ROSresponsive JAK3 covalent inhibitor prodrug and preparation method thereof, and application to treatment of rheumatoid arthritis
A covalent inhibition, rheumatoid technology, applied in the treatment of rheumatoid arthritis, ROS-responsive JAK3 covalent inhibitor prodrug field, can solve anemia, infection and other problems, achieve good therapeutic effect, excellent membrane penetration sex, low toxicity
Active Publication Date: 2020-03-17
CHINA PHARM UNIV
View PDF0 Cites 0 Cited by
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
During the test, we found that the inhibitor can inhibit the activity of JAK3 in norma
Method used
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View moreImage
Smart Image Click on the blue labels to locate them in the text.
Smart ImageViewing Examples
Examples
Experimental program
Comparison scheme
Effect test
Embodiment Construction
[0036] The following describes the substantive content of the present invention in detail in conjunction with the drawings and embodiments, but does not limit the protection scope of the present invention.
[0037] 1. Compound synthesis and structure confirmation
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more PUM
Login to view more Abstract
The invention discloses an ROSresponsive JAK3 covalent inhibitor prodrug and a preparation method thereof, and application to treatment of rheumatoid arthritis. The prodrug has a chemical structure shown in the specification. According to the JAK3 covalent inhibitor prodrug, the difference of ROS levels under physiological and pathological conditions is utilized and an active compound shown in a formula (1) in the prior art can be selectively released at an attacked part; and the prodrug has high membrane permeability, the anti-proliferation activity and the capability of regulating and controlling an STAT signal path and has the good treatment effect in a rheumatoid arthritis inflammation mouse model. The prodrug has extremely low toxicity in ICR healthy mice, so that covalent binding between JAK inhibitor molecules and thiol functional groups in various biomacromolecules or other normal physiological tissues is avoided. The prodrug can be used for preparing anti-rheumatoid arthritisdrugs.
Description
technical field [0001] The invention belongs to the field of drug synthesis, and specifically relates to a ROS-responsive JAK3 covalent inhibitor prodrug, a preparation method and an application for treating rheumatoid arthritis. Background technique [0002] Rheumatoid arthritis is a systemic, progressive chronic autoimmune disease (Therapeuticsuppression of tissue reactivity.I.Comparison of the effects of cortisone andaminopterin.Am J Med Sci 1951,221,169-75.Synthesis and Evaluation of HydrogenPeroxide Sensitive Prodrugs of Methotrexate and Aminopterin for the Treatment of Rheumatoid Arthritis.J Med Chem 2018,61,3503-3515.Therapeutic suppression of tissue reactivity.II.Effect of aminopterin in rheumatoid arthritis and psoriasis.Am J Med Sci 1951,221,17) The main manifestations are endometrial injury, cartilage erosion, bone injury and joint deformity (The comparative effectiveness of abatacept versus anti-tumor necrosis factor switching for rheumatoid arthritis patients pr...
Claims
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more Application Information
Patent Timeline
Login to view more IPC IPC(8): A61K47/54A61K31/437A61P19/02A61P37/02C07F5/02
CPCA61K31/437A61K47/54A61P19/02A61P37/02C07F5/025
Inventor 尤启冬姜正羽张梁颖鲍启超杨伟康陆朦辰郭小可徐晓莉王磊
Owner CHINA PHARM UNIV
Who we serve
- R&D Engineer
- R&D Manager
- IP Professional
Why Eureka
- Industry Leading Data Capabilities
- Powerful AI technology
- Patent DNA Extraction
Social media
Try Eureka
Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.
© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap