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Receptor patents



      
           
This page is updated frequently with new Receptor-related patent applications. Subscribe to the Receptor RSS feed to automatically get the update: related Receptor RSS feeds. RSS updates for this page: Receptor RSS RSS


Date/App# patent app List of recent Receptor-related patents
12/11/14
20140364607
 Benzoimidazol-2-yl pyrimidine modulators of the histamine h4 receptor patent thumbnailBenzoimidazol-2-yl pyrimidine modulators of the histamine h4 receptor
Benzoimidazol-2-yl pyrimidines, purification methods for the same, and pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by h4 receptor activity, including allergy, asthma, autoimmune diseases, and pruritus.. .
12/11/14
20140364583
 Beta-hairpin peptidomimetics having cxcr4 antagonizing activity patent thumbnailBeta-hairpin peptidomimetics having cxcr4 antagonizing activity
β-hairpin peptidomimetics of the general formula cyclo(—xaa1—xaa2—xaa3—cys4—xaa5—xaa6—xaa7—xaa8—arg9—tyr10—cys11—xaa12—xaa13—xaa14—xaa15—xaa16—), disulfide bond between cys4 and cys11, and pharmaceutically acceptable salts thereof, with xaa1, xaa2, xaa3, xaa5, xaa6, xaa7, xaa8, xaa12, xaa13, xaa14, xaa15 and xaa16 being amino acid residues of certain types which are defined in the description and the claims, have cxcr4 antagonizing properties and can be used for preventing hiv infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from cxcr4 receptor activity; or where immunological diseases are mediated or resulting from cxcr4 receptor activity; or for treating immunosuppression; or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptides can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy..
12/11/14
20140364473
 Oral suspension comprising telmisartan patent thumbnailOral suspension comprising telmisartan
A pharmaceutical solution with a ph value of 10 or higher contains an angiotensin ii receptor antagonist, where one or more sugar alcohols are present up to a total concentration of 40 wt. % to 70 wt.
12/11/14
20140364449
 Method and system for identifying compounds that bind and/or activate a target opioid receptor in a ph-dependent manner patent thumbnailMethod and system for identifying compounds that bind and/or activate a target opioid receptor in a ph-dependent manner
The invention relates to a method for identifying compounds that bind and preferably activate a target opioid receptor in a ph-dependent manner.. .
12/11/14
20140364448
 Quarternized buprenorphine analogs patent thumbnailQuarternized buprenorphine analogs
The present invention is directed to buprenorphine analog compounds of the formula (i), formula (ia) or formula (ib) shown below, wherein r1, r1a, r2, r8, r3a, r3b, g, x, z, y, and a® are as defined herein. Compounds of the invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and orl-1 receptors..
12/11/14
20140364445
 Pharmaceutical composition comprising a trpa1 antagonist and an anticholinergic agent patent thumbnailPharmaceutical composition comprising a trpa1 antagonist and an anticholinergic agent
The present invention relates to a pharmaceutical composition comprising a transient receptor potential ankyrin-1 receptor (“trpa1”) antagonist and an anticholinergic agent. Particularly, the present invention provides a pharmaceutical composition comprising a trpa1 antagonist having ic50 for inhibiting human trpa1 receptor activity of less than 1 micromolar and an anticholinergic agent; a process for preparing such composition; and its use in treating a respiratory disorder in a subject..
12/11/14
20140364433
 Substituted prolines / piperidines as orexin receptor antagonists patent thumbnailSubstituted prolines / piperidines as orexin receptor antagonists
The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as ox1 or ox2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention. For example, orexin receptor-modulatory compounds of the present invention can be used in treatment of an eating disorder, obesity, alcoholism or an alcohol-related disorder, drug abuse or addiction including addiction to cocaine, opiates, amphetamines, or nicotine, a sleep disorder, a cognitive dysfunction in a psychiatric or neurologic disorder, depression, anxiety, panic disorder, schizophrenia, alzheimer's disease, parkinson's disease, huntington's chorea, headache, migraine, pain, gastrointestinal diseases, epilepsy, inflammations, immune-related diseases, endocrine-related diseases, cancer, hypertension, behavior disorder, mood disorder, manic depression, dementia, sex disorder, psychosexual disorder, or renal disease..
12/11/14
20140364432
 Substituted prolines / piperidines as orexin receptor antagonists patent thumbnailSubstituted prolines / piperidines as orexin receptor antagonists
The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as ox1 or ox2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention. For example, orexin receptor-modulatory compounds of the present invention can be used in treatment of an eating disorder, obesity, alcoholism or an alcohol-related disorder, drug abuse or addiction including addiction to cocaine, opiates, amphetamines, or nicotine, a sleep disorder, a cognitive dysfunction in a psychiatric or neurologic disorder, depression, anxiety, panic disorder, schizophrenia, alzheimer's disease, parkinson's disease, huntington's chorea, headache, migraine, pain, gastrointestinal diseases, epilepsy, inflammations, immune-related diseases, endocrine-related diseases, cancer, hypertension, behavior disorder, mood disorder, manic depression, dementia, sex disorder, psychosexual disorder, or renal disease..
12/11/14
20140364427
 Estrogen receptor modulators and uses thereof patent thumbnailEstrogen receptor modulators and uses thereof
Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors..
12/11/14
20140364420
 Substituted piperazinyl-pyrrolidine compounds useful as chemokine receptor antagonists patent thumbnailSubstituted piperazinyl-pyrrolidine compounds useful as chemokine receptor antagonists
Or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of chemokine receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer or osteolytic bone disorders..
12/11/14
20140364409
Substituted pyrazolo[3',4':4,5]thieno[2,3-c]pyridazin-3-amine analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m4
In one aspect, the invention relates to substituted pyrazolo[3′,4′:4,5]thieno[2,3-c]pyridazine-3-amine analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor m4 (machr m4); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention..
12/11/14
20140364395
Pyranyl aryl methyl benzoquinolinone m1 receptor positive allosteric modulators
Which are m1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the m1 receptor is involved, such as alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the m1 receptor..
12/11/14
20140364387
Methods and systems for modulating hormones and related methods, agents and compositions
Provided herein are bitter taste receptor ligands, related agents, combinations, compositions, methods and systems for modulating release of a metabolic hormone in vitro or in vivo from cells of the gi tract of an individual.. .
12/11/14
20140364358
Method for preventing and treating hyperpermeability
A peptide is described, which consists of 7-17 adjacent amino acids and comprises the hexamer txexxe, wherein x, x and x can be any natural or non-natural amino acid, wherein the peptide has no tnf receptor binding activity and is cyclized, for the prevention and treatment of hyperpermeability of epithelial cells and endothelial cells.. .
12/11/14
20140364330
Multiplexed olfactory receptor-based microsurface plasmon polariton detector
The invention provides a bio-sensing nanodevice comprising: a stabilized g-protein coupled receptor on a support, a real time receptor-ligand binding detection method, a test composition delivery system and a test composition recognition program. The g-protein coupled receptor can be stabilized using surfactant peptide.
12/11/14
20140364325
Array of sensors functionalized with systematically varying receptor materials
A sensor array includes resonator sensors having respective receptor materials disposed thereon. The receptor materials have a physical property relevant to their ability to bind or adsorb one or more analytes in a sample.
12/11/14
20140363818
Egfr and par2 regulation of intestinal permeability
The present invention provides methods for diagnosing an immune-mediated disease, e.g., an autoimmune disease, an allergy or an inflammatory disease. Diagnosis is made by detecting a heterozygous or homozygous genotype of haptoglobin 2 or by detecting and quantifying pre-haptoglobin 2 mrna or protein.
12/11/14
20140363471
Method of inducing autophagy and activating toll-like receptor
A method of inducing autophagy in a cell is achieved by contacting the cell with graphene oxide (go) in an amount effective to induce autophagy in the cell, wherein the cell expresses at least one of tlr-4 (toll-like receptor 4) and tlr-9 (toll-like receptor 9). Differences between autophagy triggered by go and other conventional agonists such as rapamycin have been observed.
12/11/14
20140363457
2-thio-1,3,4-oxadiazoles azetidine derivatives as sphingosine-1 phosphate receptors modulators
The present invention relates to 2-thio-1,3,4-oxadiazoles azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.. .
12/11/14
20140363453
Methods for increasing efficacy of folr1 cancer therapy
Methods to improve the success of cancer therapies that target the human folate receptor 1 are provided. Kits comprising reagent useful in the methods are further provided..
12/11/14
20140363448
Cdcp1 and breast cancer
The present invention relates to a method for treating breast cancer in a subject having a hyperactivation of the epidermal growth factor receptor 1 and/or 2 (egfr and/or erbb2 her2), as compared to the normal subject population, or expressing deltaher2, which method comprises the step of administering to said subject a therapeutically effective amount of a modulator of the cub domain-containing protein 1 (cdcp1).. .
12/11/14
20140363432
Vascular endothelial cell growth factor antagonists and uses thereof
The present invention provides vascular endothelial cell growth factor (vegf) antagonists and methods of using vegf antagonists. Vegf antagonists contemplated by the invention include vegf antibodies and vegf receptor fusion proteins.
12/11/14
20140363430
Activatable antibodies that bind interleukin-6 receptor and methods of use thereof
The invention relates generally to activatable antibodies that include a masking moiety (mm), a cleavable moiety (cm), and an antibody (ab) that specifically binds to interleukin-6 receptor (il-6r), and to methods of making and using these anti-il-6r activatable antibodies in a variety of therapeutic, diagnostic and prophylactic indications.. .
12/11/14
20140363429
Binding molecules specific for her3 and uses thereof
The present invention relates to antibodies and antigen binding fragments thereof that bind the extracellular domain of the her3 receptor and inhibit various her3 receptor related functions via ligand-dependent and/or ligand-independent mechanisms. Also provided are compositions with increased half-life.
12/11/14
20140363428
Therapeutic antigen-binding molecule with a fcrn-binding domain that promotes antigen clearance
The present invention provides: a modified fcrn-binding domain having an enhanced affinity for the fc receptor neonatal (fcrn) at neutral ph; an antigen-binding molecule comprising said fcrn-binding domain, which has low immunogenicity, high stability and form only a few aggregates; a modified antigen-binding molecule having an increased fcrn-binding activity at neutral or acidic ph without an increased binding activity at neutral ph for a pre-existing anti-drug antibody; use of the antigen-binding molecules for improving antigen-binding molecule-mediated antigen uptake into cells; use of the antigen-binding molecules for reducing the plasma concentration of a specific antigen; use of the modified fcrn-binding domain for increasing the total number of antigens to which a single antigen-binding molecule can bind before its degradation; use of the modified fcrn-binding domain for improving pharmacokinetics of an antigen-binding molecule; methods for decreasing the binding activity for a pre-existing anti-drug antibody; and methods for producing said antigen-binding molecules.. .
12/11/14
20140363425
Systems and methods for identifying cancers having activated progesterone receptors
Systems and methods for identifying tumors having activated progesterone receptors are provided. Patients suspected of having a tumor susceptible to growth inhibition by anti-progestins can be treated with an anti-progestin..
12/11/14
20140363193
Air-bearing photoreceptor backer bar for eliminating transfer streaks
An apparatus for eliminating transfer streaks in a printing system is provided and comprises a hollow transfer backer bar including sealed ends. The transfer backer bar further includes a plurality of holes with the holes spaced along the photoreceptor supporting surface of the transfer backer bar.
12/11/14
20140362156
Thermal transfer ribbon marking
Objects of arbitrary shape and size are marked by a method using a thermal transfer ribbon. The method comprises the steps of creating a graphic on a thermal transfer ribbon, joining the graphic-bearing ribbon to a receptor substrate, removing the graphic-bearing ribbon from the receptor substrate, placing the graphic-bearing ribbon on a target object with the graphic in contact with a surface of the target object, applying sufficient heat and pressure to the graphic-bearing ribbon such that the graphic is transferred from the ribbon to the surface of the target object, and removing the ribbon from the surface of the target object..
12/04/14
20140358204
Method and apparatus for controlling menopausal hot flashes
A device and method for non-invasive treatment of menopausal hot flashes. The device includes a hand-held assembly sized to be held in the palm of a user's hand; a cooling plate within the assembly and a cradle which docks with the assembly.
12/04/14
20140358017
Method and apparatus for monitoring the baroreceptor reflex of a user
There is provided an apparatus for use in monitoring the baroreceptor reflex in a user, the apparatus comprising a processor configured to process a signal output by a first sensor that is attached to or located proximate to a bed to determine when the user moves from a lying position on the bed to a sitting position, and to provide an indication of the baroreceptor reflex of the user by processing the signal to determine the change in the heart rate of the user that occurs as a result of moving from the lying position to the sitting position.. .
12/04/14
20140357967
Detection device for the in vivo and/or in vitro enrichment of sample material
The invention relates to a detection device for the in vivo and/or in vitro enrichment of sample material, comprising a functional surface charged with detection receptors. To ensure the diagnosis of different diseases using a detection device of the type mentioned at the outset with less efforts and an improved precision of the diagnosis, it is provided according to the invention that the detection device comprises at least one guide element and at least two functional elements disposed at the guide element, wherein a functional surface charged with detection receptors is formed at each of them, the functional elements being designed for being detachable from each other and/or individually detachable from the guide element.
12/04/14
20140357865
Process for the preparation of benzoimidazol-2-yl pyrimidine derivatives
The present invention is directed to benzoimidazol-2-yl pyrimidine derivatives useful as histamine h4 receptor modulators and processes for the preparation of such compounds.. .
12/04/14
20140357858
P2x4 receptor antagonist
The present invention relates to a diazepine derivative represented by the following general formula (i) (in the formula, r1 and r2 represent hydrogen atom and the like, or r1 and r2 bind together to form a naphthalene ring and the like together with the benzene ring to which they bind, r3 and r4 represent hydrogen atom and the like, r5 represents hydrogen atom and the like, r6 and r7 represent hydrogen atom and the like, x represents c, ch or n, y represents n, nh or c(═o), provided that when x is n, y is not n or nh, and when x is c or ch, y is not c(═o), z represents oxygen atom or sulfur atom, a represents benzene ring and the like, b represents nhc(═o) and the like, d represents an atomic bond and the like, e represents an atomic bond and the like, g represents benzene which may be substituted and the like, and m represents an integer of 0 to 5) or a pharmacologically acceptable salt thereof, and a p2x4 receptor antagonist.. .
12/04/14
20140357849
Splice switching oligomers for tnf superfamily receptors and their use in treatment of disease
The present invention relates to compositions and methods for preparing splice variants of tnfalpha receptor (tnfr) in vivo or in vitro, and the resulting tnfr protein variants. Such variants may be prepared by controlling the splicing of pre-mrna molecules and regulating protein expression with splice switching oligonucleotides or splice switching oligomers (ssos).
12/04/14
20140357696
Rnai-related inhibition of tnf alpha signaling pathway for treatment of ocular angiogenesis
Rna interference is provided for inhibition of tumor necrosis factor α (tnfα) by silencing tnfα cell surface receptor tnf receptor-1 (tnfr1) mrna expression, or by silencing tnfα converting enzyme (tace/adam17) mrna expression. Silencing such tnfα targets, in particular, is useful for treating patients having a tnfα-related condition or at risk of developing a tnfα-related condition, such as ocular angiogenesis, retinal ischemia, and diabetic retinopathy..
