152 results about "Receptor activation" patented technology

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

The present invention relates to a serotonin 5-HT_2C receptor activator containing a compound represented by the formula

wherein ring A is a 5- or 6-membered aromatic heterocycle optionally having substituent(s), and ring B is a 7- to 9-membered ring optionally having substituent(s) other than an oxo group wherein the combination of m and n (m,n) is (1,2), (2,1), (2,2), (3,1), (3,2) or (4,1), or a salt thereof or a prodrug thereof, and a fused heterocyclic compound having a serotonin 5-HT_2C receptor activating action and the like.

The present invention provides a tricyclic heterocyclic compound having a serotonin 5-HT_2C receptor activation action and the like.

A 5-HT_2C 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.

The present invention provides novel fluorescent compounds and covalent attachment chemistries which facilitate the use of these compounds as labels for ultrasensitive and quantitative flourescent detection of low levels of biomolecules. In a preferred embodiment, the flourescent 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.