TDO2 inhibitor

By developing a new small molecule compound with an imidazoloisoindole structure, specifically inhibiting IDO1 or TDO2 enzymes, the immunosuppression and tumor resistance caused by tryptophan degradation are solved, the anti-cancer treatment effect is enhanced and treatment plans are provided for immune-related diseases.

CN115010712BActive Publication Date: 2025-07-25GENENTECH INC +1
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Patent Information

Application Number
CN202210532542.8
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Priority Date
2016-11-21
Filing Date
2016-12-23
Publication Date
2025-07-25
Estimated Expiration
2036-12-23

AI Technical Summary

Technical Problem

The prior art is difficult to effectively inhibit the activity of tryptophan 2,3-dioxygenase (TDO2), resulting in the problem of immunosuppression, tumor resistance, chronic infection, HIV infection, AIDS, autoimmune diseases and immune tolerance not effectively resolved.

Method used

A new type of compounds with an imidazoloisoindole structure have been developed that can specifically inhibit IDO1 or TDO2, or simultaneously inhibit the tryptophan degradation of these two enzymes, and regulate their activity through small-molecular compounds.

Benefits of technology

It enhances the activation ability of T cells, improves the effectiveness of anti-cancer treatments, and reduces immunosuppression and tumor resistance, providing therapeutic strategies for immune-related diseases and disorders.

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Abstract

The present invention provides inhibitors of cell-expressed TDO2 and pharmaceutical compositions thereof, which can be used to modulate the activity of tryptophan 2,3-dioxygenase; treat immunosuppression; treat medical conditions that benefit from inhibition of tryptophan degradation; enhance the effectiveness of anti-cancer treatment including administration of anti-cancer agents; and treat tumor-specific immunosuppression associated with cancer.
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