Title:
USE OF SARMS COMPOUND CONTAINING ESTER-AROMATIC PROPIONAMIDE AND METABOLITE THEREOF IN PREPARATION OF ANTI-NOVEL-CORONAVIRUS DRUG
Document Type and Number:
WIPO Patent Application WO/2022/147917
Kind Code:
A1
Abstract:
The present invention belongs to the technical field of medicine, and particularly disclosed is the use of an SARMs compound containing ester-aromatic propionamide, EG-017, and a metabolite thereof, EG-2, in the preparation of an anti-novel-coronavirus drug, the inhibition of multi-organ damage such as lung and heart damage caused by novel coronavirus, and the treatment of pulmonary fibrosis. IFA is used to evaluate the in vitro anti-novel coronavirus (SARS-CoV-2) activity and cytotoxicity of the compound, and the result verifies that EG-017 has an obvious inhibitory activity on the replication of the novel coronavirus βCoV/KOR/KCDC03/2020 strain in Vero cells, which indicates that EG-017 has application prospects in the preparation of an anti-novel-coronavirus drug. Experiments also show that EG-017 can successfully inhibit the cytotoxicity of rapamycin with a high concentration on cells. An MTT method verifies that EG-017 can significantly improve the survival rate of rat myocardial cells. An experiment of the influence of EG-017 on a TGF-β1-induced A549 lung cancer cell fibrosis process verifies that EG-017 and the metabolite thereof have potential application value in the treatment of lung lesions caused by novel coronavirus, and the treatment of lung diseases, such as pulmonary fibrosis caused by other reasons.
Inventors:
ZHU XINFA (CN)
ZHU RAN (CN)
ZHU RAN (CN)
Application Number:
PCT/CN2021/085268
Publication Date:
July 14, 2022
Filing Date:
April 02, 2021
Export Citation:
Assignee:
CHANGCHUN GENESCIENCE PHARMACEUTICAL CO LTD (CN)
International Classes:
A61K45/06; A61K31/4406; A61P9/00; A61P11/00; A61P31/14
Foreign References:
| CN103772238A | 2014-05-07 | |||
| CN112007027A | 2020-12-01 |
Other References:
WAMBIER CARLOS GUSTAVO; GOREN ANDY: "Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection is likely to be androgen mediated", JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY, MOSBY, INC, US, vol. 83, no. 1, 10 April 2020 (2020-04-10), US , pages 308 - 309, XP086181548, ISSN: 0190-9622, DOI: 10.1016/j.jaad.2020.04.032
WANG AIXIN, ET AL.: "Pathology study on effect of sex hormones on paraquat-induced acute lung injury and pulmonary fibrosis", CHINESE JOURNAL OF LUNG DISEASES (ELECTRONIC EDITION), vol. 6, no. 3, 30 June 2013 (2013-06-30), pages 222 - 226, XP055949426, DOI: 10.3877 cma.j.issn.1674-6902.2013.03.006
HUANG YUJUN, ET AL. : "Effects of Androgen on Apoptosis of Myocardial Cells of Male Rats with Chronic Heart Failure", LINCHUANG XINXUEGUANBING ZAZHI - JOURNAL OF CLINICAL CARDIOLOGY, WUHAN XIEHE YIYUAN ZAZHISHE, CN, vol. 22, no. 10, 31 October 2006 (2006-10-31), CN , pages 631 - 633, XP055949428, ISSN: 1001-1439
WANG AIXIN, ET AL.: "Pathology study on effect of sex hormones on paraquat-induced acute lung injury and pulmonary fibrosis", CHINESE JOURNAL OF LUNG DISEASES (ELECTRONIC EDITION), vol. 6, no. 3, 30 June 2013 (2013-06-30), pages 222 - 226, XP055949426, DOI: 10.3877 cma.j.issn.1674-6902.2013.03.006
HUANG YUJUN, ET AL. : "Effects of Androgen on Apoptosis of Myocardial Cells of Male Rats with Chronic Heart Failure", LINCHUANG XINXUEGUANBING ZAZHI - JOURNAL OF CLINICAL CARDIOLOGY, WUHAN XIEHE YIYUAN ZAZHISHE, CN, vol. 22, no. 10, 31 October 2006 (2006-10-31), CN , pages 631 - 633, XP055949428, ISSN: 1001-1439
Attorney, Agent or Firm:
NINGBO WITS IP SERVICES CO., LTD (CN)
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