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81 results about "Histamine H3 receptor" patented technology
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Histamine H₃ receptors are expressed in the central nervous system and to a lesser extent the peripheral nervous system, where they act as autoreceptors in presynaptic histaminergic neurons, and also control histamine turnover by feedback inhibition of histamine synthesis and release. The H₃ receptor has also been shown to presynaptically inhibit the release of a number of other neurotransmitters (i.e. it acts as an inhibitory heteroreceptor) including, but probably not limited to dopamine, GABA, acetylcholine, noradrenaline, histamine and serotonin.
Histamine H3 Receptor Agents, Preparation and Therapeutic Uses
The present invention provides a novel compound of Formula (I) or a pharmaceutically acceptable salt thereof, having histamine-113 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another, embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
Owner:FINLEY DON RICHARD +5
Cyclopropyl amines as modulators of the histamine h3 receptor
ActiveUS20070066821A1Improve breathabilityImprove permeabilityOrganic active ingredientsSenses disorderHistamine H3 receptorHistamine h
Owner:JANSSEN PHARMA NV
Diaryl-substituted tetrahydroisoquinolines as histamine H3 receptor and serotonin transporter modulators
Certain diaryl-substituted tetrahydroisoquinoline compounds are histamine H3 receptor and / or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and / or serotonin-mediated diseases.
Owner:JANSSEN PHARMA NV
2-Aminopyrimidine modulators of the histamine H4 receptor
2-Aminopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
Owner:JANSSEN PHARMA NV
Piperazines
The present invention relates, inter alia, to novel piperazines of the following formula:to the use of these compounds in the preparation of pharmaceutical compositions, to pharmaceutical compositions comprising the compounds, and to methods of treatment employing these compounds or compositions. The compounds show a high and selective binding affinity for the histamine H3 receptor, indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases or disorders related to the histamine H3 receptor.
Owner:VTV THERAPEUTICS LLC
Histamine h3 receptor agents, preparation and therapeutic uses
The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases
Owner:ELI LILLY & CO
Substituted imidazoles, their preparation and use
Disclosed is a novel class of substituted imidazole compounds, pharmaceutical compositions containing them and uses of these compounds in the treatment and / or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, these compounds are useful for the treatment and / or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial. These imidazoles compounds have the formula I wherein R1, R2, R3, R4, R5, R6, A, X, Y and Z are as defined in the specification.
Owner:VTV THERAPEUTICS LLC
Pyrazole derivative
InactiveUS20100113776A1Excellent histamine H receptor antagonistic effectNervous disorderOrganic chemistryAttention deficitsCircadian Rhythm Disorders
A novel pyrazole derivative of the following formula having a histamine H3 receptor antagonistic effect:or a pharmaceutically acceptable salt thereof or a pharmaceutical preparation comprising the same as an active ingredient is effective for prevention or treatment of dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases.
Owner:TAISHO PHARMACEUTICAL CO LTD
Diaryl-substituted tetrahydroisoquinolines as histamine h3 receptor and serotonin transporter modulators
Certain diaryl-substituted tetrahydroisoquinoline compounds are histamine H3 receptor and / or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and / or serotonin-mediated diseases.
Owner:JANSSEN PHARMA NV
Novel piperazines
The present invention relates, inter alia, to novel piperazines of the following formula: to the use of these compounds in the preparation of pharmaceutical compositions, to pharmaceutical compositions comprising the compounds, and to methods of treatment employing these compounds or compositions. The compounds show a high and selective binding affinity for the histamine H3 receptor, indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases or disorders related to the histamine H3 receptor.
Owner:VTV THERAPEUTICS LLC
Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines
Novel substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.
![Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines](https://images-eureka.patsnap.com/patent_img/8ba69290-de0a-4589-bc45-6b52af4a1527/US07186721-20070306-C00001.png "Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines")
![Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines](https://images-eureka.patsnap.com/patent_img/8ba69290-de0a-4589-bc45-6b52af4a1527/US07186721-20070306-C00002.png "Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines")
![Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines](https://images-eureka.patsnap.com/patent_img/8ba69290-de0a-4589-bc45-6b52af4a1527/US07186721-20070306-C00003.png "Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines")
Owner:HIGH POINT PHARMA
Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines
Novel substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.
![Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines](https://images-eureka.patsnap.com/patent_img/58fd7dae-39a4-4897-b809-98464c0347f7/US06906060-20050614-C00001.png "Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines")
![Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines](https://images-eureka.patsnap.com/patent_img/58fd7dae-39a4-4897-b809-98464c0347f7/US06906060-20050614-C00002.png "Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines")
![Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines](https://images-eureka.patsnap.com/patent_img/58fd7dae-39a4-4897-b809-98464c0347f7/US06906060-20050614-C00003.png "Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines")
Owner:VTV THERAPEUTICS LLC
Benzofuro- and benzothienopyrimidine modulators of the histamine H4 receptor
Benzofuro- and benzothienopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
Owner:JANSSEN PHARMA NV
Piperidine derivatives as histamine h3 receptor ligands
The invention prepares a compound of following formula and salts, enantiomorphy isomer thereof, wherein Ar<1> and Q is defined as the description, and medicine compound with the said compound. They are effective in treament especially for despondent treamnet.
Owner:ASTRAZENECA AB
2-aminopyrimidine modulators of the histamine H4 receptor
2-Aminopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
Owner:JANSSEN PHARMA NV
Novel Medicaments
Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.
Owner:VTV THERAPEUTICS LLC
Substituted piperazines and diazepanes
A novel class of substituted piperazines and diazepanes, pharmaceutical compositions comprising them and use thereof in the treatment of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.
Owner:HIGH POINT PHARMA
Bicyclic heteroaryl-substituted imidazoles as modulators of the histamine H4 receptor
Bicyclic heteroaryl-substituted imidazole compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
Owner:JANSSEN PHARMA NV
Aminopyrimidine inhibitors of histamine receptors for the treatment of disease
Owner:KALYPSYS INC +1
Histamine H3 receptor antagonists
Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.
Owner:HIGH POINT PHARMA
Diamino-pyridine, pyrimidine, and pyrazine modulators of the histamine H4 receptor
InactiveUS8841287B2Maintain good propertiesLower Level RequirementsBiocideSenses disorderDiseaseHistamine H1 receptor
Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
Owner:JANSSEN PHARMA NV
Novel Aryl- and Heteroarylpiperazines
Novel aryl- and heteroarylpiperazines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.
Owner:HIGH POINT PHARMA
Novel Medicaments
Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.
Owner:VTV THERAPEUTICS LLC
Novel compounds as histamine H3 receptor ligands
ActiveCN103443093AOrganic active ingredientsNervous disorderHistamine H3 receptorMedicinal chemistry
The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to Histamine H3 receptors.
Owner:SUVEN LIFE SCI LTD
Histamine h3 receptor agents, preparation and therapeutic uses
InactiveUS20070208024A1Selective and high affinity bindingHigh affinityBiocideNervous disorderHistamine Receptor AntagonistsTreatment use
The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases
Owner:ELI LILLY & CO
Histamine H3 receptor agents, preparation and therapeutic uses
The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
Owner:ELI LILLY & CO