摘要 |
Provided herein are small molecule triazolothienopyrimidine compounds that inhibit urea transport activity of solute transporters, particularly the UT-B transporter. The compounds described herein are useful for increasing solute clearance in states of fluid overload and for treating refractory edema associated with cardiovascular, renal, and metabolic diseases, disorders, and conditions. |
主权项 |
1. A method for treating a disease or disorder treatable by inhibiting transport of urea in a subject, said method comprising administering to the subject a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of structure (I): or a single stereoisomer, a mixture of stereoisomers, tautomer or pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted aryl or optionally substituted heteroaryl; R2 is —N(R5)(R6); R3 and R4 are each independently hydrogen, alkyl, halo or haloalkyl; R5 is hydrogen or alkyl; and R6 is optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclylalkyl, optionally substituted aralkyl, or optionally substituted heteroarylalkyl; or R5 and R6, together with the nitrogen atom to which they are attached, form an optionally substituted N-heterocycle, or optionally substituted N-heteroaryl. |