A number of DNA methylation inhibitors are described. The DNA methylation inhibitors were identified using a two-component enhanced green fluorescent protein reporter system to screen a compound library containing procainamide derivatives. The DNA methylation inhibitors can be used for cancer therapy and prevention.

A number of DNA methylation inhibitors are described. The DNA methylation inhibitors were identified using a two-component enhanced green fluorescent protein reporter system to screen a compound library containing procainamide derivatives. The DNA methylation inhibitors can be used for cancer therapy and prevention.

PROBLEM TO BE SOLVED: To provide a nasal drop reduced in irritation caused by applying steroid to the nose.SOLUTION: The nasal drop reduced in irritation contains one or more species selected from the group consisting of flunisolide beclomethasone and their derivatives one or more species selected from the group consisting of menthol camphor borneol and geraniol and one or more species selected from the group consisting of chlorobutanol lidocaine dibucaine procaine procainamide and methyl aminob...

The present invention relates to immobilized procainamide analogs as well as to a method of making immobilized procainamide analogs. These immobilized analogs are prepared by activating the carboxyl group on a substituted p-benzoic acid derivative toward nucleophilic attack; reacting the activated benzoic acid derivative with a polyamine to produce the benzoic acid derivative of Formula 3: and binding the benzoic acid derivative of Formula 3 to a latex polymer having functional groups that react...

The invention provides a therapeutic method for preventing or treating a pathological condition or symptom in a mammal such as a human wherein the infectivity of a pathogen such as a retrovirus toward mammalian cells is implicated and inhibition of its infectivity is desired comprising administering to a mammal in need of such therapy an effective amount of procaine procainamide or an analog thereof that inhibits pathogenic infectivity including pharmaceutically acceptable salts thereof.(From US...

The invention provides a therapeutic method for preventing or treating a pathological condition or symptom in a mammal such as a human wherein the infectivity of a pathogen such as a retrovirus toward mammalian cells is implicated and inhibition of its infectivity is desired comprising administering to a mammal in need of such therapy an effective amount of procaine procainamide or an analog thereof that inhibits pathogenic infectivity including pharmaceutically acceptable salts thereof.

The present invention relates to immobilized procainamide analogs as well as to a method of making immobilized procainamide analogs. These immobilized analogs are prepared by activating the carboxyl group on a substituted p-benzoic acid derivative toward nucleophilic attack; reacting the activated benzoic acid derivative with a polyamine to produce the benzoic acid derivative of Formula 3: and binding the benzoic acid derivative of Formula 3 to a latex polymer having functional groups that react...

1. A method of administering a drug for which the major clearance mechanism in humans is CYP2D6 (CYP-cytochrome P-450) mediated oxidative biotransformation or a pharmaceutically acceptable salt thereof in combination with a CYP2D6 inhibitor or a pharmaceutically acceptable salt thereof to a human in need of the intended pharmaceutical activity of such drug wherein said drug for which the major clearance mechanism in humans is CYP2D6 mediated oxidative biotransformation is selected from the group...

Novel derivatives of procainamide and N-acetylprocainamide (NAPA) are disclosed having formula (a) wherein: X = hydrogen or acetyl; R1 = an alkyl group having 1 to 3 carbon atoms; m = an integer from 2 to 10; R2 = an alkyl cycloalkyl or aryl group having 2 to 10 carbon atoms; Z = a poly(amino acid); and n = 1 to p where p = MW of Z/1000. The derivatives include maleimide conjugates of proteins or poly(amino acids) enzymes enzyme donor polypeptides and labelling substances. Novel activated hapten...

PURPOSE: To obtain a readily producible sustained release tablets free from variability of release rate affected by pH in digestive tube enzyme etc. and free from adhesion to mucosa of esophagus and digestive tube comprising a drug and fine water-insoluble cellulosic polymer.CONSTITUTION: A drug is uniformly blended with fine water-insoluble cellulosic polymer (e.g. hydroxypropyl cellulose having low degree of substitution crystalline cellulose or carboxymethyl cellulose) and if necessary an exc...