发明名称 Bivalent ligands for the treatment of neurological disorders
摘要 Bivalent ligands that contain two pharmacophores linked through a spacer, one of which interacts with the μ-opioid receptor (MOR) and the other of which interacts with the co-receptor CC chemokine receptor 5 (CCR5), are used for the treatment of neurological disorders such as those associated with AIDS.
申请公布号 US8946254(B2) 申请公布日期 2015.02.03
申请号 US201314371075 申请日期 2013.01.10
申请人 Virginia Commonwealth University 发明人 Zhang Yan;Hauser Kurt F.;Selley Dana E.
分类号 A61K31/485;C07D489/08 主分类号 A61K31/485
代理机构 Whitham Curtis Christofferson & Cook, PC 代理人 Whitham Curtis Christofferson & Cook, PC
主权项 1. A bivalent ligand of Formula I, wherein R1 and R2 may be the same or different, and are independently selected from: H; a saturated or unsaturated, branched or unbranched, substituted or unsubstituted carbon group or chain comprising from 1-20 carbon atoms; NO−; NO−2; CO; COR8 wherein R8 is H or a saturated or unsaturated, branched or unbranched, substituted or unsubstituted carbon group or chain comprising from 1-20 carbon atoms; SO3−2; and SO4−2;R3 may be present or absent and may be H; H2; O; C1-12alkyl; —COOR9 where R9 is C1-12alkyl; CR10 where R10 is a cyclic or polycyclic saturated or unsaturated homo- or heterocyclic ring system comprising 1, 2, 3, 4, or more rings with from 3 to 7 atoms per ring in the system;R4 and R5 may be present or absent; may be the same or different, and are independently selected from H; halogen; a saturated or unsaturated, branched or unbranched, substituted or unsubstituted carbon group or chain comprising from 1-20 carbon atoms; a cyclic or polycyclic saturated or unsaturated homo- or heterocyclic ring system comprising 1, 2, 3, 4, or more rings with from 3 to 7 atoms per ring in the system, which may be fused to one or more atoms of the triazole ring; and a heteroatomic group;R6 and R7 may be the same or different, and are independently selected from: H; halogen; a saturated or unsaturated, branched or unbranched, substituted or unsubstituted carbon group or chain comprising from 1-20 carbon atoms; a cyclic or polycyclic saturated or unsaturated homo- or heterocyclic ring system comprising 1, 2, 3, 4, or more rings with from 3 to 7 atoms per ring in the system, which may be fused to one or more atoms of the hexane ring; and a heteroatomic group; andX=a branched or unbranched, saturated or unsaturated carbon chain comprising from 1-20 carbon atoms, and may include a heteroatomic group;as well as salts, protonated and unprotonated and stereoisomeric forms thereof.
地址 Richmond VA US