Title:
TETRAHYDRONAPHTHO[1,2-B]FURAN-2(3H)-ONE COMPOUND AND CRYSTAL RESEARCH THEREOF
Document Type and Number:
WIPO Patent Application WO/2021/143853
Kind Code:
A1
Abstract:
Disclosed is a tetrahydronaphtho[1,2-b]furan-2(3H)-one compound and a crystal thereof. The absolute configuration of the compound is an R configuration or an S configuration. Compared with a racemate, the R configuration and the S configuration of the compound provide significantly better therapeutic effect for rat arthritis; in addition, compared with free base crystals of the compound, crystals produced by salt screening provide significantly better aqueous solubility and stability.
Inventors:
SUN QINGYAN (CN)
ZHANG WEIDONG (CN)
ZHANG WEIDONG (CN)
Application Number:
PCT/CN2021/072178
Publication Date:
July 22, 2021
Filing Date:
January 15, 2021
Export Citation:
Assignee:
SHANGHAI QINGDONG BIOTECHNOLOGY CO LTD (CN)
International Classes:
C07D307/92; A61K31/343; A61K31/365; A61P19/02; A61P29/00
Domestic Patent References:
| WO2019011285A1 | 2019-01-17 |
Other References:
DATABASE REGISTRY 1 February 2019 (2019-02-01), ANONYMOUS: "Naphtho[1,2-b]furan-2(3H)-one, 8-[(2-bromophenyl)methoxy]-3- [(dimethylamino)methyl]-3a,4,5,9b-tetrahydro-6,9-dimethyl-, (3S,3aS,9bR)- (CA INDEX NAME)", XP055828509, retrieved from STN Database accession no. 2264085-55-2
DATABASE REGISTRY 1 February 2019 (2019-02-01), ANONYMOUS: "Naphtho[1,2-b]furan-2(3H)-one, 8-[(2-bromophenyl)methoxy]-3- [(dimethylamino)methyl]-3a,4,5,9b-tetrahydro-6,9-dimethyl-, (3R,3aS,9bR)- (CA INDEX NAME)", XP055828511, retrieved from STN Database accession no. 2264085-37-0
DATABASE REGISTRY 1 February 2019 (2019-02-01), ANONYMOUS: "Naphtho[1,2-b]furan-2(3H)-one, 8-[(2-bromophenyl)methoxy]-3- [(dimethylamino)methyl]-3a,4,5,9b-tetrahydro-6,9-dimethyl-, hydrochloride (1:1), (3S,3aS,9bR)- (CA INDEX NAME)", XP055828517, retrieved from STN Database accession no. 2264085-56-3
DATABASE REGISTRY 1 February 2019 (2019-02-01), ANONYMOUS: "Naphtho[1,2-b]furan-2(3H)-one, 8-[(2-bromophenyl)methoxy]-3- [(dimethylamino)methyl]-3a,4,5,9b-tetrahydro-6,9-dimethyl-, hydrochloride (1:1), (3R,3aS,9bR)- (CA INDEX NAME)", XP055828521, retrieved from STN Database accession no. 2264085-48-3
HAO CHEN, WU GUOZHEN, GAO SHUANG, GUO RUIHUA, ZHAO ZENG, YUAN HU, LIU SHANXIANG, WU JIAN, LU XIAOLONG, YUAN XING, YU ZONGMIN, ZU X: "Discovery of Potent Small-Molecule Inhibitors of Ubiquitin-Conjugating Enzyme UbcH5c from α-Santonin Derivatives", JOURNAL OF MEDICINAL CHEMISTRY, vol. 60, no. 16, 24 August 2017 (2017-08-24), pages 6828 - 6852, XP055751984, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.6b01829
GAO, SHUANG: "Screening for Active Compounds Targeting Ubiquitin-conjugating Enzyme UbcH5c from Sesquiterpene Lactones and Study on Their Anti-inflammatory Effects", CHINESE MASTER’S THESES FULL-TEXT DATABASE, MEDICINE & HEALTH SCIENCES, no. 6, 15 June 2017 (2017-06-15), pages 1 - 93, XP055674238, ISSN: 1674--024
DATABASE REGISTRY 1 February 2019 (2019-02-01), ANONYMOUS: "Naphtho[1,2-b]furan-2(3H)-one, 8-[(2-bromophenyl)methoxy]-3- [(dimethylamino)methyl]-3a,4,5,9b-tetrahydro-6,9-dimethyl-, (3R,3aS,9bR)- (CA INDEX NAME)", XP055828511, retrieved from STN Database accession no. 2264085-37-0
DATABASE REGISTRY 1 February 2019 (2019-02-01), ANONYMOUS: "Naphtho[1,2-b]furan-2(3H)-one, 8-[(2-bromophenyl)methoxy]-3- [(dimethylamino)methyl]-3a,4,5,9b-tetrahydro-6,9-dimethyl-, hydrochloride (1:1), (3S,3aS,9bR)- (CA INDEX NAME)", XP055828517, retrieved from STN Database accession no. 2264085-56-3
DATABASE REGISTRY 1 February 2019 (2019-02-01), ANONYMOUS: "Naphtho[1,2-b]furan-2(3H)-one, 8-[(2-bromophenyl)methoxy]-3- [(dimethylamino)methyl]-3a,4,5,9b-tetrahydro-6,9-dimethyl-, hydrochloride (1:1), (3R,3aS,9bR)- (CA INDEX NAME)", XP055828521, retrieved from STN Database accession no. 2264085-48-3
HAO CHEN, WU GUOZHEN, GAO SHUANG, GUO RUIHUA, ZHAO ZENG, YUAN HU, LIU SHANXIANG, WU JIAN, LU XIAOLONG, YUAN XING, YU ZONGMIN, ZU X: "Discovery of Potent Small-Molecule Inhibitors of Ubiquitin-Conjugating Enzyme UbcH5c from α-Santonin Derivatives", JOURNAL OF MEDICINAL CHEMISTRY, vol. 60, no. 16, 24 August 2017 (2017-08-24), pages 6828 - 6852, XP055751984, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.6b01829
GAO, SHUANG: "Screening for Active Compounds Targeting Ubiquitin-conjugating Enzyme UbcH5c from Sesquiterpene Lactones and Study on Their Anti-inflammatory Effects", CHINESE MASTER’S THESES FULL-TEXT DATABASE, MEDICINE & HEALTH SCIENCES, no. 6, 15 June 2017 (2017-06-15), pages 1 - 93, XP055674238, ISSN: 1674--024
Attorney, Agent or Firm:
WAYNE INTELLECTUAL PROPERTY AGENCY CO., LTD. (CN)
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