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Title:
DEUTERATED DIPEPTIDE BORONIC ACID OR ESTER COMPOUND THEREOF, AND SYNTHESIS METHOD AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2018/171816
Kind Code:
A1
Abstract:
Disclosed in the present invention are a deuterated dipeptide boronic acid or an ester compound thereof, or a crystalline form, pharmaceutically acceptable hydrate or solvate thereof, the structure thereof being shown in formula (a), wherein: R 1, R2, R3, R4, R5, and R6 are independently selected from hydrogen, deuterium, or a halogen, or one of a plurality of deuterated or fully deuterated C1-C4 alkyl groups; and at least one of R1, R2, R3, R4, R5, or R6 is deuterated or is deuterium. The compound of the present invention can effectively inhibit proteasomes, and can effectively treat or prevent cancer, cardiovascular disease, inflammation, immune disease, kidney disease, angiogenesis or prostate disease.

Inventors:
ZHU, Yongqiang (No.1, Wenyuan Road Qixia Distric, Nanjing Jiangsu 6, 210046, CN)
LEI, Meng (No.1, Wenyuan Road Qixia Distric, Nanjing Jiangsu 6, 210046, CN)
BAI, Enhe (No.1, Wenyuan Road Qixia Distric, Nanjing Jiangsu 6, 210046, CN)
FENG, Huayun (No.1, Wenyuan Road Qixia Distric, Nanjing Jiangsu 6, 210046, CN)
Application Number:
CN2018/087761
Publication Date:
September 27, 2018
Filing Date:
May 22, 2018
Export Citation:
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Assignee:
NANJING LINGRUI PHARMACEUTICAL TECHNOLOGY CO., LTD (No.9, Weidi Road Qixia Distric, Nanjing Jiangsu 6, 210046, CN)
International Classes:
C07F5/02; A61K31/69; A61P9/00; A61P13/08; A61P13/12; A61P29/00; A61P35/00; A61P37/00; C07B59/00; C07H23/00
Attorney, Agent or Firm:
NANJING SUGAO PATENT AND TRADEMARK FIRM (ORDINARY PARTNERSHIP) (Room 1912, Longtaiguoji MansionNo.198, East Zhongshan Street, Baixia Distric, Nanjing Jiangsu 5, 210005, CN)
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