发明名称 MIF inhibitors and their uses
摘要 The invention relates to MIF inhibitors; compositions comprising an effective amount of a MIF inhibitor; and methods for treating or preventing diseases associated with MIF.
申请公布号 US9133164(B2) 申请公布日期 2015.09.15
申请号 US201214237136 申请日期 2012.04.13
申请人 INNOV88 LLC 发明人 Gaweco Anderson;Walker John;Monahan Joseph B.;Cubbage Jerry W.;Carroll Jeffery
分类号 C07D215/227;C07D401/12;C07D215/56;C07D295/185;C07D401/04;C07D401/14;C07D409/14;C07D205/04 主分类号 C07D215/227
代理机构 代理人
主权项 1. A compound of Formula III: or a pharmaceutically acceptable salt, hydrate, solvate or tautomer thereof, wherein: each of X5, X6, X7, and X8 is independently CR7 or N; L is a bond or NR2; one of W or W′ is N and the other is CH; each n and p is independently 1, 2, or 3; Y1 is a bond, —C(O)— or —NR2—; Z1 is a bond, —C(O)—, —N(R3)— or —SO2—; R1 is —C1-C6 alkyl, branched or unbranched optionally substituted with halogen or —CN, —C2-C6 alkene branched or unbranched,—C2-C6 alkyne, optionally substituted with —C1-C3 alkyl,—C3-C4 cycloalkyl, optionally substituted with —C1-C3 alkyl or —CN, or—a nonaromatic monocyclic heterocycle, optionally substituted with —C1-C3 alkyl; R2 is H or —C1-C6 alkyl; R3 is H or —C1-C6 alkyl; R5 is H, —C1-C6 alkyl, —C2-C6 alkene, —(C0-C3 alkyl)-(C3-C6)cycloalkyl, —(C2-C6 alkyl)-O—(C1-C3 alkyl), —(C2-C6 alkyl)-O—(C3-C6)cycloalkyl, —(C2-C6 alkyl)-O-aryl, —(C2-C6 alkyl)-O-heteroaryl, —(C2-C6alkyl)-NR8R9, —(C1-C3 alkyl)heteroaryl or —(C1-C3 alkyl)aryl, wherein R5 is optionally substituted; R6 is selected from the group consisting of —CN, —NO2, —CO2H, C(O)-Rx; —CO2Rx; and —CO2NRxRy, wherein Rx and Ry are each independently —C1-C6 alkyl, and wherein Rx and Ry, when taken together with the nitrogen to which they are attached, form a heterocycle containing from one to three heteroatoms selected from N, O, and S; R7 is H, F, Cl, —CF3, —CN, —CO2-alkyl, —C1-C6 alkyl, —C3-C7(cycloalkyl), —O—(C1-C6 alkyl), —OCF3, —SO2NH2 or SO2-alkyl; R8 and R9 are each independently H, —C1-C6 alkyl, —(C0-C6 alkyl)aryl, C0-C3 alkyl)-C3-C6(cycloalkyl), —C(O)—C1-C3 alkyl, —C(O)—C2-C3 alkene; or R3 and R4, when taken together with the nitrogen to which they are attached, can form a heterocycle containing from one to three heteroatoms selected from N, O, and S, and wherein R8 and R9 are optionally substituted; and Y1 and Z1 are not both a bond.
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