Use of azatryptamine derivatives as ido1 and/or tdo inhibitors

A technology of zatryptanthin and its derivatives, which is applied in the field of use of azatryptanthin derivatives as IDO1 and/or TDO inhibitors, and can solve problems such as not being involved and showing no activity
CN107260743BActive Publication Date: 2020-01-31PEKING UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
PEKING UNIV
Publication Date
2020-01-31

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Abstract

The invention discloses the use of azatryptanthin derivatives as IDO1 and / or TDO inhibitors. The derivatives are represented by the general formula (I), wherein the definition of each substituent is detailed in the description. The compound represented by the general formula (I) has inhibitory effect on indoleamine-2,3-dioxygenase 1 (IDO1) and / or tryptophan-2,3-dioxygenase (TDO), and can be used For the treatment of diseases with pathological features of tryptophan metabolism mediated by IDO1 and / or TDO, including but not limited to tumors, autoimmune diseases, infectious diseases, Alzheimer's disease, depression, anxiety.
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Description

technical field

[0001] The present invention relates to the field of medicinal chemistry, and more specifically relates to the use of an azatryptophan derivative as an inhibitor of tryptophan metabolism key enzymes along the kynuric acid pathway—IDO1 and / or TDO, for the treatment of IDO1 and / or TDO. Diseases with pathological features of TDO-mediated tryptophan metabolism, including but not limited to tumors, autoimmune diseases, infectious diseases, Alzheimer's disease, depression, anxiety. Background technique

[0002] As an essential amino acid in the human body, tryptophan can only be ingested through diet, and the content in the body is relatively small. The concentration of tryptophan in adult plasma is about 40-80μM, and about 95% of tryptophan is metabolized through the kynuric acid pathway[ Armstrong, M.D. and Stave, U. Metabolism. 1973, 22, 561–569.]. Metabolites of this pathway are immunosuppressive and play a key role in tumor immune escape. The first tryptopha...

Claims

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