发明名称 N-PHENYL ANTHRANILIC ACID DERIVATIVES AND USES THEREOF
摘要 Compounds that can be used as openers or blockers of voltage-dependent potassium channels, and which are useful in the treatment of conditions such as central or peripheral nervous system disorders through the modulation of potassium ion flux through voltage-dependent potassium channels and/or depressing or enhancing cortical and/or peripheral neuron activity, compositions containing same and methods utilizing same are disclosed. Also disclosed are modulators of voltage-dependent potassium channels, which exhibit blocking of a TRPV1 channel, and hence are useful in the treatment of TRPV1-related conditions.
申请公布号 US2014316008(A1) 申请公布日期 2014.10.23
申请号 US201414318774 申请日期 2014.06.30
申请人 Ramot at Tel-Aviv University Ltd. 发明人 ATTALI Bernard;PERETZ Asher
分类号 C07C237/20 主分类号 C07C237/20
代理机构 代理人
主权项 1. A method of blocking a transient receptor potential vanilloid 1 (TRPV1) in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of a compound represented by Formula IV: wherein: Z is an A-G(=K)-X-Y group, and wherein: A is alkyl or absent; G is selected from the group consisting of C, S and PRa; K is selected from the group consisting of O and S; X is selected from the group consisting of NRb, O, S or absent; and Y is selected from the group consisting of hydrogen, alkyl, hydroxyalkyl, cycloalkyl, heteroalicyclic, aryl and a polyalkylene glycol residue, R1 is selected from the group consisting of hydrogen, alkyl, cycloalkyl or aryl; each of R2, R3, R4, R5, R6, R7, R8, R9 and R10 is independently selected from the group consisting of hydrogen, alkyl, hydroxyalkyl, trihaloalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, heteroalicyclic, halo, hydroxy, alkoxy, aryloxy, thiohydroxy, thioalkoxy, thioaryloxy, sulfinyl, sulfonyl, cyano, nitro, an electron-withdrawing group, amino and —NR15R16, or, alternatively, at least two of R2, R3, R4, R5 and R6, of R7, R8, R9 and R10 form a five- or six-membered aromatic, heteroaromatic, alicyclic or heteroalicyclic ring; R15 and R16 are each independently selected from the group consisting of hydrogen, alkyl, cycloalkyl, aryl, carbonyl and sulfonyl, or, alternatively R15 and R16 form a five- or six-member heteroalicyclic ring; and each of said Ra and Rb is selected from the group consisting of hydrogen, alkyl, cycloalkyl and aryl.
地址 Tel-Aviv IL