185 results about "Channel blocker" patented technology

The present patent application relates to compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein one of R1, R2 and R3 is a non-cyclic acidic group having a pKa value below 8 or a group which is in vivo convertible to such a group; R4, R5 and the other two of the substituents R1, R2 and R3 are each independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro, amnino, and aryl, aralkyl, arylamino, aryloxy, aryl-CO-, or heteroaryl, wherein the aryl and heteroaryl groups may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, hydroxy, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro and amino; or R3 and R4 or R4 and R5 together form a fused 4- to 7-membered carbocyclic ring which may be unsaturated, or partially or fully saturated, while the other substituents R1, R2, R3, R4 and R5 are as defined above; Y is -CO-, -CS-, -SO2-, or -C(=N-R8)-, wherein R8 is hydrogen, alkyl, or cyano; X is -NH-, -CH2-NH-, or -SO2-NH-; Z is NR6, O, -CH=CH-, -C=C-, -N=CH-, or -CH=N-; wherein R6 is hydrogen, or alkyl; R11, R12, R13, R14 and R15 are each independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro, amino, -NHSO2-R7, -COOR7, -SO2N(R7)2, -SO2OR7 and -CO-R7, wherein R7 is hydrogen alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl or aralkyl; and aryl, aralkyl, arylamino, aryloxy, aryl-CO-, or heteroaryl, wherein the aryl and heteroaryl groups may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, hydroxy, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro and amino; or one of R11 and R12, R12 a

Preferred embodiments of the present invention are related to novel therapeutic drug combinations and methods for treating and/or preventing pulmonary arterial hypertension and/or stable angina. More particularly, aspects of the present invention are related to therapeutic combinations comprising a Rho-kinase inhibitor, such as fasudil, and one or more additional compounds selected from the group consisting of prostacyclins, such as iloprost, endothelin receptor antagonists, PDE inhibitors, calcium channel blockers, 5-HT_2A antagonists, such as sarpogrelate, selective serotonin reuptake inhibitors, such as fluoxetine, statins, and vascular remodeling modulators, such as Gleevec.

A method of preserving, storing and transplanting mammalian donor organs. The method includes the cooling of refrigeration preservation, loading pre-freezer preservation, cryopreservation and washing solutions at least containing polyvinylpyrrolidone, a calcium channel blocker, a nucleoside, potassium chloride, polyethylene glycol, at least one amino acid, and a steroid to a temperature of 2° to 4° C. and/or of 0° to 2° C., harvesting a donor organ, perfusing it with one or more of the solution, immersing it in one or more of the solutions and storing it at a temperature above 0° C. or at a temperatures below 0° C. The cryopreservation solution also contains cryopreservative agents. Preserved organs may be transplanted directly from refrigeration storage or from freezer storage by cooling the washing refrigeration preservation solutions to 2° to 4° C., perfusing the organ with washing solution and then preservation solution, and transplanting it.

Controlled release of pharmaceutical agents using microspheres or other controlled release systems are used to treat disease state characterized by aberrant electrical activity in excitable tissue. For the treatment of epilepsy, agents useful in the treatment of epilepsy may be delivered to the patient at the site of seizure origin to control seizure activity in a time release manner. The inventive system may also be useful in the treatment of cardiac arrhythmias and pre-term labor. Particularly useful pharmaceutical compositions comprising a site 1 sodium channel blocker are also provided.

The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.

The invention relates to substituted pyridine compounds of Formula I: (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R^1a, R^1b, R^2a, R^2b, R^2c, A¹, A², and X are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.

The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.

The present invention relates to sodium channel blockers. The present Invention also includes a variety of methods of treatment using these inventive sodium channel blockers.

The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.

The invention relates to substituted pyridine compounds of Formula I: (I) or a pharmaceutically acceptable salt, prodrug, or solvate thereof wherein A¹, X, A², R^1a, R^1b, R^1c, G, and z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.

The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.