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30 results about "TRPV4" patented technology
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Transient receptor potential cation channel subfamily V member 4 is an ion channel protein that in humans is encoded by the TRPV4 gene. The TRPV4 gene encodes TRPV4, initially named "vanilloid-receptor related osmotically activated channel" (VR-OAC) and "OSM9-like transient receptor potential channel, member 4 (OTRPC4)", a member of the vanilloid subfamily in the transient receptor potential (TRP) superfamily of ion channels. The encoded protein is a Ca²⁺-permeable, nonselective cation channel that has been found involved in multiple physiologic functions, dysfunctions and also disease. It functions in the regulation of systemic osmotic pressure by the brain, in vascular function, in liver, intestinal, renal and bladder function, in skin barrier function and response of the skin to ultraviolet-B radiation, in growth and structural integrity of the skeleton, in function of joints, in airway- and lung function, in retinal and inner ear function, and in pain. The channel is activated by osmotic, mechanical and chemical cues. It also responds to thermal changes (warmth). Channel activation can be sensitized by inflammation and injury.
Solid forms of GSK2798745, a TRPV4 antagonist
PCT designated stage expiredWO2025014818A1Organic active ingredientsNervous disorderMethyl benzenePyrazine
Owner:ACTIO BIOSCIENCES INC
TRPV4 inhibition to treat arrhythmic cardiomyopathy
PCT designated stage expiredWO2025029629A2Organic active ingredientsCardiovascular disorderGenomic sequencingDisease
Genome sequencing identified a new gene associated with a cardiac arrhythmic disease, TAXI -binding protein 3. From cell line models and a conditional knock-out mouse models of the gene deletion, it was found that a specific molecule, transient receptor potential vanilloid 4 (TRPV4), is up-regulated and is associated with calcium mediated arrhythmic depolarizations.
Owner:DUKE UNIV
Solid forms of TRPV4 antagonists
The present disclosure provides a solid form of 5-fluoro-1-(((5S, 7S, 8R)-8-fluoro-3-(5-(2-hydroxypropyl-2-yl) pyrazin-2-yl)-7-methyl-2-oxo-1-oxa-3-azaspiro [4.5] decane-7-yl) methyl)-1H-benzo [d] imidazole-6-formonitrile: which is useful as a TRPV4 antagonist.
Owner:ACTIO BIOSCIENCES INC
Pyrimidin-4(3H)-one derivatives as TRPV4 antagonists
This invention relates to pyrimidin-4(3H)-one derivatives of formula (I),that act as modulators of the TRPV4 receptor. The present invention also relates to processes for the preparation of novel pyrimidin-4(3H)-one derivatives of formula (I) and to their use in the treatment of a wide range of diseases, syndromes, and disorders, in particular, for the treatment of inflammation, pain, and urological diseases or disorders.
Owner:RAQUALIA PHARMA INC
Use of dasabuvir in the preparation of trpv4 inhibitors and ulcerative colitis drugs
This application discloses the application of dasabuvir as a TRPV4 inhibitor in improving diseases caused by increased TRPV4 expression or enhanced activity, particularly ulcerative colitis. Specifically, it relates to the biomedical field. Dasabuvir is a novel TRPV4 inhibitor that can improve symptoms in a DSS-induced mouse ulcerative colitis model and is suitable for use in TRPV4 inhibitor drugs and ulcerative colitis drugs. In HEK-293 cells overexpressing TRPV4, dasabuvir can dose-dependently inhibit the increase in intracellular calcium ion concentration induced by the TRPV4-specific agonist GSK1016790A within a concentration range of 0.03-30 μM, with an IC50 concentration of [missing information]. 50 At a concentration of 0.27 μM, Dasabuvir is a highly active TRPV4 inhibitor. In a DSS-induced ulcerative colitis model, Dasabuvir can improve weight loss, reduce the disease activity index, alleviate colonic shortening, reduce histopathological changes, and inhibit the expression of inflammatory factors, thus improving ulcerative colitis.
Owner:CHINA PHARM UNIV
Therapeutic compounds and methods
Owner:ACTIO BIOSCIENCES INC
Application of TRPV4 inhibitor in preparation of medicine for preventing or treating diseases caused by trimethyltin chloride poisoning
The invention belongs to the field of biological medicine, and relates to application of a TRPV4 inhibitor in preparation of a medicine for preventing or treating diseases caused by trimethyltin chloride poisoning. The TRPV4 ion channel inhibitor can remarkably prolong the incubation period of epilepsy caused by trimethyltin chloride poisoning, relieve the severity of epileptic seizure, improve nerve injury and increase the survival rate. Therefore, a new drug target is provided for diagnosis of trimethyltin chloride poisoning and drug research and development, and a new strategy is provided for clinical treatment of trimethyltin chloride poisoning.
Owner:ACADEMY OF MILITARY MEDICAL SCIENCES
Polyol derivative for antagonizing and inhibiting TRPV4-rhoa target and use thereof
Disclosed in the present invention are a compound represented by formula I, or a pharmaceutically acceptable salt thereof or an ester thereof, a prodrug thereof, an optical isomer thereof, a stereoisomer thereof, or a solvate thereof as an antagonist or an inhibitor for antagonizing and inhibiting a TRPV4-RhoA target, and use thereof in treating TRPV4-RhoA target-related diseases. The class of compounds exhibits an excellent effect of antagonizing TRPV4 and inhibiting RhoA activity, thereby laying a brand-new substance foundation for developing drugs for treating TRPV4-RhoA target-related diseases.
Owner:TAO PHARM SUZHOU CO LTD
Pharmaceutical composition comprising TRPV4 inhibitor for preventing or treating cerebral cavernous malformation (CCM)
The present invention relates to a pharmaceutical composition for preventing or treating cerebral cavernous malformation (CCM), comprising a transient receptor potential vanilloid 4 (TRPV4) inhibitor.
Owner:UNIVERSITE GRENOBLE ALPES +3
Therapeutic compounds and methods
PendingUS20250333403A1Organic active ingredientsNervous disorderOrganic chemistryMedicinal chemistry
Owner:ACTIO BIOSCIENCES INC
Benzylpiperidine derivatives as TRP4 antagonists for the treatment of inflammatory diseases
PCT designated stage expiredWO2025149498A1Organic active ingredientsNervous disorderBenzyl groupGenetic disorder
The present invention relates to substituted benzyl piperidines of Formula (I) as well as to their use as TRPV4 antagonists for use in treating e.g. inflammatory, respiratory, metabolic, dermatological, skeletal, neuromuscular or genetic diseases or disorders, cancer, or pain.
Owner:ASTRAZENECA AB
Methods for generating functional hematopoietic stem cells
Described in the present application are methods for preparing populations of hematopoietic stem cells (HSCs), e.g., autologous and / or allogenic HSCs, using mechanical stretching or Trpv4 agonists, and methods of use of the HSCs in transplantation. In some embodiments, the methods include providing a population comprising hemogenic endothelial (HE) cells, and (i) contacting the HE cells with an amount of an agonist of transient receptor potential cation channel-subfamily vanilloid member 4 (Trpv4); and / or (ii) subjecting the cells to cyclic 2-dimensional stretching, for a time and under conditions sufficient to stimulating endothelial-to-HSC transition. Also provided herein are methods for treating subjects who have, bone marrow, metabolic, and immune diseases; the methods include administering to the subject a therapeutically effective amount of hematopoietic stem cells (HSCs) obtained by a method described herein.
Owner:CHILDRENS MEDICAL CENT CORP
Polyol derivative as TRPV4 antagonist and application thereof
The invention discloses application of a compound as shown in a formula I, or pharmaceutically acceptable salt or ester, a prodrug, an optical isomer, a stereoisomer or a solvate of the compound as a TRPV4 inhibitor or antagonist and treatment of TRPV4 related diseases. The compound shows an excellent TRPV4 inhibitory activity effect, so that a brand-new material basis is laid for developing drugs for treating TRPV4 related diseases.
Owner:TAO PHARM SUZHOU CO LTD
Compounds and methods for the treatment of brain injuries
PCT designated stage expiredWO2025096549A1Nervous disorderOrganic chemistryInjury brainMTBI - Mild traumatic brain injury
Disclosed herein are methods of treating traumatic brain injuries, including mild traumatic brain injuries by administering to a subject in need a TRPV4 antagonist. The methods disclosed herein may be used to treat concussion and post-concussion syndrome.
Owner:OHIO STATE INNOVATION FOUND
Application of TRPV4 ion channel inhibitor in preparation of medicine for preventing and / or treating psoriasis
PendingCN120531714AHydroxy compound active ingredientsDermatological disorderNatural productPharmacy medicine
The invention provides an application of a TRPV4 ion channel inhibitor in preparation of a medicine for preventing and / or treating psoriasis. Specifically, through screening of natural product monomer drugs, it is found that sclareol can inhibit a TRPV4 ion channel in a dose-dependent mode, application of sclareol in the field of psoriasis prevention and treatment is further developed, and a new strategy is provided for clinical treatment of psoriasis.
Owner:HANGZHOU THIRD PEOPLES HOSPITAL (HANGZHOU HUIMIN HOSPITAL HANGZHOU THIRD AFFILIATED HOSPITAL OF ZHEJIANG UNIV OF TRADITIONAL CHINESE MEDICINE)
Skin barrier function improving agent
To provide a tight junction formation promoter, to provide a TRPV4 activating agent, to provide a skin barrier function improving agent that maintains skin elasticity and improves skin to a smooth and moisturized state, and to provide a cosmetic product containing the same.SOLUTION: Aromatic water obtained from Citrus sudachi and Citrus depressa is used.SELECTED DRAWING: None
Owner:NAT AGRI & FOOD RES ORG +1
TRPV4, application of TRPV4 inhibitor, head and neck cancer medicine and in-vitro non-therapeutic inhibition method
The invention relates to application of TRPV4 and an inhibitor thereof, a head and neck cancer medicine and an in-vitro non-therapeutic inhibition method. According to the application of the TRPV4 as a head and neck cancer treatment target, the TRPV4 protein is remarkably and highly expressed in head and neck cancer tissues, and proliferation and migration of head and neck cancer cells can be inhibited and apoptosis can be promoted by knocking down the expression of the TRPV4 protein. The invention provides a novel therapeutic target for the head and neck cancer, and the target can be effectively used for judging and / or treating the head and neck cancer, so that a novel diagnostic and / or therapeutic agent is provided for the field and has a clinical application prospect.
Owner:SHENZHEN LONGGANG DISTRICT OTOLARYNGOLOGY HOSPITAL (SHENZHEN OTOLARYNGOLOGY RES INST SHENZHEN LONGGANG DISTRICT ORAL MEDICINE RES INST)
Compound for specifically enhancing spatial coupling degree of TRPV4-KCa2.3 complex and use thereof
The present disclosure provides a compound for specifically enhancing the spatial coupling degree of a TRPV4-KCa2.3 complex and use thereof, and belongs to the field of chemical medicine. The compound with a structure shown in a general formula (I) in the present disclosure is mainly used for re-coupling two uncoupled proteins and restoring the proteins to a normal state under uncoupling of TRPV4 and KCa2.3 in hypertensive patients. Under normal conditions of the TRPV4 and the KCa2.3, a signal of calcium ions is received by the TRPV4. As the calcium ions flow in, potassium ions in a KCa2.3 channel in the downstream are stimulated to flow out. Due to depolarization, vasodilation is caused, and therefore, the blood pressure of the hypertensive patients is returned to a normal level.
Owner:JIANGNAN UNIV
Fusion protein capable of regulating and controlling neuron activity, system for remotely controlling neuron activity and application
The invention provides a fusion protein capable of regulating and controlling neuron activity, a system for remotely controlling neuron activity and application, and belongs to the technical field of nerve regulation and control. The invention discloses a fusion protein with neuron regulation activity. The fusion protein is obtained by fusion expression of a delta TRPV4 protein and a magnetic receptor protein MagR. The MagR protein and a mechanically sensitive ion channel TRPV4 are subjected to fusion expression, the MagR enables a delta TRPV4 channel to be opened under the action of a magnetic field to trigger a cell calcium influx biological effect, intracellular calcium signal transduction is further regulated, the neuronal function is controlled, and then accurate and controllable regulation of brain region neuron subpopulation excitability is achieved.
Owner:ACADEMY OF MILITARY MEDICAL SCIENCES
Treatment of retinal ganglion cell loss
PendingUS20260048098A1Organic active ingredientsSenses disorderGrammostola spatulataMedicinal chemistry
The present invention is directed to methods of treating or preventing glaucoma comprising administering an effective amount of one or more compounds selected from the group consisting of transient receptor potential vanilloid 4 (TRPV4) antagonists, Grammostola spatulata MTx4 peptide and D-Grammostola spatulata MTx4 peptide to a subject in need thereof.The present invention is further directed to methods of treating or preventing retinal ganglion cell loss comprising administering an effective amount of one or more compounds selected from the group consisting of transient receptor potential vanilloid 4 (TRPV4) antagonists, Grammostola spatulata MTx4 peptide and D-Grammostola spatulata MTx4 peptide to a subject in need thereof.
Owner:PS THERAPY INC
Compositions and methods for the modulation of piezo1 and TRPV4
Described herein are methods and compositions for treating or reducing the likelihood of a subject developing a pancreatic disease or disorder or keloids. In one embodiment, the method comprises administering a therapeutically effective amount of one or more of a Piezol antagonist, a PLA2 antagonist, a TRPV4 antagonist, or combinations thereof.
