发明名称 PRO-DRUG COMPOUNDS
摘要 A compound according to formula (I) or a hydrate, solvate, or pharmaceutically acceptable salt thereof: wherein where the integers Q, R2, A, R1, Z1, Z2, and Z3 are as defined in claim 1.;
申请公布号 US2016016929(A1) 申请公布日期 2016.01.21
申请号 US201314776151 申请日期 2013.12.23
申请人 PROXIMAGEN LIMITED 发明人 SAVORY Edward;HILL Daniel;KOCIAN Oldrich
分类号 C07D311/68;C07D405/12;C07D403/12 主分类号 C07D311/68
代理机构 代理人
主权项 1. A compound according to formula (I) or a hydrate, solvate, or pharmaceutically acceptable salt thereof: wherein: Z1, Z2, and Z3 are each independently selected from H, F, and Cl; Q is O; R2 is H; A is a direct bond, —C(O)O*—, —C(R3)(R4)O*—, or —C(O)NH*, wherein the atom marked * is directly connected to R1; R3 and R4 are selected independently from H, fluoro, C1-4 alkyl, and C1-4 fluoroalkyl; or R3 and R4 together with the atom to which they are attached form a cyclopropyl group; R1 is selected from any one of the groups [1], [2], [3], [4], [5], [6], [7], [8], [9] and [10], wherein the atom marked ** is directly connected to A: n is 0, 1, 2, or 3; R5 is hydrogen; R6 is —CH2CH(OH)CH2OH, or —CH2CH2R9; R7 and R7b are independently selected from H, C1-4 alkyl, and C1-4 fluoroalkyl, R8 and R8b are independently selected from H, C1-4 alkyl, C1-4 fluoroalkyl, and the side chain of a natural or unnatural alpha-amino acid; or R7 and R8 together with the atom to which they are attached form a C3-7 carbocyclic ring; R9 is selected from —N(R11)(R12), —N+(R11)(R12)(R13)X−, —N(R11)C(O)R14, —SO3H, and —OP(O)(OH)2; wherein R11, R12, and R13 are independently selected from H, C1-4 alkyl, and C1-4 fluoroalkyl; or R11 and R12 together with the nitrogen atom to which they are attached form a 4-7 membered heterocyclic ring optionally substituted with one or more groups selected from H, fluoro, C1-4 alkyl, C1-4 fluoroalkyl, C1-4 alkoxy, and —C(O)R3; or in the case where R1 is group [7] and R9 is —NR11R12, wherein R11 is hydrogen, C1-4 alkyl, or C1-4 fluoroalkyl, and R12 is C1-4 alkyl, or C1-4 fluoroalkyl, then R12 may join together with R8b such that R12 and R8b, together with the nitrogen to which R12 is attached, form a 5 or 6 membered cyclic amine group; R14 is H, C1-4 alkyl, or C1-4 fluoroalkyl; X− is a pharmaceutically acceptable anion; R15 is 3-pyridyl or 1,4-dihydro-1-methyl-pyridin-3-yl; Y is —O—, —CH2—, —N(H)—, or —N(CH3)—; R27 is H, C1-4 alkyl, or C1-4 fluoroalkyl, and R28 is H, C1-4 alkyl, or C1-4 fluoroalkyl.
地址 London GB