US 12,240,841 B2
FXR small molecule agonist and preparation method therefor and use thereof
Huaqiang Xu, Pudong Shanghai (CN); Jia Li, Pudong Shanghai (CN); Jingjing Shi, Pudong Shanghai (CN); Yi Zang, Pudong Shanghai (CN); Dandan Sun, Pudong Shanghai (CN); Mingliang Liu, Pudong Shanghai (CN); Rongrong Xie, Pudong Shanghai (CN); Erli You, Pudong Shanghai (CN); Lixin Gao, Pudong Shanghai (CN); and Qian Tan, Pudong Shanghai (CN)
Assigned to SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES, Shanghai (CN); and VAN ANDEL RESEARCH INSTITUTE, Grand Rapids, MI (US)
Appl. No. 17/603,823
Filed by Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai (CN); and Van Andel Research Institute, Grand Rapids, MI (US)
PCT Filed Apr. 20, 2020, PCT No. PCT/CN2020/085713
§ 371(c)(1), (2) Date Oct. 14, 2021,
PCT Pub. No. WO2020/211872, PCT Pub. Date Oct. 22, 2020.
Claims priority of application No. 201910319757.X (CN), filed on Apr. 19, 2019; and application No. 201910969552.6 (CN), filed on Oct. 12, 2019.
Prior Publication US 2022/0213083 A1, Jul. 7, 2022
Int. Cl. C07D 413/14 (2006.01); A61P 1/16 (2006.01); C07D 487/08 (2006.01)
CPC C07D 413/14 (2013.01) [A61P 1/16 (2018.01); C07D 487/08 (2013.01)] 15 Claims
 
1. A compound represented by general formula I, or enantiomer, diastereomer, tautomer, racemate, solvate, prodrug or pharmaceutically acceptable salt thereof,

OG Complex Work Unit Chemistry
wherein, R11, R12, R13, R14 and R15 are each independently hydrogen, halogen, halogenated C1-6 alkyl, halogenated C1-C6 alkoxy, C1-C6 alkyl, C1-6 alkoxy, C3-C6 cycloalkyl, C3-C6 cycloalkoxy, cyano or nitro;
R2 is C6-C12 aryl, C1-C6 alkyl or C3-C6 cycloalkyl;
Q is

OG Complex Work Unit Chemistry
wherein N is attached to A;
A is the following substituted or unsubstituted group: phenyl, pyridyl, thienyl, furyl, indazolyl, indolyl, benzothienyl, benzofuranyl, and the “substituted” means that there is one, two or three substituents selected from the group consisting of halogen, C1-C6 alkyl, halogenated C1-6 alkyl, halogenated C1-C6 alkoxy, C3-C6 cycloalkyl, C1-C6 alkoxy, and C3-C6 cycloalkoxy;
X is O or S.