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46 results about "5-HT3 receptor" patented technology
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The 5-HT₃ receptor belongs to the Cys-loop superfamily of ligand-gated ion channels (LGICs) and therefore differs structurally and functionally from all other 5-HT receptors (5-hydroxytryptamine, or serotonin) receptors which are G protein-coupled receptors. This ion channel is cation-selective and mediates neuronal depolarization and excitation within the central and peripheral nervous systems.
Organic compounds
ActiveUS9745300B2Strong therapeutic activitySide effect can be reduced and minimizedOrganic active ingredientsIsotope introduction to heterocyclic compoundsDisease5-HT3 receptor
The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and / or pathways involving dopamine D1 / D2 receptor signaling systems, and / or the treatment of residual symptoms.
Owner:INTRA CELLULAR THERAPIES INC
Organic compounds
ActiveUS20170183350A1To promote metabolismImproves in vitro hepatic microsome stabilityOrganic active ingredientsNervous disorderDisease5-HT3 receptor
The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and / or pathways involving dopamine D1 / D2 receptor signaling systems, and / or the treatment of residual symptoms.
Owner:INTRA CELLULAR THERAPIES INC
Methods and Compositions for Treating or Preventing Narcotic Withdrawal Symptoms
ActiveUS20100144754A1Reduces physical dependenceAlleviate withdrawal symptomsBiocideNervous disorderDrug withdrawal symptomsPhysical dependence
This invention provides methods and pharmaceutical compositions for preventing or treating physical dependence and / or withdrawal associated with narcotic use, in particular by modulating a 5-HT3 receptor. Using a computational genetic approach in mice, a gene conserved between mice and humans was identified as candidate as a modulator of physical dependence to morphine. Administration of compounds that modulate 5-HT3 receptors was found to control withdrawal from morphine in mice and humans.
Owner:THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIV
Methods of treating gastro-esophogeal reflux disease using (-) norcisapride in combination with proton pump inhibitors or H2 receptor antagonists
InactiveUS6548518B2Prevent and alleviate symptomReducing and avoiding adverse effectBiocideDigestive systemNorcisapride5-HT3 receptor
Owner:SEPACOR INC
5-HT3 receptor antagonists and methods of use
The subject invention provides useful and novel 5-HT3 antagonists. The subject invention also provides methods for synthesizing the compounds of invention. The invention also provides methods for the treatment of irritable bowel syndrome and other such conditions.
Owner:ARYX THERAPEUTICS
Method and compositions using (+) norcisapride in combination with proton pump inhibitors or H2 receptor antagonist
InactiveUS6353005B1Prevent and alleviate symptomReducing and avoiding adverse effectBiocidePeptide/protein ingredientsNorcisapride5-HT3 receptor
The invention relates to methods and compositions for the prevention, treatment, or management of gastrointestinal disorders or symptoms thereof, employing two or more agents or compounds to provide a triple site action on 5-HT3 receptors, 5-HT4 receptors, and at least one of H2 receptors and proton pumps.
Owner:SEPACOR INC
Serotonin 5-Ht3 Receptor Agonist
InactiveUS20070265277A1Reduce disadvantagesHigh binding affinityOrganic active ingredientsOrganic chemistrySerotoninHydrogen atom
A serotonin 5-HT3 receptor agonist containing a compound represented by the general formula (1) [R1, R3 and R5 represent hydrogen atom, a lower alkyl group, a lower alkenyl group, a halogen atom, hydroxyl group, amino group, a lower alkoxy group, carboxyl group, carbamoyl group, or nitro group, R2 and R4 represent a halogen atom, hydroxyl group, or amino group, R6 represents hydrogen atom, a lower alkyl group, or a lower alkenyl group, R7 represents hydrogen atom, a lower alkyl group, a lower alkenyl group, or an aralkyl group, and m and n are integers of 1 to 3] or a physiologically acceptable salt thereof as an active ingredient and having both a serotonin 5-HT3 receptor antagonistic action and a serotonin 5-HT3 receptor activating action.
Owner:RES FOUND ITSUU LAB
5-ht3 receptor modulators, methods of making, and use thereof
Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
Owner:ALBANY MOLECULAR RESEARCH INC
Effect of morinda officinalis extract on improving or treating sexual disorder, and application thereof
InactiveCN102198184AAluminium/calcium/magnesium active ingredientsSexual disorder5-HT1 receptorPituitary gland
The invention relates to the effect of a morinda officinalis extract on improving or treating sexual disorder, and an application thereof. The substance for treating or improving the sexual disorder has an effect on integrally regulating the hypothalamus, the pituitary gland, the sex gland and the adrenocortical function to improve or treat the sexual disorder, and simultaneously has selective specificity on different 5-HT receptors, i.e., the substance can selectively excite the 5-HT1 receptor, but has no excitation on the 5-HT2 receptor and the 5-HT3 receptor. The morinda officinalis extract can be used as a medicament and / or food for treating or assisting to improve the sexual disorder.
