBINATORIAL TECHNOLOGY
    • C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B30/00—Methods of screening libraries
    • C40B30/04—Methods of screening libraries by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/45—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/52—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/16—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/04—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length on carriers
    • C07K1/047—Simultaneous synthesis of different peptide species; Peptide libraries
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64—Cyclic peptides containing only normal peptide links
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G01N33/6803—General methods of protein analysis not limited to specific proteins or families of proteins
    • G01N33/6845—Methods of identifying protein-protein interactions in protein mixtures
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/16—Systems containing only non-condensed rings with a six-membered ring the ring being unsaturated
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/90—Enzymes; Proenzymes
    • G01N2333/914—Hydrolases (3)
    • G01N2333/924—Hydrolases (3) acting on glycosyl compounds (3.2)
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/20—Screening for compounds of potential therapeutic value cell-free systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Medicinal Chemistry (AREA)
  • Biophysics (AREA)
  • Immunology (AREA)
  • Analytical Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Physics & Mathematics (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • General Engineering & Computer Science (AREA)
  • Bioinformatics & Computational Biology (AREA)
  • Cell Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Food Science & Technology (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)

Abstract

L'invention concerne des composés selon la formule I, dans laquelle la ligne en pointillé représente une double liaison présente dans l'une des deux positions possibles; R1 à R4 sont choisis indépendamment l'un de l'autre dans le groupe comprenant hydrogène, des groupes alkyle C1-C20, des groupes alcényle C2-C20, des groupes aryle C4-C20, des groupes aralkyle C5-C20 et des groupes alkaryle C5-C20, tous ces groupes pouvant contenir un ou plusieurs hétéroatomes du groupe comprenant N, O et S, et pouvant porter au moins un substituant du groupe comprenant des groupes hydroxyl et des groupes alkyle ester C1-C4; ou l'un des substituants NR1R2 et NR3R4 est un groupe guanidino de la formule NR5-C(NR6R7)=NR8, dans laquelle les substituants R5 à R8 ont indépendamment l'un de l'autre la signification donnée ci-dessus aux substituants R1 à R4. R9 est un groupe alkyle C1-C4, ou un sel ou un solvate physiologiquement acceptable de ceux-ci dans n'importe quelle forme stéréo-isomère ou des mélanges de ceux-ci dans n'importe quel rapport. L'invention concerne également un procédé de fabrication d'une bibliothèque de composants qui peuvent se lier à la neuraminidase, notamment la neuraminidase de la grippe. Ledit procédé consiste: i) à choisir plusieurs molécules portant une fonctionnalité susceptible d'interagir avec un site de liaison de la neuraminidase, lesdites molécules présentant également un groupe de liaison pouvant interagir avec d'autres groupes de liaison sous la formation de liaisons réversibles; ii) à faire réagir les molécules portant la fonctionnalité avec une molécule selon la formule I définie dans la revendication 1 en présence de la cible, dans les cas où survient une formation de liaisons réversibles entre les groupes de liaison sur la molécule I et sur les molécules portant une fonctionnalité.
PCT/EP2002/011526 2001-10-15 2002-10-15 Procede de fabrication d'inhibiteurs de la neuraminidase au moyen de la chimie combinatoire dynamique et composes ainsi obtenus WO2003033437A2 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US32880201P 2001-10-15 2001-10-15
US60/328,802 2001-10-15
US35673102P 2002-02-15 2002-02-15
US60/356,731 2002-02-15

Publications (2)

Publication Number Publication Date
WO2003033437A2 WO2003033437A2 (fr) 2003-04-24
WO2003033437A3 true WO2003033437A3 (fr) 2003-12-18

Family

ID=26986521

Family Applications (2)

Application Number Title Priority Date Filing Date
PCT/EP2002/011526 WO2003033437A2 (fr) 2001-10-15 2002-10-15 Procede de fabrication d'inhibiteurs de la neuraminidase au moyen de la chimie combinatoire dynamique et composes ainsi obtenus
PCT/EP2002/011520 WO2003034071A2 (fr) 2001-10-15 2002-10-15 Procede de formation d'une bibliotheque combinatoire dynamique faisant appel a une structure d'echafaudage

