发明名称 FUNCTIONALIZED FURAN-2-SULFONAMIDES EXHIBITING ENDOTHELIAL LIPASE INHIBITION
摘要 The present invention relates to pharmaceutical compositions comprising furan-2-sulfonamide derivatives. The present invention further relates to methods of treatment of diseases or conditions associated with endothelial lipase activity, including coronary artery disease and low HDL-C.
申请公布号 US2016257672(A1) 申请公布日期 2016.09.08
申请号 US201415028164 申请日期 2014.10.06
申请人 TEMPLE UNIVERSITY-OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION ;SHIFA BIOMEDICAL CORPORATION 发明人 Abou-Gharbia Magid;Childers Wayne E.;Martinez Rogelio;Ghidu Victor P.;Meyers Harold;Mousa Shaker A.;Elshourbagy Nabil
分类号 C07D405/12;C07D487/08;C07D471/08 主分类号 C07D405/12
代理机构 代理人
主权项 1. A compound having the formula (I): including hydrates, solvates, enantiomers, diastereomers, pharmaceutically acceptable salts, prodrugs and complexes thereof, wherein:A is selected from a group consisting of CR1aR1b, sulfur, oxygen, and NR7;X is selected from a group consisting of oxygen, sulfur, and NH;Z isR1a and R1b are each independently selected from a group consisting of optionally substituted C1-C6 alkyl, optionally substituted C3-C8 cycloalkyl, optionally substituted aryl, optionally substituted arylalkyl, and optionally substituted heteroaryl;R1a and R1b are taken together with the atoms to which they are bound to form a ring containing 3 to 6 atoms;R2 is selected from a group consisting of optionally substituted C3-C7 cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted biphenyl,R3 is selected from a group consisting of hydrogen, C1-C6 alkyl, and C3-C7 cycloalkyl;R4 is selected from a group consisting of hydrogen, C1-C6 alkyl, and C3-C7 cycloalkyl;R5a nd R5b are at each occurrence independently selected from a group consisting of hydrogen, optionally substituted C1-C6 alkyl, and optionally substituted C3-C7 cycloalkyl;R5a and R5b are taken together with the atoms to which they are bound to form a ring containing 3 to 6 atoms;R6a nd R6b are at each occurrence independently selected from a group consisting of hydrogen, optionally substituted C1-C6 alkyl, and optionally substituted C3-C7 cycloalkyl;R6a and R6b are taken together with the atoms to which they are bound to form a ring containing 3 to 6 atoms;R6a and R6b are taken together with the atoms to which they are bound to form a ring containing 3 to 6 atoms;R7 is selected from a group consisting of hydrogen, optionally substituted C1-C6 alkyl, and optionally substituted C3-C7 cycloalkyl;R8 at each occurrence is independently selected from a group consisting of hydrogen, halogen, cyano, optionally substituted C1-C6 alkyl, optionally substituted C1-C6 alkoxy, optionally substituted C3-C8 cycloalkyl, OH, NH2, NH(C1-C6 alkyl), N(C1-C6 alkyl)2, NO2, C1-3 haloalkyl, C1-3 haloalkoxy, SH, S (C1-C6 alkyl), and 3-10 membered cycloheteroalkyl containing 1 to 4 heteroatoms selected from N, O and S;m=1, 2, 3, or 4;n=1, 2, 3, or 4;y=0, 1, or 2; with the proviso that the compound is not the compound of formula (II):
地址 Philadelphia PA US