37 results about "Melatonin receptor" patented technology

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 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.

The invention relates to split-ring lupinane derivatives, a medicinal composition containing the split-ring lupinane derivative and application of the split-ring lupinane derivatives in the preparation of medicine for prevention, treatment or slow-down of diseases of the central nervous system related to agonism of melatonin receptors. In the invention, through a semi-synthesis method, the structural limitation of natural products in the prior art is changed, a series of split-ring lupinane derivatives is designed and synthesized, and the agonist activity of the split-ring lupinane derivatives over the melatonin receptor in vitro is verified; through further experiments, the split-ring lupinane derivative compound can be applied to the research of the medicine for the treatment of the diseases related to a dysfunction of the central nervous system.

The invention provides naphthalene derivatives or stereisomers, tautomers, nitric oxides, metabolites, pharmaceutically acceptable salts or prodrugs thereof for exciting a melatonin receptor. The invention discloses pharmaceutical compositions containing the compounds, and use of the compounds or the pharmaceutical compositions of the compound for treating central nervous system dysfunction of mammal, especially human.

The invention provides melatonin and application of a melatonin composition in preparation of a medicine for treating and adjunctively treating osteosarcoma. It is found in experimental research thatthe expression of melatonin receptor MT1 in osteosarcoma cells is increased, and tumor cell homogeneous CIC increasing is observed, using of melatonin can inhibit the CIC key pathway Rho / ROCK throughthe cAMP / PKA signal pathway, so that the homogeneous CIC can be inhibited, the mitochondrial physiology of osteosarcoma cells can be intervened, and the anti-osteosarcoma invasion and anti-metastasiseffects can be provided. Finally, application of melatonin and a better melatonin composition in preparation of medicine for treatment and adjuvant therapy of osteosarcoma is provided, and new treatment targets and directions are provided for clinic.

The invention provides a series of indole derivatives or stereoisomers, tautomers, nitrogen oxides, metabolic products and pharmaceutically acceptable salts or prodrugs thereof. The indole derivatives can be taken as melatonin receptor stimulants. The invention also discloses a pharmaceutical composition containing the compounds, and a use of the compounds or the pharmaceutical composition of the compounds in treating the functional disorder of the central nervous system of mammal and in particular human.

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.

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.

The invention provides an application of albiflorin or pharmaceutically acceptable salts of albiflorin to preparation of human melatonin system function improving products. Albiflorin or the pharmaceutically acceptable salts of albiflorin serving as an endogenous melatonin secretion accelerant and a melatonin receptor stimulant can be used for preparing drugs, food, health care products, food additives or nutritional supplements for improving and treating sub-health statuses and / or diseases caused by melatonin system dysfunction, wherein the sub-health statuses are selected from one or more of biological rhythm disorder type sleep disorder, senile sleep disorder, affective disorder, cognitive disorder and immune system dysfunction; the diseases are selected from one or more of depression, anxiety disorder, Alzheimer's disease and Parkinson's disease.

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.

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.

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 invention discloses application of ramelteon in preparation of a drug for treating ischemic brain injury. Ramelteon can alleviate acute focal cerebral ischemic injury and neurological dysfunctioncaused by permanent middle cerebral artery embolization in mice, inhibit pathological inflammatory response, and promote neural functional recovery in the late stage of ischemia. The use of ramelteonis achieved primarily by the following mechanism: ramelteon can inhibit cell autophagy during cerebral ischemia and reduces autophagic death of neurons by stimulating the MT2 melatonin receptor; in addition, ramelteon can also inhibit the release of inflammatory factors secondary to cerebral ischemia, reduce inflammatory cell damage, and ultimately exert a therapeutic effect against cerebral ischemia. The application provided by the invention has the beneficial effects of providing a new use of ramelteon, and providing a basis for screening new drugs.

The present invention refers to a pharmaceutical composition that comprises the synergistic combination of an antagonist agent of the NMDA receptor, such as the active principle: ketamine and an agonist agent of the MT1 and MT2 melatonin receptors, as is the active principle: melatonin, which are in a pharmaceutical composition, which is indicated for the control and treatment of psychiatric diseases.

The invention discloses a method for improving the in-vitro maturation and development rate of porcine oocytes by adopting agomelatine. Particularly, the method for improving the in-vitro maturation and development rate of the porcine oocytes by adopting a melatonin receptor stimulant agomelatine is adopted, so that porcine cumulus cell expansion, oocyte in vitro maturation (IVM), oocyte development related gene expression and parthenogenetic embryo developmental ability are obviously improved.

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 relates to novel pyridine derivatives of formula (I) as A2B adenosine receptor antagonists and ligands of MT3 melatonin receptor, to processes for their preparation, to pharmaceutical compositions comprising said compounds and to the use of said for manufacturing a medicament for the treatment of pathological conditions or diseases that can improve by antagonizing the adenosine A2B receptor and by inhibition of MT3 melatonin receptor, such as respiratory disease, metabolic disorders, neurological disorders and cancer.

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 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 relates to an N-[2-(7-methoxyl-1-naphthyl) ethyl] acetamide (compound 1) and a preparing method for an intermediate thereof. The compound 1-agomelatine is another drug of vital importance for curing mental diseases, and is the first melatonin receptor stimulant and a 5-hydroxytryptamine2C (S-HTx) receptor antagonist. Animal experiments and clinical research show that the drug has the effects of anti-depression, anti-anxiety, sleep rhythm adjustment and internal clock adjustment, has few untoward effects, brings no influence on sexual function, and adopts the following structure (refer to the specification).

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 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 field of molecular biology and discloses an active pharmaceutical ingredient screening method based on a melatonin receptor 2 molecular probe. The active pharmaceutical ingredient screening method includes constructing the melatonin receptor 2 molecular probe and establishing an Flp-In T-Rex HEK293 cell line for induced expression of a G-protein-coupled receptor molecular probe. The melatonin receptor 2 molecular probe is established by a fluorescence resonance energy transfer method, and is high in sensitivity, low in noise, high in throughput, capable of screening not only receptor agonist but also antagonist / inverse agonist and immune to interference of downstream signals. The reasonably designed molecular probe can screen traditional Chinese medicine mixtures and screen lead compounds specific in molecular action target at the receptor level in a one-step manner.

The invention discloses a method for synthesizing intermediates and an improved method for synthesizing melatonin receptor antagonist. The problems that in the prior art, synthesis raw materials for synthesizing target compounds cis-1 can not be bought easily and are high in cost are solved. The method includes the steps that 2-naphthol, lewis acid and benzene serve as reaction raw materials and are stirred till a reaction is completed, and the intermediates shown in the formula (I) (please see the specification for the formula (I)) are obtained after the reaction liquid is extracted, dried and separated. The target compounds cis-1 (please see the specification for the chemical general formula of the cis-1) are obtained through the intermediates shown in the formula (I). The method and the improved method have the advantages that the raw materials can be more easily obtained, the price is lower, operation is easier and more convenient, and the yield of the target product is higher.

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: