65 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.

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.

This invention relates to tetrahydro-naphthalene and urea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene and urea derivatives of the present invention have vanilloid receptor (VR1) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor overactivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).

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.

Compounds having formula (I) or formula (II) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A, N, X, Y, R1, R2 and R3 are as defined in the specification. These compounds are particularly useful in the treatment of pain, inflammatory hyperalgesia, and urinary dysfunctions, such as bladder overactivity and urinary incontinence.

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 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.

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.

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 is directed to compounds of formula (I) wherein variables X1, X2, Y, R1a, R1b, R2a, R2b, A1, A2, A3, and A4 are as defined in the description, and methods of use to treat pain, neuropathic pain, allodynia, pain associated with inflammation or an inflammatory disease, inflammatory hyperalgesia, bladder overactivity, and urinary incontinence.

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.

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

One of the major disabling symptoms of gastroparesis is nausea and vomiting which can be difficult to control with currently available treatments. It is postulated that signaling of gastrointestinal causes of nausea starts with activation of vagal afferent nerves that trigger the central emetic pathway. Most vagal afferent nerves are unmyelinated C-fibers, many of which express the vanilloid receptor TRPV1 and respond to capsaicin. Resiniferatoxin is a very potent capsaicin analogue that has a much more favorable ratio of desensitization to excitation than capsaicin leading to more effective desensitization without irritation. The present invention demonstrates that desensitization of TRPV1 responsive gastric sensory neurons would attenuate nausea and vomiting.

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.

The present invention relates to methods and compositions for the treatment and / or the prevention of conditions related to high levels of expression and / or activity of the transient receptor potential vanilloid-1 (TRPV1). Amongst others, the conditions to be treated are eye conditions such as discomfort and altered sensitivity of the cornea following refractive surgery, use of contact lenses, dry eyes and diabetic retinopathy.

This invention relates to bicyclic amide, carbamate or urea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The bicyclic amide, carbamate or urea derivative of the present invention has vanilloid receptor (VR1) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor oeractivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).

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 relates to methods and compositions for the treatment and / or the prevention of conditions related to high levels of expression and / or activity of the transient receptor potential vanilloid-1 (TRPV1). Amongst others, the conditions to be treated are eye conditions such as discomfort and altered sensitivity of the cornea following refractive surgery, use of contact lenses, dry eyes and diabetic retinopathy.

The invention provides compounds for use in a method of treating oral pharyngeal dysphagia in an individual and related products. One embodiment of the invention comprises administering to an individual an effective amount of a vanilloid receptor 1 (VR-1) agonist or high-affinity partial agonist to promote a swallow reflex.

Substituted pyrimidyl-4-ylamine analogues are provided, of the Formula: (I) wherein variables are as described herein. Such compounds are ligands that may be used to modulate Vanilloid receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.