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1. WO2004101781 - CRYSTAL STRUCTURE OF HUMAN CORONAVIRUS 229E MAIN PROTEINASE, AND USES THEREOF FOR DEVELOPING SARS INHIBITORS

Publication Number WO/2004/101781
Publication Date 25.11.2004
International Application No. PCT/EP2004/005109
International Filing Date 13.05.2004
IPC
C07K 14/165 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
005from viruses
08RNA viruses
165Coronaviridae, e.g. avian infectious bronchitis virus
C12N 9/50 2006.01
CCHEMISTRY; METALLURGY
12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
9Enzymes, e.g. ligases (6.); Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating, or purifying enzymes
14Hydrolases (3.)
48acting on peptide bonds, e.g. thromboplastin, leucine aminopeptidase (3.4)
50Proteinases
CPC
A61P 31/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
14for RNA viruses
C07K 14/005
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
005from viruses
C07K 2299/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
2299Coordinates from 3D structures of peptides, e.g. proteins or enzymes
C12N 2770/20022
CCHEMISTRY; METALLURGY
12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
2770ssRNA Viruses positive-sense
00011ssRNA Viruses positive-sense
20011Coronaviridae
20022New viral proteins or individual genes, new structural or functional aspects of known viral proteins or genes
C12N 9/506
CCHEMISTRY; METALLURGY
12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
9Enzymes; Proenzymes; Compositions thereof
14Hydrolases (3)
48acting on peptide bonds (3.4)
50Proteinases ; , e.g. Endopeptidases (3.4.21-3.4.25)
503derived from viruses
506derived from RNA viruses
Applicants
  • UNIVERSITÄT ZU LÜBECK [DE]/[DE] (AllExceptUS)
  • HILGENFELD, Rolf [DE]/[DE] (UsOnly)
  • ANAND, Kanchan (UsOnly)
  • ZIEBUHR, John [DE]/[DE] (UsOnly)
  • MESTERS, Jeroen, R. [DE]/[DE] (UsOnly)
  • WADHWANI, Parvesh (UsOnly)
Inventors
  • HILGENFELD, Rolf
  • ANAND, Kanchan
  • ZIEBUHR, John
  • MESTERS, Jeroen, R.
  • WADHWANI, Parvesh
Agents
  • BIEHL, Christian
Priority Data
60/469,81813.05.2003US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) CRYSTAL STRUCTURE OF HUMAN CORONAVIRUS 229E MAIN PROTEINASE, AND USES THEREOF FOR DEVELOPING SARS INHIBITORS
(FR) STRUCTURE CRISTALLINE DE LA PROTEINASE PRINCIPALE 229E DES CORONAVIRUS HUMAINS ET UTILISATIONS DE CETTE DERNIERE POUR DEVELOPPER DES INHIBITEURS DU SRAS
Abstract
(EN)
The invention relates to SARS inhibitors. Human coronaviruses are major causes of upper respiratory tract illness in humans, in particular, the common cold. Recent investigations have shown that a novel coronavirus causes the Severe Acute Respiratory Syndrome (SARS), a disease that is characterized by high fever, malaise, rigor, headache, non-productive cough or dyspnea and which is rapidly spreading. Within the scope of the invention, based on the structural analysis of the binding mode of the SARS Mpro enzyme a group of prototype inhibitors is provided that acts as suitable drugs targeting a majority of viral infections of the respiratory tract, including SARS.
(FR)
L'invention concerne des inhibiteurs du syndrome respiratoire aigu sévère (SRAS). Les coronavirus humains sont des causes majeures de l'affection des voies respiratoires supérieures chez les humains, en particulier le rhume. De récentes enquêtes ont révélé qu'un nouveau coronavirus est à l'origine du syndrome respiratoire aigu sévère (SRAS), une maladie à propagation rapide caractérisée par une forte fièvre, un malaise, une rigidité, des maux de tête, une toux non productive ou une dyspnée. Selon la présente invention, l'analyse structurelle du mode de liaison de l'enzyme SRAS Mpro a permis de développer un groupe d'inhibiteurs prototypes agissant comme des médicaments appropriés ciblant une majorité d'infections virales des voies respiratoires, notamment le SRAS.
Also published as
US11273270
Latest bibliographic data on file with the International Bureau