243 results about "Potassium channel" patented technology

This invention includes pharmaceutical compositions, methods and kits for the treatment or diagnosis of a malignant tumors, including brain tumors, and diseases or disorders characterized by abnormal brain tissue.

Drug-naive and drug-free schizophrenic PBL were screened to identify additional markers that are differentially expressed compared to healthy individuals using microarray and quantitative real-time PCR (QRT-PCR) techniques. Genes for dopamine D2 receptor (DRD2) and inwardly rectifying potassium channel (Kir2.3) were found to be overexpressed in microarray analysis. Increased mRNA levels were confirmed by QRT-PCR using SybrGreen method and dual labeled TaqMan probes.The invention relates to a method for diagnosing schizophrenia in a subject comprising assessing the level or the expression level of at least one of the following genes or proteins: Kir2.3 or DRD2 or a gene encoding Kir2.3 or DRD2. The invention further relates to agents and uses thereof, said agents specifically binding to said proteins or nucleic acids encoding them, diagnostic kits and screening methods.Use of both molecular markers allow prediction of schizophrenia and help to follow efficiency of drugs in therapy in order to provide a more tailored medication for schizophrenic patients.

Compounds, compositions and methods are provided which are useful in the treatment of conditions such as central or peripheral nervous system disorders through the modulation of potassium ion flux through voltage-dependent potassium channels and / or depressing cortical and / or peripheral neuron activity are disclosed. Novel derivatives of N-phenylanthranilic acid are also disclosed.

The present invention provides novel N-substituted fluorooxindoles having the general Formula I wherein the wavy bond represents the racemate, the (R)-enantiomer or the (S)-enantiomer and m, n, p, q, A, B, D, Q, X, and Z are as defined below, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of potassium channels.

The present invention provides compositions and methods for the treatment of central nervous system damage in a subject. More particularly, the invention provides a combination therapy for the treatment of a central nervous system ischemic condition or a central nervous system traumatic injury comprising the administration to a subject of a potassium ion channel modulator in combination with a cyclooxygenase-2 selective inhibitor.

Analogs of ShK toxin and methods for using such ShK analogs. The ShK analogs generally comprise ShK toxin attached to a chemical entity (e.g. an atom, molecule, group, residue, compound, moiety, etc.) that has an anionic charge. In some embodiments the chemical entity attached to the ShK toxin may comprise an amino acid residue. The ShK analogs may be administered to human or non-human animal subjects to cause inhibition of potassium channels or to otherwise treat diseases or disorders. In some embodiments, the chemical entity to which the ShK toxin is attached may be chosen to provide selective inhibition of certain potassium channels (e.g., Kv1.3 channels) over other potassium channels (e.g., Kv1.1 channels). In come embodiments, the chemical entity to which the ShK toxin is attached may include a fluorophore, thereby providing a fluorophore tagged ShK analog. Such fluorophore tagged ShK analogs may be used in flow cytometry alone, or in conjunction with class II tetramers that can detect autoreactive cells.

Flavonoids, especially luteolin, are shown to be effective against insulin dependent (Type I) and insulin independent (Type II) diabetes mellitus. It is demonstrated that luteolin works in mammals by binding and blocking the Kv1.3 potassium channel of T-cell and Beta cells. Antidiabetic and anti-autoimmune compounds can be selected by measuring their ability to bind to and block the Kv1.3 channel.

The present invention concerns certain isoquinolinone compounds and their utility as inhibitors of voltage-dependent potassium channels or currents, such as Kv1.5 and IKur, that could serve as targets for the treatment of cardiac arrhythmias especially atrial arrhythmias. The present invention also provide a method for treating or preventing conditions which respond to the inhibition of potassium channels or currents, such as cardiac arrhythmias and more especially atrial arrhythmias. The present invention further includes pharmaceutical formulations and a process of making a pharmaceutical composition comprising a compound of certain isoquinolinone or its pharmaceutically acceptable salts, hydrates, solvates, crystal forms, and stereoisomers thereof, and a pharmaceutically acceptable carrier.

The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.

The present invention provides amine derivatives represented by formula I, its isomers, racemes or optical isomers, pharmaceutical salts thereof, its amides or esters, pharmaceutical compositions containing said compounds and the preparation methods thereof. The invention also relates to the use of the above mentioned compounds in the preparation of drugs for the prophylaxis or treatment of cardiovascular diseases, diabetes, bronchial and urinary smooth muscle spasm as well as ischemic and anoxic nerve injury. The above compounds can be used to treat hypertension, angina diaphragmatic, myocardial infarction, congestive heart failure, arrhythmia, diabetes, spasmodic bronchial diseases, spasmodic bladder or ureter diseases, and depression.

