公开(公告)号：US08486945B2

公开(公告)日：2013-07-16

申请号：US12808152

申请日：2008-12-12

申请人： Andrey Ivashchenko ,  Yan Lavrovsky ,  Sergey Malyarchuk ,  Ilya Okun ,  Nikolay Savchuk ,  Sergey Tkachenko ,  Alexander Khvat ,  Alexander Ivashchenko

发明人： Andrey Ivashchenko ,  Yan Lavrovsky ,  Sergey Malyarchuk ,  Ilya Okun ,  Nikolay Savchuk ,  Sergey Tkachenko ,  Alexander Khvat ,  Alexander Ivashchenko

IPC分类号： A01N43/58 ,  A61K31/50 ,  C07D487/00

CPC分类号： C07D487/04 ,  A61K9/0019 ,  A61K9/2018 ,  A61K9/205 ,  A61K9/2059 ,  A61K9/4858 ,  C07D215/58 ,  C07D401/04 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

摘要： The invention relates to novel heterocyclic compounds and to the use thereof, to pharmaceutical compositions containing said chemical compounds as an active ingredient and to the use thereof for producing medicinal preparations for the human being and warm-blood animals for treating diseases caused by the aberrant activity of an Hedgehog (Hh)-signal system, in particular oncological diseases. The invention also relates to the use of the above-mentioned compounds in the form of ‘molecular pharmacological tools’ for examining (in vitro and in vivo) the biochemical features of the Hh-signal system, in particular, the interaction of Hh protein and transmembrane proteins, namely, suppressor Patched (Ptc) and protooncogenic proteins. The eight groups of the claimed compounds comprise the derivatives of 2,6-dihydro-7H-pyrazolo[3,4-d]pyridazine-7-one and 1,4-dihydropyrazolo[3,4-b][1,4]thiazine-5-one; N-acidylated 4-imidazo[1,2-a]pyrimidine-2-il-anilines; ([4H-thino[3,2-b]pyrrol-5-il) carbonyl]piperidine-4-carbonic acid amides; 2-(4carbomoilpyperidine-1-il)-isonicotinic acid amides; N-sylphonyl-1,2,3,4-tetrahydroquinoline-6-carbonic acid amides; and pyridine 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]N-acidylated 3-azole derivatives.

摘要翻译： 本发明涉及新颖的杂环化合物及其用途，含有所述化合物作为活性成分的药物组合物及其用于生产用于治疗由异常活性引起的疾病的人和温血动物的药物制剂的用途 刺猬（Hh） - 信号系统，特别是肿瘤疾病。 本发明还涉及以“分子药理学工具”形式的上述化合物用于检查（体外和体内）Hh信号系统的生化特征的用途，特别是Hh蛋白和 跨膜蛋白，即抑制剂Patched（Ptc）和原癌蛋白。 所要求保护的八个化合物组包括2,6-二氢-7H-吡唑并[3,4-d]哒嗪-7-酮和1,4-二氢吡唑并[3,4-b] [1,4] 噻嗪-5-酮; N-酸化的4-咪唑并[1,2-a]嘧啶-2-基]苯胺; （[4H-噻吩并[3,2-b]吡咯-5-基）羰基]哌啶-4-碳酸酰胺; 2-（4-氰基吡啶-1-基） - 异烟酰胺; N-磺酰基-1,2,3,4-四氢喹啉-6-碳酸酰胺; 和吡啶2-氨基-4,5,6,7-四氢噻吩并[2,3-c] N-酸化的3-唑衍生物。