发明名称 Heteroaryl derivatives and uses thereof
摘要 The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.
申请公布号 US9409893(B2) 申请公布日期 2016.08.09
申请号 US201314074819 申请日期 2013.11.08
申请人 Jacobus Pharmaceutical Company, Inc. 发明人 Heffernan Gavin David;Jacobus David Penman;Saionz Kurt William;Schiehser Guy Alan;Shieh Hong-Ming;Zhao Wenyi
分类号 A61K31/535;A61K38/00;A61P33/00;A01N37/18;C07D413/04;A61K31/343;A61K31/381;A61K31/415;A61K31/4418;A61K31/4439;A61K31/47;A61K31/496;A61K31/505;A61K31/536;A61K31/5377;A61K45/06;C07D213/38;C07D213/64;C07D213/73;C07D215/14;C07D231/12;C07D239/26;C07D307/81;C07D333/28;C07D333/58;C07D213/84;C07D217/16;C07D401/10;C07D241/12;C07D213/36;C07D213/61;C07D213/65;C07D307/80 主分类号 A61K31/535
代理机构 Baker & Hostetler LLP 代理人 Baker & Hostetler LLP
主权项 1. A compound of Formula I: wherein: R1 is heteroaryl attached through a carbon atom of the heteroaryl ring, optionally substituted with 1, 2, or 3 R5; A, B and D are independently are CH or CR2, provided that at least one of A, B, or D is CR2; each R2 is independently C1-10 alkyl, C1-10 haloalkyl, halo, cyano, C3-10 cycloalkyl, —SO2C1-6 alkyl, C6-10 aryl optionally substituted with 1, 2, or 3 R5, or heteroaryl attached through a carbon atom of the heteroaryl ring optionally substituted with 1, 2, or 3 R5; R3 and R3a are independently hydrogen or C1-10 alkyl; R4 and R4a independently are hydrogen, C1-10 alkyl, C1-10 haloalkyl, C3-10 cycloalkyl, C1-10alkC3-10cycloalkyl, or C1-10alkNR7R7a, wherein R7 and R7a are independently H or C1-10alkyl, or R4 and R4a together with the nitrogen through which they are attached, form a heterocyclic ring of 4 to 7 ring atoms, where one carbon ring atom may be optionally replaced with NR6 or O, and where any carbon ring atom may be optionally substituted with C1-6 alkyl or C1-6 alkoxy; each R5 is independently halo, cyano, hydroxy, C1-10 alkyl, C1-10 haloalkyl, C1-10 alkoxy, C1-10 haloalkoxy, C3-10 cycloalky, C3-10 cycloalkoxy, amino, C1-10 alkylamino, C1-10 dialkylamino, C3-10 cycloalkyamino, pyrrolidinyl, C1-10 alkylsulfonyl, sulfamoyl, C1-10 alkylsulfamoyl or C1-10 dialkylsulfamoyl; and R6 is C1-10 alkyl or acetyl; or a pharmaceutically acceptable salt, enantiomer, or diastereoisomer thereof.
地址 Princeton NJ US