Invention Grant
- Patent Title: Oral GSNOR inhibitor and pharmaceutical use thereof
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Application No.: US17628904Application Date: 2021-04-25
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Publication No.: US11667616B2Publication Date: 2023-06-06
- Inventor: Yong Ji , Liping Xie , Shuang Zhao , Tianyu Song , Yi Han
- Applicant: NANJING MEDICAL UNIVERSITY
- Applicant Address: CN Jiangsu
- Assignee: NANJING MEDICAL UNIVERSITY
- Current Assignee: NANJING MEDICAL UNIVERSITY
- Current Assignee Address: CN Jiangsu
- Agency: JCIPRNET
- Priority: CN 2011622515.7 2020.12.31
- International Application: PCT/CN2021/089594 2021.04.25
- International Announcement: WO2022/141977A 2022.07.07
- Date entered country: 2022-01-21
- Main IPC: C07D277/02
- IPC: C07D277/02 ; A61P11/06 ; C07D417/14

Abstract:
Disclosed are a thiazolone derivative of N6022 and a pharmaceutical use thereof. The characteristic structure of the thiazolone derivative of N6022 is:
Compared to N6022, the compound of the present disclosure has good oral bioavailability and a longer half-life period. In in-vitro experiments, administering the compound of the present disclosure can improve migration ability, tube formation ability and, the permeability of human umbilical vein endothelial cells caused by high glucose, and administering the compound of the present disclosure at an animal level can obviously promote the angiogenesis and blood flow recovery of ischemic lateral limbs of diabetic mice. Overall, it suggests that the compound of the present disclosure can be used for treating diseases related to diabetic vascular complications.
Compared to N6022, the compound of the present disclosure has good oral bioavailability and a longer half-life period. In in-vitro experiments, administering the compound of the present disclosure can improve migration ability, tube formation ability and, the permeability of human umbilical vein endothelial cells caused by high glucose, and administering the compound of the present disclosure at an animal level can obviously promote the angiogenesis and blood flow recovery of ischemic lateral limbs of diabetic mice. Overall, it suggests that the compound of the present disclosure can be used for treating diseases related to diabetic vascular complications.
Public/Granted literature
- US20220372007A1 ORAL GSNOR INHIBITOR AND PHARMACEUTICAL USE THEREOF Public/Granted day:2022-11-24
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