发明名称 MODULATION OF K2P CHANNELS
摘要 Disclosed herein inter alia are compositions and methods useful in the treatment of diseases, for example pain, neurodegeneration, or mood disorders, and for modulating the activity of a K2P channel.
申请公布号 US2016031814(A1) 申请公布日期 2016.02.04
申请号 US201514815480 申请日期 2015.07.31
申请人 The Regents of the University of California 发明人 Minor, JR. Daniel L.;Bagriantsev Sviatoslav N.;Renslo Adam R.
分类号 C07D209/88;C07D401/06 主分类号 C07D209/88
代理机构 代理人
主权项 1. A method of treating a disease in a patient in need of such treatment, said method comprising administering a therapeutically effective amount of a compound to said patient, wherein said disease is selected from the group consisting of a neurological disease, pain, migraine, ischemic injury, brain ischemia, stroke, a neurodegenerative disease, a mood disorder, depression, and decompression sickness; and wherein said compound has the formula: wherein L1 is a bond, substituted or unsubstituted alkylene, substituted or unsubstituted heteroalkylene, substituted or unsubstituted cycloalkylene, substituted or unsubstituted heterocycloalkylene, substituted or unsubstituted arylene, or substituted or unsubstituted heteroarylene; L2 is a bond, —O—, —S—, —NH—, —C(O)—, —C(O)NH—, —NHC(O)—, —S(O)—, or —S(O)2—; R1, R2, R4, and R5 are independently hydrogen, halogen, —CF3, —CCl3, —CN, —OH, —NH2, —COOH, —CONH2, —NO2, —SH, —SO2Cl, —SO3H, —SO4H, —SO2NH2, —NHNH2, —ONH2, —NHC═(O)NHNH2, —NHC═(O)NH2, —NHSO2H, —NHC═(O)H, —NHC(O)—OH, —NHOH, —OCH3, —OCF3, —OCHF2, —N3,—C(CH3)3, —OCH2CCH, —NHCH2CCH, —NHCH3, —N(CH3)2, —NHS(O)CH3, —C(O)CH3, —CH3, —CH2CCH, —NHC(O)CH3, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; where R4 and R5 may optionally be joined to form a substituted or unsubstituted cycloalkyl or substituted or unsubstituted heterocycloalkyl; R3 is hydrogen, halogen, —CX3, —CN, —SO2Cl, —SO1R10, —SOvNR7R8, —NHNH2, —ONR7R8, —NHC═(O)NHNH2, —NHC═(O)NR7R8, —N(O)m, —NR7R8, —C(O)R9, —C(O)OR9, —C(O)NR7R8, —OR10, —NR7SO2R10, —N(R7)C═(O)R9, —NR7C(O)—OR9, —NR7OR9, —OCX3, —OCHX2, —OPO(OH)2, —PO(OH)2, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R7, R8, R9, and R10, are independently hydrogen, oxo, halogen, —C(O)CH3, —CF3, —CN, —OH, —NH2, —COOH, —CONH2, —NO2, —SH, —SO2Cl, —SO3H, —SO4H, —SO2NH2, —NHNH2, —ONH2, —NHC═(O)NHNH2, —NHC═(O)CH3, —NHC═(O)NH2, —NHSO2H, —NHC═(O)H, —NHC(O)—OH, —NHOH, —OCF3, —OCHF2, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; where R7 and R8 are bonded to the same nitrogen atom, they may optionally be joined to form a substituted or unsubstituted heterocycloalkyl or substituted or unsubstituted heteroaryl; W is —O—, —S—, —S(O)—, —S(O)2—, or —C(R4)(R5)—; y is 0 or 1; m and v are independently 1 or 2; n is independently 0 to 4; t1 and t2 are independently 1 to 4; X is independently —Cl, —Br, —I, or —F.
地址 Oakland CA US