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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

Gpcr fusion protein containing an n-terminal autonomously folding stable domain, and crystals of the same

Gpcr fusion protein containing an n-terminal autonomously folding stable domain, and crystals of the same

Date/App# patent app List of recent Receptor-related patents
 Sulfonylpyrazole and sulfonylpyrazoline carboxamidine derivatives as 5-ht6 antagonists patent thumbnailSulfonylpyrazole and sulfonylpyrazoline carboxamidine derivatives as 5-ht6 antagonists
And derivatives thereof, which are antagonists of 5-ht6 receptors, wherein the symbols have the meanings given in the description. The invention also concerns methods for the preparation of these compounds, to novel intermediates useful for their synthesis, and to uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in treating at least on disease or condition chosen from parkinson's disease, huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, irritable bowel syndrome, obesity and type-2 diabetes..
 Gpcr fusion protein containing an n-terminal autonomously folding stable domain, and crystals of the same patent thumbnailGpcr fusion protein containing an n-terminal autonomously folding stable domain, and crystals of the same
Certain embodiments provide a gpcr fusion protein. In particular embodiments, the gpcr fusion protein comprises: a) a g-protein coupled receptor (gpcr); and b) an autonomously folding stable domain, where the autonomously folding stable domain is n-terminal to the gpcr and is heterologous to the gpcr.
 Use of edg receptor binding agents in cancer patent thumbnailUse of edg receptor binding agents in cancer
Provided is a method for treating solid tumors, e.g tumor invasiveness, and particularly inhibiting or controlling deregulated angiogenesis, using a sphingosine-1-phosphate receptor agonist, optionally in combination with a chemotherapeutic agent. The invention also comprises a combination of a sphingosine-1-phosphate receptor agonist with a chemotherapeutic agent..
 Dual-acting imidazole antihypertensive agents patent thumbnailDual-acting imidazole antihypertensive agents
Wherein: ar, r, r2-3, x, and r5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have at1 receptor antagonist activity and neprilysin inhibition activity.
 Dosing regimen for a selective s1p1 receptor agonist patent thumbnailDosing regimen for a selective s1p1 receptor agonist
The present invention relates to a dosing regimen for a selective s1p1 receptor agonist, whereby the selective s1p1 receptor agonist is administered to a subject in such a way that during the initial treatment phase the selective s1p1 receptor agonist is administered at a dose which induces desensitization of the heart wherein said dose is below the target dose, and at a dosing frequency that sustains desensitization of the heart, until no further acute heart rate reduction occurs, followed by dose up-titration to the target dose of the selective s1p1 receptor agonist.. .
 Inhibitors of rgs proteins patent thumbnailInhibitors of rgs proteins
G-protein coupled receptors are a diverse group that are the target of over 50% of marketed drugs. Activation of these receptors results in the exchange of bound gdp for gtp in the gα subunit of the heterotrimeric g-protein.
 Compounds and pharmaceutical compositions for treating disorders associated with the 5-ht1a and 5-ht2a receptors patent thumbnailCompounds and pharmaceutical compositions for treating disorders associated with the 5-ht1a and 5-ht2a receptors
This invention is related to the alkyl-piperazine-phenyl 4 (3h)-quinazolinones general formula (i) compounds, pharmacologicaly active and able to act on the 5-ht1a and 5-ht2a serotonin receptors in a manner that promotes the control, relief or cure of disorders associated with these receptors, and pharmaceutical compositions containing the compounds for the treatment of disorders associated with these receptors. These compounds and their pharmaceutical compositions are useful in the treatment of conditions such as depression, anxiety, phobias, addictions, aggressiveness, impulsiveness, panic, psychotic, eating and sleep disorders, obsessive-compulsive disorder and female sexual dysfunctions, among other disorders associated with these receptors..
 Acylaminocycloalkyl compounds suitable for treating disorders that respond to modulation of dopamine d3 receptor patent thumbnailAcylaminocycloalkyl compounds suitable for treating disorders that respond to modulation of dopamine d3 receptor
R5 is inter alia c1-c6 alkyl, fluorinated c1-c3 alkyl, c1-c2-alkoxy-c1-c4-alkyl, fluorinated c1-c2-alkoxy-c1-c4-alkyl, hydroxy-c1-c4-alkyl, fluorinated hydroxy-c1-c4-alkyl, oxetanyl, fluorinated oxetanyl, oxolanyl, fluorinated oxolanyl, c3-c5 cycloalkyl, fluorinated c3-c5 cycloalkyl, etc.. .
 2,4-pyridinediamine compounds and their uses patent thumbnail2,4-pyridinediamine compounds and their uses
The present invention provides 2,4-pyrimidinediamine compounds that inhibit the ige and/or igg receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the ige and/or igg receptor signaling cascades.. .
 Compounds and methods of treating hypertension patent thumbnailCompounds and methods of treating hypertension
Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor α2b antagonists.
Novel quinuclidine derivatives and medicinal compositions containing the same
A compound according to formula (i) wherein z© is a phenyl ring, a c4 to c9 heteroaromatic compound containing one or more heteroatoms, or a naphthalenyl, 5,6,7,8-tetrahydronaphthalenyl or biphenyl group; r1, r2 and r3 each independently represent a hydrogen or halogen atom, or a hydroxy group, or a phenyl, —or4, —sr4, —nr4r5, —nhcor4, —conr4r5, —cn, —no2, —coor4 or —cf3 group, or a straight or branched lower alkyl group which may optionally be substituted, for example, with a hydroxy or alcoxy group, wherein r4 and r5 each independently represent a hydrogen atom, straight or branched lower alkyl group, or together form an alicyclic ring; or r1 and r2 together form an aromatic, alicyclic or heterocyclic ring; n is an integer from 0 to 4; a represents a —ch2—, —ch═cr6, —cr6═ch—, —cr6r7—, —co—, —o—, —s—, —s(o)—, so2 or nr6— group, wherein r6 and r7 each independently represent a hydrogen atom, straight or branched lower alkyl group, or r6 and r7 together form an alicyclic ring; in is an integer from 0 to 8; provided that when m=0, a is not —ch2—; p is an integer from 1 to 2 and the substitution in the azoniabicyclic ring may be in the 2, 3 or 4 position including all possible configurations of the asymmetric carbons; b represents a group of formula (i) or (ii), wherein r10 represents a hydrogen atom, a hydroxy or methyl group; and r8 and r9 each independently represents formulae (a), (b), (c), (d) and wherein r11 represents a hydrogen or halogen atom, or a straight or branched lower alkyl group and q represents a single bond, —ch2—, —ch2—ch2, —o—, —o—ch2—, —s—, —s—ch2— or —ch═ch—, and when (i) or (ii) contain a chiral centre they may represent either configuration; x represents a pharmaceutically acceptable anion of a mono or polyvalent acid, which shows high affinity for muscarinic m3 receptors (hm3).. .
Novel peptidomimetics and their application
Novel peptidomimetics exhibiting affinity for opioid receptors, possessing general formula show on fig. 1, for gastrointestinal or peripheral administration in the form of a pill, infusion, injection or implant in the treatment of peripheral opioids side effects, particularly constipation or/and respiratory depression..
Tsp-1, tsp-2, il-17br and hb-egf associated with stem cell activity and use thereof
Thrombospondin 1 (tsp-1), tsp-2, interleukin 17b receptor (il-17br) and heparin-binding epidermal growth factor-like growth factor (hb-egf) associated with stem cell activity and use thereof.. .
Hemoglobin-based oxygen carrier-containing pharmaceutical composition for cancer targeting treatment and prevention of cancer recurrence
The present invention provides a pharmaceutical composition containing a hemoglobin-based oxygen carrier for treating cancer, preventing recurrence and metastasis of cancerous tumor. The composition can be used alone or in combination with at least one chemotherapeutic agent such as 5fu, bortezomib, doxorubicin, cisplatin, or any combination thereof.
Glp-1 derivatives
The invention relates to a derivative of a glp-1 peptide, which peptide has two lys residues, namely a first and a second lys residue, and a maximum of eight amino acid changes as compared to glp-1(7-37) (seq id no: 3), which derivative comprises two protracting moieties attached to the epsilon amino group of said first and second lys residue, respectively, via a linker, wherein the protracting moiety is selected from chem. 15: hooc—(ch2)x-co—*, and chem.
Selective gpcr ligands
In the past decade a great deal of structural information for class a-gpcrs (g protein-coupled receptors) has emerged. However, the structural and electronic basis of ligand selectivity for closely related receptor subtypes such as the angiotensin receptors at1ar and at2r, which present completely diverse biological functions in response to the same ligand, is poorly understood.
Reversible reaction sensors and assemblies
A reversible reaction sensor provides for detecting medical, biologic or explosive airborne compounds. The sensor may be formed in semiconductor material and is activated by radiation from sources to provide sensing of particular airborne compounds optically detectable by detectors, and reversed by other radiation from a source (or removal of activating radiation) to take away such airborne compounds from the sensor.
Compounds for modulating integrin cd11b/cd18
The application describes an assay for the identification of small molecule modulators of integrin cd11b/cd18 and small molecules capable of modulating activity of this receptor. Such compounds may be used in certain embodiments for treating a disease or condition selected from inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, bullous pemphigoid, neonatal obstructive nephropathy, and cardiovascular disease, or in other embodiments for the treatment of a disease or condition selected from immune deficiency, acquired immune deficiency syndrome (aids), myeloperoxidase deficiency, wiskott-aldrich syndrome, chronic granulomatous disease, hyper-igm syndromes, leukocyte adhesion deficiency, chediak-higashi syndrome, and severe combined immunodeficiency..
Modified effector cell (or chimeric receptor) for treating disialoganglioside gd2-expressing neoplasia
A modified effector cell includes a non-reversibly produced vector-encoded anti-gd2-bb-ζ chimeric receptor for use in disialoganglioside gd2-expressing neoplasia, which is inserted in the cell, to obtain an effector cell that stably produces the anti-gd2-bb-ζ chimeric receptor, the chimeric receptor having two distinct mutually fused portions, i.e. An intra-cytoplasmic portion and an extra-cytoplasmic portion..
Diagnosis of pulmonary and/or cardiovascular disease
Described are methods and kits for determining the likelihood of the presence of cardiovascular disease (cvd) or pulmonary disease (pd) in a subject using st2/interleukin 1 receptor like 1 (il1rl1) and/or interleukin 33 (il-33), and a biomarker for cvd, e.g., a natriuretic peptide, e.g., brain natriuretic peptide (bnp), prohormone bnp (probnp), n-terminal probnp (nt-probnp), atrial natriuretic peptide (anp), proanp, or nt-proanp.. .
Identification of bitter ligands that specifically activate human t2r receptors and related assays for identifying human bitter taste modulators
The present invention relates to the discovery that specific human taste receptors in the t2r taste receptor family respond to particular bitter compounds. Also, the invention relates to the discovery of specific ht2r9 alleles and their disparate activity in functional assays with the same biter ligands.
Electro-photographic photoreceptor and image forming apparatus including the same
Provided is a photoreceptor having an appropriate surface frictional force that enables a cleaning angle, at which the slipping between the surface of the photoreceptor surface and the blade is prevented and the overturning and vibrating of the blade are prevented, to be easily obtained.. .
Cysteine peptide-containing health drink
An object is to provide a health drink which gives a real feeling of a preventive effect and ameliorative effect against skin aging and stress, and it is confirmed that when a drink in which glutathione is added to a conventional drink containing chondroitin, hyaluronic acid, and vitamins is taken, a concentration of blood dhea-s, which is considered to be an indicator of rejuvenation, is significantly elevated, promoting gene expressions of olfactory receptors and the like, and remarkably ameliorating skin condition, total mood disturbance, autonomic nerve balance, and overall health condition.. .
Methods for treating cardiovascular disorders
There is provided a once-a-day therapeutically synergistic pharmaceutical dosage form for treatment of cardiovascular disorders, wherein the dosage form comprises a fixed dose combination of metoprolol in extended release form and one or more calcium channel blocker, angiotensin ii receptor blocker or angiotensin converting enzyme inhibitor along with one or more rate controlling excipient.. .
Cannabinoid receptor binding agents, compositions and methods
A composition comprising a cannabinoid receptor binding agent contained in a particle for the treatment of skin conditions. The particle may be a nanoparticle, such as nanocrystalline cellulose.
Use of toll-like receptor ligands as adjuvants to vaccination therapy for brain tumors
Compositions comprising dendritic cells pulsed with tumor lysate and at least one toll-like receptor (tlr) ligand which may be used for eliciting a specific immune response in a mammal in need thereof for treating diseases including a tumor are disclosed. Also disclose are methods of activating dendritic cells, comprising providing at least one toll-like receptor (tlr) ligand; and pulsing a dendritic cell with the at least one tlr ligand.
Pharmaceutical composition comprising cannabinoids having reduced psychoactivity through the combination of cbd and non-decarboxylated thc
The present invention relates to a pharmaceutical composition comprising non-decarboxylated Δ9 tetrahydrocannabinol (thc), cannabidiol (cbd), and at least one small molecule selected from citric acid, ascorbic acid, citrus essential oil(s), lecithin, one or more sugar(s), resvertrol, and combinations thereof, wherein the composition exhibits an increased but negated psychoactivity with concurrent enhancement in therapeutic potency of thc and/or cbd. The present invention is further directed to methods of treating one or more disease(s) or disorder(s) modulated by the activation of the cannabinoid cb1 and/or cb2 receptors, by administering a therapeutically effective amount of the composition of the present invention to a subject in need thereof..
Modulators of c3a receptors
Heterocyclic compounds that modulate c3a receptors and their use in the treatment or prevention of inflammatory diseases, infectious diseases, cancers, metabolic disorders, obesity, type 2 diabetes, metabolic syndrome and associated cardiovascular diseases are described. The use of the compounds in stimulating or suppressing an immune response is also described together with pharmaceutical compositions comprising the compounds or their pharmaceutically acceptable salts..
Soluble urokinase receptor (supar) in diabetic kidney disease
Methods and compositions are provided for diagnosing and treating a diabetic kidney disease (dkd) in an individual. In aspects of the methods, the levels of soluble circulating urokinase receptor (supar) in the blood are measured to predict a dkd, diagnose a dkd, or provide a prognosis pertaining to a dkd.
Compositions for the treatment of rheumatoid arthritis and methods of using same
The present invention provides compositions and methods of treating and improving the symptoms of rheumatoid arthritis using an antibody or antigen-binding fragment thereof that specifically binds human interleukin-6 receptor (hil-6r) with a dmard.. .
Combination therapy to enhance nk cell mediated cytotoxicity
The function of natural killer (nk) cells is regulated by inhibitory and activating signals delivered by cell surface receptors, 1-7f9 is a fully human monoclonal antibody (mab) directed against kir2dl1 and k1r2dl2/3 receptors that blocks its interaction with its hla-c ligands breaking nk cell tolerance to autologous tumor ceils. Lεnalidomide has been shown to increase nk cell cytotoxicity in vitro.
Broadly neutralizing human antibody that recognizes the receptor-binding pocket of influenza hemagglutinin
The invention features a novel influenza antibody that specifically binds to influenza hemagglutinin and reduces or inhibits hemagglutinin binding to sialic acid. The invention also provides methods, compositions, and kits featuring the novel antibody and its use in preventing or treating influenza infection..