Owner:CHENGDU YIPING MEDICAL SCI & TECH
Preparation of condensed ring indole compounds
ActiveCN101302216AHigh purityHigh industrial application valueOrganic chemistryChloride salt5-HT3 receptor
The invention discloses a method for preparing fused ring indole type compounds as shown in formula I. The method is characterized in that: in a solvent, a fused ring indole carboxylic acid type compound as shown in formula II reacts with chloride salt which is 1-10 times the molar quantity of the compound at the temperature between 80 and 150 DEG C; (as shown in a figure) wherein R1 is H, F, Cl, Br, I, methyl or ethyl. The method can prepare the key intermediate fused ring indole type compounds of high-purity medicine (5-HT3 receptor). The method is simple in process, convenient to operate and easy to apply to large-scale industrial production, thereby having high industrial application value.
Owner:CHINA GATEWAY PHARMA DEV CO LTD
Phenyl piperazine compounds, pharmaceutical composition including the same and use thereof
The present invention relates to novel piperazine derivatives or pharmaceutically acceptable salts thereof, a process for preparing the same, and in particular, a high binding for Serotonin 1A(5-hydroxytryptamine; 5-HT1A) receptor, a pharmaceutical composition for treatment and / or prevention of depression and anxiety including an effective amount of the piperazine compound, and a method of treating depression, anxiety and other conditions related to 5-HT1A receptor in a mammal.
Owner:BIOPHARM
Serotonin 5-HT3 Receptor Antagonists for Use in the Treatment of Lesional Vestibular Disorders
ActiveUS20120064094A1Suitable restorative effectReduces functional alterationAntibacterial agentsBiocideSerotoninVestibular disorders
Owner:INST NAT DE LA SANTE & DE LA RECHERCHE MEDICALE (INSERM)
Transgenic mammal having 5-HT3 transgene overexpression in the CMS
InactiveUS6252131B1Decrease in ethanol consumptionHigh expressionSugar derivativesTissue cultureAlcoholMammal
The invention relates to transgenic mammals characterized by 5-HT3 receptor over-expression in the central nervous system (CNS) . The mammals have particular utility as models for studying the role of 5-HT3 receptors in the CNS, especially for the study of reward pathways for alcohol and other substances of abuse.
Owner:STC UNM +1
Tricyclic compounds, compositions, and methods useful in the treatment or prophylaxis of 5-HT6 receptor-related disorders
The present invention relates to compounds of the formula (I)wherein A, X and R1 to R9 are as described herein; to pharmaceutical compositions comprising the said compounds; to processes for their preparation; and to the use of the compounds as medicaments against 5-HT6 receptor-related disorders.
Owner:PROMIMAGEN LTD
Method of treating post operative nausea and vomiting
Owner:HELSINN HEALTHCARE SA
Fast Acting Orally Disintegrating Film
ActiveUS20170056374A1Act quicklyOrganic active ingredientsDigestive systemOral medication5-HT3 receptor
A fast acting orally disintegrating film (ODF) for treatment of various medical conditions including emesis that has a simple formulation, easy to manufacture and has similar pharmacokinetic profile to currently commercially available orally administered drug products is provided. The ODF comprises an active pharmaceutical ingredient such as ondansetron or a pharmaceutical acceptable salt thereof in an amount of 2 to 24 mg, at least one hydrophilic film forming polymer in an amount of at least 8% by weight of the film, wherein the at least one hydrophilic film forming polymer is characterized by having a molecular weight of 5000 to 50000 Da, and a water soluble excipient in an amount of 10 to 30% by weight of the film. The present invention also provides a method for preparing the ODF that remains stable over a period of time under a normal pharmacologically storage condition and a method for treating or preventing various medical conditions such as nausea or vomiting or a treatment method mediated through antagonizing action of 5HT at 5-HT3 receptor by administering the ODF to a patient in need thereof.
