ПЕЛЛЕТЬЕ Марк Ф. (US),ФАРР Джордж Уилльам (US),МАКГИРК Пол Роберт (US),ХОЛЛ Кристофер Х. (US),БОРОН Уолтер Ф. (US)
申请号：
RU2014148984
公开号：
RU2014148984A
申请日:
2013.05.08
申请国别(地区):
RU
年份:
2016
代理人:
摘要：
1. A method of treating or controlling a disease or condition selected from edema, epilepsy, optoneuromyelitis, migraine, hyponatremia, retinal ischemia and delayed excess fluid, comprising administering to a patient in need thereof an effective amount of a compound of formula 1a: in which R, R, R , R and R are selected from H, halogen, halogenated alkyl C, and a cyano group； and R6 is selected from H and a physiologically hydrolyzable and acceptable acyl； in free form or in the form of a pharmaceutically acceptable salt. 2. A method for treating or controlling an aquaporin-mediated disease or condition selected from myocardial ischemia, myocardial infarction, myocardial hypoxia and congestive heart failure, comprising administering to a patient in need thereof phenylbenzamide in an amount effective to inhibit aquaporin in which phenylbenzamide is a compound of the formula 1a: in which R, R, R, R and R are selected from H, halogen, halogenated alkyl C, and a cyano group； and R is selected from H and a physiologically hydrolyzable and acceptable acyl； in free form or in the form of a pharmaceutically acceptable salt. 3. The method according to claim 1 or 2, in which R is selected from trifluoromethyl, chlorine, fluorine, and bromine； R and R are the same or different and are selected from trifluoromethyl, chlorine, fluorine and bromine； and R and Roba are H.4. The method of claim 3, wherein R is selected from chlorine and bromine； R and Roba are trifluoromethyl； and R and R, and R are all H.5. The method of claim 1 or 2, wherein R is a phosphono group which may or may not be substituted. The method of claim 1 or 2, wherein the compound of formula 1a is selected from: 7. A method according to claim 1, wherein the compound of formula 1a is in free form or in the form of a pharmaceutically acceptable salt. The method of claim 1, in the cat1. Способ лечения или контроля заболевания или состояния, выбранного из отека, эпилепсии, оптиконевромиелита, мигрени, гипонатриемии,