Anti-c-met tandem fc bispecific antibodies
Provided herein are tandem fcs and tandem fc antibodies (“tfcas”), e.g., tandem fc bispecific antibodies (“tfcbas”), which comprise one or at least two binding sites that specifically bind to one or more cell surface receptors. The binding sites are connected through a tfc, which tfc comprises a first fc region and a second fc region, wherein the first and the second fc regions are linked through a tfc linker to form a contiguous polypeptide and dimerize to form an fc dimer.
Suppression of neuroendocrine diseases
The present invention relates to a method for suppressing neuroendocrine disease. The therapy employs use of a non-cytotoxic protease, which is targeted to a neuroendocrine tumour cell, preferably via a somatostatin or cortistatin receptor, a ghrh receptor, a ghrelin receptor, a bombesin receptor, a urotensin receptor a melanin-concentrating hormone receptor 1; a kiss-1 receptor or a prolactin-releasing peptide receptor.
Methods for coupling targeting peptides onto recombinant lysosomal enzymes for improved treatments of lysosomal storage diseases
Described herein are methods of making targeting peptides conjugated to recombinant lysosomal enzymes by modifying the amino (n)-terminus and one or more lysine residues on recombinant human lysosomal enzymes using a first crosslinking agent to give rise to first crosslinking agent modified recombinant human lysosomal enzymes, modifying the first amino acid within a short linker at the amino (n)-terminus on a variant igf-2 peptide using a second crosslinking agent to give rise to a second crosslinking agent modified variant igf-2 peptide, and then conjugating the first crosslinking agent modified recombinant human lysosomal enzyme to the second crosslinking agent modified variant igf-2 peptide containing a short linker. Also described herein are conjugates synthesized characterized as having higher affinities for the igf2/ci-mpr receptor and cellular uptake using the methods disclosed herein.
Fully human, anti-mesothelin specific chimeric immune receptor for redirected mesothelin-expressing cell targeting
The present invention relates to compositions and methods for treating diseases, disorders or conditions associated with dysregulated expression of mesothelin. In one embodiment, the invention relates to a fully human chimeric antigen receptor (car) wherein the car is able to target mesothelin..
Targeted disruption of t cell receptor genes using engineered zinc finger protein nucleases
Disclosed herein are methods and compositions for modifying tcr genes, using nucleases (zinc finger nucleases or tal nucleases) to modify tcr genes.. .
Low molecular weight thyroid stimulating hormone receptor (tshr) agonists
Disclosed are oxo-hydroquinazolines that are useful as selective tshr agonists. The compounds may be used for detecting or treating thyroid cancer, or treating a bone degenerative disorder..
Induction of thyroid iodide-handling gene expression in human cancers
Dual suppression of the map kinase and pi3k/akt pathways showed synergistic or greatly enhanced anti-melanoma cell effects, compared to suppression of a single pathway, including the inhibition of cell proliferation, transformation and invasion, induction of g0/g1 cell cycle arrest and, importantly, cell apoptosis. Remarkably, suppression of either pathway induces the expression of thyroid iodide-handling genes and dual suppression of the two pathways synergistically and robustly induces expression of these genes, accompanied by uptake of radioiodine in the cells.
Image forming apparatus
An image forming apparatus includes an image carrier; an image forming unit; a processor for controlling the image forming unit according to a predetermined image forming condition setting data; an image density sensor to detect an image density of the toner pattern formed on the image carrier; a reference rotary position detector; an image density fluctuation data acquisition unit to obtain an image density fluctuation data of more than one circumferential length of the photoreceptor drum with reference to the reference rotary position detected by the reference rotary position detector based on a result related to the toner pattern formed on the image carrier detected by the image density sensor; and a correction data generator to generate a correction data to correct a reference image forming condition setting data with a correction amount corresponding to each rotary position of the rotary member to thus reduce the image density fluctuation.. .
Torque tool
A torque tool for torqueing a receptacle lug having at least one pair of opposite sides. The tool including a block portion, a pair of protrusions, a protruding annulus, a bore, and a receptor for accepting a torque drive.
Crop resistance to nematodes
Methods of inhibiting plant parasitic nematodes, methods of obtaining transgenic plants useful for inhibiting such nematodes, and transgenic plants that are resistant to plant parasitic nematodes through inhibition of plant nematode cle peptide receptor genes are provided. Methods for expressing genes at plant parasitic nematode feeding sites with plant nematode cle peptide receptor gene promoters are also provided, along with nematode cle peptide receptor gene promoters that are useful for expressing genes in nematode feeding sites as well as transgenic plants and nematode resistant transgenic plants comprising the promoters..
4-aryl-1-(biarylmethylene) piperidine compounds
The 4-aryl-1-(biarylmethylene)piperidine compounds are piperadine compounds having a biaryl substituent linked to the nitrogen atom of the piperidine ring by a methylene (—ch2—) group, and an aryl moiety attached to the 4-position of the piperidine ring. The aryl moiety may be a methoxy quinoline group, a 2-oxo quinoline group, or a 2-oxo, 3,4-dihydroxy quinoline group.
L-setastine hydrochloride and preparation method thereof
The present invention relates to the field of medicine, and disclosed are an l-setastine hydrochloride and a preparation method therefor. The compound of the present invention has the advantages of stronger histamine hi receptor antagonism and small side effect; the yield of the preparation method is more than 80%, and the product purity is high.
Novel therapeutic use of p75 receptor antagonists
The present disclosure relates to the use of a p75 receptor antagonist or its pharmaceutically acceptable salts for the preparation of a medicament for use in the treatment and/or prevention of overactive bladder.. .
Aptamers and diagnostic methods for detecting the egf receptor
The present invention provides aptamers that specifically bind to the egf receptor in a sample, and diagnostic and analytical methods using those aptamers.. .
Hla-restricted, peptide-specific antigen binding proteins
Antigen binding proteins with tcr-like paratopes, that is, with an antigen binding region specific for an hla-a2 restricted peptide are disclosed. The antigen binding proteins encompass antibodies in a variety of forms, including full-length antibodies, substantially intact antibodies, fab fragments, f(ab′)2 fragments, and single chain fv fragments.
Antagonist peptide of the bond between cd47 and a protein belonging to the thrombospondin family
Antagonist peptide of the bond between cd47 and a protein belonging to the thrombospondin family has the sequence s1 r1-r2-r3-s-q-l-l-k-g-r4-r5-r6 and interacts specifically with the c-terminal end of the tsp, at the site of the bond between the tsp and the cd47 receptor. Interaction between the cd47 receptor and the protein is prevented.
Non-peptide bdnf neurotrophin mimetics
Methods and compounds for treating neurological and other disorders are provided. Included is the administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for a trkb receptor molecule..
Epidermal growth factor receptor (egfr) and methods of use in adenoviral-associated virus type 6 (aav6) transduction
Comparative gene analysis (cga) was combined with pathway visualization software to identify a positive correlation between aav6 transduction and epidermal growth factor receptor (egfr) expression. It was found that egfr is necessary for vector internalization and functions as a co-receptor for aav6.
Novel tissue protective erythropoietin receptor (nepor) and methods of use
Methods of determining whether a patient is suitable for erythropoietin (epo) therapy, including (a) isolating a tissue sample from said patient; (b) determining the level of expression of eph-b4 in said sample; and (c) correlating a presence of eph-b4 expression to a negative physiological response to epo therapy). In addition, methods of enhancing the effectiveness of epo therapy in a patient by administering to said patient, in conjunction with epo therapy, an sirna specific for eph-b4..
Novel cannabinoid receptor 2 (cb2) inverse agonists and therapeutic potential for multiple myeloma and osteoporosis bone diseases
Wherein: r1 and r2 are independently h, alkyl, or alkenyl; r3 is alkyl, alkenyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl; r4 and r5 are independently a bond, alkylenyl, or alkenylenyl; each r6 and r7 is independently selected from the group consisting of oh, f, cl, br, i, (c1-c6)alkyl, alkoxy, amino, cooh, conh2, so3h, po3h2, cn, sh, no2 and cf3; and p and q are independently 0, 1, 2, 3, 4, or 5. Such compounds may be used to treat osteoporosis or multiple myeloma..
Methods and compositions associated with the granulocyte colony-stimulating factor receptor
Some embodiments include compositions and methods of using or identifying compounds that modulate the activity of the granulocyte colony-stimulating factor receptor (gcfr). Some embodiments include use of compounds to treat certain disorders, such as hematopoietic or neurological disorders..
Therapeutic uses of compounds having affinity to the serotonin transporter, serotonin receptors and noradrenalin transporter
Therapeutic uses of 4-[2-(4-methylphenylsulfanyl)phenyl]piperidine and therapeutically acceptable salts thereof are provided.. .
Methods for screening a brca1 loss-of-function in a subject suffering from a cancer
The present invention relates to a method for screening a brca1 loss-of-function in a subject comprising the step consisting of determining the level of serine 211 phosphorylated glucocorticoid receptor (gr p-ser211) expression in a tissue sample obtained from said subject.. .
Combinations of an opioid/tlr4 antagonist and an alpha-2-delta ligand for use in the treatment of pain
Disclosed are compositions for treatment of pain comprising, a first compound and a second compound, the first compound is an opioid antagonist that treats pain by blocking toll-like receptor (tlr4) and the second compound is an alpha-2-delta ligand that enhances the pain treatment effect of the first compound. Examples of opioid antagonist include naltrexone, naloxone and nalmefene.
Treatment of pain using a composition of opioid/toll-like receptor 4 antagonists and dextro enantiomers thereof
This invention relates to the use of a composition comprising opioid/toll-like receptor 4 (tlr4) antagonists and dextro enantiomers thereof for the treatment of pain, where the opioid antagonists treat pain by blocking tlr4. More preferably, the dextro opioid/tlr4 antagonist enantiomer treats pain by blocking tlr4 while not affecting the opioid receptors and therefore avoiding adverse effects associated with blocking the opioid receptors.
Method and compositions for treatment or prevention of inflammatory conditions
Pharmaceutical compositions and methods for treating or preventing an inflammatory condition in a patient are disclosed. The pharmaceutical compositions and methods include the use of vincamine or a vincamine derivative, either alone or in combination with one or more additional therapeutic agents, including a steroid (preferably a corticosteroid), an angiotensin ii receptor (type 1) antagonist, an angiotensin-converting enzyme (ace) inhibitor, and a non-steroidal anti-inflammatory drug..
4-phenylpiperazine derivatives with functionalized linkers as dopamine d3 receptor selective ligands and methods of use
Dopamine d3 receptor antagonists and partial agonists are known to modulate the reinforcing and drug-seeking effects induced by cocaine and other abused substances. By introducing functionality into the butylamide linking chain of the 4-phenylpiperazine class of ligands, improved d3 receptor affinity and selectivity, as well as water solubility, is achieved.
Methods and compositions for predicting resistance to anticancer treatment
The instant application provides methods and related compositions pertaining to the identification of resistance to anticancer treatment in a patient. In a particular embodiment, the invention provides biomarkers for the identification of resistance to anticancer treatment in a lung cancer patient, wherein a reduced expression of a mediator and/or sw1/snf complex gene in the lung cancer cells of the patient indicates that the lung cancer cells in the patient may be resistant to treatment with a receptor tyrosine kinase inhibitor, such as gefitinib and/or erlotinib.
Wherein l, r, r3, r4, r5, r6, r7, x1, x2, x3, x4, y, m and n have the meaning according to the claims, are positive allosteric modulators of the fsh receptor, and can be employed, inter alia, for the treatment of fertility disorders.. .