Analogs of ShK toxin and methods for using such ShK analogs. The ShK analogs generally comprise ShK toxin attached to a chemical entity (e.g. an atom, molecule, group, residue, compound, moiety, etc.) that has an anionic charge. In some embodiments the chemical entity attached to the ShK toxin may comprise an amino acid residue. The ShK analogs may be administered to human or non-human animal subjects to cause inhibition of potassium channels or to otherwise treat diseases or disorders. In some embodiments, the chemical entity to which the ShK toxin is attached may be chosen to provide selective inhibition of certain potassium channels (e.g., Kv1.3 channels) over other potassium channels (e.g., Kv1.1 channels). In come embodiments, the chemical entity to which the ShK toxin is attached may include a fluorophore, thereby providing a fluorophore tagged ShK analog. Such fluorophore tagged ShK analogs may be used in flow cytometry alone, or in conjunction with class II tetramers that can detect autoreactive cells.

A compound of formula (I)wherein A, R1, R3, and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment of arrhythmia, maintaining normal sinus rhythm, IKur-associated disorders, and other disorders mediated by ion channel function.

The invention discloses a hair-growing composition and application thereof. The hair-growing composition is mainly prepared from the following components in parts by mass: 0.1 to 5 parts of pyrrolidyldiaminopyrimidine oxide and 0.1 to 5 parts of dimethyl sulfone, wherein the pyrrolidyl diaminopyrimidine oxide can promote the telophase in the hair life cycle to be changed into anagen; the dimethylsulfone provides an organic sulfur nutrient source as a necessary condition for the synthesis of keratin fibers and also can remove free radicals and inhibit inflammation; by combined use of the twosubstances, multiple effects of promoting blood circulation, opening potassium channels, and promoting the proliferation of hair follicle cells and the expression of human keratin fibers can be realized; a good hair growth effect is achieved from inside to outside.

The present invention relates to compounds of structural formula I: I useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.

Compositions of matter comprising 5-phenoxyalkoxypsoralen compounds and their method of synthesis and use. The compounds are useable to treat diseases or disorders in human or animal subjects, including autoimmune diseases. The compounds inhibit potassium channels, including the Kv1.3 channel and at least some of the therapeutic effects of such compounds may be due at least in part to potassium channel inhibition. In some embodiments, the compounds are more selective for certain potassium channels (e.g., Kv1.3 channels) than other potassium channels (e.g., Kv1.5 channels).

The invention is related to a novel primate specific brain isoform of the potassium channel KCNH2 and genetic association with risk for schizophrenia.

A compound of formula (I) wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur associated disorders, and other disorders mediated by ion channel function.

A hybrid protein contains a protein that binds to a receptor of mastocytes and basophils and is endocyted by them. The protein can be IgE; IgE fragment; IgE Fc fragment; antibody against IgE receptor of mastocytes and basophils; fragment of the antibody against the IgE receptor of mastocytes and basophils; antibody against mastocyte specific potassium channel; and mast cell degranulating peptide. The hybrid protein also contains a protease cleaving proteins of the secretion process of the mastocytes and basophils so as to inhibit the secretion process without killing the mastocytes and basophils. The protease can be light chain Clostridium botulinum toxin; proteolytically active fragment of the light chain of a Clostridium botulinum toxin containing an amino acid sequence His-Xaa-Xaa-Xaa-His-Xaa-Xaa-His wherein Xaa is an amino acid; light chain of the tetanus toxin; proteolytically active fragment of the light chain of the tetanus toxin containing His-Asp-Leu-Ile-His-Val-Leu-His; IgA protease of Neisseria gonorrhoeae; and proteolytic domain of the IgA protease of Neisseria gonorrhoeae.

This invention provides a bypass bridge comprising a tract of gap junction-coupled cells having a first end and a second end, both ends capable of being attached to two selected sites in a heart so as to allow the conduction of a pacemaker and / or electrical signal / current across the tract between the two sites, wherein the cells functionally express a sodium channel. The invention also provides related methods of making the bypass bridge, methods of implanting same in a heart, and methods of treating a disorder associated with an impaired conduction in a subject's heart.

