Title:
NOVEL SMALL MOLECULE COMPOUND INHIBITING SIGNAL TRANSMISSION PATH OF TLR7 AND TLR9 AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2021/020807
Kind Code:
A1
Abstract:
The present invention relates to a small molecule compound inhibiting a toll-like receptor (TLR) signal transmission path and, more specifically, to a compound having a structure expressed by a particular chemical formula, a TLR inhibitory composition comprising same, and an autoimmune disease or inflammatory disease prevention or therapeutic composition comprising the TLR inhibitory composition. In the present invention, a TLR inhibitory compound TIC10, inhibiting a TLR7- and TLR9-mediated signal transmission path, and a derivative TIC10-7 thereof have been confirmed. The novel compounds block the TNF-α secretion by inhibiting the expression and activation of NF-κB- and MAPK-related proinflammatory genes, and thus can be utilized as a therapeutic agent for many autoimmune diseases, such as systemic lupus erythematosus, psoriasis and psoriatic arthritis, associated with a hyperactivity of a nucleic acid detection TLR.
Inventors:
CHOI SANGDUN (KR)
MUHAMMAD HASEEB (KR)
PATRA MAHESH (KR)
CHOI YANG-SEON (KR)
MUHAMMAD HASEEB (KR)
PATRA MAHESH (KR)
CHOI YANG-SEON (KR)
Application Number:
PCT/KR2020/009732
Publication Date:
February 04, 2021
Filing Date:
July 23, 2020
Export Citation:
Assignee:
UNIV AJOU IND ACADEMIC COOP FOUND (KR)
International Classes:
A61K31/4168; C07D233/88; A61K31/4178; A61P29/00; A61P37/00; C07D405/04
Domestic Patent References:
| WO2007058990A2 | 2007-05-24 |
Foreign References:
| US20130143927A1 | 2013-06-06 | |||
| EP2399578A1 | 2011-12-28 | |||
| US20070032531A1 | 2007-02-08 | |||
| US20130317032A1 | 2013-11-28 |
Other References:
LESTER S.NLI K., J. MOL. BIOL., vol. 426, no. 6, 2014, pages 1246 - 1264
BARTON G.M.KAGAN J.C.MEDZHITOV R, NAT. IMMUNOL., vol. 7, no. l, 2006, pages 49 - 56
BARRAT F.J. ET AL., J. EXP. MED., vol. 202, no. 9, 2005, pages 1171 - 1177
KRIEG A.MVOLLMER J., IMMUNOL. REV., vol. 220, 2007, pages 251 - 269
CALCATERRA C. ET AL., J. IMMUNOL., vol. 181, no. 9, 2008, pages 6132 - 6139
BALAK D.M. ET AL., CLIN. IMMUNOL., vol. 174, 2017, pages 63 - 72
HANAGATA N., INT. J. NANOMEDICINE, vol. 7, 2012, pages 2181 - 2195
JURK M.HEIL F. ET AL., NAT. IMMUNOL., vol. 3, no. 6, 2002, pages 499
SLIWOSKI G. ET AL., PHARMACOL. REV., vol. 66, no. 1, 2014, pages 334 - 395
OHTO U. ET AL., IMMUNITY, vol. 48, no. 4, 2018, pages 649 - 658
SALUNKE D.B. ET AL., J. MED. CHEM., vol. 55, no. 18, 2012, pages 8137 - 8151
KUZNIK A. ET AL., J. IMMUNOL., vol. 186, no. 8, 2011, pages 4794 - 4804
IRWIN J.J., J. CHEM. INF. MODEL, vol. 52, no. 7, 2012, pages 1757 - 1768
WATERHOUSE A., NUCLEIC ACIDS RES., vol. 46, no. Wl, 2018, pages W296 - W303
ZHANG Z., IMMUNITY, vol. 45, no. 4, 2016, pages 737 - 748
OHTO U. ET AL., NATURE, vol. 520, no. 7549, 2015, pages 702 - 705
YOO E. ET AL., ORG. BIOMOL. CHEM., vol. 11, no. 38, 2013, pages 6526 - 6545
See also references of EP 4006013A4
BARTON G.M.KAGAN J.C.MEDZHITOV R, NAT. IMMUNOL., vol. 7, no. l, 2006, pages 49 - 56
BARRAT F.J. ET AL., J. EXP. MED., vol. 202, no. 9, 2005, pages 1171 - 1177
KRIEG A.MVOLLMER J., IMMUNOL. REV., vol. 220, 2007, pages 251 - 269
CALCATERRA C. ET AL., J. IMMUNOL., vol. 181, no. 9, 2008, pages 6132 - 6139
BALAK D.M. ET AL., CLIN. IMMUNOL., vol. 174, 2017, pages 63 - 72
HANAGATA N., INT. J. NANOMEDICINE, vol. 7, 2012, pages 2181 - 2195
JURK M.HEIL F. ET AL., NAT. IMMUNOL., vol. 3, no. 6, 2002, pages 499
SLIWOSKI G. ET AL., PHARMACOL. REV., vol. 66, no. 1, 2014, pages 334 - 395
OHTO U. ET AL., IMMUNITY, vol. 48, no. 4, 2018, pages 649 - 658
SALUNKE D.B. ET AL., J. MED. CHEM., vol. 55, no. 18, 2012, pages 8137 - 8151
KUZNIK A. ET AL., J. IMMUNOL., vol. 186, no. 8, 2011, pages 4794 - 4804
IRWIN J.J., J. CHEM. INF. MODEL, vol. 52, no. 7, 2012, pages 1757 - 1768
WATERHOUSE A., NUCLEIC ACIDS RES., vol. 46, no. Wl, 2018, pages W296 - W303
ZHANG Z., IMMUNITY, vol. 45, no. 4, 2016, pages 737 - 748
OHTO U. ET AL., NATURE, vol. 520, no. 7549, 2015, pages 702 - 705
YOO E. ET AL., ORG. BIOMOL. CHEM., vol. 11, no. 38, 2013, pages 6526 - 6545
See also references of EP 4006013A4
Attorney, Agent or Firm:
LEE, Cheo Young et al. (KR)
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