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Prodrug of a ROS-responsive JAK3 covalent inhibitor, preparation method and use for treating rheumatoid arthritis

A covalent inhibition, rheumatoid technology, applied in the treatment of rheumatoid arthritis, ROS-responsive JAK3 covalent inhibitor prodrug field, can solve problems such as anemia, infection, achieve good therapeutic effect, low toxicity, excellent The effect of membrane permeability

Active Publication Date: 2020-12-15
CHINA PHARM UNIV
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  • 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 normal tissues and organs, which may lead to toxic side effects such as anemia and infection

Method used

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  • Prodrug of a ROS-responsive JAK3 covalent inhibitor, preparation method and use for treating rheumatoid arthritis
  • Prodrug of a ROS-responsive JAK3 covalent inhibitor, preparation method and use for treating rheumatoid arthritis
  • Prodrug of a ROS-responsive JAK3 covalent inhibitor, preparation method and use for treating rheumatoid arthritis

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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

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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

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Application Information

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Patent Type & Authority Patents(China)
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
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