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160 results about "Receptor activation" patented technology
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Receptor activation is an effect on receptor function equivalent to that produced by the natural neurotransmitter at a particular synapse. Activation of a receptor may slow down or speed up the process, depending on the function of that particular receptor.
Device and Method for Treating Weight Disorders
An apparatus and a method for treating a weight disorder in a subject are provided. The apparatus comprising an implantable device such as an inflatable balloon and electrodes capable of sensing a physiological change associated with food ingestion or hunger and a mechanism adapted for directly stimulating a region such as the duodenum which is responsive to a gastrointestinal satiety agent, such a mechanism can be a drug reservoir containing a drug such as CCK or analogs thereof which is contained within an inflatable balloon being implantable in a stomach of the subject. The apparatus and method provided here combine synergistic approaches to limiting meal size, i.e., chemo and mechano receptor activation of vagal satiety stimuli, electric stimulation of specific vagal pathways and limitations of gastric space.
Owner:DUOCURE
Substituted biphenyl-4-carboxylic acid arylamide analogues
Substituted biphenyl-4-carboxylic acid arylamide analogues capable of modulating receptor activity, are provided. Such ligands may be used to modulate receptor activity in vivo or in vitro, and are particularly useful in the treatment of pain and other conditions associated with receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for receptor localization studies.
Owner:NEUROGEN
Methods and compositions for alleviating pain
ActiveUS7345065B2Reduced activityReduce expressionBiocideNervous disorderChronic painReceptor activation
The present invention provides a method for the long-term relief of chronic pain in a subject by activating in the subject an analgesic α-adrenergic receptor in the absence of α-2A receptor activation over a period of at least three days, such that relief of chronic pain is maintained in the absence of continued activation of said receptor. The analgesic α-adrenergic receptor can be, for example, the α-2B receptor.
Owner:ALLERGAN INC
Heteroaryl Substituted Piperazinyl-Pyridine Analogues
InactiveUS20080124384A1Inhibit bindingGood for weight lossBiocideOrganic active ingredientsArylDisease
Substituted biaryl piperazinyl-pyridine analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
Owner:NEUROGEN
Substituted quinazolin-4-ylamine analogues
Substituted quinazolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
Owner:NEUROGEN
Novel methods and compositions for alleviating pain
The present invention provides a method for the long-term relief of chronic pain in a subject by activating in the subject an analgesic alpha-adrenergic receptor in the absence of alpha-2A receptor activation over a period of at least three days, such that relief of chronic pain is maintained in the absence of continued activation of said receptor. The analgesic alpha-adrenergic receptor can be, for example, the alpha-2B receptor.
Owner:ALLERGAN INC
Substituted quinolin-4-ylamine analogues
InactiveUS20050070547A1Inhibit bindingReduction in mechanical allodynia, mechanical hyperalgesia and/or thermal hyperalgesiaBiocideNervous disorderDiseaseReceptor activation
Substituted quinolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders-are provided, as are methods for using such ligands for receptor localization studies.
Owner:NEUROGEN
LPA analogs as agonists of the Edg2 LPA receptor
InactiveUS6380177B1Improve bindingBiocidePhosphorous compound active ingredientsDiseaseLPA Receptors
Applicant has probed the Edg2 lysophosphatidic acid (LPA) receptor with a series of LPA analogs to determine receptor activation. The present invention is drawn to a series of LPA analogs which function as Edg2 receptor agonists, and methods of using such compounds to activate the Edg2 receptor of the surface of a cell. The compounds of the invention comprise a glycerol backbone with an Sn1 ester-linked saturated or unsaturated alkyl group, substitutions of the hydroxyl group (-OH) at carbon two of the glycerol backbone, and optional replacement of the phosphate di-anion with either a hydroxyl group or a dimethylated phosphate. These LPA analogs may find uses in cancer and neurological disorders.
Owner:APOLLO ENDOSURGERY INC
Antibodies blocking fibroblast growth factor receptor activation and methods of use thereof
ActiveUS20100047251A1Strong specificityHigh affinityImmunoglobulins against growth factorsAntibody ingredientsFGF ReceptorReceptor activation
The present invention is related to antibodies with binding affinity to fibroblast growth factor receptor 2 (FGFR2) optionally with binding affinity to other FGF receptors, which block both ligand-dependent and constitutive ligand independent receptor activation. Specifically, the present invention relates to antibodies with high affinity to more than one FGF receptor subtype, and fragments thereof, useful in treating disorders including cell proliferative diseases.
Owner:FIBRON
Inhibitory immunoglobulin polypeptides to human PDGF beta receptor
InactiveUS7060271B2Peptide/protein ingredientsImmunoglobulins against cell receptors/antigens/surface-determinantsHuman typeReceptor activation
The present invention is directed towards immunoglobulin polypeptides that specifically bind to the extracellular domain of the human type beta PDGF receptor. The binding of the immunoglobulin polypeptides to the receptor inhibits PDGF-induced (or stimulated) receptor activation as indicated by inhibition of receptor phosphorylation and dimerization, and by inhibition of PDGF-mediated mitogenesis, chemotaxis and migration of cells displaying the human PDGF type beta receptor on the cell surface. Nucleic acids encoding the immunoglobulin polypeptides are also included in the invention. The immunoglobulin polypeptides have diagnostic and therapeutic uses.
Owner:MILLENNIUM PHARMA INC
Conjugate comprising oxyntomodulin and an immunoglobulin fragment, and use thereof
ActiveUS20140212440A1Reduces food intakeSuppresses gastric emptyingPeptide/protein ingredientsMetabolism disorderSide effectReceptor activation
The present invention relates to a conjugate comprising oxyntomodulin, an immunoglobulin Fc region, and non-peptidyl polymer wherein the conjugate being obtainable by covalently linking oxyntomodulin to immunoglobulin Fc region via non-peptidyl polymer, and a pharmaceutical composition for the prevention or treatment of obesity comprising the conjugates. The conjugate comprising oxyntomodulin and the immunoglobulin Fc of the present invention reduces food intake, suppresses gastric emptying, and facilitates lipolysis without side-effects, unlike native oxyntomodulin, and also shows excellent receptor-activating effects and long-term sustainability, compared to native oxyntomodulin. Thus, it can be widely used in the treatment of obesity with safety and efficacy.
Owner:HANMI SCI CO LTD
Polynucleotides encoding GFRα3
InactiveUS7026138B1Facilitating identification and characterizationEasy to detectSugar derivativesTissue cultureNucleotideReceptor activation
The present invention relates to nucleotide sequences, including expressed sequence tags (ESTs), oligonucleotide probes, polypeptides, vectors and host cells expressing, and immunoadhesions and antibodies to mammalian GFRα3, a novel α-subunit receptor of the GDNF (i.e. GFR) receptor family. It further relates to an assay for measuring activation of an α-subunit receptor by detecting tyrosine kinase receptor activation (i.e., autophosphorylation) or other activities related to ligand-induced α-subunit receptor homo-dimerization or homo-oligomerization.
Owner:GENENTECH INC
Novel oxyntomodulin derivatives and pharmaceutical composition for treating obesity comprising the same
ActiveUS20140128318A1Reduces food intakeSuppresses gastric emptyingCell receptors/surface-antigens/surface-determinantsSugar derivativesSide effectReceptor activation
The present invention relates to a novel peptide showing more excellent activities on a glucagon like peptide-1 receptor and a glucagon receptor than native oxyntomodulin, and a composition for the prevention or treatment of obesity comprising the peptide as an active ingredient. Unlike native oxyntomodulin, the novel peptide of the present invention reduces food intake, suppresses gastric emptying, and facilitates lipolysis with reduced side-effects, and also shows excellent receptor-activating effects. Thus, it can be widely used in the treatment of obesity with safety and efficacy.
Owner:HANMI SCI CO LTD
Therapeutic and diagnostic cloned MHC-unrestricted receptor specific for the MUC1 tumor associated antigen
The invention provides an isolated nucleic acid encoding a receptor, other than an immunoglobulin, wherein the receptor binds to a MUC1 tumor antigen independently of an major histocompatibility complex (MHC). The invention provides a method of activating a signaling pathway and / or killing a cancer cell using a receptor that is similar to or is a T cell receptor
Owner:UNIVERSITY OF PITTSBURGH
Substituted heterocyclic diarylamine analogues
Substituted heterocyclic diarylamine analogues of Formula I are provided: wherein X, Y and Z are independently N or optionally substituted C, and other variables are as described in the specification. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
Owner:NEUROGEN
Methods for measuring platelet reactivity of patients that have received drug eluting stents
InactiveUS20070243632A1Reduce capacityEnhance signal transductionElcosanoid active ingredientsMicrobiological testing/measurementThrombusReceptor activation
A method is providing for measuring platelet reactivity of a PCI patient that has a (DES). A blood sample is obtained from the patient. The blood sample is mixed in combination with 1) an anticoagulant; 2) sufficient buffer to maintain the pH and salt concentration of the anticoagulated blood within a range suitable for platelet aggregation; 3) a platelet GPIIb / IIIa receptor ligand immobilized on a solid surface; 4) one or more agents to enhance a signal transduction pathway and 5) a receptor activator. The combination is incubated under conditions for agglutinating particles. Platelet-mediated agglutination is assessed in the mixture. The absence of agglutination indicates that the patient has reduced ability to form platelet thrombi.
Owner:ACCUMETRICS INC
Green and orange fluorescent labels and their uses
InactiveUS7317111B2Facilitates creation and useOrganic chemistryOrganic compound preparationReceptor activationPyrene
The present invention provides novel fluorescent compounds and covalent attachment chemistries which facilitate the use of these compounds as labels for ultrasensitive and quantitative fluorescent detection of low levels of biomolecules. In a preferred embodiment, the fluorescent labels of this invention are novel derivatives of the hydroxy-pyrene trisulphonic and disulphonic acids which may be used in any assay in which radioisotopes, colored dyes or other fluorescent molecules are currently used. Thus, for example, any assay using labeled antibodies, proteins, oligonucleotides or lipids, including fluorescent cell sorting, fluorescence microscopy (including dark-field microscopy), fluorescence polarization assays, ligand, receptor binding assays, receptor activation assays and diagnostic assays can benefit from use of the compounds disclosed herein.
