发明名称 COMPOUNDS FOR THE TREATMENT OF MALARIA
摘要 Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of malaria.;
申请公布号 US2016152617(A1) 申请公布日期 2016.06.02
申请号 US201414900245 申请日期 2014.06.20
申请人 THE BROAD INSTITUTE, INC. ;PRESIDENT AND FELLOWS OF HARVARD COLLEGE 发明人 COMER Eamon;MUNOZ Benito;BEAUDOIN Jennifer A.;LE QUEMENT Sebastian T.;SCHERER Christina;DUVALL Jeremy;KATO Nobutaka;MAETANI Micah;BRAIBANT Bertrand
分类号 C07D471/20;C07D498/22 主分类号 C07D471/20
代理机构 代理人
主权项 1. A compound according to Formula (I): wherein a and b are independently 0, 1, or 2; c is 0, 1, 2, 3, or 4; R1 is hydrogen, C1-C6 alkyl, C2-C9 heteroaryl, C3-C10 carbocyclyl C1-C6 alkyl, C6-C10 aryl C1-C6 alkyl, C2-C9 heteroaryl C1-C6 alkyl, —C(O)NR7R8, —C(O)OR9, —C(O)R10, or —S(O)2R11; each R2 is independently hydroxyl, halogen, or —OR12; R3 is hydrogen or C1-C6 alkyl; R4 is hydrogen or C1-C6 alkyl; R5 is C1-C6 alkyl, or —(CH2)nX1R13, or R5 and R6 together with the carbon and nitrogen atoms to which they are respectively attached, combine to form a 5-8-membered heterocycle; R6 is hydrogen, C1-C6 alkyl, C1-C6 perfluoroalkyl, C3-C10 carbocyclyl C1-C6 alkyl, C6-C10 aryl C1-C6 alkyl, C2-C9 heteroaryl C1-C6 alkyl, C2-C9 heterocyclyl C1-C6 alkyl, N-protecting group, —C(O)R15, —C(O)NR16R17, or —S(O)2R18; R7 is hydrogen or C1-C6 alkyl; R8 is C6-C10 aryl, C2-C9 heteroaryl, C2-C9 heterocyclyl, or C3-C10 carbocyclyl; R9 is C1-C6 alkyl or C6-C10 aryl; R10 is C1-C6 alkyl, C6-C10 aryl, C2-C9 heterocyclyl, C6-C10 aryl C1-C6 alkyl, or C2-C9 heteroaryl C1-C6 alkyl; R11 is C1-C6 alkyl, C6-C10 aryl, or C6-C10 aryl C1-C6 alkyl; each R12 is C1-C6 alkyl or C1-C6 acyl; n is 1, 2, 3, 4, 5, or 6; X1 is absent, 0, or NR14; R13 is hydrogen, C1-C6 alkyl, C1-C6 heteroalkyl, C1-C6 perfluoroalkyl, C1-C6 acyl, C6-C10 aryl C1-C6 alkyl, an O- or N-protecting group, or R13 and R14 combine to form a 5-8-membered heterocycle; R14 is hydrogen or C1-C6 alkyl; R15 is C1-C6 alkyl, C1-C6 perfluoroalkyl, C1-C6 heteroalkyl, C3-C10 carbocyclyl, C2-C9 heterocyclyl, C6-C10 aryl, C6-C10 aryl C1-C6 alkyl; R16 and R17 are independently hydrogen, C1-C6 alkyl, or C6-C10 aryl; and R18 is C1-C6 alkyl, C1-C6 perfluoroalkyl, C3-C10 carbocyclyl, or C6-C10 aryl; wherein the compound is not compound 12, compound 15, or any one of compounds 78-135 of Table 1, or a pharmaceutically acceptable salt thereof.
地址 Cambridge MA US