Title:
BENZENE SULFONAMIDE COMPOUND CONTAINING FIVE-MEMBERED HETEROCYCLE, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2021/155781
Kind Code:
A1
Abstract:
The present invention relates to a benzene sulfonamide compound containing a five-membered heterocycle represented by formula (I), and an enantiomer, a diastereomer, and a racemate thereof and a mixture thereof, and a pharmaceutically acceptable salt, crystalline hydrate, and solvate thereof, as well as a use of such a compound in the preparation of a CA inhibitor, and a pharmaceutical composition containing such a compound. As a carbonic anhydrase inhibitor, the compound of the present invention shows good development potential. In comparison with the commonly used carbonic anhydrase (CA) inhibitor, acetazolamide diamox, in clinical practice, the compound of the present invention has stronger inhibitory activity on CAI, and shows a strong inhibitory ability on both CAI and CAII, reaching an IC50 of nanomolar levels, and is expected to avoid the loss of in vivo efficacy caused by the imbalance of acetazolamide diamox.
Inventors:
HE XINHUA (CN)
ZHOU TAO (CN)
YANG ZHAOFU (CN)
LI AILING (CN)
CHEN LIANG (CN)
LI TAO (CN)
HAN QIUYING (CN)
WANG JING (CN)
ZHOU TAO (CN)
YANG ZHAOFU (CN)
LI AILING (CN)
CHEN LIANG (CN)
LI TAO (CN)
HAN QIUYING (CN)
WANG JING (CN)
Application Number:
PCT/CN2021/074831
Publication Date:
August 12, 2021
Filing Date:
February 02, 2021
Export Citation:
Assignee:
ACAD OF MILITARY MEDICAL SCIENCE (CN)
International Classes:
C07D277/56; A61K31/426; A61K31/433; A61K31/496; A61K31/5377; A61P3/04; A61P9/10; A61P19/02; A61P25/08; A61P27/06; A61P35/02; C07D285/135; C07D417/12
Foreign References:
| CN111233786A | 2020-06-05 | |||
| CN1681557A | 2005-10-12 | |||
| CN101243063A | 2008-08-13 | |||
| CN107922345A | 2018-04-17 |
Other References:
YANG CHAOFU; WANG JING; CHENG YUNYUN; YANG XU; FENG YAN; ZHUANG XIAOMEI; LI ZHENWANG; ZHAO WANGYU; ZHANG JIWEN; SUN XIANYU; HE XIN: "N-Quinary heterocycle-4-sulphamoylbenzamides exert anti-hypoxic effects as dual inhibitors of carbonic anhydrases I/II", BIOORGANIC CHEMISTRY, ACADEMIC PRESS INC., NEW YORK, NY., US, vol. 100, 17 May 2020 (2020-05-17), US, XP086186293, ISSN: 0045-2068, DOI: 10.1016/j.bioorg.2020.103931
ABDEL-AZIZ ALAA A.-M.; EL-AZAB ADEL S.; GHIATY ADEL H.; GRATTERI PAOLA; SUPURAN CLAUDIU T.; NOCENTINI ALESSIO: "4-Substituted benzenesulfonamides featuring cyclic imides moieties exhibit potent and isoform-selective carbonic anhydrase II/IX inhibition", BIOORGANIC CHEMISTRY, ACADEMIC PRESS INC., NEW YORK, NY., US, vol. 83, 19 October 2018 (2018-10-19), US, pages 198 - 204, XP085602090, ISSN: 0045-2068, DOI: 10.1016/j.bioorg.2018.10.037
ABDEL-AZIZ ALAA A.-M.; EL-AZAB ADEL S.; GHIATY ADEL H.; GRATTERI PAOLA; SUPURAN CLAUDIU T.; NOCENTINI ALESSIO: "4-Substituted benzenesulfonamides featuring cyclic imides moieties exhibit potent and isoform-selective carbonic anhydrase II/IX inhibition", BIOORGANIC CHEMISTRY, ACADEMIC PRESS INC., NEW YORK, NY., US, vol. 83, 19 October 2018 (2018-10-19), US, pages 198 - 204, XP085602090, ISSN: 0045-2068, DOI: 10.1016/j.bioorg.2018.10.037
Attorney, Agent or Firm:
KINGSOUND & PARTNERS (CN)
Download PDF: