|| List of recent Receptor-related patents
|Method of exploring the flexibility of macromolecular targets and its use in rational drug design|
It comprises a method of exploring the flexibility of macromolecules, where an available ensemble of structures of a receptor, such as one coming from a molecular dynamics trajectory or a set of experimentally derived structures, is used to generate an ensemble of structures for a closely related receptor, such as a receptor mutant, a receptor with a series of post-translational modifications, or one that is non-covalently bound to a second molecule. In this way, new ensembles of the pertubed receptor can be accessed without the need to explicitely simulate the new system.
|Il-1 receptor antagonist-coated electrode and uses thereof|
The present invention provides an electrode designed for implantation into the central nervous system (cns) of a mammal, wherein said electrode is substantially coated with interleukin-1 receptor antagonist (il-1ra) or a coating composition comprising it, and the il-1ra actively inhibits scarring on or around the surface of the electrode when implanted into the cns. The electrode of the invention may be used for brain recording and/or stimulation, and can thus be used for treatment of a brain dysfunction, a brain disease or disorder, or a brain injury, as well as for brain computer interface, brain machine interface, or electrotherapy..
|Novel indole derivatives as selective androgen receptor modulators (sarms)|
The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.. .
|7-azoniabicyclo[2.2.1]heptane derivatives, methods of production, and pharmaceutical uses thereof|
Muscarinic acetylcholine receptor antagonists and methods of using them for the treatment of muscarinic acetylcholine receptor-mediated diseases, such as pulmonary diseases, are provided. .
|Compounds act at multiple prostaglandin receptors giving a general anti-inflammatory response|
Con(r7)so2r7 wherein r1, r2, r3, r4, and r7 are as defined in the specification. The compounds may be administered to treat dp1, fp, ep1, ep3, tp and/or ep4 receptor mediated diseases or conditions..
|5-[5-[2-(3,5-bis(trifluoromethyl)phenyl)-2-methylpropanomethylpropanoylmethylamino]-4-(4-fluoro-2-methylphenyl)]-2-pyridinyl-2-alkyl-prolinamide as nk1 receptor antagonists|
Useful in the treatment of diseases and conditions for which antagonism of nk1 receptor is beneficial.. .
|Methods of treating patients suffering from movement disorders|
The present invention is directed to methods of treating movement disorders by administering an effective amount of one or more adenosine a2a receptor antagonists to a patient in need thereof. The present invention also provides methods of decreasing the adverse effects of l-dopa in patients receiving l-dopa therapy in the treatment of parkinson's disease.
|Treatment for gastroparesis using sepiapterin|
The present invention discloses that diabetic rats showed a reduction in nitrergic relaxation of the gastric, impaired nnos dimerization, decreased bh4 and gtpch1 levels and thus, are more susceptible to develop diabetic gastroparesis. The use of tetrahydrobiopterin and its derivatives and sex steroid hormones as disclosed herein provides a novel strategy for therapeutic intervention of diabetic gastroparesis and any other gut-related diseases.
|1,4-diazabicyclo[3.2.2]nonanes as neuronal nicotinic acetylcholine receptor ligands|
The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including inflammatory diseases and diseases associated with dysfunction of the central nervous system (cns).. .
|Pim kinase inhibitors and methods of their use|
New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase.
|Neuroactive 13, 17-substituted steroids as modulators for gaba type-a receptors|
The present disclosure is generally directed to neuroactive 13,17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to gaba function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds..
|Combination of compounds for treating or preventing skin diseases|
A combination of compounds for treating skin diseases and particularly rosacea and ocular rosacea is described. The combination of a compound of the avermectin family or of the mylbemycin family with a compound of the family of the alpha-1 or alpha-2 adrenergic receptor agonists is also described.
|Delta-opioid receptor selective analgesics|
Methods and materials are provided for the production of glycosylated peptides that exhibit high affinity and specificity for delta opioid receptors. The methods and materials of the present invention may be used for treatment of conditions involving pain, such as acute pain and nociceptic pain, neuralgia and myalgia..
|Peptides and pharmaceutical compositions for use in the treatment by nasal administration of patients suffering from anxiety and sleep disorders|
The present invention provides peptides for use in a medicament which is administered nasally, wherein the peptide is an agonist of neuropeptide s receptor (npsr), of the receptor tgr23 and/or of vasopressin receptor-related receptor 1 (vrr1) or for use in the treatment of a patient by causing, promoting or increasing relieve or healing of phobic anxiety, avoidance anxiety, dissociative anxiety such as flashbacks, depersonalization, derealization, intrusions, vegetative symptoms related to anxiety symptoms, especially in panic attacks, in posttraumatic stress disorder, in generalised anxiety disorder and in anxiety accompanying depressive, or psychotic episodes, arousal, awakening, alertness, activity, spontaneous movement, an anxiolytic effect or a combination thereof in the patient, wherein the peptide is administered nasally or for use in the prophylaxis and/or treatment of an anxiety or sleep disorder, especially in any type of hypersomnia like idiopathic hypersomnia, wherein the peptide is administered nasally. Further provided are pharmaceutical compositions for nasal administration comprising at least one of said peptides, uses of said peptide or said pharmaceutical composition.
|Methods of treating neuropathic pain|
The disclosure relates, at least in part, to methods of treating neuropathic pain in a patient in need thereof by administering an effective amount of a disclosed compound, e.g. A peptide nmda receptor partial agonist..
|Method for the early diagnosis of clinically latent placental insufficiency associated with defective placental maturation|
The present invention relates to a method for the early diagnosis of a clinically latent placental insufficiency in pathological placental maturation, and the prophylaxis of an intrauterine fetal hypoxia/asphyxia at the due date or after a prolonged gestation, comprising determining the amount and/or the concentration of the biomarker prokineticin 1 (eg-vegf) and/or its receptor pkr1 and/or pkr2 in a sample from the pregnant subject and/or the pregnancy. In a preferred embodiment, the invention is based on determining the ratio of the amount and/or the concentration of bfgf/pk1 as a measure of current functional condition and an indicator of latent clinical problems such as placental dysfunction resulting in fetal hypoxia..
|Cell-based methods for coupling protein interactions and binding molecule selection and diversification|
The invention relates to cell-based methods for diversifying, expressing and selecting binding molecules, e.g., antibodies, and target molecules to which they bind, all of which are expressed in the same cell. The target molecule can be a member of a ligand binding pair comprising a cell-surface expressed ligand binding receptor molecule and its cognate ligand, which interact within the cell.
|Biochemical detection unit and biochemical device having the same|
A biochemical detection unit for detecting a sample and a biochemical device having the biochemical detection unit and a releasing unit are provided. The biochemical detection unit includes a photoconductor plate, a receptor, and a resistance sensing component.
|Zcytor19 polynucleotides, polypeptides, antibodies and methods of use|
Novel polypeptides, polynucleotides encoding the polypeptides, and related compositions and methods are disclosed for zcytor19, a novel class ii cytokine receptor. The polypeptides may be used within methods for detecting ligands that stimulate the proliferation and/or development of hematopoietic, lymphoid and myeloid cells in vitro and in vivo.
|Cloned glucagon-like peptide-2 receptors|
The invention relates to nucleotides and amino acid sequences encoding glucagon-like peptide-2 receptors, recombinant host cells transformed with such nucleotides, and methods of using the same in drug screening and related applications.. .
|Assays for identifying compounds that modulate bitter taste|
The present invention is based on applicants' discovery, disclosed herein, of agonists for the tas2r receptors tas2r1, tas2r4, tas2r9, tas2r13, tas2r14, tas2r16, tas2r44, tas2r46, and tas2r60. The assignment of agonists to these receptors makes assays for identifying compounds that modulate bitter taste possible.
|Isoforms of the human sst5 receptor originated by alternative splicing and oligonucleotide pairs to detect them by pcr|
The present invention is referred to two human nucleic 5 acids that comprise sequences encoding two new isoforms of the human somatostatin receptor type 5 originated by alternative splicing, named sst5b and sst5c, with possible involvement in tumor processes. In addition, the invention is referred to oligonucleotide pairs allowing 10 their differential detection in several tissues using the pcr technique..
|Method for detecting hiv-1 co-receptor tropism|
A method for determining hiv-1 co-receptor tropism in an hiv-infected patient includes preparing an hiv-1 envelope protein coding sequence from a sample, introducing the hiv-1 envelope protein coding sequence into a first expression construct using yeast homologous recombination, and using the first expression construct in a cell to cell fusion assay to determine hiv-1 co-receptor tropism.. .
|Divalent-metal coated nanoparticles for delivery of compositions into the central nervous system by nasal insufflation|
The compositions and methods of the disclosure particularly target the divalent metal transporter expressed on olfactory nerve terminals to transport divalent cation-coated or cation-containing nanoparticles to all regions of brain. It has been found that such divalent cation-containing nanoparticles, including those nanoparticles comprising manganese have affinity for the metal transport receptor proteins.
