TRPV1 (transient receptor potential cation channel, subfamily V, member 1) antagonists, and preparation method and medical application thereof

Abstract

The invention relates to compounds shown as a general formula (1) and salts of the compounds. The compounds are TRPV1 (transient receptor potential cation channel, subfamily V, member 1) antagonists, and have better analgesic action. The invention also relates to a preparation method for the compounds, medicinal preparations containing the compounds, and application of the compounds and medicinal compositions thereof in treatment of pain.

Description

technical field The invention relates to the field of medicinal chemistry, in particular to a class of TRPV1 antagonists. The invention also discloses a preparation method thereof, a pharmaceutical composition containing the compounds as active ingredients, and their application in treating pain. Background technique Pain is a complex physiological and psychological activity, and it is one of the most common clinical symptoms. Due to the complexity of pathological mechanisms, pain has become one of the major unmet medical needs. There are two main types of analgesic drugs currently used clinically: opioids and nonsteroidal anti-inflammatory drugs (NSAIDs). Opioid analgesics produce analgesic effect by binding to opioid receptors and activating opioid receptors. These drugs usually work quickly and can significantly reduce or eliminate pain. But the biggest side effect of this class of drugs is: continuous repeated use will produce drug resistance and lead to addiction, o...

AI Technical Summary

Problems solved by technology

The natural product capsaicin, as the first discovered TRPV1 receptor agonist, has extremely high application research value, but the application of capsaicin will produce some side effects, such as local application of capsaicin will cause a burning sensation, and it will cause pain after a few days to a few weeks Loss and loss of response to various noxious stimuli