发明名称 Inhibitors of beta-catenin in treatment of colorectal cancer
摘要 Compounds are disclosed which are effective for inhibiting β-catenin or disrupting a β-catenin/Tcf-4 complex, and for causing effective attenuation of colon carcinogenesis. The compounds may be effective treatment for colorectal cancer (CRC) when administered in an effective dose to a patient afflicted therewith.
申请公布号 US9616047(B2) 申请公布日期 2017.04.11
申请号 US201514788373 申请日期 2015.06.30
申请人 Regents of University of Minnesota 发明人 Bode Ann Marie;Dong Zigang;Kanamata Reddy Srinivasa Reddy
分类号 A61K31/404;A61K31/4184;A61K31/454;A61K31/4545;C07D209/34;C07D209/38 主分类号 A61K31/404
代理机构 Schwegman, Lundberg & Woessner, P.A. 代理人 Schwegman, Lundberg & Woessner, P.A.
主权项 1. A method of inhibiting β-catenin or disrupting a β-catenin/Tcf-4 complex, comprising contacting the β-catenin with an effective amount or concentration of a compound of formula (II): and pharmaceutically acceptable salts thereof, wherein: q is 2, two adjacent R8 groups, together with the carbon atoms to which they are attached, form a substituted or unsubstitued (C6-C12)aryl group or a (C4-C12) heterocyclyl group, and Q is (C4-C12)heterocyclyl or (C6-C12)aryl; q is 1, R8 is independently hydrogen, (C1-C6)alkyl, (C1-C6)haloalkyl, SR7 (wherein R7 is hydrogen or (C1-C6)alkyl), OR7, amino, —O(C1-C6)alkyl, —(C6-C12)aryl or halo, and Q is (C4-C12)heterocyclyl or (C6-C12)aryl; or q is 0 and Q is a pyrydinyl group; X is O, S or NR7; s is 0, 1, 2, 3 or 4; each R10 is independently hydrogen, SR7, OR7, amino, —O(C1-C6)alkyl, —(C6-C12)aryl or halo; X3 is absent, O, S, C(R7)2 or NR7; t is 0, 1, 2, 3, or 4; each R9 is independently hydrogen, SR7 , OR7, amino, —O(C1-C6)alkyl, —(C6-C12)aryl or halo; and R11 is hydrogen, (C1-C6)alkyl or (C6-C12)aryl-(C1-C6)alkyl; or R11 is absent when the nitrogen to which R11 would otherwise be attached, is attached to Q; or an R10 and an R9 group, together with the atoms to which they are attached, form an substituted or unsubstituted ring; or two adjacent R9 groups, together with the atoms to which they are attached, form a substituted or unsubstitued (C6-C12)aryl or a (C4-C12)heterocyclyl.
地址 Minneapolis MN US