|Methods and compositions for enhancing an immune response, blocking monocyte migration, amplifying vaccine immunity and inhibiting tumor growth and metastasis|
Provided are methods of enhancing an immune response and methods for reducing the recruitment of monocytes to a lymph node by administering to an individual an angiotensin ii receptor blocker or a compound of formula (i) in conjunction with an antigen. The invention also provides relate methods for amplifying vaccine immunity by administering to an individual an angiotensin ii receptor blocker or a compound of formula (i) in conjunction with an vaccine.
|Recombinant proteins and their therapeutic uses|
A recombinant protein expressing one or more human growth factors, tumor antigens, and/or receptors or epitopes thereof on or within an immunogenic expression creating a recombinant protein in which one or more epitopes are presented on the surface of the sequence in their natural configuration. The growth factor, tumor antigen, and/or receptor, sequence(s) may be expressed within the encoding sequence at appropriate internal positions or at the termini as single expressions or as two or more tandem repeats..
|Modulation of cellular migration|
Methods, kits, and compositions are provided for addressing cancer through the interaction of bradykinin (bk) and the bradykinin-2-receptor (b2r). This interaction controls cellular invasion, as has been unexpectedly observed in glioma cells, a composition is provided for the treatment of cancer by disrupting this interaction using an inhibitor or bk or b2r that can.
|Fc receptor binding proteins|
This disclosure provides, inter alia, proteins that bind to fcrn, e.g., immunoglobulins that inhibit fcrn with high affinity and selectivity. The fcrn-binding proteins can be used to treat a variety of disorders including autoimmune disorders..
|Medicinal agent for preventing exacerbation of malignant tumor, comprising combination of natriuretic peptide receptor gc-a and gc-b agonists|
Provided are a medicinal agent which is highly safe for use as the treatment of a malignant tumor and is capable of efficiently treating a malignant tumor, that is, a medicinal agent for treating a malignant tumor or for suppressing or preventing the exacerbation thereof, comprising at least one kind of natriuretic peptide receptor gc-a agonist and at least one kind of natriuretic peptide receptor gc-b agonist to be administered in combination; a therapeutic method comprising administering the agent; etc.. .
|Therapeutic antibodies binding il 12rbeta1|
The present invention relates to antibodies that specifically bind to il12rβ1, the non-signal transducing chain of the heterodimeric il12 receptor (together with il12rβ2 chain) as well as il23 receptor (together with il23rα chain). The invention more specifically relates to specific antibodies that are il12 and il23 receptor antagonists capable of inhibiting il12/il18 induced ifny production of t cells and compositions and methods of use for said antibodies to treat pathological disorders that can be treated by inhibiting ifny production, such as rheumatoid arthritis, psoriasis or inflammatory bowel diseases or other autoimmune and inflammatory disorders..
|Use of toll-like receptor agonist for treating cancer|
The present invention is directed to methods and agents used for treating cancer in toll-like receptor 5-expressing tissues by providing a toll-like receptor agonist such as flagellin. The present invention also relates to protecting the liver from a liver toxicity using a toll-like receptor agonist..
|Human progenitor t-cells|
Human progenitor t cells that are able to successfully engraft a murine thymus and differentiate into mature human t and nk cells are described. The human progenitor t cells have the phenotype cd34+cd7+cd1a−cd5− or cd34+cd7+cd1a−cd5+ and are derived from human hematopoietic stem cells, embryonic stem cells and induced pluripotent stem cells by coculture with cells expressing a notch receptor ligand (op9-dl1 or op9-dl4).
|Mesenchymal stem cells expressing tnf-alpha receptors|
Mesenchymal stem cells which express tnf-α receptor type i in an amount of at least 13 pg/106 cells. Such mesenchymal stem cells inhibit the proliferation of lymphocytes and may be employed, in particular, in the treatment of graft-versus-host disease..
|Humanized t cell co-receptor mice|
The invention provides genetically modified non-human animals that express chimeric human/non-human t cell co-receptor polypeptides (e.g., cd4, cd8α, cd8β), as well as embryos, cells, and tissues comprising the same. Also provided are constructs for making said genetically modified animals and methods of making the same..
|Method and apparatus for determining circadian input|
A method and apparatus for determining the circadian input of a light source includes selecting a circadian input to be measured based on an action spectrum corresponding to a wavelength sensitivity of photoreceptors for a circadian regulation system, where the circadian input is configured to stimulate a retinaldehyde photopigment, and for measuring spectral intensity across the action spectrum to determine the circadian input of the light source.. .
|Imidazolothiazole compounds for the treatment of disease|
Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.. .
|Antibodies comprising chimeric constant domains|
Antibodies, antigen-binding proteins and fc-fusion proteins that comprise recombinant polypeptides containing a chimeric heavy chain constant region sequence are provided that bind to certain fc receptors however have reduced effector functions. Methods of making constructs for expression of such chimeric fc-containing antibodies, antigen-binding proteins and fc-fusion proteins in cell systems, and methods of producing and isolating the chimeric fc-containing proteins are provided..
|Cyclic amine derivatives as ep4 receptor agonists|
The present invention therefore relates to novel cyclic amine derivative compounds, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of prostaglandin e mediated diseases such as pain, glaucoma, ulcerative colitis and osteoporosis.. .
|Piperidinyl alkyne orexin receptor antagonists|
The present invention is directed to piperidinyl alkyne compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the piperidinyl alkyne compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved.
|Compounds modulating c-fms and/or c-kit activity and uses therefor|
Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof..
|Methods and compositions for treating anxiety disorders or symptoms thereof|
The present invention relates to methods and compositions for reducing distress dysfunction, including emotional and physical distress. The invention entails co-administration of at least one receptor switcher and at least one endorphin enhancer.
|Sulfonamide compounds and their use in the modulation retinoid-related orphan receptor|
Wherein r1 to r7 are as defined in claim 35.. .
|Method of preventing and treating hepatic disease using a2b adenosine receptor antagonists|
The invention is related to methods of preventing and treating hepatic fibrosis using a2b adenosine receptor antagonists and utility in the treatment and prevention of liver damage caused by alcohol abuse, surgical intervention, viral hepatitis, the ingestion of hepatotoxic drugs, or other hepatic diseases. The invention also relates to pharmaceutical compositions for use in the method..
|Use of serotonin receptor agonists for treatment of movement disorders|
The present invention relates to the combined use of compounds which are activators of the kcnq family potassium ion channels and compounds which are serotonin 5-ht1 receptor agonists. The combined use of kcnq channel activators and 5-ht1 receptor agonists is useful in the treatment of for example movement disorders.
|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.
|Synthesis of functionalized octahydro-isoquinolin-1-one-8-carboxylic esters and analogs, and therapeutic methods|
A functionalized polycyclic compound can have a structure of formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined diels-alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor.
|Pyrrolopyrimidine compounds for the treatment of cancer|
The ectopic expression of mer receptor tyrosine kinase (mer) has been identified as a tumor cell survival gene product in acute lymphoblastic leukemia (all) cells and a potential cause of all chemoresistance. Hence, we investigated whether the development of small molecule mer inhibitors was possible.
|Novel octahydrothienoquinoline derivative, pharmaceutical composition comprising derivative, and use of these|
The present invention provides compounds represented by the general formula (i): or pharmaceutical acceptable salts thereof, wherein r1 is cyano or the like; r2 and r3 are hydrogen or the like; r4 is c1-6 alkyl or the like; r5 is c1-6 alkyl, halo-c1-6 alkyl, cycloalkyl, cycloalkyl-c1-6 alkyl, aralkyl or the like; r6 and r7 are each hydrogen, c1-6 alkyl, halo-c1-6 alkyl, cycloalkyl, c1-6 alkoxy-c1-6 alkyl, r12r13n—c1-6 alkyl or the like, which exhibit potent dopamine d2 receptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof..
|Pyrazole azetidine derivatives as sphingosine 1-phosphate (s1p) receptor modulators|
The present invention relates to pyrazole azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.. .
|Pyrazole derivatives as sphingosine 1-phosphate (s1p) receptor modulators|
The present invention relates to pyrazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.. .
|Composition for diagnosing ovarian cancer metastasis using cpg methylation status of gene promoter and use thereof|
The present invention relates to a composition, a kit and a method for diagnosing ovarian cancer metastasis or predicting the risk of metastasis by detecting methylation levels at cpg sites of one or more gene promoters selected from the group consisting of agr2 (anterior gradient 2), ca9 (carbonic adj anhydrase 9), gabrp (gamma-aminobutyric acid receptor pi subunit), ifitm1 (interferon-induced transmembrane 1) and muc13 (mucin 13).. .
