5-pyrimidine-6-oxy-pyrazolopyridine derivatives, and preparation method and application thereof
By developing a novel 5-pyrimidine-6-oxo-pyrazolopyridine derivative, Hsp110 and HDAC6 were inhibited, solving the problem that existing drugs could not effectively intervene in pulmonary vascular remodeling and achieving a significant therapeutic effect on pulmonary hypertension.
CN122167424APending Publication Date: 2026-06-09CENT SOUTH UNIV
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- CENT SOUTH UNIV
- Filing Date
- 2026-02-12
- Publication Date
- 2026-06-09
AI Technical Summary
Technical Problem
Existing drugs for pulmonary hypertension cannot effectively stop the progression of the disease, and there is a lack of small molecule inhibitors that can inhibit Hsp110 and HDAC6, thus failing to effectively intervene in pulmonary vascular remodeling.
Method used
We developed a novel 5-pyrimidine-6-oxo-pyrazolopyridine derivative and prepared an anti-pulmonary vascular remodeling drug by inhibiting two targets, Hsp110 and HDAC6, to intervene in pulmonary vascular remodeling-related pathways.
Benefits of technology
It achieved a significant therapeutic effect on pulmonary hypertension by simultaneously inhibiting Hsp110 and HDAC6, significantly reducing pulmonary vascular remodeling, and exhibiting a significant anti-vascular remodeling effect.
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Figure CN122167424A_ABST
Abstract
The application belongs to the technical field of pharmaceutical chemistry, and relates to a 5-pyrimidine-6-oxygen-pyrazolopyridine derivative as well as a preparation method and application thereof. The 5-pyrimidine-6-oxygen-pyrazolopyridine derivative is a compound, an optical isomer, a crystal or a pharmaceutically acceptable salt thereof shown in the following structure: wherein R1 is selected from C1-C8 linear or branched alkyl; R2 is selected from -CONH2-(CH2) n -CONHR7, -CONHNH-R8; n is an integer of 2-8. The compound synthesized by the application can obviously intervene in Hsp110 and HDAC6 double channels, has obvious anti-vascular remodeling effect, has obvious treatment effect on pulmonary arterial hypertension disease, and can be used for candidate clinical drug development.
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