发明名称 Substituted Triazines for Malaria Treatment and Chemoprophylaxis
摘要 Disclosed herein are triazine compounds and methods of making and using thereof to treat malaria, provide chemoprophylaxis, and/or treat or inhibit infection by one or more Plasmodium spp.
申请公布号 US2015210652(A1) 申请公布日期 2015.07.30
申请号 US201414426275 申请日期 2014.03.13
申请人 The United States of America, as represented by the Secretary of the Army, on behalf of the Walter 发明人 Sciotti Richard J.;Reichard Gregory A.;Pannone Kristina M.;Zottig Victor E.
分类号 C07D251/22;A61K45/06;C07D401/04;C07D471/08;C07D487/08;C07D251/18;A61K31/5377;A61K31/53;C07D401/12 主分类号 C07D251/22
代理机构 代理人
主权项 1. A compound of formula Iwherein R1 is a 5-10 membered aromatic ring having 0-4 ring heteroatoms each independently selected from the group consisting of nitrogen, oxygen, and sulfur, wherein each substitutable ring carbon is independently substituted by —Rc, and wherein each substitutable ring nitrogen is independently substituted by —R, or R1 is benzopyan, branched or unbranched —(C1-C6)alkyl, orwherein Y is —CH, —CR, or N; R2 is a nitrogen attached 5-8 membered monocyclic ring or a nitrogen attached 7-8 membered bicyclo ring system, and further having 0-2 ring heteroatoms each independently selected from the group consisting of nitrogen, oxygen, and sulfur, wherein each substitutable ring carbon is independently substituted by —Rc, and wherein and each substitutable ring nitrogen is independently substituted by —R, or R2 isand wherein: L and L′ are each independently a linker selected from the group consisting of a bond, a substituted or unsubstituted —(C1-C6)alkyl- which may be branched or unbranched, andwherein Ring L is a 5-7 membered cyclic or aromatic ring and m and m′ are independently 0-3; Ra and Ra′ are each independently H or branched or unbranched —(C1-C6)alkyl; Rb and Rb′ are each independently —CO2R, branched or unbranched —(C1-C6)alkyl, branched or unbranched —(C2-C8)alkyl substituted with an —OR, —NRR′, or —N(O)RR′ group on one of the C2-C8 carbons, naphthyl, or a 3-7 membered ring having 0-2 ring heteroatoms each independently selected from the group consisting of nitrogen, oxygen, and sulfur, wherein each substitutable ring carbon is independently substituted by —Rc, and wherein each substitutable ring nitrogen is independently substituted by —R; Rc and Rc′ are each independently selected from the group consisting of H, halo, trihalomethyl, trihalomethoxy, branched or unbranched —(C1-C6)alkyl, phenyl, branched or unbranched —(C1-C6)alkyl-OR, —C(═O)R, —CO2R, —S(O)2R, —OR, —NO2, —CN, —NH2, —NRR′, —NHC(═O)R, —NHC(OR)═O, —C(O)NRR′, —S(O)nR, and —SO2NRR′ (wherein NRR′ can form a 4 to 6 member ring), wherein n is 0, 1, or 2; and R and R′ are each independently H, branched or unbranched —(C1-C6)alkyl, branched or unbranched —(C1-C6)alkyl alcohol, or —CO2—(C1-C6)alkyl; wherein where nitrogen is present as a heteroatom, it is at least 2 carbon atoms from any nitrogen atom attached to the triazine ring, and wherein the ring carbons next to a ring nitrogen are not substituted with —OR, —NO2, —NH2, —NRR′, —NHC(O)R, —NHC(O)OR, —S(O)nR, or —SO2NRR; or a pharmaceutically acceptable salt thereof.
地址 Fort Detrick MD US