Owner:ARIES ASSOCS
GFRalpha3 and its uses
InactiveUS20060216289A1Facilitating identification and characterizationEasy to detectFungiSenses disorderAutophosphorylationReceptor activation
The present invention relates to nucleotide sequences, including expressed sequence tags (ESTs), oligonucleotide probes, polypeptides, vectors and host cells expressing, and immunoadhesions and antibodies to mammalian GFRα3, a novel α-subunit receptor of the GDNF (i.e. GFR) receptor family. It further relates to an assay for measuring activation of an α-subunit receptor by detecting tyrosine kinase receptor activation (i.e., autophosphorylation) or other activities related to ligand-induced α-subunit receptor homo-dimerization or homo-oligomerization.
Owner:DE SAUVAGE FREDERIC +3
Substituted Pyridazinyl- and Pyrimidinyl-Quinolin-4-Ylamine Analogues
InactiveUS20080175794A1Inhibit bindingGood for weight lossBiocideNervous disorderReceptor activationIn vivo
Substituted pyridazinyl- and pyrimidinyl-quinolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
Owner:NEUROGEN
Compositions comprising novel PPAR ligands and anti-hyperlipemic agents
InactiveUS20070054949A1Convenient treatmentPrevent goodBiocideAntipyreticDyslipidemiaTG - Triglyceride
Methods are provided for treating or preventing conditions comprising hypertension and dyslipidemia using antihyperlipemic agents and compounds that antagonize the angiotensin II type 1 (AT1) receptor, function as partial or full activators of peroxisome proliferator activated receptors (PPARs) and lower triglycerides or elevate blood HDL-cholesterol. Compositions are provided for treating or preventing conditions comprising hypertension and dyslipidemia, comprising antihyperlipemic agents which lower triglycerides and inhibit cholesterol synthesis such as statins, and compounds that antagonize or block the angiotensin II type 1 (AT1) receptor, activate PPARs and lower triglycerides or elevate blood HDL-cholesterol such as sartans.
Owner:BETHESDA PHARMA
Antibodies blocking fibroblast growth factor receptor activation and methods of use thereof
The present invention is related to antibodies with binding affinity to fibroblast growth factor receptor 2 (FGFR2) optionally with binding affinity to other FGF receptors, which block both ligand-dependent and constitutive ligand independent receptor activation. Specifically, the present invention relates to antibodies with high affinity to more than one FGF receptor subtype, and fragments thereof, useful in treating disorders including cell proliferative diseases.
Owner:FIBRON
Substituted quinolin-4-ylamine analogues
InactiveUS7488740B2Reduction in mechanical allodynia, mechanical hyperalgesia and/or thermal hyperalgesiaBiocideNervous disorderReceptor activationIn vivo
Substituted quinolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
Owner:NEUROGEN
Inhibitors of tlr signaling by targeting tir domain interfaces
ActiveUS20130203649A1Cell receptors/surface-antigens/surface-determinantsPeptide/protein ingredientsReceptor activationCell biology
Owner:UNIV OF MARYLAND
Sterol absorption inhibitor compositions
The present invention provides compositions, therapeutic combinations and methods including: (a) at least one peroxisome proliferator-activated receptor activator; and (b) at least one substituted azetidinone or substituted β-lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity and lowering plasma levels of sterols.
Owner:ORGANON LLC
Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues
Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
Owner:NEUROGEN CORP
Fused heterocyclic compound and use thereof
InactiveUS20090131402A1Enhance the imageGood durationBiocideElectrotherapyReceptor activationProdrug
Owner:TAKEDA PHARMA CO LTD
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
Method of transporting a chimeric hybrid molecule across the blood brain barrier
InactiveUS7214657B2Little or no opioid dependence formationBiocideNervous disorderAbuse drugsReceptor activation
The present invention provides a method of transporting a pharmacologically active peptide across the blood brain barrier by administering to a living subject a conjugate molecule of a general class of chimeric hybrid conjugate molecules capable of simultaneous activation of MOR and SPR receptors within the CNS that is intrinsically a function of this class of molecules to permeate the mammalian BBB as an intact chemical entity. Accordingly, the chemical and pharmacological integrity of each of the receptor activating domains functionally enables BBB transport of its covalently bonded reciprocal receptor activating domain. As such, the requirement for an intact chimeric hybrid conjugate molecule as the only viable transport vehicle for equivalent BBB transport of each of its MOR and SPR receptor activation domains distinguishes the present invention as novel and unknown to the literature of CNS analgesic and anti-abuse drugs.
Owner:CHIMERACOM LLC
Heteroaryl Substituted Quinolin-4-Ylamine Analogues
Heteroaryl substituted quinolin-4-ylamine analogues of Formula I are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
Owner:NEUROGEN
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