4-(penyl-piperidin-4-ylidene-methyl)-benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders

Abstract

Compounds of general formula I[Chemical formula should be inserted here. Please see paper copy] R1 is selected from any one of phenyl, pyridinyl, pyrrolyl, thienyl, furanyl, imidazolyl, triazolyl, and pyridine N-oxide; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1,2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety and functional gastrointestinal disorders.

Description

field of invention [0001] The present invention relates to a new compound, its preparation method, use and pharmaceutical composition containing the new compound. The new compounds are suitable for the treatment, in particular, of pain, anxiety and functional gastrointestinal disorders. Background of the invention [0002] It has been established that delta receptors play a role in many bodily functions such as the circulatory and pain systems. It has thus been found that ligands for the delta receptor may be useful as analgesic and / or antihypertensive agents. Ligands for the delta receptor have also been shown to have immunomodulatory activity. [0003] At least three distinct opioid receptors (μ, δ, and κ) have now been identified, and all three receptors are clearly seen in the central and peripheral nervous systems of many species, including humans. Analgesia has been observed in various animal models when one or more of these receptors is activated. [0004] With fe...

AI Technical Summary

Problems solved by technology

[0006] It has been determined that the analgesics present in the prior art have a number of disadvantages, namely their poor pharmacokinetics and inability to analgesia when administered systemically

Furthermore, it has been demonstrated that the preferred delta agonist compounds described in the prior art exhibit a pronounced convulsive effect when administered systemically

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