54 results about "Vanilloids" 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.

A 3,4-dihydrobenzoxazine compound of the present invention is represented by the following formula [1] (wherein X is a nitrogen atom or CR³; R¹ is a hydrogen atom or a halogen atom; R² is a C1-6 alkoxy group which may be substituted with the same or different 1 to 5 substituents selected from a halogen atom and a hydroxyl group; and R³ is a halogen atom. However, R¹ is a halogen atom when X is CR³). This compound is effective in treating diseases to which the vanilloid receptor subtype 1 (VR1) activity is involved, such as pain, etc.

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 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.

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.

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 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.

The invention relates to a 1,2,3,4-tetrahydro-9H-pyridino[3,4-b]indole transient receptor potential vanilloid 1 (TRPV1) antagonist or a pharmaceutically-acceptable salt thereof. The structure generalformula is shown in the specifications, in the formula, R is H, or F, or Cl, or Br, or I, or CF3, or methyl, or isopropyl, or tertiary butyl, or cyclopropyl, or propenyl, or acetenyl, or hydroxyl, orphenoxyl, or acetyl or phenyl; n is 1, or 2 or 3; L is triazole, or tetrazole, or carbamido or thioureido; Ar is phenyl, or pyridyl, or isoquinolyl, or quinolyl or pyrimidyl. Through tests, it is found that 1,2,3,4-tetrahydro-9H-pyridino[3,4-b]indole compounds have good TRPV1 inhibitory activity, and the activity of part of the compounds is far higher than that of a TRPV1 receptor antagonist BCTC;compared with the BCTC, the side effect of body temperature increasing is almost avoided. Therefore, the 1,2,3,4-tetrahydro-9H-pyridino[3,4-b]indole compounds as shown in the general formula and medicinal salts thereof are safe and effective and have a high analgesic effect.

4-(methylsulfonylamino)phenyl analogues as potent vanilloid receptor antagonists and pharmaceutical compositions comprising the same. The compounds are useful as analgesics to prevent, alleviate or treat pain diseases or inflammatory disease including 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, inflammatory disease and urgent urinary incontinence.

The present invention is related to new vanilloid analogues containing resiniferatoxin pharmacophores, pharmaceutical compositions comprising such analogues, and their uses as vanilloid receptor agonists and potent analgesics. The present invention provides a pharmaceutical composition for treating acute, chronic, inflammatory or neuropathic pains or for treating bladder hypersensitivity.

Novel diphenylurea and benzylbenzenesulfonamide compounds are disclosed along with methods of inhibiting the activity of TRPV1 and methods of treating pain associated with transient receptor potential vanilloid type 1 (TRPV1) using such compounds.

Augmented or synergized anti-inflammatory constructs are disclosed including anti-inflammatory amino acids covalently conjugated with other anti-inflammatory molecules such as nonsteroidal anti-inflammatory drugs, vanilloids and ketone bodies. Further conjugation with a choline bioisostere or an additional anti-inflammatory moiety further augments the anti-inflammatory activity.

The present embodiments relate to selection of agents effective in reducing or preventing gastrointestinal pain in a subject. Such an agent is selected and identified if it is capable of reducing spontaneous and/or induced transient receptor potential vanilloid 1 (TRPV1) activation.