37 results about "Melatonin receptor" patented technology

A method of treating, preventing, or ameliorating a pathological condition associated with a melatonin receptor in a mammal by using a pharmaceutical composition containing a compound of formula (I) as a ligand interacting with the melatonin receptor,R1, R2, R3, R4 and R7 are independently H, halo, alkyloxyl, alkyl or hydroxyl, provided that one of R1, R2, R3 and R7 is X—(CH2)n—R8; R5 is alkyl or arylalkyl; R6 is H or alkyl; X is a bond, O, S, SO, SO2, CO or NH; n=0-10; R8 is alkenyl, substituted or unsubstituted aryl, NR9R10, or OR9; R9 is H, substituted or unsubstituted arylmethyl, or alkenyl; and R10 is H or alkyl.

The invention provides a number of naphthalene derivatives or stereoisomers, tautomers, nitrogen oxides, metabolites, pharmaceutically acceptable salts or prodrugs thereof which are used for excitement of melatonin receptors. The invention also discloses pharmaceutical compositions containing such compounds and application thereof in treatment of central nervous system dysfunction of mammals, especially human.

In alternative embodiments, provided are methods for: modifying circadian rhythmicity or timing in a mammal, treating psychiatric conditions or symptoms due to alterations in a human circadian regulatory system, treating sleep problems in a mammal, or inducing sleep or activity suppression, or causing an arousal or wakening reaction, comprising administration to a mammal or human a compound or composition capable of modifying a prokineticin 2 (PK2) expression or activity, and / or a PKR2 (PK2 receptor), a vasopressin receptor (VR), and / or a melatonin receptor (MR) expression or activity.

The present invention provides a prophylactic or therapeutic agent for an autism spectrum disorder containing compound (I) having melatonin receptor affinity. A compound represented by the formula:wherein each symbol is as described in the specification, or a salt thereof.

The present invention provides the polybenzyl derivative (1‑12) represented by structural formula (I) or its pharmaceutical composition, its preparation method, its application in the preparation of melatonin receptor agonist, and its preparation in the treatment or Use in drugs for the prevention of diseases of the central nervous system associated with melatonin receptors.

The invention discloses an anti-insomnia composition, an application of the composition, a multi-phase pulse immediate-release preparation prepared by use of the composition and a preparation method of the preparation. The anti-insomnia composition consists of a component A and a component B, wherein the component A is one or more of melatonin, melatonin analogue and corresponding salt, melatonin receptor stimulant, 5-hydroxytryptamine 2C, receptor antagonist and 5-HTP (5-hydroxytryptophan); the component B is one or more of petroselinum neapolitanum extract, melissa extract, tuber fleeceflower stem extract, chamomile extract, passion flower extract, radix paeoniae alba extract, manyprickle acanthopanax extract, polygala tenuifolia extract, hyperforin perforatum extract, flos albiziae extract, lily extract and prunella vulgaris extract. The composition and the multi-phase pulse immediate-release preparation prepared by use of the composition have the characteristic of better anti-insomnia effect than a common melatonin preparation, and can effectively solve and improve the problem of difficult sleep of human or mammals while effectively solving and improving the insomnia problems such as light sleep or dreaminess or early awakening or difficult sleep after wakeup of human or mammals.

The invention provides new compounds of formula (I) wherein R1, R2, R3, R4, and X have different meanings. Preparative processes, pharmaceutical compositions, and uses thereof in the treatment or prevention of conditions mediated by melatonin receptors are also provided.

The invention provides a new application of 7-alkoxy fangchinoline derivatives or pharmaceutically acceptable salts thereof in the preparation of GSK-3β inhibitors and in the treatment and improvement of depressive symptoms. The compound 1‑8 with the structure of formula (I) has shown the effect of promoting the phosphorylation of glycogen synthesis kinase ‑3β (GSK‑3β) at the level of cells and whole animals, and then inhibiting its activity; the results of animal experiments found that compound 1‑8 May be enhanced by 5‑HT 1A Receptor and melatonin receptor function, inhibits 5‑HT 2A Receptor function, inhibit GSK‑3β activity, improve depressive symptoms such as hopelessness, loss of pleasure, anxiety and sleep disorders.

The invention relates to the pharmaceutical synthesis field and discloses N-(naphthoxyalkyl)heteroarylpiperidine compounds and a preparation method and applications thereof. The compounds disclosed by the invention are the compound shown in the formula I and pharmaceutically acceptable acid addition salts thereof, wherein n is 0, 1, 2 or 3; R is acetamino, acetoxy, acethythio, oximido, amino, aminocarbonyl, dimethylamino, diethylamino, hydroxyl, trifluoromethyl, trifluoroacetyl, cyano, phenyl, aldehyde group, benzoyl, fluorine, chlorine, bromine or iodine. The preparation method is as follows: 7-methoxynaphthalene compound used as raw material and 6-fluoro-3-(4-piperidyl)-1,2-benzoisoxazole are used to perform N-alkylation reaction. The N-(naphthoxyalkyl)heteroarylpiperidine compounds can act on 5-HT2A receptor, dopamine D2 receptor and melatonin receptor, are the compounds with the multi-target function and have the antipsychotic function.

A method for improving memory in healthy subjects is disclosed. This method makes use of melatonin receptor antagonists such as luzindole and / or K-185 to reverse the inhibitory effect of melatonin. This invention is particularly relevant among subjects that do not show signs of central nervous system disorders and wish to improve their cognitive performance, especially in tasks.

The present invention relates to as A 2B Adenosine receptor antagonists and MT 3 Novel pyridine derivatives of formula (I) as ligands for the melatonin receptor, processes for their preparation, pharmaceutical compositions comprising said compounds and manufacture for the treatment of 2B receptor and by inhibiting MT 3 Use in medicine for pathological conditions or diseases ameliorated by melatonin receptors such as respiratory diseases, metabolic disorders, neurological disorders and cancers: