Title:
GONADOTROPIN-RELEASING HORMONE ANTAGONIST, AND PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/072284
Kind Code:
A1
Abstract:
The present invention relates to a class of gonadotropin-releasing hormone antagonists, which have antagonistic activity to gonadotropin-releasing hormone and can be used for preventing or treating sex hormone-dependent diseases, such as benign prostatic hypertrophy, hysteromyoma, endometriosis, metrofibroma, precocious puberty, amenorrhea, premenstrual syndrome, and dysmenorrhea; or a prodrug, a pharmaceutically acceptable salt, a hydrate or a solvate thereof, and a pharmaceutical composition containing same. (I)
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Inventors:
TIAN JINGWEI (CN)
ZOU FANGXIA (CN)
YU DAWEI (CN)
YE LIANG (CN)
LU JING (CN)
ZHANG RUI (CN)
ZHANG JIANZHAO (CN)
WANG WENYAN (CN)
ZOU FANGXIA (CN)
YU DAWEI (CN)
YE LIANG (CN)
LU JING (CN)
ZHANG RUI (CN)
ZHANG JIANZHAO (CN)
WANG WENYAN (CN)
Application Number:
PCT/CN2022/128588
Publication Date:
May 04, 2023
Filing Date:
October 31, 2022
Export Citation:
Assignee:
SHANDONG LUYE PHARMACEUTICAL CO LTD (CN)
International Classes:
C07D495/04; A61K31/519; A61P13/08; A61P15/00; A61P15/08; A61P15/18; A61P35/00
Domestic Patent References:
| WO2021023877A2 | 2021-02-11 | |||
| WO2021023876A1 | 2021-02-11 | |||
| WO2003064429A1 | 2003-08-07 |
Foreign References:
| CN114907370A | 2022-08-16 | |||
| CN113754679A | 2021-12-07 | |||
| CN111925379A | 2020-11-13 | |||
| CN1768065A | 2006-05-03 | |||
| CN111943960A | 2020-11-17 |
Other References:
ZOU FANGXIA, WANG YAO, YU DAWEI, LIU CHUNJIAO, LU JING, ZHAO MIN, MA MINGXU, WANG WENYAN, JIANG WANGLIN, GAO YONGLIN, ZHANG RUI, Z: "Discovery of the thieno[2,3-d]pyrimidine-2,4-dione derivative 21a: A potent and orally bioavailable gonadotropin-releasing hormone receptor antagonist", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 242, 1 November 2022 (2022-11-01), AMSTERDAM, NL , pages 114679, XP093060366, ISSN: 0223-5234, DOI: 10.1016/j.ejmech.2022.114679
MIWA, K. ET AL.: "Discovery of 1-{4-[1-(2, 6-Difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2, 4-dioxo-1, 2, 3, 4-tetrahydrothieno[2, 3-d] pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a Potent, Orally Active, Non-Peptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor", JOURNAL OF MEDICINAL CHEMISTRY, vol. 54, no. 14, 9 June 2011 (2011-06-09), pages 4998 - 5012, XP055012890, DOI: 10.1021/jm200216q
MIWA, K. ET AL.: "Discovery of 1-{4-[1-(2, 6-Difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2, 4-dioxo-1, 2, 3, 4-tetrahydrothieno[2, 3-d] pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a Potent, Orally Active, Non-Peptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor", JOURNAL OF MEDICINAL CHEMISTRY, vol. 54, no. 14, 9 June 2011 (2011-06-09), pages 4998 - 5012, XP055012890, DOI: 10.1021/jm200216q
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