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71 results about "Amine receptor" patented technology
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Biogenic amine receptor are a variety of neurotransmitter receptors that are sensitive to biogenic amine neurotransmitters. They mostly belong to the G protein-coupled receptor (GPCR) family of transmembrane receptors, specifically within GPCR "Family A" (Rhodopsin-like receptors). A notable exception is the serotonin 5-HT 3 receptor, which is a ligand-gated ion channel.
Spiroazacyclic compounds as monoamine receptor modulators
The present invention relates to spiroazacyclic compounds as monoamine receptor modulators; compositions comprising the same; methods of inhibiting an activity of a monoamine receptor with said compounds; methods of treating a disease condition associated with a monoamine receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.
Owner:ACADIA PHARMA INC
Spiroazacyclic compounds as monoamine receptor modulators
Owner:ACADIA PHARMA 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
Compositions and methods for treating colic
InactiveUS20040185032A1BiocideBacteria material medical ingredientsHistamine H1 Receptor AntagonistsGastrointestinal disorder
Compositions and methods for providing relief from pain and / or discomfort associated with gastrointestinal disorders, including, for example, bloating, crying, gas, cramping, regurgitation, diarrhea and gastrointestinal pain, associated with colic comprising, at least one antiflatulent, at least one histamine H1-receptor antagonist, and optionally, one or more prebiotic and / or one or more probiotic.
Owner:LIFESCAPE BIOSCIENCE INC
Organic compounds
ActiveUS10077267B2Similar biological activityTo promote metabolismOrganic active ingredientsIsotope introduction to heterocyclic compoundsDisease5-HT4 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
Ligands for monoamine receptors and transporters, and methods of use thereof
One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
Owner:SEPACOR INC
Composition comprising cocoa
InactiveUS20040005347A1Improve obesityReducing appetite and carbohydrate cravingBiocideOrganic active ingredientsDecreased LibidoAmine receptor
The invention pertains to a composition and a method for the treatment of mood disorders, in particular of treating, preventing or alleviate depression, mood disorders or insufficient mood, obesity, overweight, premenstrual syndrome, craving, carbohydrate craving, chocolate craving, menopausal complaints, erectile dysfunction and / or reduced libido. The composition contains cocoa or one or more of its pharmacologically active components, and a dopamine D2 receptor agonist.
Owner:NV NUTRICIA
Nanoparticulate ebastine formulations
The invention is directed to compositions comprising at least one nanoparticulate H1-histamine receptor antagonist, such as ebastine or a salt or derivative thereof, having improved dissolution rate providing a faster onset of drug availability. The nanoparticulate H1-histamine receptor antagonist particles, such as ebastine, have an effective average particle size of less than about 2000 nm and are useful in the treatment of seasonal and perennial allergic rhinitis and related diseases.
Owner:ELAN PHRMA INT LTD
Dopamine D3 acceptor portion agonist and its application
InactiveCN1948298AReduce the number of jumpsReduce weight lossOrganic active ingredientsNervous disorderChemical structureNervous system
The present invention relates to a dopamine D3 receptor portion excitant or its pharmaceutically acceptable salt and its application for curing diseases of central nervous system. Said invention also provides its chemical structure general formula, and provides detailed description.
Owner:SOUTHEAST UNIV
Application and preparation method of berberine compound
ActiveCN103816152ALong-acting analgesic effectEasy to synthesizeOrganic active ingredientsNervous disorderPharmacologic effectsD2 dopamine receptors
The invention provides application of a compound with the structure as shown in the formula (I) in the specification, or a medical salt, a hydrate or a solvate, of the compound, in preparation of a medicine for treating nervous system diseases relevant to the dopamine receptor, and a preparation method of the compound with the structure as shown in the formula (I) in the specification or the medical salt, the hydrate or the solvate, of the compound. The compound has multiple pharmacologic functions such as mu-opioid receptor excitation and dopamine D2 receptor blocking, and has good physicochemical properties and oral bioavailability, and integral animal experiment shows that the compound has remarkable and long-lasting analgesia and calm activity and can be applied to treatment on pain and other mental diseases.
Owner:DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI +1
Use of glutamate antagonists for the treatment of cancer
InactiveUS20050054650A1Remarkable effectImprove tumor killing abilityBiocideAnimal repellantsGlycineDepressant
Owner:IKONOMIDOU HRISSANTHI
Organic compounds
ActiveUS10688097B2Inhibit the serotonin re-uptake transporterModulate dopaminergic protein phosphorylationOrganic active ingredientsNervous disorderDiseaseSerotonin transporter
Owner:INTRA CELLULAR THERAPIES INC
Compounds as neuronal histamine receptor-3 antagonists and uses thereof
Owner:XWPHARMA LTD
Dopamine d3 receptor antagonists having a bicyclo moiety
ActiveUS20180222918A1Organic active ingredientsNervous disorderAmine receptorDopamine receptor antagonist
Owner:INDIVIOR UK
Use of clove oil, eugenol and derivatives thereof in the preparation of medicines for histamine H3 receptor antagonists or inverse agonists
InactiveCN102258577AClear efficacyQuality is easy to controlNervous disorderEther/acetal active ingredientsEugenolEfficacy
The present invention provides the application of clove oil, eugenol and derivatives thereof in the preparation of antagonists or inverse agonists of histamine H3 receptors, and also provides a method of using clove oil, eugenol or eugenol derivatives as The main active ingredient, together with other active ingredients, forms a new H3 receptor antagonist or inverse agonist drug, which can be used to prevent and treat senile dementia and depression. The H3 receptor antagonist or inverse agonist medicine provided by the invention has clear efficacy, controllable quality and safety, and provides a new choice for clinical practice.
Owner:CHENGDU MEDICAL COLLEGE
Pyrrolidine compounds, salts thereof, applications of compounds or salts thereof in nuclear magnetic probes and medicines, reagent, and medicine
The invention provides pyrrolidine compounds, salts thereof, applications of the compounds or the salts thereof in nuclear magnetic probes and medicines, a reagent, and a medicine. The benzamide methylpyrrolidine compounds have a chemical structure represented by general formula (I); and in the formula (I), R<1> is selected from a methyl group, an ethyl group, a methoxy group, an ethoxy group and halogen, R<2> is selected from a methyl group, an ethyl group, a methoxy group, an ethoxy group and halogen, R<3> is selected from C1-5 alkyl groups and H, X<1> is selected from C1-10 alkylene groups or is deleted, X<2> is selected from -(CH2CH2O)n- (n is 1-5) or is deleted, X<3> is selected from C1-5 alkyl groups, X<4> is selected from oxygen, sulfur and a methylene group, and Ln is selected from Gd and Eu. The compounds have a gadolinium and europium chelating structure formed by combining with a dopamine D2 receptor and depending on intramolecular chelating groups, and specifically enhance the contrast of dopamine D2 receptor expression tissues on images in magnetic resonance imaging.
Owner:BEIJING NEUROSURGICAL INST
N-linked quinolineamide m1 receptor positive allosteric modulators
The present invention is directed to N-linked quinoline amide compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
Owner:MERCK SHARP & DOHME LLC
Ligands for monoamine receptors and transporters, and methods of use thereof
One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
Owner:SEPACOR INC
Dopamine d2 receptor ligands
ActiveUS20180155283A1More selectivityMore functionalityNervous disorderReceptors for neuromediatorsDopamine receptor D1Functional selectivity
The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopammode inergic activity. The present invention relates to novel compounds that modulate dopamine D2 receptors. In particular, compounds of the present invention show functional selectivity at the dopamine D2 receptors and exhibit selectivity downstream of the D2 receptors, on the 0-arrestin pathway and / or on the cAMP pathway.
Owner:THE BROAD INST INC +1
Solid preparation of cariprazine for oral administration
The invention relates oral phamiaceuticai compositions for the modified release delivery of cariprazine (trans-N-{4-[2-[4-(2,3-dichlorophenyl)-piperazin-l-yl]-ethyl]-cyclohexyl}-N',N'- dimethylurea) or pharmaceutically acceptable salts thereof for less than daily dosing. The invention also relates to the use of said compositions in the treatment and / or prevention of pathological conditions which require the modulation of dopamine receptors. The invention also relates to the process for the preparation of said modified release pharmaceutical compositions.
Owner:RICHTER GEDEON NYRT
Domperidone orally disintegrating tablets as well as preparation method and quality control method thereof
InactiveCN101406462AOrganic active ingredientsDigestive systemSide effectOrally disintegrating tablet
The invention discloses a domperidone oral disintegrating tablet, and a method for preparing the same and a method for quality control. The domperidone oral disintegrating tablet is prepared from domperidone and auxiliary materials, and the quality thereof is controllable and stable. The domperidone oral disintegrating tablet is a peripheral dopamine receptor agonist which is safe and effective. Compared with the prior art, the domperidone oral disintegrating tablet has the advantages of rapid disintegration, convenient taking, no vomiting, rapid effect, and low side effect.
Owner:SHAANXI BUCHANG PHARMA
Ophthalmic compositions and methods of use
InactiveUS20190008920A1Significant comprehensive benefitsExtended releaseOrganic active ingredientsSenses disorderAntigenBeta blocker
The present invention relates to an ophthalmic composition comprising at least two active pharmaceutical ingredients. In particular, the active pharmaceutical ingredients are selected from the group consisting of: an alpha 2 adrenergic receptor agonist; a beta-adrenergic receptor agonist; an immunosuppressant; a lymphocyte associated antigen antagonist; an anti-inflammatory; a beta-blocker; a prostaglandin analog; a histamine receptor antagonist; a carbonic anhydrase inhibitor; and an antibiotic. In some embodiments, the composition of the invention is a nanoemulsion formulation. In one particular embodiment, the first active pharmaceutical ingredient is an alpha 2 adrenergic receptor agonist. The present invention also provides a method for treating various clinical conditions associated with an eye disorder or eye disease using the composition of the invention.
Owner:OCUGEN INC
Novel diazabicyclic biaryl derivatives
This invention relates to novel diazabicyclic biaryl derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
Owner:NEUROSEARCH AS
Novel dopamine d3 receptor ligands and preparation and medical uses of the same
The present invention relates to a novel piperazine derivative represented by Formula I having an activity for regulating dopamine D3 receptor, stereoisomers thereof, pharmaceutically acceptable salts or solvates, and a pharmaceutical composition comprising the compound, a process for preparing the same, and use thereof in the prevention or treatment of a disease associated with central nervous system dysfunction, such as Parkinson's disease, schizophrenia, drug addiction and relapse, as well as kidney protection and immunoregulation, or as a tool for researching D3R function or diseases associated with D3R dysfunction.
Owner:INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
Solid preparation of cariprazine for oral administration
InactiveUS20200222391A1Improved profileOrganic active ingredientsNervous disorderCariprazineOral medication
The invention relates oral pharmaceutical compositions for the modified release delivery of cariprazine (trans-N-{4[2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl]-cyclohexyl}-N′,N′-dimethylurea) or pharmaceutically acceptable salts thereof for less than daily dosing. The invention also relates to the use of said compositions in the treatment and / or prevention of pathological conditions which require the modulation of dopamine receptors. The invention also relates to the process for the preparation of said modified release pharmaceutical compositions.
Owner:RICHTER GEDEON NYRT
Chromeno[4,3,2-de]isoquinolines as potent dopamine receptor ligands
Novel dopamine receptor ligands of the formula: pharmaceutical formulations of such compounds, and a method using such compounds for treating a patient suffering from dopamine-related dysfunction of the central or peripheral nervous system, are described. The compounds are expected to be useful in treating Parkinson's disease, improving cognition, improving memory, improving the negative symptoms of schizophrenia, improving attention-deficit hyperactivity disorder and related developmental disorders, treating substance abuse disorders, and in treating various peripheral conditions where changes in dopamine receptor occupation affects physiological function, including organ perfusion, cardiovascular function, and selected endocrine and immune system functions.
![Chromeno[4,3,2-de]isoquinolines as potent dopamine receptor ligands](https://images-eureka.patsnap.com/patent_img/14d38f0e-66fa-4e44-98f2-5f030de30476/US06916832-20050712-D00000.png "Chromeno[4,3,2-de]isoquinolines as potent dopamine receptor ligands")
![Chromeno[4,3,2-de]isoquinolines as potent dopamine receptor ligands](https://images-eureka.patsnap.com/patent_img/14d38f0e-66fa-4e44-98f2-5f030de30476/US06916832-20050712-D00001.png "Chromeno[4,3,2-de]isoquinolines as potent dopamine receptor ligands")
![Chromeno[4,3,2-de]isoquinolines as potent dopamine receptor ligands](https://images-eureka.patsnap.com/patent_img/14d38f0e-66fa-4e44-98f2-5f030de30476/US06916832-20050712-D00002.png "Chromeno[4,3,2-de]isoquinolines as potent dopamine receptor ligands")
Owner:THE UNIV OF NORTH CAROLINA AT CHAPEL HILL +1
Pharmaceutical composition for treating posttraumatic stress disorder
ActiveUS20180064707A1Inhibit expressionRelieve symptomsCompounds screening/testingOrganic active ingredientsDiseaseScreening method
Provided are a posttraumatic stress disorder (PTSD) animal model in which dopamine receptor subtype 4 (D4R) is damaged or deficient, a method for preparing the same, a method for screening a drug for treating PTSD using the same, and a pharmaceutical composition for treating PTSD comprising a drug detected by the screening method. As it is identified that a specific type of dopamine receptor is associated with a mechanism for fear memory expression induced by long-term depression (LTD), the understanding of pathogenesis of PTSD may be heightened, the animal model exhibiting similar clinical conditions of PTSD and the method for preparing the same may be applied in analyses for stability and effectiveness of a therapeutic agent for PTSD and screening of a therapeutic drug. Further, an agonist of D4R contained in the composition has been approved by the US FDA and clinically used for psychiatric diseases such as schizophrenia, and thus may be immediately used for clinical applications for PTSD symptoms.
Owner:POSTECH ACAD IND FOUND
Application of dopamine receptor 1 antagonist in preparing drugs for treatment of ketamine-induced schizoid symptoms in mice
InactiveCN110833621ANervous disorderHeterocyclic compound active ingredientsPharmaceutical drugAmine receptor
The invention belongs to the technical field of biomedicine and particularly relates to a novel pharmaceutical use of a dopamine receptor 1 antagonist, and to a novel use of the dopamine receptor 1 antagonist in preparing drugs for the treatment of ketamine-induced schizoid symptoms in mice. The dopamine receptor 1 antagonist is selected from SCH23390 having a molecular formula of C17H18ClNO.HCl,and is one or only one effective ingredient to the drugs. A drug for the treatment of ketamine-induced schizoid symptoms in mice comprises the dopamine receptor 1 antagonist having the effective amount (5 mg / kg). The dopamine receptor 1 antagonist is used as one means to treat ketamine-induced schizoid behaviors of mice, and scientific basis is provided for the research and development of a methodto effectively relieve schizoid symptoms in mice.
Owner:中国医科大学
Compositions and methods for modulating d1-d2 dopamine receptor interaction and function
InactiveUS20120134991A1Organic active ingredientsNervous disorderAmine receptorDopamine Receptor Interactions
The present invention provides for prevention and / or treatment of neurological or neuropsychiatric disorders involving abnormal D1-D2 dopamine receptor coupling and / or activation. Methods and agents are provided for modulating dopamine receptor function arising from D1-D2 coupling and / or activation. Agents of the present invention include fragments of D2 receptor or D1 receptor that can disrupt D1-D2 coupling.
Owner:CENT FOR ADDICTION & MENTAL HEALTH
Antiflatulents in combination with histamine H1-receptor antagonists for treating gastrointestinal disorders
InactiveCN1761460ABacteria material medical ingredientsDigestive systemDiseaseHistamine H1 Receptor Antagonists
Compositions and methods for providing relief from pain and / or discomfort associated with gastrointestinal disorders, including, for example, bloating, crying, gas, cramping, regurgitation, diarrhea and gastrointestinal pain, associated with colic comprising, at least one antiflatulent, at least one histamine H1-receptor antagonist, and optionally,one or more prebiotic and / or one or more probiotic.
Owner:LIFESCAPE BIOSCIENCE INC
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