12/04/14
20140357694
Rnai-mediated inhibition of tumor necrosis factor alpha-related conditions
Rna interference is provided for inhibition of tumor necrosis factor α (tnfα) by silencing tnfα cell surface receptor tnf receptor-1 (tnfr1) mrna expression, or by silencing tnfα converting enzyme (tace/adam17) mrna expression. Silencing such tnfα targets, in particular, is useful for treating patients having a tnfα-related condition or at risk of developing a tnfα-related condition such as the ocular conditions dry eye, allergic conjunctivitis, or ocular inflammation, or such as dermatitis, rhinitis, or asthma, for example..
12/04/14
20140357690
Processes for the preparation of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid and salts thereof
The present invention relates to processes and intermediates useful in the preparation of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of formula (ia) and salts thereof, an s1p1 receptor modulator that is useful in the treatment of s1p1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis).. .
12/04/14
20140357682
Androgen receptor ligands
Non ligand binding pocket antagonists for the human androgen receptor. The androgen receptor (ar) is a member of the nuclear receptor (nr) family and its role is to modulate the biological effects of the endogenous androgens, testosterone (tes) and dihydrotestosterone (dht).
12/04/14
20140357674
Nicotinic receptor compounds
Compounds and compositions for promoting smoking cessation or decreasing tobacco use or nicotine addiction are provided. The compounds are 2′-fluoro-3′-(substituted phenyl) deschloroepibatidine analogs.
12/04/14
20140357656
Bivalent ligands for the treatment of neurological disorders
Bivalent ligands that contain two pharmacophores linked through a spacer, one of which interacts with the μ-opioid receptor (mor) and the other of which interacts with the co-receptor cc chemokine receptor 5 (ccr5), are used for the treatment of neurological disorders such as those associated with aids.. .
12/04/14
20140357655
Spiroindoline derivatives as gonadotropin- releasing hormone receptor antagonists
Spiroindoline derivatives, process for their preparation and pharmaceutical compositions thereof, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially sex-hormone-related diseases in both men and women, in particularly those selected from the group of endometriosis, uterine fibroids, polycystic ovarian disease, hirsutism, precocious puberty, gonadal steroid-dependent neoplasia such as cancers of the prostate, breast and ovary, gonadotrope pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hypertrophy, contraception and infertility (e.g., assisted reproductive therapy such as in vitro fertilization). The present application relates in particular to spiroindoline derivatives as gonadotropin-releasing hormone (gnrh) receptor antagonists..
12/04/14
20140357653
Chemical compounds
The invention relates to a novel compound of formula (i) or a stereoisomer, or a racemate or a mixture or a pharmaceutically acceptable salt thereof: wherein: r is phenyl or a 5- or 6-membered heteroaryl ring containing 1 to 3 heteroatoms selected from s, n and o, such rings may be optionally substituted with n groups q; q is selected from a group consisting of: c1-c4 alkyl, halogen, halo c1-c4 alkyl, c1-c4 alkoxy, cn, so2ch3 or a group —o[(cr1r2]pq1; or q may be a group q2; q1 is phenyl, which may be optionally substituted with n substituents selected from a group consisting of: c1-c4 alkyl, halogen, halo c1-c4 alkyl, c1-c4 alkoxy, cn, or a group q2; or corresponds to 2,2-difluoro-benzo[d][1,3]dioxol-4-yl; q2 is a 5- or 6-membered heteroaryl containing at least one nitrogen atom, which may optionally substituted with n substituents selected from a group consisting of: cl c1-c4 alkyl, halogen, halo c1-c4 alkyl, c1-c4 alkoxy, cn; p is a 6-membered heteroaryl or a 8-1 1 membered bicyclic heteroaryl group, which may be substituted with n substituents selected from a group consisting of: c1-c4 alkyl, halogen, halo c1-c4 alkyl, c1-c4 alkoxy, cn; r1 is hydrogen or c1-c3 alkyl; r2 is hydrogen or c1-c3 alkyl; n is 1, 2 or 3; p is 0, 1 or 2; and with the proviso that when r corresponds to phenyl, p is substituted by at least one cf3; processes for the preparation of those compounds, pharmaceutical compositions containing one or more compounds of formula (i) and their use as dual antagonists of the orexin 1 and orexin 2 receptors.. .
