Title:
17-PYRIDYL-10α-METHYL-STEROID DERIVATIVE AND INTERMEDIATE COMPOUND, PREPARATION METHOD THEREFOR, USE THEREOF, AND PHARMACEUTICAL COMPOSITION THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/155846
Kind Code:
A1
Abstract:
The present invention relates to a 17-pyridyl-10α-methyl-steroid derivative and intermediate compound, a preparation method therefor, a use thereof, and a pharmaceutical composition thereof. A methyl group at a C-10 position of the steroid derivative of the present invention has an inverted α configuration, and the steroid derivative is a novel compound, and has a strong inhibitory effect on all of prostate cancer, breast cancer, colon cancer and lung cancer cells. In order to prepare the steroid derivative, a series intermediates corresponding to the steroid derivative are further synthesized in the present invention. The steroid derivative of the present invention can be used as a drug to effectively treat cancer, particularly cancer such as prostate cancer, breast cancer, colon cancer or lung cancer. The methyl group at the C-10 position of the steroid derivative of the present invention has an α configuration; compared with a β configuration, reaction activity with enzymes is greatly reduced, tolerance to in-vivo enzymes is good, in-vivo metabolism is expected to be slow, a drug effect duration is longer, and the development of long-effect formulations is facilitated.
Inventors:
LIU XIRONG (CN)
TANG JIE (CN)
JIANG HONGPING (CN)
HE QUN (CN)
LUO GUIFANG (CN)
ZHANG MU (CN)
LI LONG (CN)
WU SIQING (CN)
TANG JIE (CN)
JIANG HONGPING (CN)
HE QUN (CN)
LUO GUIFANG (CN)
ZHANG MU (CN)
LI LONG (CN)
WU SIQING (CN)
Application Number:
PCT/CN2023/076540
Publication Date:
August 24, 2023
Filing Date:
February 16, 2023
Export Citation:
Assignee:
SHANGHAI STEROL PHARMACEUTICAL TECH CO LTD (CN)
International Classes:
A61K31/58; C07J43/00; A61P13/08; A61P35/00
Domestic Patent References:
| WO1993020097A1 | 1993-10-14 |
Foreign References:
| US20110118228A1 | 2011-05-19 | |||
| CN107614062A | 2018-01-19 | |||
| US20160031929A1 | 2016-02-04 | |||
| CN111450103A | 2020-07-28 |
Other References:
LI LONGXIANG, XIE LONGYONG, WANG FENGJUN, HE WEIMIN, XIANG JIANNAN: "Synthesis and Antitumor Activity of 17-(2',5'-Disubstituted-oxazolyl)-androsta-4,16-dien-3-one Derivatives", CHINESE JOURNAL OF ORGANIC CHEMISTRY, SCIENCE PRESS, BEIJING., CN, vol. 34, no. 9, 5 May 2014 (2014-05-05), CN , pages 1864 - 1869, XP093086371, ISSN: 0253-2786, DOI: 10.6023/cjoc201402032
Attorney, Agent or Firm:
EASTNATION ATTORNEYS AT LAW (CN)
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