A method for treatment of cardiac arrhythmias is disclosed. The method comprises the combining of a sodium channel blocking medication and a potassium channel blocking medication into a therapeutic dosage and the delivery of the therapeutic dosage to a patient in treatment of a heart rhythm problem. The heart rhythm problems being treated include atrial fibrillation and atrial or ventricular tachycardia. Preferably, the therapeutic dosage is at least one tablet and the concentration of each medication is determined based upon the heart problem being treated, the underlying heart rate, the QT interval and other comorbid conditions of the patient. A pharmaceutical composition for the therapeutic treatment of cardiac arrhythmias in a patient is also provided having a combination of a sodium channel blocking medication and a potassium channel blocking medication. Under certain conditions of the patient, the composition can also include a beta blocking medication.

The present invention provides substituted 3,3-diphenyl indanone, indane and indole compounds, as well as analogues thereof which are specific, potent and safe inhibitors of the Ca.sup.2+-activated potassium channel (Gardos channel) of erythrocytes. The compounds can be used as efficacious drugs in the treatment of sickle cell disease and diseases characterized by unwanted or abnormal cell proliferation, and in particular inflammatory diseases associated with unwanted cellular proliferation.

This invention relates to novel aromatic heterocyclic carboxylic acid amide derivatives of formula (I) that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels.

The present invention provides compounds of formula (I): (Formula (I); wherein A, R1, R2, R3I, V, X, and Z are defined herein, which are potassium channel inhibitors. The invention further provides pharmaceutical compositions comprising the compounds of formula (I) and their use in therapy, in particular in treatment of diseases or conditions that are mediated by Kir3.1 and / or Kir3.4 or any heteromultimers thereof, or that require inhibition of Kir3.1 and / or Kir3.4 or any heteromultimers thereof.

The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.

The present invention discloses a category of isoquinoline compounds or the salts as shown in the right formula, the preparation method and the application in preparation of anti-arrhythmic drugs. Wherein, R1 and R2 represent OCH3, OCH2Ph or are connected to be -OCH2O-. The compound pf the present invention has strong anti-arrhythmic activity, and in particular, has activity of blocking the potassium channel and the function of anti-chamber abnormity.

Potassium channels Kv1.3 are known to be implicated in immunological diseases and graft rejections. Disclosed are peptides capable of blocking with high affinity and specificity potassium channels Kv1.3, their pharmaceutical compositions, and methods for their use to block Kv1.3 potassium channels, to treat various immunological conditions and to diagnostic applications. Methods for their chemical synthesis and correct folding are also disclosed. Exemplary peptides correspond to protein components (Vm23 and Vm24) isolated from the venom of the Mexican scorpion Vaejovis mexicanus smithi. Vm23 and Vm24 bind to hKv1.3 channels in an almost irreversible manner, showing a Kd value in the order of 3 picomolar range, when applied to human lymphocytes cultures in vitro. Vm24 was chemically synthesized and used in in vivo experiments to successfully treat sensitized rats (on the DTH-response). Neither Vm24 nor synthetic Vm24 is toxic to mice when injected at relatively high concentrations (assayed up to 10,000 micrograms per kilogram mouse body weight). These peptides (Vm24 and Vm23) and their functional equivalent analogs with at least 83% of sequence identity are lead compounds, candidates for the treatment of various immunological conditions and diagnostic applications.

Disclosed are methods of selectively delivering a medicant to an abnormal brain region and / or to a malignant tumor in a mammalian subject, including a human. A medicant is administered simultaneously or substantially simultaneously with a potassium channel agonist (other than bradykinin or a bradykinin analog), such as NS-1619,1-EBIO, a guanylyl cyclase activator, a guanylyl cyclase activating protein, minoxidil, pinacidil, cromakalim, or levcromakalim, whereby the medicant is delivered selectively to the cells of the abnormal brain region and / or to the tumor, compared to normal tissues. Thus, among the disclosures is a method of treating a malignant tumor in a human subject. Also disclosed are pharmaceutical compositions that combine a potassium channel agonist together with a medicant and a kit for enhancing the delivery of a medicant to an abnormal brain region and / or to a malignant tumor.

The invention relates to the field of a biotechnology, especially to a molecular design of a targeted potassium channel Kv1.3 active polypeptide and its preparation and application thereof. The polypeptide provided by the invention has an amino acid sequence as shown in the SEQ ID NO:1. The polypeptide has higher selectivity and lower potential toxic effects than polypeptide which is applied as a potassium channel Kv1.3 blocker in the prior art, and is an efficient low-toxicity blocker of a targeted potassium channel Kv1.3.