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THERAPEUTIC AGENTS AIMED AT SHORTENED PROTEINS OF ADENOMATOUS POLYPOSIS COLI (APC)

机译:腺瘤性息肉(APC)缩短蛋白中产生的治疗剂

摘要

FIELD: medicine; pharmaceuticals.;SUBSTANCE: invention relates to a compound of formula I-b:; ;(Formula I-b),;where L is SO2, each R1 and R2 is independently selected from a group consisting of H and C1-4 alkyl; R3 is selected from a group consisting of C1-3 alkyl, optionally substituted with R21; ring is selected from a group consisting of; , , , , , , , , , , and $; each R4, R5, R7 and R8 is independently selected from a group consisting of H, F, Cl, Br, C1-4 alkyl, N3, NH2, CF3, OCHF2, OCF3, OC1-4 alkyl, benzoyl, -OCH2C≡CH, CN, and NO2; R6 is selected from a group consisting of H, Br and R17; R9 is H; R10 is H or Br; each R11, R12 and R13 independently represents H, F, Cl or Br; each R14, R15 and R16 independently represents H, methyl or ethyl; R17 is phenyl, optionally substituted with one or more substitutes selected from the group consisting of NO2 and -NR18CO-(C1-4alkyl); each R18 independently represents H; each R21 is independently selected from a group, consisting of H, CN and OR22; each R22 independently represents H; and to compounds of similar structure, presented by specific chemical formulas, as well as to a pharmaceutical composition for treating colon cancer, comprising a therapeutically effective amount of such compounds, and a method of treating colon cancer.;EFFECT: therapeutic agents aimed at truncated proteins of adenomatous polyposis coli (APC) are proposed.;9 cl, 62 dwg, 1 tbl, 3 ex
机译:领域:医学;物质:本发明涉及式I-b的化合物: ;(式Ib),;其中L是SO 2 ,每个R 1 和R 2 独立地选自H和C 1-4 烷基; R 3 选自C 1-3 烷基,其任选地被R 21 取代;环选自: ,<图像文件=” 00000417.JPG“ he =” 15“ imgContent =” undefined“ imgFormat =” JPEG“ wi =” 14“ />,<图像文件= “ 00000418.JPG” he =“ 15” imgContent =“未定义” imgFormat =“ JPEG” wi =“ 21” />,<图像文件=“ 00000419.JPG” he =“ 19” imgContent =“未定义” imgFormat =“ JPEG“ wi =” 15“ />,<图像文件=” 00000420.JPG“ he =” 17“ imgContent =” undefined“ imgFormat =” JPEG“ wi =” 18“ />,<图像文件=” 00000421.JPG “ he =” 12“ imgContent =” undefined“ imgFormat =” JPEG“ wi =” 18“ />,<图像文件=” 00000422.JPG“ he =” 16“ imgContent =” undefined“ imgFormat =” JPEG“ wi = “ 18” />,<图像文件=“ 00000423.JPG” he =“ 16” imgContent =“ undefined” imgFormat =“ JPEG” wi =“ 18” />,<图像文件=“ 00000424.JPG” he =“ 13“ imgContent =” undefined“ imgFormat =” JPEG“ wi =” 17“ />,和$ ; R 4 ,R 5 ,R 7 和R 8 分别独立地选自H, F,Cl,Br,C 1-4 烷基,N 3 ,NH 2 ,CF 3 ,OCHF 2 ,OCF 3 ,OC 1-4 烷基,苯甲酰基,-OCH 2 C≡CH,CN,和NO 2 ; R 6 选自H,Br和R 17 ; R 9 是H; R 10 为H或Br; R 11 ,R 12 和R 13 分别独立地表示H,F,Cl或Br。 R 14 ,R 15 和R 16 分别独立地表示氢,甲基或乙基。 R 17 是苯基,可选地被一个或多个选自NO 2 和-NR 18 CO-(C < Sub> 1-4 烷基);每个R 18 独立代表H;每个R 21 独立地选自H,CN和OR 22 ;每个R 22 独立代表H;以及具有特定化学式的结构相似的化合物以及用于治疗结肠癌的药物组合物,其包括治疗有效量的此类化合物,以及用于治疗结肠癌的方法。提出了腺瘤性息肉病大肠杆菌(APC)的蛋白质。; 9 cl,62 dwg,1 tbl,3 ex

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