Title:
N-SUBSTITUTED ACRYLAMIDE DERIVATIVE AS DHODH INHIBITOR, AND PREPARATION AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2019/196714
Kind Code:
A1
Abstract:
An N-substituted acrylamide derivative, represented by general formula I, as a DHODH inhibitor, and preparation and use thereof. The N-substituted acrylamide derivative has excellent DHODH inhibiting activity, and thus can be used for treating or preventing DHODH-mediated diseases, including, but not limited to, autoimmune diseases, such as cancers, rheumatoid arthritis, lupus erythematosus, and organ graft rejections, and inflammatory diseases, such as colitis and rhinitis.
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Inventors:
XU XIAOYONG (CN)
LI HONGLIN (CN)
LI ZHONG (CN)
LI SHILIANG (CN)
ZENG FANXUN (CN)
WANG RUI (CN)
ZHANG LETIAN (CN)
ZHU LILI (CN)
QI TIANTIAN (CN)
LI HONGLIN (CN)
LI ZHONG (CN)
LI SHILIANG (CN)
ZENG FANXUN (CN)
WANG RUI (CN)
ZHANG LETIAN (CN)
ZHU LILI (CN)
QI TIANTIAN (CN)
Application Number:
PCT/CN2019/081066
Publication Date:
October 17, 2019
Filing Date:
April 02, 2019
Export Citation:
Assignee:
UNIV EAST CHINA SCIENCE & TECH (CN)
International Classes:
C07C233/55; A61K31/196; A61K31/343; A61K31/357; A61K31/47; A61P13/12; A61P19/02; A61P35/00; C07C231/02; C07C235/38; C07D213/56
Foreign References:
| US6046239A | 2000-04-04 | |||
| CN101094829A | 2007-12-26 | |||
| CN102164887A | 2011-08-24 | |||
| CN1273579A | 2000-11-15 | |||
| CN103228275A | 2013-07-31 | |||
| US3940422A | 1976-02-24 | |||
| JPS50135047A | 1975-10-25 | |||
| JPS59122449A | 1984-07-14 | |||
| JPS5738759A | 1982-03-03 | |||
| JPS5283429A | 1977-07-12 | |||
| JPS6019754A | 1985-01-31 | |||
| JPS6097946A | 1985-05-31 |
Other References:
DIAO, Y. Y. ET AL.: "Discovery of Diverse Human Dihydroorotate Dehydrogenase Inhibitors as Immunosuppressive Agents by Structure-Based Virtual Screening", J. MED. CHEM., vol. 55, 17 September 2012 (2012-09-17), pages 8341 - 8349, XP055643334
KERMANY, E. T. ET AL., SYNTHESIS OF 2-ALKENYL-4H-3, 1 -BF.NZOXAZTN-4-ONF UNDER ACIDIC AND BASIC MEDIA, vol. 4, no. 1, 31 December 2014 (2014-12-31), pages 17 - 21, XP055643343
MCCARTHY, D. J. ET AL.: "Use of Structure-Based Drug Design Approaches to Obtain Novel Anthranilic Acid Acyl Carrier Protein Synthase Inhibitors", J. MED. CHEM., vol. 48, 16 November 2005 (2005-11-16), pages 7960 - 7969, XP055643346
WILLIAMS, S. J. ET AL.: "3',4'-Bis-difluoromethoxycinnamoylanthranilate (FT061): An orally- active antifibrotic agent that reduces albuminuria in a rat model of progressive diabetic nephropathy", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 23, 8 October 2013 (2013-10-08), pages 6868 - 6873, XP028788001, DOI: 10.1016/j.bmcl.2013.09.100
KERMANY, E. T. ET AL., SYNTHESIS OF 2-ALKENYL-4H-3, 1 -BF.NZOXAZTN-4-ONF UNDER ACIDIC AND BASIC MEDIA, vol. 4, no. 1, 31 December 2014 (2014-12-31), pages 17 - 21, XP055643343
MCCARTHY, D. J. ET AL.: "Use of Structure-Based Drug Design Approaches to Obtain Novel Anthranilic Acid Acyl Carrier Protein Synthase Inhibitors", J. MED. CHEM., vol. 48, 16 November 2005 (2005-11-16), pages 7960 - 7969, XP055643346
WILLIAMS, S. J. ET AL.: "3',4'-Bis-difluoromethoxycinnamoylanthranilate (FT061): An orally- active antifibrotic agent that reduces albuminuria in a rat model of progressive diabetic nephropathy", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 23, 8 October 2013 (2013-10-08), pages 6868 - 6873, XP028788001, DOI: 10.1016/j.bmcl.2013.09.100
Attorney, Agent or Firm:
XU & PARTNERS, LLC. (CN)
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