Title:
COMPOUNDS SERVING AS GPR17 AND CYSLT1 DUAL ANTAGONISTS, PREPARATION METHOD THEREFOR, AND USES THEREOF
Document Type and Number:
WIPO Patent Application WO/2017/088725
Kind Code:
A1
Abstract:
Disclosed are compounds as shown in General Formula (I), a preparation method therefor, and uses thereof. The compounds are weak in GPR17 antagonistic activity and strong in CysLT1 antagonism, can be used for preventing and treating central lesions and neurodegenerative diseases such as multiple sclerosis and leukodystrophy, and can also be used for treating CysLT1-mediated asthma, rhinitis, allergy and other inflammatory diseases.
Inventors:
NAN FAJUN (CN)
XIE XIN (CN)
CHEN HUAYAN (CN)
GONG CHAOJUN (CN)
WANG ZHILONG (CN)
GUO YUE (CN)
XIE XIN (CN)
CHEN HUAYAN (CN)
GONG CHAOJUN (CN)
WANG ZHILONG (CN)
GUO YUE (CN)
Application Number:
PCT/CN2016/106714
Publication Date:
June 01, 2017
Filing Date:
November 22, 2016
Export Citation:
Assignee:
SHANGHAI INST MATERIA MEDICA CAS (CN)
International Classes:
C07D209/42; A61K31/403; A61K31/4709; A61P11/02; A61P11/06; A61P25/00; A61P29/00; A61P37/02; A61P37/08; C07D207/34; C07D401/12
Domestic Patent References:
| WO2008121836A1 | 2008-10-09 |
Foreign References:
| EP0384450A1 | 1990-08-29 | |||
| US20130059899A1 | 2013-03-07 |
Other References:
CHEN, HUAYAN ET AL.: "Discovery of 3-Substituted 1H-Indole-2-carboxylic Acid Derivatives as a Novel Class of CysLT1 Selective Antagonists.", ACS MED. CHEM. LETT., vol. 7, no. 3, 22 January 2016 (2016-01-22), pages 335 - 339, XP055385649, ISSN: 1948-5875
BAQI, Y. ET AL.: "Improved Synthesis 4-/6-Substituted 2-Carboxy-1H-Indole-3-Propionic Acid Derivatives and Structure-Activity Relationships as GPR17 Agonists.", CHEM. COMMUN, vol. 5, 22 November 2013 (2013-11-22), pages 86 - 92, XP055385651, ISSN: 2040-2503
BAQI, Y. ET AL.: "Improved Synthesis 4-/6-Substituted 2-Carboxy-1H-Indole-3-Propionic Acid Derivatives and Structure-Activity Relationships as GPR17 Agonists.", CHEM. COMMUN, vol. 5, 22 November 2013 (2013-11-22), pages 86 - 92, XP055385651, ISSN: 2040-2503
Attorney, Agent or Firm:
KINGSOUND & PARTNERS (CN)
Download PDF: