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137 results about "Receptor subtype" patented technology
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The receptor subtype is also defined by the pharmacological characteristics of the site and is based on the availability of selective agonists and antagonists for the subtypes. For example, beta-adrenoceptors are subdivided into beta-1 adrenoceptors, beta-2 adrenoceptors, and beta-3 adrenoceptors.
Active variants of FGF with improved specificity
InactiveUS7288406B2Enhanced receptor specificityImprove in vivo activitySugar derivativesPeptide/protein ingredientsDiseaseReceptor subtype
The present invention provides active fibroblast growth factor variants demonstrating enhanced receptor subtype specificity. The preferred novel variants retain binding to FGF Receptor Type 3 (FGFR3) triggering intracellular downstream mechanisms leading to activation of a biological response. Methods of utilizing preferred FGF mutants in preparation of medicaments for the treatment of malignancies and skeletal disorders including osteoporosis and enhancing fracture healing and wound healing processes are provided.
Owner:PROCHON BIOTECH
Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
Compound of formula (I) are novel VR1 antagonist that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.
Owner:ABBVIE INC
Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.
Owner:ABBOTT LAB INC
Chromanylurea compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor and uses thereof
Compounds that are antagonists of the VR1 receptor, having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R7, R8, R9, X, Y, Z, L, n, and m, are as defined herein, and are useful in disorders prevented or ameliorated by inhibiting the VR1 receptor.
Owner:ABBVIE INC
5-HT1a receptor subtype agonist
The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT1A receptor subtype, comprising as an active ingredient a carbostyril derivative or a salt thereof represented by the formula (1): wherein the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or a double bond.
Owner:OTSUKA PHARM CO LTD
Remedies for urinary frequency
InactiveUS20060100195A1Suppress pollakiuriaEffective preventionBiocidePeptide/protein ingredientsEccentric hypertrophyUnstable bladder
The present invention relates to an agent for the treatment and / or prevention of pollakiuria comprising a compound having an antagonism to an EP1 receptor which is a prostaglandin E2 receptor subtype. A compound having an antagonism to an EP1 receptor antagonistically acts on an EP1 receptor which is a prostaglandin PGE2 receptor subtype and significantly shows a suppressive activity for urination frequency in models where pollakiuria is induced. Therefore, it is effective for the treatment and / or prevention of pollakiuria (that which is due to nurogenic bladder, nervous bladder, stimulated bladder, unstable bladder, benign prostatic hypertrophy, etc.).
Owner:ONO PHARMA CO LTD
FGF variants and methods for use thereof
ActiveUS7563769B2High activityHigh affinityPeptide/protein ingredientsSkeletal disorderDiseaseReceptor subtype
The present invention provides fibroblast growth factor variants demonstrating enhanced receptor subtype specificity and / or affinity. Preferred embodiments include both variants having enhanced activity that act as improved agonists and variants having reduced activity that act as antagonists. Methods of utilizing preferred FGF variants in preparation of medicaments for the treatment of skeletal disorders including skeletal dysplasia, osteoporosis and enhancing bone fracture healing and cartilage healing processes are provided.
Owner:PROCHON BIOTECH
Benzimidazolidinone derivatives as muscarinic agents
InactiveUS6951849B2Inhibition formationInhibit progressBiocideNervous disorderMuscarinic antagonistReceptor subtype
Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and / or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.
Owner:ACADIA PHARMA INC
Method of identifying properties of substance with respect to human prostaglandin D2 receptors
An object of the present invention is to provide a method of identifying a substance which acts on a newly found second human prostaglandin D2 receptor subtype that differs from the DP receptor, and is useful for treating or preventing various diseases. In order to attain the object, the present invention provides a method of identifying properties of a test substance with respect to a human prostaglandin D receptor, by establishing correlation between the effect of a test substance on human CRTH2 with the effect of the test substance on the human prostaglandin D receptor.
Owner:BML INC
3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors
The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
![3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors](https://images-eureka.patsnap.com/patent_img/8b04a2d6-588d-4ccd-b5d6-e968e664d154/US20110306642A1-20111215-C00001.png "3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors")
![3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors](https://images-eureka.patsnap.com/patent_img/8b04a2d6-588d-4ccd-b5d6-e968e664d154/US20110306642A1-20111215-C00002.png "3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors")
![3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors](https://images-eureka.patsnap.com/patent_img/8b04a2d6-588d-4ccd-b5d6-e968e664d154/US20110306642A1-20111215-C00003.png "3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors")
Owner:ADDEX PHARM SA +1
Benzimidazolidinone derivatives as muscarinic agents
InactiveUS7087593B2Increase acetylcholine signaling and effectHigh selectivityBiocideSenses disorderReceptor subtypeMuscarinic Agents
Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and / or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.
Owner:ACADIA PHARMA INC
Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity, wherein X1, X2, X3, X4, X5, R5, R6, R7, R8a, R8b, R9, Z1, Z2 and L are as defined in the description.
Owner:ABBVIE INC
BENZOIMIDAZOLE, TETRAHYDRO-QUINOXALINE, BENZOTRIAZOLE, DIHYDRO-IMIDAZO[4,5-c] PYRIDINONE AND DIHYDRO-ISOINDOLONE DERIVATIVES
This invention relates to compounds of the formulawherein A, R1 to R3 are as defined in the specification and G is benzoimidazole, quinoxaline, benzotriazole, dihydro-imidazo[4,5-c]pyridine and dihydro-isoindolone group as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and / or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
![BENZOIMIDAZOLE, TETRAHYDRO-QUINOXALINE, BENZOTRIAZOLE, DIHYDRO-IMIDAZO[4,5-c] PYRIDINONE AND DIHYDRO-ISOINDOLONE DERIVATIVES](https://images-eureka.patsnap.com/patent_img/a9d7fd51-4942-4540-8f6c-ca73efd365e5/US20080249101A1-20081009-C00001.png "BENZOIMIDAZOLE, TETRAHYDRO-QUINOXALINE, BENZOTRIAZOLE, DIHYDRO-IMIDAZO[4,5-c] PYRIDINONE AND DIHYDRO-ISOINDOLONE DERIVATIVES")
![BENZOIMIDAZOLE, TETRAHYDRO-QUINOXALINE, BENZOTRIAZOLE, DIHYDRO-IMIDAZO[4,5-c] PYRIDINONE AND DIHYDRO-ISOINDOLONE DERIVATIVES](https://images-eureka.patsnap.com/patent_img/a9d7fd51-4942-4540-8f6c-ca73efd365e5/US20080249101A1-20081009-C00002.png "BENZOIMIDAZOLE, TETRAHYDRO-QUINOXALINE, BENZOTRIAZOLE, DIHYDRO-IMIDAZO[4,5-c] PYRIDINONE AND DIHYDRO-ISOINDOLONE DERIVATIVES")
![BENZOIMIDAZOLE, TETRAHYDRO-QUINOXALINE, BENZOTRIAZOLE, DIHYDRO-IMIDAZO[4,5-c] PYRIDINONE AND DIHYDRO-ISOINDOLONE DERIVATIVES](https://images-eureka.patsnap.com/patent_img/a9d7fd51-4942-4540-8f6c-ca73efd365e5/US20080249101A1-20081009-C00003.png "BENZOIMIDAZOLE, TETRAHYDRO-QUINOXALINE, BENZOTRIAZOLE, DIHYDRO-IMIDAZO[4,5-c] PYRIDINONE AND DIHYDRO-ISOINDOLONE DERIVATIVES")
Owner:F HOFFMANN LA ROCHE & CO AG
Pyridine, quinoline and pyrimidine derivatives
This invention is concerned with compounds of the formula wherein A, R1 to R5 are as defined in the specification and G is a pyridine, quinoline or pyrimidine group as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and / or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
Owner:F HOFFMANN LA ROCHE INC
4,4-disubstituted piperidine derivatives
This invention relates to 4,4-disubstituted piperidine derivatives of the formulawherein A and R1 to R5 are as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and / or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
Owner:F HOFFMANN LA ROCHE & CO AG
Combination treatment of specific forms of epilepsy
InactiveUS20170071949A1Reduce seizuresEliminate side effectsAnhydride/acid/halide active ingredientsHeterocyclic compound active ingredientsSide effectCo morbidity
Formulations for and methods of treatment of Dravet syndrome that avoid side effects are disclosed. The formulations comprise a 5-HT receptor agonists which does not agonize selected 5-HT receptor subtypes, and in particular does not agonize the receptor subtype 5-HT2B. Also disclosed are combinations of such 5-HT receptor agonists. Also disclosed are combinations of such 5-HT receptor agonists and SSRIs, SNRIs, and triptans for treating co-morbidities associated with Dravet syndrome.
Owner:ZOGENIX INT
Conformationally constrained backbone cyclized somatostatin analogs
InactiveUS6930088B2Improve stabilityHigh selectivityNervous disorderPeptide/protein ingredientsSomatostatin analogReceptor subtype
Novel peptides which are conformationally constrained backbone cyclized somatostatin analogs, having somatostatin receptor subtype selectivity are disclosed. These patterns or receptor subtype selectivity provide compounds having improved therapeutic utility. Methods for synthesizing the somatostatin analogs and for screening of the somatostatin analogs are also disclosed. Furthermore, pharmaceutical compositions comprising somatostatin analogs, and methods of using such compositions are disclosed.
Owner:CORTENDO
Prevention and treatment of skeletal disorder with EP2 receptor subtype selective prostaglandin E2 agonists
This invention relates to the use of EP2 receptor subtype selective prostaglandin E2 agonists to augment bone mass including the prevention and treatment of skeletal disorders in mammals, including humans.
Owner:PFIZER INC
FGF variants and methods for use thereof
ActiveUS20050148511A1High affinityImprove biological activityPeptide/protein ingredientsSkeletal disorderDiseaseReceptor subtype
The present invention provides fibroblast growth factor variants demonstrating enhanced receptor subtype specificity and / or affinity. Preferred embodiments include both variants having enhanced activity that act as improved agonists and variants having reduced activity that act as antagonists. Methods of utilizing preferred FGF variants in preparation of medicaments for the treatment of skeletal disorders including skeletal dysplasia, osteoporosis and enhancing bone fracture healing and cartilage healing processes are provided.
