Title:
SMALL-MOLECULE INHIBITORS OF CORONAVIRAL MAIN PROTEASE, THEIR PREPARATION AND USE
Document Type and Number:
WIPO Patent Application WO/2006/042478
Kind Code:
A1
Abstract:
The present invention is directed to a series of small-molecule inhibitors of general formula (I), which are designed on the crystal structure of SARS coronaviral main protease. Preparation of the said small-molecule inhibitors, pharmaceutical composition containing the same as well as their use in the manufacture of a medicament for treating or preventing a variety of coronaviral infections are also provided.
Inventors:
YANG HAITAO (CN)
XUE XIAOYU (CN)
BARTLAM MARK (GB)
YANG KAILIN (CN)
MA DAWEI (CN)
XIE WEIQING (CN)
XUE XIAOYU (CN)
BARTLAM MARK (GB)
YANG KAILIN (CN)
MA DAWEI (CN)
XIE WEIQING (CN)
Application Number:
PCT/CN2005/001748
Publication Date:
April 27, 2006
Filing Date:
October 24, 2005
Export Citation:
Assignee:
UNIV TSINGHUA (CN)
SHANGHAI INST ORGANIC CHEM (CN)
RAO ZIHE (CN)
YANG HAITAO (CN)
XUE XIAOYU (CN)
BARTLAM MARK (GB)
YANG KAILIN (CN)
MA DAWEI (CN)
XIE WEIQING (CN)
SHANGHAI INST ORGANIC CHEM (CN)
RAO ZIHE (CN)
YANG HAITAO (CN)
XUE XIAOYU (CN)
BARTLAM MARK (GB)
YANG KAILIN (CN)
MA DAWEI (CN)
XIE WEIQING (CN)
International Classes:
C07D207/26; A61K31/40; A61K31/42; A61P31/12; C07D261/08; C07D413/12; C07K5/027
Domestic Patent References:
| WO2005066123A1 | 2005-07-21 | |||
| WO1999057135A1 | 1999-11-11 | |||
| WO1998043950A1 | 1998-10-08 |
Foreign References:
| US6355807B1 | 2002-03-12 |
Other References:
MA D ET AL: "An efficient and tunable route to AG7088, a rhinovirus protease inhibitor.", TETRAHEDRON LETTERS., vol. 45, no. 43, pages 8103 - 8105
DRAGOVICH P S ET AL: "Structure-Based Design, Synthesis, and Biological Evaluation of Irreversible Human Rhinovirus 3C Protease Inhibitors. 4. Incorporation of P1 Lactam Moieties as L-Glutamine Replacements.", JOURNAL OF MEDICINAL CHEMISTRY., vol. 42, no. 7, 1999, pages 1213 - 1224
WEBBER S E ET AL: "Design and synthesis of irreversible depsipeptidyl human rhinovirus 3C protease inhibitors.", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS., vol. 11, no. 20, 2001, pages 8 - 9
ZHANG R ET AL: "Liquid chromatography-mass spectometry and liquid chromatography-NMR characterization of in vitro metabolites of a potent and irreversible peptidomimetic inhibitor of rhinovirus 3C protease.", DRUG METABOLISM AND DISPOSITION., vol. 29, no. 5, 2001, pages 729 - 734
DRAGOVICH P S ET AL: "Structure-Based Design, Synthesis, and Biological Evaluation of Irreversible Human Rhinovirus 3C Protease Inhibitors. 4. Incorporation of P1 Lactam Moieties as L-Glutamine Replacements.", JOURNAL OF MEDICINAL CHEMISTRY., vol. 42, no. 7, 1999, pages 1213 - 1224
WEBBER S E ET AL: "Design and synthesis of irreversible depsipeptidyl human rhinovirus 3C protease inhibitors.", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS., vol. 11, no. 20, 2001, pages 8 - 9
ZHANG R ET AL: "Liquid chromatography-mass spectometry and liquid chromatography-NMR characterization of in vitro metabolites of a potent and irreversible peptidomimetic inhibitor of rhinovirus 3C protease.", DRUG METABOLISM AND DISPOSITION., vol. 29, no. 5, 2001, pages 729 - 734
Attorney, Agent or Firm:
NTD PATENT & TRADEMARK AGENCY LTD. (Block A Investment Plaz, 27 Jinrongdajie Beijing 2, CN)
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