Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorder
Noah Bell,Christopher Carreras,Dominique Charmot,Jeffrey W. Jacobs,Michael Robert Leadbetter,Marc Navre
申请号：
US14592200
公开号：
US09408840B2
申请日:
2015.01.08
申请国别(地区):
US
年份:
2016
代理人:
摘要：
The present disclosure is directed to compounds of the structure (X):CoreL-NHE)n (X)wherein:n is 2 or 3NHE has the structurewherein:R1 is H or —SO2—NR7R8—R2 is selected from H, —NR7(CO)R8, —SO2—NR7R8— and —NR7R8R3 is hydrogenR7 is hydrogenR8 is a bond linking to LL is a polyalkylene glycol linker andCore has the following structure:wherein:X is selected from the group consisting of a bond, —O—, —NH—, NHC(═O)—, —NHC(═O)NH— and —NHSO2— andY is selected from the group consisting of a bond, optionally substituted C1-6 alkylene, optionally substituted benzene, pyridinyl, a polyethylene glycol linker and —(CH2)1-6O(CH2)1-6—, and methods of using such compounds for the treatment of irritable bowel syndrome, chronic kidney disease and end-stage renal disease.