12/04/14
20140357642
Ip receptor agonist heterocyclic compounds
The present invention provides heterocyclic derivatives which activate the ip receptor. Activating the ip receptor signaling pathway is useful to treat many forms of pah, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients.
12/04/14
20140357641
Ip receptor agonist heterocyclic compounds
The present invention provides heterocyclic derivatives which activate the ip receptor, processes for preparing them, pharmaceutical compositions comprising said derivatives and uses thereof. Activating the ip receptor signaling pathway is useful to treat many forms of pah, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients.
12/04/14
20140357634
Substituted 4-aminocyclohexane derivatives
The invention relates to compounds that have an affinity to the μ-opioid receptor and the orl 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.. .
12/04/14
20140357615
Substituted 1h-pyrazolo[3',4',4,5]thieno[2,3-b]pyridin-3-amine analogs as positive allosteric modulators of the muscarinic acetycholine receptor m4
In one aspect, the invention relates to substituted 1h-pyrazolo[3′,4′:4,5]thieno[2,3-b]pyridin-3-amine analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor m4 (machr m4); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention..
12/04/14
20140357614
Diamino-pyridine, pyrimidine, and pyrazine modulators of the histamine h4 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.. .
12/04/14
20140357613
Aminoheteroaryl compounds and preparation method and use thereof
The present invention refers to aminoheteroaryl compounds of the following formula (i) as well as the preparation method and use thereof, wherein r1 and r3 are defined in the description in details. The aminoheteroaryl compounds of the present invention are inhibitors of hepatocyte growth factor receptor (c-met), have favorable inhibitory effect against c-met and inhibitory effect against the proliferation of cancer cells, such that they may be used as therapeutic agents for the treatment of tumors and related diseases..
12/04/14
20140357605
Bis(fluoroalkyl)-1,4-benzodiazepinone compounds
Wherein: r1 is —ch2cf3 or —ch2ch2cf3; r2 is —ch2cf3, —ch2ch2cf3, or —ch2ch2ch2cf3; r3 is h or —ch3; each ra is independently f, cl, —cn, —och3, and/or —nhch2ch2och3; and z is zero, 1, or 2. Also disclosed are methods of using such compounds to inhibit the notch receptor, and pharmaceutical compositions comprising such compounds.
12/04/14
20140357575
Melanocortin receptor-specific heptapeptides
Or a pharmaceutically acceptable salt thereof, where z, xaa1, xaa2, xaa3, xaa4, xaa5, xaa6, xaa7 and y are as defined in the specification, compositions and formulations including the peptides of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes.. .
12/04/14
20140357548
Methods for preventing or treating certain disorders by inhibiting binding of il-4 and/or il-13 to their respective receptors
The present disclosure relates to methods of treating, ameliorating or preventing a disorder comprising administering a therapeutically effective amount of a composition comprising a protein which inhibits il-4 and/or il-13 from binding to their respective receptors to a subject in need thereof. In some embodiments, the disorder is preferably associated with an increase of the th2 immune response.
12/04/14
20140356875
Evaluation of the potential risk of drug induced mood disturbance and suicide: use of a dedicated platform
The present invention relates to in vitro methods for the determination of the potential toxicity of test compounds. The invention also comprises in vitro methods for the selection of therapeutical compounds useful for the treatment of pathology related to an alteration of the mechanism of the mrna editing of adar dependent a to 1 mrna editing of the serotonin 2c receptor (5htr2c).
12/04/14
20140356380
Neutralizing antibodies and methods of use thereof
This invention provides monoclonal antibodies that recognize the toll-like receptor 4/md-2 receptor complex, and monoclonal antibodies that recognize the tlr4/md2 complex as well as tlr4 when not complexed with md-2. The invention further provides methods of using the monoclonal antibodies as therapeutics.
