Title:
ARYL OR HETEROARYL PYRIDONE OR PYRIMIDONE DERIVATIVE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2021/249563
Kind Code:
A1
Abstract:
Provided are an aryl or heteroaryl pyridone or pyrimidone derivative, a preparation method therefor, and an application thereof. The compound has a structure represented by formula (I). Also provided are a preparation method of the compound and a use thereof as a KRAS G12C inhibitor. The compound has an excellent selective inhibitory effect on KRAS G12C, improved pharmacodynamics and pharmacokinetic properties, as well as lower toxic side effects.
Inventors:
LV BINHUA (CN)
CUI DAWEI (CN)
LIU LIANJUN (CN)
CUI DAWEI (CN)
LIU LIANJUN (CN)
Application Number:
PCT/CN2021/099875
Publication Date:
December 16, 2021
Filing Date:
June 11, 2021
Export Citation:
Assignee:
SUZHOU ZELGEN BIOPHARMACEUTICALS CO LTD (CN)
SHANGHAI ZELGEN PHARMA TECH CO LTD (CN)
SHANGHAI ZELGEN PHARMA TECH CO LTD (CN)
International Classes:
A61K31/519; C07D471/04; A61K31/5377; A61K31/675; A61P35/00; A61P35/02; C07F9/6561
Domestic Patent References:
| WO2019213516A1 | 2019-11-07 | |||
| WO2019241157A1 | 2019-12-19 | |||
| WO2020106647A2 | 2020-05-28 | |||
| WO2021113595A1 | 2021-06-10 | |||
| WO2021081212A1 | 2021-04-29 | |||
| WO2020236948A1 | 2020-11-26 | |||
| WO2020239077A1 | 2020-12-03 | |||
| WO2021011417A1 | 2021-01-21 | |||
| WO2021076655A1 | 2021-04-22 | |||
| WO2021120045A1 | 2021-06-24 | |||
| WO2021121367A1 | 2021-06-24 | |||
| WO2021121330A1 | 2021-06-24 | |||
| WO2021126816A1 | 2021-06-24 |
Foreign References:
| CN110366550A | 2019-10-22 | |||
| TW201906821A | 2019-02-16 | |||
| TW201922739A | 2019-06-16 | |||
| US20190374542A1 | 2019-12-12 | |||
| CN111205286A | 2020-05-29 | |||
| CN112920183A | 2021-06-08 | |||
| CN111377918A | 2020-07-07 | |||
| CN111484477A | 2020-08-04 | |||
| CN112585129A | 2021-03-30 | |||
| CN112552294A | 2021-03-26 | |||
| CN112159405A | 2021-01-01 | |||
| CN112225734A | 2021-01-15 | |||
| CN112390818A | 2021-02-23 | |||
| CN112390796A | 2021-02-23 | |||
| CN112574199A | 2021-03-30 | |||
| CN113286794A | 2021-08-20 | |||
| CN113061132A | 2021-07-02 | |||
| CN113105448A | 2021-07-13 |
Other References:
BRIAN A LANMAN; JENNIFER R ALLEN; JOHN G ALLEN; ALBERT K AMEGADZIE; KATE S ASHTON; SHON K BOOKER; JIAN JEFFREY CHEN; NING CHEN; MI: "Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors", JOURNAL OF MEDICINAL CHEMISTRY, vol. 63, no. 1, 9 January 2019 (2019-01-09), pages 52 - 65, XP055666907, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.9b01180
XIAO XUANZHENG; LAI MENGZHEN; SONG ZILAN; GENG MEIYU; DING JIAN; XIE HUA; ZHANG AO: "Design, synthesis and pharmacological evaluation of bicyclic and tetracyclic pyridopyrimidinone analogues as new KRASG12C inhibitors", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 213, 4 December 2020 (2020-12-04), pages 1 - 17, XP086503244, ISSN: 0223-5234, DOI: 10.1016/j.ejmech.2020.113082
CHEN HAO, SMAILL JEFF B., LIU TONGZHENG, DING KE, LU XIAOYUN: "Small-Molecule Inhibitors Directly Targeting KRAS as Anticancer Therapeutics", JOURNAL OF MEDICINAL CHEMISTRY, vol. 63, no. 23, 23 November 2020 (2020-11-23), US, pages 14404 - 14424, XP055879585, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.0c01312
XIAO XUANZHENG; LAI MENGZHEN; SONG ZILAN; GENG MEIYU; DING JIAN; XIE HUA; ZHANG AO: "Design, synthesis and pharmacological evaluation of bicyclic and tetracyclic pyridopyrimidinone analogues as new KRASG12C inhibitors", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 213, 4 December 2020 (2020-12-04), pages 1 - 17, XP086503244, ISSN: 0223-5234, DOI: 10.1016/j.ejmech.2020.113082
CHEN HAO, SMAILL JEFF B., LIU TONGZHENG, DING KE, LU XIAOYUN: "Small-Molecule Inhibitors Directly Targeting KRAS as Anticancer Therapeutics", JOURNAL OF MEDICINAL CHEMISTRY, vol. 63, no. 23, 23 November 2020 (2020-11-23), US, pages 14404 - 14424, XP055879585, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.0c01312
Attorney, Agent or Firm:
XU&PARTNERS, LLC. (CN)
Download PDF: