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37 results about "5-HT2C receptor" patented technology
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The 5-HT2C receptor is a subtype of 5-HT receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). It is a G protein-coupled receptor (GPCR) that is coupled to Gq/G₁₁ and mediates excitatory neurotransmission. HTR2C denotes the human gene encoding for the receptor, that in humans is located at the X chromosome. As males have one copy of the gene and in females one of the two copies of the gene is repressed, polymorphisms at this receptor can affect the two sexes to differing extent.
Methods for treating idiopathic hyperhidrosis and associated conditions
InactiveUS20040192754A1Reduced activityAlleviate and treat symptomBiocideAnimal repellantsAllosteric modulatorMianserin Hydrochloride
The subject invention provides methods for treating symptoms and / or conditions associated with idiopathic hyperhidrosis by using compounds that decrease the activity of serotonin 5-HT2C receptors. Compounds that can ameliorate symptoms of idiopathic hyperhidrosis and associated conditions include 5-HT2C receptor antagonists (i.e., ketanserin, ritanserin, mianserin, mesulergine, cyproheptadine, fluoxetine, mirtazapine, olanzapine, and ziprasidone) as well as 5-HT2C receptor modulators (i.e., inverse agonists, partial agonists, and allosteric modulators).
Owner:SHAPIRA NATHAN ANDREW +2
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
Organic compounds
ActiveUS20190231780A1Avoid side effectsInhibit the serotonin re-uptake transporterOrganic active ingredientsNervous disorderDisease5-HT4 receptor
The invention relates to particular substituted deuterated 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
Amide derivative or salt thereof
InactiveUS20090062363A1High antagonistic activitySuperior IBS-treating effectBiocideOrganic chemistryDisease5-HT6 receptor
[Problem] To provide a compound which can be used for the prevention and / or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).[Means for Resolution] It was found that an amide derivative characterized by the possession of a nitrogen-containing bicyclic hetero ring (e.g., an indole or the like), or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and / or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).
Owner:ASTELLAS PHARMA INC
Tricyclic heterocyclic compound and use thereof
The present invention provides a tricyclic heterocyclic compound having a serotonin 5-HT2C receptor activation action and the like.A 5-HT2C receptor activator containing a compound represented by the formula (I):wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.
Owner:TAKEDA PHARMACEUTICALS CO LTD
Organic compounds
ActiveUS20170037048A1Avoid side effectsStrong therapeutic activityOrganic 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
Organic compounds
ActiveUS10245260B2Convenient treatmentCompliance difficultNervous disorderOrganic chemistryDisease5-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 the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and / or the μ-opioid receptor.
Owner:INTRA CELLULAR THERAPIES INC
5ht2c Receptor antagonists in the treatment of schizophrenia
The present invention relates to the use of certain 5-HT2C receptor antagonists in the manufacture of medicaments for the treatment of mental disorders, in particular aspects of schizophrenia, cognitive impairment and suicidality, as well as to methods for determining the suitability of compounds for such a use.
Owner:CURIDIUM
Pyrrole Derivative or Salt Thereof
InactiveUS20090036421A1High antagonistic activityGood effectBiocideOrganic chemistryDisease5-HT6 receptor
[Problem] To provide a compound which may be used for the prevention and / or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).[Means for Resolution] It was found that a pyrrole derivative characterized by the possession of a guanidinocarbonyl group or amido group as a substituent group at the 3-position, or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and / or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).
Owner:ASTELLAS PHARMA INC
Agent for prophylaxis and treatment of pancreatitis
InactiveUS20090075974A1Inhibit bindingHigh binding activityBiocideCompound screeningDrug5-HT2C receptor
Disclosed is a pharmaceutical composition for prophylaxis and treatment of pancreatitis comprising a 5-HT2A receptor antagonist as an effective component, wherein the binding activity (pKi) of the 5-HT2A receptor antagonist to a 5-HT2A receptor is higher at least by 1.0 than the binding activities to a 5-HT2B receptor and a 5-HT2C receptor. Preferably the binding activity (pKi) of the 5-HT2A receptor antagonist to the 5-HT2A receptor is at least 7.0, and more preferably at least 8.0. The present invention also provides a method of identifying a candidate substance for prophylactic and therapeutic agent for pancreatitis, comprising determining whether a test substance has a 5-HT2A receptor antagonistic activity.
Owner:CYTOPATHFINDER INC
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
Pyridooxazepine derivative and use thereof
The present invention provides a compound having a superior serotonin 5-HT2C receptor activating action, which is represented by the formulawherein A is —OR1 or —S(O)pR2, R1 and R2 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), or a heterocyclic group to optionally having substituent(s), and p is 0, 1 or 2, or a salt thereof.
Owner:TAKEDA PHARMA CO LTD
Pyrazole derivatives which modulate human 5-serotonin receptors
Disclosed herein are non-endogenous, constitutively activated forms of the human 5-HT2A and human 5-HT2C receptors and uses of such receptors to screen candidate compounds. Further disclosed herein are candidate compounds identified by the screening method which act at the 5HT2A receptors. Yet further disclosed is a new class of compounds (I) which act at the 5HT2A receptors. This new class encompasses the candidate compounds. In Formula (A) W is F, Cl, Br, I, C1-8 straight chain or branched alkyl, C3-8 cycloalkyl, C4-9 alkylcycloalkyl, or C2-8 alkenyl; X is O or S or NR<2>; Y is NR<3>R<4>, or (CH2)mR<5>, or O(CH2)nR<6>; m is an integer between 0 and 4, inclusive; n is an integer between 0 and 4, inclusive; Z is H, C1-8 straight chain or branched alkyl, C3-8 cycloalkyl, C4-9 alkylcycloalkyl, or C2-8 alkenyl; R<1>, R<2>, R<3> and R<10> are as defined in the application.
Owner:ARENA PHARMA +1
Bicyclic heterocyclic compound and use thereof
The present invention provides a bicyclic heterocyclic compound having a serotonin 5-HT2C receptor activation action and the like.A compound represented by the formula (I):wherein each symbol is as defined in the specification, or a salt thereof.
Owner:TAKEDA PHARMA CO LTD
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
Pyridooxazepine derivative and use thereof
The present invention provides a compound having a superior serotonin 5-HT2C receptor activating action, which is represented by the formulawherein A is —OR1 or —S(O)pR2, R1 and R2 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), or a heterocyclic group to optionally having substituent(s), and p is 0, 1 or 2, or a salt thereof.
Owner:TAKEDA PHARMA CO LTD
Amide derivative or salt thereof
InactiveUS7985764B2High antagonistic activitySuperior IBS-treating effectBiocideOrganic chemistry5-HT6 receptorDisease
It was found that a compound according to the following formula:or a pharmaceutically acceptable salt thereof, has a strong antagonism for both the 5-HT2B and 5-HT7 receptors. In addition, the compound shows good pharmacological action as compared to antagonists selective for only one of these receptors. Based on the above, the compound of the present invention is useful for the prevention and / or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).
Owner:ASTELLAS PHARMA 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
Application of radix bupleuri total saponin and monomer saponin thereof in pharmacy
InactiveCN105055471AAppetite suppressantInhibitionOrganic active ingredientsMetabolism disorderWeight gaining5-HT2C receptor
The invention provides an application of radix bupleuri total saponin and monomer saponin thereof in preparation of medicines for preventing and treating obesity, and a pharmaceutical composition taking the radix bupleuri total saponin and the monomer saponin as active components. A pharmacological experiment proves that the radix bupleuri total saponin and a monomer compound thereof have obvious agonist activity on a 5-HT2C receptor, has obvious effects of inhibiting appetite and inhibiting weight gain on SD rats in an animal experiment, and can be applied to prevention and treatment of obesity.
Owner:KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
Preventives/remedies for stress urinary incontinence and method of screening the same
InactiveUS8685924B2Efficient screeningEnabled measurementBiocideNervous disorderSerotoninAndrogen binding
Owner:TAKEDA PHARMA CO LTD
Tricyclic chinoline and quinoxaline derivatives
The invention relates to application of tricyclic chinoline and quinoxaline derivatives as well as a pharmaceutical composition containing the tricyclic chinoline and quinoxaline derivatives as a modifier, in particular agonists or partial agonists of a 5-HT2C receptor, application of the tricyclic chinoline and quinoxaline derivatives to preparing drugs for preventing or treating regulation response conditions and diseases of the 5-HT2c receptor, a method used for preventing or treating the regulation response conditions and diseases of the 5-HT2c receptor, and a method for preparing the compounds and the composition.
Owner:ABBVIE DEUTSHLAND GMBH & CO KG
Agent for preventing and treating pancreatitis
A pharmaceutical composition for preventing and treating pancreatitis comprising as an active ingredient, a 5-HT2A receptor antagonist, characterized in that the binding activity (pKi) of the 5-HT2A receptor antagonist to 5-HT2A receptor is higher by a value of not less than 1.0 than the binding activity to 5-HT2B and 5-HT2C receptors is disclosed. The binding activity (pKi) of the 5-HT2A receptor antagonist to 5-HT2A receptor is preferably 7.0 or higher and more preferably 8.0 or higher. The invention also provides a method of identifying a candidate substance of the agent for preventing / treating pancreatitis comprising measuring whether or not a test substance has a 5-HT2A receptor antagonism.
Owner:CYTOPATHFINDER INC
Pyrrole derivative or salt thereof
InactiveUS8222274B2High antagonistic activityGood effectBiocideOrganic chemistryDisease5-HT6 receptor
[Problem] To provide a compound which may be used for the prevention and / or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).[Means for Resolution] It was found that a pyrrole derivative characterized by the possession of a guanidinocarbonyl group or amido group as a substituent group at the 3-position, or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and / or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).
Owner:ASTELLAS PHARMA INC
Benzazepine compound
[Problem] Provided is a compound which is useful as an agent for treating or preventing 5-HT 2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like. [Means for Solution] The present inventors have investigated compounds having a 5-HT 2C receptor agonist activity, which is promising as an active ingredient of a pharmaceutical composition for treating or preventing incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like, and have found that the benzazepine compounds of the present invention have an excellent 5-HT 2C receptor agonist activity, thereby completing the present invention. That is, the benzazepine compounds of the present invention have a 5-HT 2C receptor agonist activity and can be used as an agent for treating or preventing 5-HT 2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like.
Owner:ASTELLAS PHARMA INC
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