Family Applications After (1)

Application Number Title Priority Date Filing Date
PCT/EP2002/011520 WO2003034071A2 (fr) 2001-10-15 2002-10-15 Procede de formation d'une bibliotheque combinatoire dynamique faisant appel a une structure d'echafaudage

Country Status (2)

Country Link
AU (1) AU2002346915A1 (fr)
WO (2) WO2003033437A2 (fr)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003290304A1 (en) 2002-12-23 2004-07-14 Astex Technology Limited Synthesis and screening of ligands using x-ray crystallography
JP2007521252A (ja) * 2003-04-11 2007-08-02 エスジーエックス ファーマシューティカルズ，インコーポレイティド 化合物ライブラリーおよび薬剤発見方法
EP1496039B1 (fr) * 2003-07-11 2018-02-14 Kirschfeld, Andreas Méthode de création d'une chimiothèque combinatoire dynamique
EP1496038A1 (fr) * 2003-07-11 2005-01-12 Therascope AG Méthode de synthèse d'une chimiothèque combinatoire dynamique faisant intervenir des nitrones
WO2009068321A1 (fr) * 2007-11-26 2009-06-04 Forschungsverbund Berlin E.V. Criblage haut débit dirigé
DE102011117128A1 (de) * 2011-10-28 2013-05-02 Christian-Albrechts-Universität Zu Kiel Verbindungen zur Therapie der Influenza
JP6754997B2 (ja) * 2013-08-26 2020-09-16 国立大学法人 東京大学 大環状ペプチド、その製造方法、及び大環状ペプチドライブラリを用いるスクリーニング方法
CN107325040B (zh) * 2016-04-28 2019-05-03 广州市恒诺康医药科技有限公司 环己烯类衍生物或其药学上可接受的盐及其用途

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999031047A1 (fr) * 1997-12-12 1999-06-24 Gilead Sciences, Inc. Carboxylates de cyclohexene utilises comme inhibiteurs de neuraminidase

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6008058A (en) * 1993-06-18 1999-12-28 University Of Louisville Cyclic peptide mixtures via side chain or backbone attachment and solid phase synthesis
JPH10501818A (ja) * 1994-06-16 1998-02-17 スミスクライン・ビーチャム・コーポレイション 鋳型指向性環化
US5958702A (en) * 1995-02-06 1999-09-28 Benner; Steven Albert Receptor-assisted combinatorial chemistry
DE19619373A1 (de) * 1996-05-14 1997-11-20 Hoechst Ag Neue Substanzbibliothek und damit hergestellte supramolekulare Komplexe
US20020068301A1 (en) * 1997-05-28 2002-06-06 Hung-Sen Lai Cyclic peptide libraries and methods of use thereof to identify binding motifs
CA2284459C (fr) * 1999-10-04 2012-12-11 Neokimia Inc. Synthese combinatoire de bibliotheques de composes macrocycliques utiles pour la decouverte de medicaments
EP1130009A1 (fr) * 2000-03-01 2001-09-05 Therascope AG Préparation et screening d'une bibliothèque de chimie combinatoire dynamique

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999031047A1 (fr) * 1997-12-12 1999-06-24 Gilead Sciences, Inc. Carboxylates de cyclohexene utilises comme inhibiteurs de neuraminidase

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
LEW W ET AL: "A new series of C3-aza carbocyclic influenza neuraminidase inhibitors: synthesis and inhibitory activity", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 8, no. 23, 1 December 1998 (1998-12-01), pages 3321 - 3324, XP004143751, ISSN: 0960-894X *

Also Published As

Publication number Publication date
WO2003033437A2 (fr) 2003-04-24
AU2002346915A1 (en) 2003-04-28
WO2003034071A2 (fr) 2003-04-24
WO2003034071A3 (fr) 2004-03-11

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