Owner:DUKE UNIV
PYRIMIDIN-4(3H)-ON-DERIVATE ALS TRPV4-ANTAGONISTEN
Owner:RAQUALIA PHARMA INC
Application of chemical fiber formula of fortune euonymus herb in treatment of hepatic fibrosis
The invention discloses an application of a fortune euonymus herb chemical fiber formula in treatment of hepatic fibrosis, and relates to the field of biological medicines. According to the present invention, the anti-hepatic fibrosis effect is provided by inhibiting hepatic stellate cell activation and reducing extracellular matrix deposition, and the hepatic fibrosis is the chronic liver injury pathological stage caused by viral hepatitis, alcoholic liver disease, non-alcoholic fatty liver disease or drug-induced liver injury; in an in-vitro experiment, the euonymus fortunei chemical fiber formula also plays a role in resisting hepatic fibrosis by inhibiting a transient receptor potential vanillic acid subtype 4 signal channel. The method has the following comprehensive advantages that (1) HSC activation and ECM deposition are inhibited through multi-component and multi-target cooperation; (2) key signal channels such as TGF-beta1 / Smad, TRPV4 and the like can be regulated and controlled at the same time; (3) liver function indexes are obviously improved, and tissue structure damage is relieved; and (4) the medicine is natural in source, high in safety and suitable for long-term application.
Owner:CHONGQING TRADITIONAL CHINESE MEDICINE HOSPITAL +1
Application of narirutin targeting to TRPV4 channel in preparation of medicine or preparation for treating alopecia
The invention discloses an application of Narirutin (NR) of a targeted TRPV4 (transient receptor potential vanilloid 4) channel in preparation of a medicine or a preparation for treating alopecia. The narirutin is an active component separated from citrus, and experiments prove that the narirutin can promote activation of hair follicle melanocyte and melanin synthesis and effectively relieve androgen-induced alopecia, so that the phenotype of a mouse with androgenetic alopecia is improved, and hair growth is promoted. The narirutin is high in safety and convenient to use, so that the narirutin has wide application prospects in the fields of pharmaceutical preparations, cosmetics, care products, health care products, beauty products and the like for preventing, nursing and treating less hair and alopecia and promoting hair health and growth.
Owner:HANGZHOU THIRD PEOPLES HOSPITAL (HANGZHOU HUIMIN HOSPITAL HANGZHOU THIRD AFFILIATED HOSPITAL OF ZHEJIANG UNIV OF TRADITIONAL CHINESE MEDICINE)
Compositions and methods for hair follicle regeneration
Among the various aspects of the present disclosure is the provision of compositions and methods for treating hair regeneration disorders or conditions such as hair loss or thinning. An aspect of the present disclosure provides for a method of treating hair loss, promoting hair growth, or treating hair loss, such as alopecia or telogen effluvium, comprising administering a TRPV4 activating agent to a subject.
Owner:WASHINGTON UNIV IN SAINT LOUIS
Application of relieving and moisturizing effects of cineole in facial dermatitis rehabilitation
The invention belongs to the technical field of application of cineole, discloses application of relieving and moisturizing effects of cineole in facial dermatitis rehabilitation, and comprises application of cineole in preparation of a medicine for facial dermatitis rehabilitation. The Cin can play an antioxidant role by regulating expression of gene transcription and protein levels of Bax, Bcl-2 and inflammatory factors IL-1beta and regulating ROS, SOD and MDA, and plays a role in protecting H2O2-induced HaCaT cells and menadione-induced oxidative stress of zebrafish, so that the cineole is proved to have a protective role in epidermal keratinocytes under oxidative stress, and the cineole can be used for preparing a medicine for treating the oxidative stress of the zebrafish. Treating zebra fish with sodium chloride, observing the influence of the tail area of the zebra fish, and evaluating the moisturizing effect of Cin; by inhibiting expression of TRPV1 and TRPV4, opening of ion channels is inhibited, nerve impulse conduction is inhibited to play a soothing role, and dermatitis or skin discomfort caused by stimulation of ultraviolet rays, polluted air, drugs and the like on skin can be treated or relieved.
Owner:GUANGZHOU DERMATOLOGY HOSPITAL (GUANGZHOU CENTER FOR SKIN DISEASES & STI CONTROL & PREVENTION)
TRPV4 inhibition to treat arrhythmic cardiomyopathy
PCT designated stage expiredWO2025029629A3Organic active ingredientsMicrobiological testing/measurementDiseaseReceptor potential
Genome sequencing identified a new gene associated with a cardiac arrhythmic disease, TAXI -binding protein 3. From cell line models and a conditional knock-out mouse models of the gene deletion, it was found that a specific molecule, transient receptor potential vanilloid 4 (TRPV4), is up-regulated and is associated with calcium mediated arrhythmic depolarizations.
Owner:DUKE UNIV
Pyrimidin-4(3H)-one derivatives as TRPV4 antagonists
The present invention relates to a pyrimidine-4(3H)-one derivative, which is used as a modulator of TRPV4 receptor. The present invention also relates to a process for preparing a novel pyrimidine-4(3H)-one derivative and its use in treating various diseases, syndromes and disorders, especially in treating inflammatory, painful and urinary diseases and disorders.
Owner:RAQUALIA PHARMA INC
Therapeutic compounds and methods
Owner:ACTIO BIOSCIENCES INC