12/04/14
20140356372
Methods for treating allergy and enhancing allergen-specific immunotherapy by administering an il-4r inhibitor
The present invention provides methods for treating, preventing or reducing the severity of allergic reactions. The present invention also provides methods for enhancing the efficacy and/or safety of an allergen-specific immunotherapy (sit) regimen.
12/04/14
20140356364
Anti-b7-h4 antibodies and their uses
The present invention relates to antibodies (including anti-b7-h4 antibodies) and their antigen-binding fragments and to other molecules (including fusion proteins that bind to the cognate antigen/receptor, etc.) that are capable of immunospecifically binding to b7-h4 and the uses of such molecules in the diagnosis and the treatment of cancer and other diseases. The invention particularly concerns the use of such molecules to retard or prevent tumor growth, inhibit tumor-mediated suppression, eliminate tumors and/or deplete or block the activity of tumor associated macrophages (“tams”) so as to alter their activity and/or decrease tam—mediated immune suppression..
12/04/14
20140356359
Human growth hormone receptor antagonist antibodies and methods of use thereof
The present invention provides antagonizing antibodies that bind to growth hormone receptor (ghr). The invention further relates to therapeutic methods for use of these antibodies to reduce igf-1 levels and/or for the treatment and/or prevention of diseases associated with excessive igf-1, including treatment of acromegaly, gigantism, cancer, diabetic nephropathy, arthritis, and lung inflammation..
12/04/14
20140356358
Variant fc-polypeptides with enhanced binding to the neonatal fc receptor
Described herein are variant fc-fragments that contain an insertion within or adjacent to a loop that bind to the neonatal fc receptor (fcrn) with higher affinity and/or higher binding activity at ph 5-6 and approximately the same or lower affinity at a physiologic ph as compared to a control fc-fragment, that is, little or no binding activity at a physiologic ph. Also described are variant fc-polypeptides that comprise these variant fc-fragments.
12/04/14
20140356355
Il-17 receptor a antigen binding proteins
The present invention relates to il-17 receptor a (il-17ra or il-17r) antigen binding proteins, such as antibodies, polynucleotide sequences encoding said antigen binding proteins, and compositions and methods for diagnosing and treating diseases mediated by il-17 receptor a activation by one or more il-17 ligands. The present invention relates to the identification of neutralizing determinants on il-17 receptor a (il-17ra or il-17r) and antibodies that bind thereto.
12/04/14
20140356342
Human beta-adrenergic receptor kinase polypeptide and methods
Various embodiments of the invention provide human kinases and phosphatases (kpp) polypeptides and polynucleotides which identify and encode kpp. Embodiments of the invention also provide expression vectors, host cells, antibodies, agonists, and antagonists.
12/04/14
20140356318
Adoptive cell therapy with specific regulatory lymphocytes
The present invention comprises a method of treatment of an autoimmune disease involving a specific tolerance induction (“sti”) event, wherein the method includes: collecting a first sample from the patient prior to the sti event; detecting an sti event or performing a procedure that correlates in time to an sti event; collecting a second sample from the patient after the sti event; preparing lymphocytes from the first and second samples; preparing and sequencing dna or cdna from the prepared lymphocytes; identifying sequences of prevalent t or b cell receptors (“prevalent receptor sequences”) among the lymphocytes of the second sample; selecting a regulatory lymphocyte that carries at least one prevalent receptor sequence, which selected regulatory lymphocyte (i) expresses at least one prevalent receptor sequence or (ii) is generated from an autologous or allogeneic naïve lymphocyte, which naïve lymphocyte is engineered and induced to become a regulatory lymphocyte that expresses at least one prevalent receptor sequence; culturing the selected regulatory lymphocyte, thereby generating daughter cells of said regulatory lymphocyte; and administering the daughter cells to the patient.. .
12/04/14
20140356286
Polypeptides targeting vascular endothelial growth factor receptor-2 and alpha v beta 3 integrin
Polypeptides comprising variant vascular endothelial growth factor sequences are provided. The polypeptides are useful in cancer imaging, cancer diagnosis, monitoring and treatment as well as treatment of diseases characterized by excessive neovascularization..


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