25 results about "Channel blocker" patented technology

This invention provides a method for improving the antidepressant effect of an NMDAR pore channel blocker, comprising: (1) performing behavioral, pharmacological, or physical measures before or during the plasma half-life of the NMDAR pore channel blocker to open ion channels of a larger proportion of NMDAR molecules in the lateral habenula (LHb); and optionally (2) performing behavioral, pharmacological, or physical measures after administration of the NMDAR pore channel blocker to prevent or reduce the dissociation of NMDAR pore channel blocker molecules from NMDAR. Treatment regimens and drug combinations for effectively treating depression are also provided. This disclosure further provides a drug delivery system comprising an implantable unit capable of controlled, repeatable, and precise in vivo delivery of an NMDAR pore channel blocker, as well as an initiator and / or enhancer, to an LHb region of a subject's brain, thereby achieving improved therapeutic effects.

Methods are provided to prevent and to treat diabetic retinopathy by using Calcium channel blockers, Angiotensin-Converting Enzyme (ACE) Inhibitors, or angiotensin receptor blockers (ARB), and more particularly, to a method to prevent and treat diabetic retinopathy by using calcium channel blockers, Angiotensin-Converting Enzyme Inhibitors, or angiotensin receptor blockers that may not need to be taken orally, but may also be administered by ophthalmic preparation directly onto or into the eye where diabetic retinopathy is formed, to increase the capillary network and augment the blood supply to the anatomy of the eye.

A pharmaceutical composition comprising an influenza A M2 protein channel blocker for use in the treatment or prevention of the virulence of an aminoadamantane resistant influenza A, such as the H1N1 subtype, in a subject is provided. Further provided is a pharmaceutical composition comprising the influenza A M2 protein channel blocker for preventing entry, shelling and / or release from influenza A cells.

The present invention is related to methods of treating cardiac arrhythmia, angina, or a migraine in a patient in need thereof, with a therapeutically effective amount of a compound having a structure according to the formula:the method comprising nasally administering to the patient (i) a first dose, and (ii) a second dose of an aqueous composition comprising a pharmaceutically acceptable acetate or methanesulfonate salt of compound I, or a racemate or enantiomer thereof, wherein the acetate or methanesulfonate salt of compound I, or the racemate or enantiomer thereof, is dissolved in the aqueous composition at a concentration of 350 mg / mL±50 mg / mL, and wherein the second dose of the compound is administered between 5 minutes and 25 minutes after the first dose.

Provided are a tetrodotoxin conjugate, a method for preparing same, and use thereof. A carboxyl-containing macromolecular compound and tetrodotoxin are used as the starting materials, and after a catalyst and a solvent are added, the tetrodotoxin conjugate is obtained by means of a coupling reaction. The carboxyl-containing macromolecular compound is selected from carboxylated dextran, carboxylated β-cyclodextrin, alginic acid, and polyacrylic acid. The tetrodotoxin conjugate can be used in the preparation of a sodium channel blocker and a medicament for treating neuropathic pain caused by chemotherapy, and possesses an analgesic effect associated with tetrodotoxin (TTX). In addition, the therapeutic window is increased, thereby greatly improving the safety.

The embodiment of the invention provides a buccal product, the buccal product provided by the embodiment of the invention comprises an active substance, a TRPM5 channel blocker, a first bitterness inhibitor and a second bitterness inhibitor, the first bitterness inhibitor is used for embedding the active substance, and the second bitterness inhibitor is used for enhancing sweetness and / or covering bitterness. The active substance is embedded in the first bitter inhibitor, so that the release rate of the active substance can be controlled through the first bitter inhibitor; the TRPM5 channel blocking agent can block a bitter receptor TRPM5 channel and weaken the bitter perception capability, and then the second bitter inhibitor is combined to enhance the sweet taste and / or cover the bitter taste, so that a triple bitter inhibition mechanism is realized, a bitter perception path is blocked, and the use comfort and market acceptance of the buccal product are improved; therefore, the buccal product provided by the embodiment of the invention can effectively improve the problem of poor user experience caused by too strong natural bitter taste of the existing buccal product.

Disclosed herein are methods for treating hot flushes in a subject. In one embodiment, treating hot flushes includes administering to a subject in need of such treatment, a therapeutically effective amount of a transient receptor potential channel (TRP channel) blocker or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods for amelioration, alleviation, or prevention of the thermal discomfort in hot flushes, comprising: selecting a subject in need of treatment for hot flushes, administering to the subject a therapeutically effective amount of a TRP channel blocker, such as a TRPV1 blocker, or a pharmaceutically acceptable salt thereof.

The invention discloses an application of a CCL2 / CCR2 signal channel blocker in relieving chemotherapeutic drug-induced heart injury, and belongs to the technical field of biological medicines. The invention finds that a CCL2 / CCR2 signal channel blocker, particularly a CCL2 neutralizing antibody, has an obvious effect of improving the chronic cardiotoxicity induced by the chemotherapeutic drug adriamycin, and also can cooperate with the therapeutic effect of the chemotherapeutic drug at the same time. On the basis, the invention provides a combined treatment strategy based on a CCL2 neutralizing antibody, and the cardiotoxicity problem and tumor drug resistance challenge in the clinical application of the adriamycin are solved at the same time through targeted regulation and control of a CCL2 signal channel.

The present disclosure provides a novel salt of 5-chloro-2-fluoro-4-((4-fluoro-2-(methyl(2-(methylamino)ethyl)amino)phenyl)amino)-N-(thiazol-4-yl)benzenesulfonamide and a method for preparing the same. The mesylate salt of 5-chloro-2-fluoro-4-((4-fluoro-2-(methyl(2-(methylamino)ethyl)amino)phenyl)amino)-N-(thiazol-4-yl)benzenesulfonamide, which may be prepared using methanesulfonic acid and, without wishing to be bound by theory, can exhibit reduced hygroscopicity and improved physicochemical stability and solubility. In some aspects, the present disclosure provides a pharmaceutical composition for preventing or treating a sodium channel blocker-related disease, comprising the mesylate salt of 5-chloro-2-fluoro-4-((4-fluoro-2-(methyl(2-(methylamino)ethyl)amino)phenyl)amino)-N-(thiazol-4-yl)benzenesulfonamide.

An insecticidal composition containing cybenzoxasulfyl and the use thereof. The insecticidal composition contains active ingredient A and active ingredient B, wherein active ingredient A is cybenzoxasulfyl, and active ingredient B is selected from one or more of the following compounds: an acetylcholinesterase inhibitor, a nicotinic acetylcholine receptor (nAChR) channel blocker, nicotinic acetylcholine receptor (nAChR) allosteric modulator site I, a nicotinic acetylcholine receptor (nAChR) competitive modulator, a glutamate-gated chloride channel (GluCl) allosteric modulator, etc. The composition has reasonable components, good insecticidal effects, and low administration costs, and also has the characteristics of a reduced application amount, safety to crops, reduced pesticide residues, etc.

The application relates to the technical field of medicines, in particular to a K + Application of a channel blocker in preparation of a medicine for treating liver fibrosis. The application provides a K + New use of an old drug, a channel blocker (sotalol), sotalol is clinically used as an antiarrhythmic drug, and simultaneously has the characteristics of inhibiting K + Channel, experiments show that sotalol can effectively inhibit liver fibrosis and reduce the expression of fibrosis-related protein a-SMA, and the specific approach is to regulate the expression and / or function of autophagy and EMT molecules to realize the inhibition of liver stellate cell fibrosis, thereby providing a new drug selection for clinically treating liver fibrosis.

To provide formulations for providing pain relief in humans and animals by administering a preservative-free intranasal dose of a local anesthetic formulation for the treatment of tri-geminal neuralgia, facial neuropathic pain, facial cancer induced neuropathic pain, migraine pain, and cluster headache pain.SOLUTION: A nasal spray formulation comprises from about 5% to about 30% w / v of a locally active sodium channel blocker, from about 0.25% to about 5% w / v of a buffering agent, and from about 5% to about 99% w / v of a pharmaceutically acceptable carrier for nasal administration. The nasal spray formulation is preferably contained in a mechanical multi-dose pump which sprays a unit dose of the nasal spray formulation with a wide plume and small droplet size, and the unit dose is administered by actuating the mechanical multi-dose spray pump device and spraying a certain amount of the nasal spray formulation into each nostril of a human subject. Preferably, the nasal spray formulation does not include a preservative.SELECTED DRAWING: None

The present disclosure provides a method for delaying preliminary tumor metastasis. The method involves: (a) preparing a composition containing at least one calcium channel blocker (CCB), or a pharmaceutically acceptable salt thereof, either alone or in combination with one or more therapeutic compounds; and (b) administering a therapeutically effective amount of the composition, typically in the range of 2-16 mg, to a subject in need. The disclosure particularly pertains to the use of such compositions for delaying tumor metastasis, with Amlodipine being the most preferred calcium channel blocker in the formulation.

Provided herein is a pharmaceutical composition comprising two or more compounds, wherein each compound is independently a phosphodiesterase inhibitor, an adenosine receptor antagonist, a calcium channel blocker, a histamine H1-receptor agonist, a histamine H2-receptor agonist, a histamine H3-receptor antagonist, or a β2-adrenoreceptor agonist. Also provided herein is a method of treating, preventing, or ameliorating a cardiovascular disease in a subject, comprising administering to the subject in need thereof two or more compounds, wherein each compound is independently a phosphodiesterase inhibitor, an adenosine receptor antagonist, a calcium channel blocker, a histamine H1-receptor agonist, a histamine H2-receptor agonist, a histamine H3-receptor antagonist, or a β2-adrenoreceptor agonist.

The invention discloses an external eye protection liquid for relieving asthenopia and a preparation method thereof.The eye protection liquid comprises a plant-derived calcium channel blocker, a divalent metal ion source, a temperature-sensitive gel matrix and a deep eutectic solvent system, has unique reversible phase change characteristics, is flowing sol during low-temperature storage, and can be used for relieving asthenopia. And after contacting the ocular surface, in-situ phase change is rapidly generated to form semi-solid gel. In the preparation process, a choline chloride-propylene glycol deep eutectic solvent is adopted to carry out low-temperature in-situ extraction on plant raw materials, an extracting solution is directly used as a functional component to be reserved in the preparation, and a cold-soluble compounding process of a poloxamer matrix is matched, so that the damage of high temperature to active components in the whole process is avoided. The problems that a traditional aqueous solution is short in retention time on the ocular surface and low in bioavailability, and the drug effect is damaged by a high-temperature process are solved, and deep eyestrain is effectively relieved through physical and physiological dual mechanisms.

The present invention provides compositions and methods of preventing, alleviating, or treating a subject with a toxic agent-induced injury. The present invention also provides compositions and methods of preventing, alleviating, or treating a tissue damage caused by exposure to a toxic agent or restoring at least a portion of normal tissue function. In some embodiments, the methods include administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising at least one potassium channel blocker. In some embodiments, the potassium channel blocker comprises 4-aminopyridine, a derivative thereof, or a combination thereof. In some embodiments, the pharmaceutical composition can be administered with an additional therapeutic agent, such as an anticonvulsant.

An insecticidal composition containing oxazosulfyl and a use thereof, relating to the technical field of pesticides. The insecticidal composition comprises an active ingredient A and an active ingredient B, wherein the active ingredient A is oxazosulfyl; and the active ingredient B is selected from one or more of the following compounds: an acetylcholinesterase inhibitor, a nicotinic acetylcholine receptor (nAChR) channel blocker, an nAChR allosteric modulator site I, an nAChR competitive modulator, a glutamate-gated chloride channel (GluCl) allosteric modulator, etc. The composition has a reasonable formulation, good insecticidal efficacy, and low application costs, and has the characteristics of reduced application amount, safety to crops, reduced pesticide residue, etc.

The present disclosure relates to methods and pharmaceutical compositions of angiotensin converting enzyme inhibitor and calcium channel blocker, particularly stable oral liquid compositions including angiotensin converting enzyme inhibitor, calcium channel blocker and one or more pharmaceutically acceptable excipients for the treatment of hypertension, coronary artery disease, heart failure, acute myocardial infarction and other related cardiovascular diseases.

The present invention relates to a synergistic pesticidal composition for controlling pest infection in plants, more particularly to a synergistic composition comprising at least three active ingredients selected from (I) a mitochondrial complex I electron transport inhibitor selected from Tolfenpyrad; (II) acetyl-CoA carboxylase inhibitor selected from Spidoxamat, Spirodiclofen, Spiromesifen, Spiropidion, and Spirotetramat; and (III)nicotinic acetylcholine receptor (nAChR) channel blocker is selected as Thiocyclam Hydrogen Oxalate. The invention further relates to a process of preparing said composition along with one or more inactive excipient and formulation thereof. The composition overcomes the pest infestations much more efficiently and provides the advantages of overcoming the resistance of the pest to the use of the individual components of the pesticide composition, improved shelf life, increased spectrum of activity, better crop quality, enhanced efficacy, and economic and ecological advantages i.e. more yield, less expensive and environmentally safe composition.

Compositions and methods for treating or preventing a condition related to myocardial infarction and infarct expansion, extension, and / or dilation following a cardiovascular disorder incident (e.g., post-myocardial infarction) using an effective amount of RRx-001, or a pharmaceutically acceptable salt thereof, are described. In some embodiments, an agent (such as a statin, an angiotension-converting-enzyme (ACE) inhibitor, aspirin, oxygen, a nitric oxide donor, a drug-eluting stent, an anticoagulant or antiplatelet therapy, a phosphodiesterase-5 inhibitor, a calcium channel blocker, an angiotensin II receptor blocker (ARB), a beta blocker, an aldosterone antagonist, a loop diuretic, an epigenetic inhibitor, and / or a nitrite) is administered prior to, concurrently with, or subsequent administering the effective amount of RRx-001, or a pharmaceutically acceptable salt thereof. In some embodiments, the effective amount of RRx-001, or a pharmaceutically acceptable salt thereof, is administered as a composition comprising a blood product and / or the agent.

To provide a method for treating hot flash in a subject.SOLUTION: A method has administering a therapeutically effective amount of a transient receptor potential channel (TRP channel) blocker or pharmaceutically acceptable salt thereof. Preferably, the TRP channel blocker is a TRP channel subfamily V member 1 (TRPV1) blocker, or a pharmaceutical equivalent, analog, derivative, or salt thereof.SELECTED DRAWING: None

The present disclosure relates to methods and pharmaceutical compositions of angiotensin converting enzyme inhibitor and calcium channel blocker, particularly stable oral liquid compositions including angiotensin converting enzyme inhibitor, calcium channel blocker and one or more pharmaceutically acceptable excipients for the treatment of hypertension, coronary artery disease, heart failure, acute myocardial infarction and other related cardiovascular diseases.

A method and composition for modulating male fertility are disclosed, centered on the targeted alteration of transmembrane channel-like (TMC) protein function, activity, or gene expression. Small molecules or pharmaceutically acceptable salts or solvates thereof are provided to modulate the activity or expression of TMC proteins, such as TMC5, in testis tissue. The compositions may include TMC5 channel blockers, dimerization inhibitors, TMC5-CIB1 interaction inhibitors, or small interfering RNAs targeting TMC5 mRNA, optionally formulated with a pharmaceutically acceptable carrier and capable of crossing the blood-testis barrier. Methods of diagnosing male infertility are also provided, comprising quantitating TMC5 expression or activity and comparing to a standard to identify infertility. These approaches enable reversible, non-hormonal regulation of spermatogenesis and fertility, offering new therapeutic strategies for male contraception and infertility treatment.