Pyrimido[4,5-d]pyrimidinyl compounds, pharmaceutical compositions and uses thereof
A compound of formula (i) or (ii) and use of the compound in the preparation of drugs for treating cancer are disclosed. The study shows that the compounds can inhibit the growth of many kinds of tumor cells, can be used for targeting epidermal growth factor receptor (egfr), and particularly can inhibit tumor cells with single or multiple mutations of egfr (t790m).
Substituted phenoxypropylcycloamine derivatives as histamine-3 (h3) receptor ligands
Their use as h3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.. .
Compounds and methods for treatment of hypertension
Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor α2b antagonists.
Substituted piperidinyl compounds useful as gpr119 agonists
Substituted piperidinyl compounds of the formula (i): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well.
Assay for predictive biomarkers of anti-estrogen efficacy
Biomarkers associated with anti-estrogen sensitivity in cancers, methods for detecting and quantitating the biomarkers, and methods for treating cancer patients that exhibit the biomarkers are provided. The biomarkers are activated estrogen receptor foci (aef) found in the nuclei of certain tumor cells.
Combinations comprising antimuscarinic agents and beta-adrenergic agonists
Combinations comprising (a) a β2 agonist and (b) an antagonist of m3 muscarinic receptors which is 3(r)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane, in the form of a salt having an anion x, which is a pharmaceutically acceptable anion of a mono or polyvalent acid are useful, e.g., for the treatment of respiratory disease, e.g., asthma or chronic obstructive pulmonary disease.. .
Nk1 antagonists
Or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by nk1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.. .
Methods and compositions for the treatment of gastrointestinal disorders
Compositions and related methods for treating ibs and other gastrointestinal disorders and conditions (e.g., gastrointestinal motility disorders, functional gastrointestinal disorders, gastroesophageal reflux disease (gerd), duodenogastric reflux, crohn's disease, ulcerative colitis, inflammatory bowel disease, functional heartburn, dyspepsia (including functional dyspepsia or nonulcer dyspepsia), gastroparesis, chronic intestinal pseudo-obstruction (or colonic pseudoobstruction), and disorders and conditions associated with constipation, e.g., constipation associated with use of opiate pain killers, post-surgical constipation, and constipation associated with neuropathic disorders as well as other conditions and disorders are described. The compositions feature peptides that activate the guanylate cyclase c (gc-c) receptor..
Angiotensin-(1-7) as a chemoprevention agent
Disclosed is the use of angiotensin-(1-7) peptide as an anti-cancer and chemoprevention therapeutic. Embodiments of the present invention comprise methods and compositions to prevent cancer or to reduce the risk of cancer in an individual comprising administering to the individual a pharmaceutically effective amount of an agonist for the angiotensin-(1-7) receptor to inhibit at least one of formation of a tumor (tumorigenesis), the proliferation of tumor cells, the growth of tumor cells, or metastasis of tumor cells in the individual.
Truncated glp-1 derivatives and their therapeutical use
The invention relates to truncated glp-1 analogues, in particular a glp-1 analogue which is a modified glp-1(7-35) (seq id no 1) having: i) a total of 2, 3, 4, 5 6, 7, 8, or 9 amino acid substitutions as compared to glp-1(7-35), including a) a glu residue at a position equivalent to position 22 of glp-1(7-35), and b) an arg residue at a position equivalent to position 26 of glp-1(7-35); as well as derivatives thereof, and therapeutic uses and compositions. These analogues and derivatives are highly potent, have a good binding affinity to the glp-1 receptor, also to the extracellular domain of the glp-1 receptor, which is of potential relevance achieving long-acting, stable glp-1 compounds with a potential for once weekly administration..
Regulation of receptor expression through delivery of artificial transcription factors
The invention relates to an artificial transcription factor comprising a polydactyl zinc finger protein targeting specifically a receptor gene promoter fused to an inhibitory or activatory protein domain, a nuclear localization sequence, and a protein transduction domain. In particular examples these receptor gene promoters regulate the expression of the endothelin receptor a, the endothelin receptor b, the toll-like receptor 4 or the high-affinity ige receptor.

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