Owner:PROCHON BIOTECH
Benzimidazolidinone derivatives as muscarinic agents
InactiveUS20060205785A1Increase acetylcholine signaling and effectHigh selectivityBiocideSenses disorderReceptor subtypeMuscarinic Agents
Owner:ACADIA PHARMA INC
Pyrimidine, quinazoline, pteridine and triazine derivatives
Owner:F HOFFMANN LA ROCHE & CO AG
Remedies for depression containing EP1 antagonist as the active ingredient
InactiveUS7335776B2Shorten immobility timeInhibition effectBiocideNervous disorderEndogenous depressionReactive Depression
A pharmaceutical composition for the treatment and / or prevention of depression comprising a compound having an antagonistic activity for EP1 receptor which a prostaglandin E2 receptor subtype.EP1 antagonist is useful for the treatment of depression, for example, endogenous depression, reactive depression, weatherability depression, neurological depressed state, the depressed state of brain organic mental disorder.
Owner:ONO PHARMA CO LTD
Photo-active backbone cyclized somatostatin analogs for photodynamic therapy and imaging
InactiveUS7700717B2Unique and superior chemicalUnique and superior and metabolicPeptide/protein ingredientsPhotodynamic therapySomatostatin analogReceptor subtype
Owner:DEVELOGEN ISRAEL
Sphingosine 1-phosphate antagonism
InactiveUS20090226453A1Good curative effectAnimal cellsTetracycline active ingredientsSphingosine-1-phosphatePhosphoric acid
Materials and Method for treating cancer and screening for anti-neoplastic agents are provided. These materials and methods can include sphingosine 1-phosphate antagonists that bind to sphingosine-1 phosphate receptor subtype 3. Antibodies and aptamers that selectively bind to an epitope in the extracellular loop between transmembrane domains two and three of sphingosine-1-phosphate receptor subtype 3 are provided.
Owner:EXPRESSION DRUG DESIGNS
Flourene Derivative
This invention relates to a novel fluorene derivative having a characteristic structure in which guanidino group or the like functional group is linked to the fluorene structure via carbonyl group, or a salt thereof.The compound of the invention has an advantage in that it has high affinity for serotonin receptor subtypes, particularly for 5-HT2B receptor and 5-HT7 receptor, and shows excellent pharmacological effects in comparison with the conventional compounds which have only one of the antagonistic activities of 5-HT2B receptor and 5-HT7 receptor, this is useful as a prophylactic antimigraine agent having high safety and excellent effect.
Owner:ASTELLAS PHARMA INC
Benzimidazolidinone derivatives as muscarinic agents
InactiveUS20060025402A1Increase acetylcholine signaling and effectHigh selectivityBiocideNervous disorderReceptor subtypeMuscarinic Agents
Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and / or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.
Owner:ACADIA PHARMA INC
Treating neuropathic pain with neuropeptide FF receptor 2 agonists
The invention described below relates to the discovery of the neuropeptide FF receptor subtype that mediates acute nociception and chronic neuropathic pain, compounds that selectively interact with this receptor subtype and methods for treating acute pain and chronic neuropathic pain.
Owner:ACADIA PHARMA INC
Treating neuropathic pain with neuropeptide FF receptor 2 agonists
InactiveUS20050136444A1Relieve pain symptomsRelieve symptomsOrganic active ingredientsCompound screeningReceptor subtypeAgonist
The invention described below relates to the discovery of the neuropeptide FF receptor subtype that mediates acute nociception and chronic neuropathic pain, compounds that selectively interact with this receptor subtype and methods for treating acute pain and chronic neuropathic pain.
Owner:ACADIA PHARMA INC
Combination treatment of specific forms of epilepsy
InactiveUS20180325909A1Reduce seizuresEliminate side effectsAnhydride/acid/halide active ingredientsHeterocyclic compound active ingredientsSide effectCo morbidity
Formulations for and methods of treatment of Dravet syndrome that avoid side effects are disclosed. The formulations comprise a 5-HT receptor agonists which does not agonize selected 5-HT receptor subtypes, and in particular does not agonize the receptor subtype 5-HT2B. Also disclosed are combinations of such 5-HT receptor agonists. Also disclosed are combinations of such 5-HT receptor agonists and SSRIs, SNRIs, and triptans for treating co-morbidities associated with Dravet syndrome.
Owner:ZOGENIX INT
Methods for treating Parkinson's disease
The invention pertains to a method of treating Parkinson's disease (PD) in a mammal, comprising administering a first pharmaceutical agent and a second pharmaceutical agent, wherein the first pharmaceutical agent is an antagonist of the adenosine receptor 2 (A2A) and the second pharmaceutical agent is an antagonist of the N-methyl-D-aspartate (NMDA) receptor subtype NR2B.
Owner:UCB PHARMA SRL +1
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