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Title:
STACHYDRINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND APPLICATIONS THEREOF IN PREPARATION OF DRUGS FOR TREATING CARDIOVASCULAR AND CEREBROVASCULAR DISEASES
Document Type and Number:
WIPO Patent Application WO/2018/072689
Kind Code:
A1
Abstract:
The present invention provides a stachydrine derivative, a preparation method therefor, and applications thereof in the preparation of drugs for treating cardiovascular and cerebrovascular diseases. The stachydrine derivative is a component represented by formula (I), or a stereoisomer thereof or a pharmaceutically-acceptable salt form thereof. The synthesis method for the stachydrine derivative comprises: enabling Lproline and formaldehyde to have a hydrogenation reaction under the action of a catalyst to prepare N-methyl-L-proline; and enabling the N-methyl-L-proline and H-X-R1 to have a condensation reaction under the action of dicyclohexylcarbodiimide to prepare the component represented by formula (I). Proved by pharmacological experiments in the present invention, the stachydrine derivative provided in the present invention has the effect for protecting nerves, and has the effect for treating cardiovascular and cerebrovascular diseases. The present invention also provides applications of the stachydrine derivative in the preparation of drugs for treating cardiovascular and cerebrovascular diseases.

Inventors:
LI, Wenbao (LIU Lili, No.23 Hongkong East Road Laoshan Distric, Qingdao Shandong 1, 266061, CN)
LI, Feng (LIU Lili, No.23 Hongkong East Road Laoshan Distric, Qingdao Shandong 1, 266061, CN)
ZHANG, Liang (LIU Lili, No.23 Hongkong East Road Laoshan Distric, Qingdao Shandong 1, 266061, CN)
ZHANG, Peng (LIU Lili, No.23 Hongkong East Road Laoshan Distric, Qingdao Shandong 1, 266061, CN)
DAI, Long (LIU Lili, No.23 Hongkong East Road Laoshan Distric, Qingdao Shandong 1, 266061, CN)
GUAN, Huashi (LIU Lili, No.23 Hongkong East Road Laoshan Distric, Qingdao Shandong 1, 266061, CN)
Application Number:
CN2017/106555
Publication Date:
April 26, 2018
Filing Date:
October 17, 2017
Export Citation:
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Assignee:
MARINE BIOMEDICAL RESEARCH INSTITUTE OF QINGDAO CO., LTD. (LIU Lili, No.23 Hongkong East Road Laoshan Distric, Qingdao Shandong 1, 266061, CN)
International Classes:
C07D207/16; A61K31/401; A61K38/05; A61P9/00; A61P9/10; A61P25/00; C07K5/078
Foreign References:
CN102670592A2012-09-19
CN101596232A2009-12-09
US5589182A1996-12-31
Other References:
CORNELIUS, D.A.: "Synthesis of Highly Deuterated Amino Acids and Related Compounds. L-proline-d7. S-benzyl-DL-cysteine-d3. Carbobenzoxyglycine-d2-amide. Synthesis of N-methyl-L-prolyl-L-proline", DISS. ABSTR. INT. B, vol. 33, no. 3, 31 December 1972 (1972-12-31), pages 1051 - 1052
DAI, LIANGPING ET AL.: "Advances in the Study of Pharmacological Action of Stachydrine", CHINESE JOURNAL OF EXPERIMENTAL TRADITIONAL MEDICAL FORMULAE, vol. 22, no. 19, 4 August 2016 (2016-08-04), pages 189 - 193, ISSN: 1005-9903
Attorney, Agent or Firm:
QINGDAO HECHUANG INTELLECTUAL PROPERTY AGENCY FIRM (GENERAL PARTNERSHIP) (WANG, XiaoxiaoRoom 1803, Building B, Hisense Chuangzhi,Valley, 20 Zhuzhou Road, Laoshan Distric, Qingdao Shandong 1, 266101, CN)
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