Title:
PHENYL TRIAZOLE MLL1-WDR5 PROTEIN-PROTEIN INTERACTION INHIBITOR
Document Type and Number:
WIPO Patent Application WO/2019/205687
Kind Code:
A1
Abstract:
Disclosed in the present invention are a phenyl triazole MLL1-WDR5 protein-protein interaction inhibitor (I) and a preparation method therefor; pharmacodynamic tests have proven that the compound of the present invention has strong MLL1-WDR5 protein-protein interaction inhibitory activity.
Inventors:
YOU QIDONG (CN)
GUO XIAOKE (CN)
LI DONGDONG (CN)
CHEN WEILIN (CN)
WANG ZHIHUI (CN)
GUO XIAOKE (CN)
LI DONGDONG (CN)
CHEN WEILIN (CN)
WANG ZHIHUI (CN)
Application Number:
PCT/CN2018/123500
Publication Date:
October 31, 2019
Filing Date:
December 25, 2018
Export Citation:
Assignee:
UNIV CHINA PHARMA (CN)
International Classes:
C07D249/06; A61K31/496; A61K31/5377; A61K31/551; A61P35/02; C07D401/12; C07D403/10; C07D405/12
Domestic Patent References:
| WO2017147700A1 | 2017-09-08 | |||
| WO2017147701A1 | 2017-09-08 |
Foreign References:
| CN105175284A | 2015-12-23 | |||
| CN108715585A | 2018-10-30 |
Other References:
BOLSHAN, YURI ET AL.: "Synthesis, Optimization, and Evaluation of Novel Small Molecules as Antagonists of WDR5-MLL Interaction", ACS MEDICINAL CHEMISTRY LETTERS, vol. 4, no. 3, 4 February 2013 (2013-02-04), pages 353 - 357, XP055412290, ISSN: 1948-5875, DOI: 10.1021/ml300467n
LI, DONGDONG ET AL.: "High-affinity Small Molecular Blockers of Mixed Lineage Leukemia 1 (MLL1)-WDR5 Interaction Inhibit MLL1 Complex H3K4 Methyltransferase Activity", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 124, 20 August 2016 (2016-08-20), pages 480 - 489, XP055649028, ISSN: 0223-5234, DOI: 10.1016/j.ejmech.2016.08.036
LI, DONGDONG ET AL.: "Structure-based Design and Synthesis of Small Molecular Inhibitors Disturbing the Interaction of MLL1-WDR5", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 118, 13 April 2016 (2016-04-13), pages 1 - 8, XP029562555, ISSN: 0223-5234, DOI: 10.1016/j.ejmech.2016.04.032
GETLIK, MATTHAUS ET AL.: "Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1", JOURNAL OF MEDICINAL CHEMISTRY, vol. 59, no. 6, 9 March 2016 (2016-03-09), pages 2478 - 2496, XP055413735, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.5b01630
EUR. J. MED. CHEM., vol. 124, 2016, pages 480 - 489
See also references of EP 3786157A4
LI, DONGDONG ET AL.: "High-affinity Small Molecular Blockers of Mixed Lineage Leukemia 1 (MLL1)-WDR5 Interaction Inhibit MLL1 Complex H3K4 Methyltransferase Activity", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 124, 20 August 2016 (2016-08-20), pages 480 - 489, XP055649028, ISSN: 0223-5234, DOI: 10.1016/j.ejmech.2016.08.036
LI, DONGDONG ET AL.: "Structure-based Design and Synthesis of Small Molecular Inhibitors Disturbing the Interaction of MLL1-WDR5", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 118, 13 April 2016 (2016-04-13), pages 1 - 8, XP029562555, ISSN: 0223-5234, DOI: 10.1016/j.ejmech.2016.04.032
GETLIK, MATTHAUS ET AL.: "Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1", JOURNAL OF MEDICINAL CHEMISTRY, vol. 59, no. 6, 9 March 2016 (2016-03-09), pages 2478 - 2496, XP055413735, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.5b01630
EUR. J. MED. CHEM., vol. 124, 2016, pages 480 - 489
See also references of EP 3786157A4
Attorney, Agent or Firm:
NANJING JINGWEI PATENT & TRADEMARK AGENCY CO., LTD (CN)
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