Owner:TAHO PHARMA
Methods and compositions for treating or preventing narcotic withdrawal symptoms
Owner:THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIV
Methods of treating lesional vestibular disorders by administering serotonin 5-HT3 receptor antagonists
ActiveUS8580730B2Suitable restorative effectReduces functional alterationAntibacterial agentsBiocideSerotoninDisease
Owner:INST NAT DE LA SANTE & DE LA RECHERCHE MEDICALE (INSERM)
Pharmaceutical uses of indole piperazine derivatives
The invention belongs to the field of pharmacy, relates to medicinal use of an indole piperazine derivative, and in particular relates to appetency of the indole piperazine derivative to dopamine D3 receptor and 5-HT1A and 5-HT2A receptors, function characteristics and use in preparation of medicines for nervous system disease; adrenergic beta-2 receptor crystal structure is used as a template for the construction of a dopamine 5-HT1A receptor model; by accuracy verification on the receptor model and molecular dynamics simulation, a flexible receptor conformation can be obtained; active sites of the flexible receptor conformation can be detected; detection results are superimposed and a dynamic receptor effective-mass model is constructed; an existing compound database is screened and the activity is tested; and results show that the screened compound FDFWHF003 and its derivatives have good activity to the dopamine receptor and 5-HT receptors, can be used for preparation of anti-schizophrenia medicines, and especially is suitable for the preparation of medicines for treating schizophrenia caused by dopamine system and 5-HT system functional disorders.
Owner:FUDAN UNIV
Tricyclic quinoline and quinoxaline derivatives
The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.
Owner:ABBVIE INC +1
Medicinal use of indole piperazine derivative
InactiveCN103977004AHave dopamine receptorsCtiveOrganic active ingredientsNervous disorder5-HT3 receptor5-HT4 receptor
The invention belongs to the field of pharmacy, relates to medicinal use of an indole piperazine derivative, and in particular relates to appetency of the indole piperazine derivative to dopamine D3 receptor and 5-HT1A and 5-HT2A receptors, function characteristics and use in preparation of medicines for nervous system disease; adrenergic beta-2 receptor crystal structure is used as a template for the construction of a dopamine 5-HT1A receptor model; by accuracy verification on the receptor model and molecular dynamics simulation, a flexible receptor conformation can be obtained; active sites of the flexible receptor conformation can be detected; detection results are superimposed and a dynamic receptor effective-mass model is constructed; an existing compound database is screened and the activity is tested; and results show that the screened compound FDFWHF003 and its derivatives have good activity to the dopamine receptor and 5-HT receptors, can be used for preparation of anti-schizophrenia medicines, and especially is suitable for the preparation of medicines for treating schizophrenia caused by dopamine system and 5-HT system functional disorders.
Owner:FUDAN UNIV
Compositions and methods related to serotonin 5-HT1A receptors
Contemplated substituted arylpiperazinyl compounds, and most preferably 18F-Mefway, exhibit desirable in vitro and in vivo binding characteristics to the 5-HT1A receptor. Among other advantageous parameters, contemplated compounds retain high binding affinity, display optimal lipophilicity, and are radiolabeled efficiently with 18F-fluorine in a single step. Still further, contemplated compounds exhibit high target to non-target ratios in receptor-rich regions both in vitro and in vivo, and selected compounds can be effectively and sensitively displaced by serotonin, thus providing a quantitative tool for measuring 5-HT1A receptors and serotonin concentration changes in the living brain.
Owner:RGT UNIV OF CALIFORNIA
5-ht3 receptor modulators, methods of making, and use thereof
ActiveUS20120219641A1High affinityInhibit serotonin-induced bradycardiaBiocideNervous disorderDisease5-HT3 receptor
Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
Owner:ALBANY MOLECULAR RESEARCH INC
5-ht2b receptor antagonists
The present invention relates to novel fluorinated piperidine derivatives having antagonistic activity at the 5-HT2B receptor, pharmaceutical compositions comprising these compounds and their use as a medicine.
Owner:JANSSEN PHARMA NV
Acylguanidine derivative or salt thereof
InactiveUS8076348B2High antagonistic activityExcellent IBS treating effect and migraine preventing effectBiocideNervous disorderDisease5-HT4 receptor
Owner:ASTELLAS PHARMA INC
Tricyclic quinoline and quinoxaline derivatives
The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.
Owner:ABBVIE DEUTSHLAND GMBH & CO KG
5-HT3 receptor modulators, methods of making, and use thereof
ActiveUS8124600B2High affinityInhibit serotonin-induced bradycardiaBiocideNervous disorderDisease5-HT3 receptor
Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
Owner:ALBANY MOLECULAR RESEARCH INC
5ht3 receptors of nematodes, polynucleotide molecules encoding same, and antagonists thereof
Invertebrate 5-HT3 receptors, especially from the nematode Ceanorhabditis elegans, and polynucleotide molecules encoding same are disclosed. The receptors and polynucleotide molecules may be used in assays to identify and / or assess candidate compounds for use as nematicidal, insecticidal and / or other pesticidal use.
Owner:COMMONWEALTH SCI & IND RES ORG
5-ht3 receptor modulators, methods of making, and use thereof
Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
Owner:ALBANY MOLECULAR RESEARCH INC
5-Ht3 Receptor Antagonists
The present invention provides 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
Owner:TAKEDA PHARMA CO LTD
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