|Chimeric antigen receptor|
Provided are a chimeric antigen receptor comprising an extracellular domain capable of binding to an antigen, a transmembrane domain and at least one intracellular domain, the chimeric antigen receptor being characterized in that an intracellular domain of a glucocorticoid-induced tumor necrosis factor receptor (gitr) is contained as the intracellular domain; a nucleic acid encoding the chimeric antigen receptor; a cell expressing the chimeric antigen receptor; and a method for producing the cell.. .
|Method for predicting response or prognosis of lung adenocarcinoma with egfr-activating mutations|
The invention provides a method for predicting the response of an egfr-activating mutant subject suffering from a lung adenocarcinoma and receiving treatment with epidermal growth factor receptor tyrosine kinase inhibitor (egfr-tki) and a method for predicting prognosis in an egfr-activating mutant subject suffering from a lung adenocarcinoma and receiving treatment with egfr-tki. In the methods of the invention, clustered genomic alterations in specific chromosomes (in particular chromosomes 5p, 7p, 8q or 14q) are determined as a tool for predicting the response or prognosis..
|Electrophotographic photoreceptor and image forming apparatus including the same|
An electrophotographic photoreceptor includes a cylindrical base and a photosensitive layer disposed on the cylindrical base. The photosensitive layer has a photoconductive layer disposed on the cylindrical base, a charge injection blocking layer disposed on the photoconductive layer, and a surface layer disposed on the charge injection blocking layer.
|Anti-aging composition for vitalization of retinoic acid receptor that contains mixed extract of chinese matrimony vine and pine needles as effective component|
The present invention relates to an anti-aging composition that contains a mixed extract of chinese matrimony vine and pine needles as an effective component. More specifically, the present invention relates to a composition for an external application to the skin, wherein a mixed extract of chinese matrimony vine and pine needles, which are the natural ingredients, is contained such that excellent anti-aging or wrinkle improvement effects to the skin can be obtained through the vitalization of a retinoic acid derivative..
|Compositions for inhibition of insect sensing|
In one aspect, the invention relates to chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in airborne insects such as mosquitos.
The present invention provides an immunogenic composition comprising one or more antigens and a toll-like receptor (tlr) 7 agonist in an orally (e.g. Sublingually) administered composition..
|Modulation of the vps10p-domain receptor family for the treatment of mental and behavioural disorders|
The present invention relates to methods for modulating the activity of one or more vps10p-domain receptors selected from the group consisting of sortilin, sorla, sorcs1, sorcs2 and sorcs3, in an animal and methods for preparation of a medicament for the treatment of mental and behavioral disorders. The modulation is carried out by inhibiting or promoting the binding of ligands to the vps10p-domain receptor.
|Cartilage/bone destruction suppressor|
An object of the present invention is to provide a cartilage/bone destruction suppressor which can suppress the destruction of cartilage or bone seen in rheumatoid arthritis, osteoarthritis, bone metastasis of malignant tumor, or the like. The present invention relates to a cartilage or bone destruction suppressor comprising an antibody against folate receptor β or a complex of the antibody and a biologically or chemically active substance..
|Frizzled 2 as a target for therapeutic antibodies in the treatment of cancer|
Disclosed herein are methods of treating cancer in a subject, and methods for inhibiting growth, migration and/or invasion of a cancer cell in the subject, comprising administering to the subject a therapeutically effective amount of an antibody or antigen binding fragment thereof that downmodulates fzd2. The antibody may specifically bind fzd2, and may promote internalization of the fzd2 receptor by the cancer cells and/or prevent ligand binding to fzd2.
|Krt19 stabilizing her2 and use thereof|
Provided is a method of decreasing the stability of her2 (human epidermal growth factor receptor 2) in a cell or individual comprising administering an effective amount of an expression or activity inhibitor of krt19 (cytokeratin 19) to the cell or individual.. .
|Methods and compositions for delivering interleukin-1 receptor antagonist|
Methods and compositions generating and using an interleukin-1 receptor antagonist (il-1ra)-rich solution. Methods for generating and isolating interleukin-1 receptor antagonist include incubating adipose tissue and/or adipocytes with polyacrylamide beads to produce interleukin-1 receptor antagonist.
|Multimeric il-15 soluble fusion molecules and methods of making and using same|
The present invention features compositions and methods featuring alt-803, a complex of an interleukin-15 (il-15) superagonist mutant and a dimeric il-15 receptor α/fc fusion protein useful for enhancing an immune response against a neoplasia (e.g., multiple myeloma, melanoma, lymphoma) or a viral infection (e.g., human immunodeficiency virus).. .