85 results about "Vanilloid Receptors" patented technology

The present inventions relate to therapeutic compositions comprising, and methods utilizing, arachidonic acid derivatives and analogs for treatment of patients demonstrating symptoms of pathological conditions. Specifically, the inventions relate to therapeutic compositions for activating transient receptor potential vanilloid-1 channels (TRPV1). Additionally, therapeutic compositions are provided for increasing TRPV1-type responses. These pathological conditions include, but are limited to, hypertension, in particular salt induced hypertension, and cardiovascular complications, including myocardial infarction, kidney dysfunction, diabetes, and inflammation. Further, the inventions relate to drug screening methods for providing additional therapeutic compounds.

This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receotor 1; VR1; TRPV1 )antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, and heart disease.

Improved treatments of joint diseases, such as, e.g. osteoarthritis and rheumatoid arthritis, and pain, wherein a strontium-containing compound is administered alone or in combination with one or more second therapeutically and / or prophylactically active substances, selected from the group consisting of bisphosphonates, glucosamine, pallitative agents, analgesic agents, disease modifying anti-rheumatic compounds (DMARDs), selective estrogen receptor modulators (SERMs), aromatase inhibitors, non-steroidal anti-inflammatory agents (NSAIDs), COX-2 inhibitors, COX-3 inhibitors, opioids, inhibitors / antagonists of IL-1, inhibitors / antagonists of TNF-alpha, inhibitors of matrix metallo-proteinases (MMPs), cathepsin K inhibitors, inhibitors / antagonists of RANK-ligand, statins, glucocorticoids, chondroitin sulphate, NMDA receptor antagonists, inhibitors of interleukin-I converting enzyme, Calcitonin gene related peptide antagonists, glycine antagonists, vanilloid receptor antagonists, inhibitors of inducible nitric oxide synthetase (iNOS), N-acetylcholine receptor agonists, neurokinin antagonists, neuroleptic agents, PAR2 receptor antagonists and anabolic growth factors acting on joint tissue components. Pharmaceutical compositions comprising a strontium-containing compound and a second therapeutically and / or prophylactically active substance as defined above.

The present invention relates to DNA enzymes of type 10-23 with certain modifications of specific nucleotides in the core sequence rendering the DNA enzymes particularly stable and additionally exhibiting substantially the same or a higher cleavage efficiency with respect to their substrate when compared against the corresponding unmodified DNA enzymes. The present application further provides host cells containing the DNA enzymes according to the invention. In addition there is provided a pharmaceutical formulation which contains the DNA enzymes or host cells according to the invention. The DNA enzymes and further subjects are directed in particular against the vanilloid receptor 1 (VR1), or picornaviruses. The present invention further provides small interference RNA molecules (siRNA) directed against VR1, and host cells containing the siRNA. The siRNA and corresponding host cells are suitable as pharmaceutical formulations or for the preparation of pharmaceutical formulations, in particular for the treatment of pain and other pathological conditions associated with VR1.

This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to β-aminotetralin-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.

The present application is directed to compounds that are TRPV1 antagonists and have formula (I)wherein variables Ar1, L1, R1, R2, R3, R4, R5, Y1, Y2, and Y3, are as defined in the description, which are useful for treating disorders caused by or exacerbated by vanilloid receptor activity.

The present invention provides methods and kits for the selective ablation of pain-sensing neurons. The methods comprise administration of a vanilloid receptor agonist to a ganglion in an amount that causes death of vanilloid receptor-bearing neurons. Accordingly, the present invention provides methods of controlling pain and inflammatory disorders that involve activation of vanilloid receptor-bearing neurons.

The present invention relates to the induction of hypothermia in humans in a predictable and dose responsive fashion by use of a pharmaceutical composition comprising a vanilloid receptor agonists, capsaicinoid or capsaicinoid-like agonist capable of inducing hypothermia, thereby benefiting patients suffering from illnesses characterized by tissue anoxia.

The invention described herein encompasses methods and compositions of preventing or treating cancer comprising the administration of a combination of catechins and vanilloids. Compositions of catechins include but not limited to, epigallocatechin gallate (EGCg), epicatechin (EC), epicatechin gallate (ECG), epigallocatechin (EGC). In a preferred embodiment the catechins have been treated with tannase. Compositions of vanilloids include, but are not limited to vanillylamine, the head group of capsaicin. The unique compositions of the invention contain various combinations of the catechins and vanilloids, in combination with each other or other therapeutic agents and are used to treat primary and metastatic cancers in humans. The invention also encompasses various modes of administration of the therapeutic compounds, including formulations which may be used as a dietary or nutritional supplement or as a therapeutic compound.

Substituted cyclic carboxamide and urea compounds, a process for their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds for the treatment and / or inhibition of pain and other conditions mediated by the vanilloid receptor 1.

This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1 )antagonist; and a pharmaceuticalcomposition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.

The present invention relates to novel thiourea derivatives as a modulator for vanilloid receptor (VR) and the pharmaceutical compositions containing the same. As diseases associated with the activity of vanilloid receptor, pain acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.

The invention relates to a compound in a general formula (I) and a salt of the compound, wherein the compound is a TRPV1 / COX-2 dual inhibitor and has a good analgesic effect. The invention also relates to a preparation method of the compound, a medicinal preparation containing the compound, and application thereof in preparation of the analgesic medicament.

The invention relates to applications of dragon's blood and a flavonoid chemical component thereof in serving as an antagonist of a capsaicin receptor TRPV1 (transient receptor potential vanilloid 1) and in preparing a medicament for treating diseases related to TRPV1 receptors, wherein the flavonoid chemical component is cochinchinenin A or a mixture of at least two of cochinchinenin A, cochinchinenin B and loureirin B. The invention also relates to a medicinal composition comprising the dragon's blood and and the flavonoid chemical component thereof. Independent component of the dragon's blood or the cochinchinenin A, or a combination of every two of the cochinchinenin A, the cochinchinenin B and the loureirin B, or a combination comprising the cochinchinenin A, the cochinchinenin B and the loureirin B has strong capsaicin receptor TRPV1 activation inhibition effect and excellent pharmacological action based on the inhibition effect, so that the dragon's blood or the flavonoid chemical component thereof serving as an active component can be used for preparing medicaments for treating or preventing TRPV1 related diseases, such as nociceptive pains, neurogenic pains, cancer pains, headache, urinary bladder functional disorder, inflammation and the like.

This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.

The present invention features vanilloid receptor polypeptides and vanilloid receptor-related polypeptides, specifically the capsaicin receptor subtypes VR1 and VR2 (VRRP-1), as well as the encoding polynucleotide sequences. In related aspects the invention features expression vectors and host cells comprising such polynucleotides. In other related aspects, the invention features transgenic animals having altered capsaicin receptor expression, due to, for example, the presence of an exogenous wild-type or modified capsaicin receptor-encoding polynucleotide sequence. The present invention also relates to antibodies that bind specifically to a capsaicin receptor polypeptide, and methods for producing these polypeptides. Further, the invention provides methods for using capsaicin receptor, including methods for screening candidate agents for activity as agonists or antagonists of capsaicin receptor activity, as well as assays to determine the amount of a capsaicin receptor-activating agent in a sample. In other related aspects, the invention provides methods for the use of the capsaicin receptor for the diagnosis and treatment of human disease and painful syndromes.

The present invention relates to a TRPV3 (transient receptor potential vanilloid 3) activity inhibitor, more precisely to a method for inhibiting TRPV3 activity including the step of treating isopentenyl pyrophosphate and a method for treating skin disease containing the step of administering isopentenyl pyrophosphate to a subject with skin disease or applying the same on the skin of the subject. Isopentenyl pyrophosphate of the present invention controls increase of sensory cell reactivity to current or migration and proliferation of skin cells induced by TRPV3, so that it can be effectively used for the development of a pain reliever or a therapeutic agent for skin disease.

Described herein are compounds, pharmaceutical compositions and medicaments that include such compounds, and methods of using such compounds to modulate transient receptor potential vanilloid 1 receptor (TRPV1) activity.

Provided are compositions comprising a vanilloid and tea catechins in amounts and proportions which combat virus infections in a human or animal. The vanilloid can be provided in the form of a dried pepper preparation and the tea catechins can be provided in the form of a green tea extract (or concentrate). These active ingredients can be provided separately or in combination. The administration of a such nutritional or other composition, desirably oral administration (in an amount effect) results in reduced virus infection or ameliorated symptoms of virus infection in a human or an animal in need of such a composition.

The present invention describes methods of retarding the development of visceral and somatic hypersensitivities in an individual. Further, the present invention describes a potentially important role for the transient receptor potential vanilloid 1 (TRPV1) in initiation and maintenance of the chronic visceral hypersensitivity and its role in development of irritable bowel syndrome.

Methods and kits for controlling bleeding from a disrupted blood vessel, wherein a vanilloid receptor agonist is administered to the site of the disruption of the blood vessel in a quantity sufficient to control the bleeding.

Composition comprising: a carrier; a first active ingredient comprising capsaicin, a capsaicin analog, another vanilloid receptor agonist or mixtures thereof; and at least one second active ingredient that functions as a topical anesthetic to cause localized numbness to induced skin irritation. Technique for treating the symptoms of pruritus comprising the step of applying a composition comprising a carrier, a first active ingredient comprising capsaicin, a capsaicin analog, another vanilloid receptor agonist or mixtures thereof, and at least one second active ingredient that functions as a topical anesthetic, to cause localized numbness to induced skin irritations.

The present invention relates to a method for activating TRPV3 (transient receptor potential vanilloid 3) using FPP (farnesyl diphosphate) and a method for screening a TRPV3 activity inhibitor. FPP of the present invention has TRPV3 specific activity and therefore it can be effectively used for the study on TRPV3 mechanism and functions and for the development of a TRPV3 based pain reliever.

The present invention relates to the induction of hypothermia in humans in a predictable and dose responsive fashion by use of a pharmaceutical composition comprising a combination of (1) vanilloid receptor agonists, capsaicinoids or capsaicinoid-like agonists reaching and binding to vanilloid receptors, and (2) cannabinoids or cannabimimetic agonists reaching and binding to cannabinoid receptors, thereby inducing hypothermia, thus benefiting patients suffering from illnesses characterized by tissue anoxia.

The present invention provides methods and kits for the selective ablation of pain-sensing neurons. The methods comprise administration of a vanilloid receptor agonist to a ganglion in an amount that causes death of vanilloid receptor-bearing neurons. Accordingly, the present invention provides methods of controlling pain and inflammatory disorders that involve activation of vanilloid receptor-bearing neurons.

The present invention is related to new vanilloid analogues containing resiniferatoxin pharmacophores, pharmaceutical compositions that have such analogues, and their uses as vanilloid receptor agonists and potent analgesics. The present invention provides a pharmaceutical composition for preventing, alleviating or treating pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neutopathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease, inflammatory disease or urgent urinary incontinence.

Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence, or bladder overactivity.