abstract |
(57) Formula I: A method of treating a mammal afflicted with a disease responsive to sodium channel blockade, comprising administering to a mammal in need of such treatment an effective amount of Formula I: Wherein Y represents oxygen or sulfur; R 1 , R 21 , R 22 and R 23 independently represent hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl Or R 22 and R 23 together with N form a heterocyclic ring; A 1 and A 2 are each independently optionally substituted aryl, heteroaryl, saturated or X is singly or O, S, NR 24 , CR 25 R 26 , C (O), NR 24 C (O), which is a partially unsaturated carbocycle or a saturated or partially unsaturated heterocycle. , C (O) NR 24 , SO, SO 2 or a covalent bond; R 24 , R 25 and R 26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl Or a carbocyclic or heterocyclic substituted semicarbazone or thiosemicarbazone, or a pharmaceutically acceptable salt or a prodrug thereof, and a systemic and topical thereof. For the treatment of neuronal loss after sexual ischemia, for the treatment or prevention of neurodegenerative diseases such as ALS, for the treatment or prevention of ototoxic and ophthalmic diseases associated with glutamate toxicity, for the treatment or improvement of pain, It provides use as a convulsant, antidepressant, local anesthetic, antiarrhythmic, and in the treatment or prevention of diabetic neuropathy and urinary incontinence. |