公开(公告)号：US20110136853A1

公开(公告)日：2011-06-09

申请号：US13059419

申请日：2009-08-03

申请人： Andrey Alexandrovich Ivaschenko ,  Nikolay Filippvich Savchuk ,  Alexander Vasilievich Ivashchenko

发明人： Andrey Alexandrovich Ivaschenko ,  Nikolay Filippvich Savchuk ,  Alexander Vasilievich Ivashchenko

IPC分类号： A61K31/437 ,  A61P25/00 ,  A61P25/28 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P9/10 ,  A61P3/04

CPC分类号： A61K31/437 ,  C07D471/04

摘要： The present invention is directed to the novel ligand with wide range of pharmacological activity including activity to GPCR receptors, ion channels and monoamine transporters representing 3-methyl-9-benzyl-1,2,3,4-tetrahydrocarboline naphthalene-1,5-disulfonate of formula 1 The invention is also directed to the novel drug substance, Pharmaceutical formulation comprising the novel drug substance, and to the method for its preparation, to the novel medicaments, and method for treatment of CNS diseases including neurodegenerative diseases and cognitive disorders at humans and warm blooded animals.

摘要翻译： 本发明涉及具有广泛的药理学活性的新型配体，包括GPCR受体的活性，离子通道和代表3-甲基-9-苄基-1,2,3,4-四氢咔啉萘-1,5-二酮的单胺转运体， 式1的二磺酸盐本发明还涉及新药物，包含新药物的药物制剂及其制备方法，新药物和治疗CNS疾病的方法，包括神经变性疾病和认知障碍 人类和温血动物。

公开(公告)号：US20110053915A1

公开(公告)日：2011-03-03

申请号：US12808152

申请日：2008-12-12

申请人： Andrey Alexandrovich Ivaschenko ,  Yan Vadimovich Lavrovsky ,  Sergey Viktorovich Malyarchuk ,  Ilya Matusovich Okun ,  Nikolay Filippovich Savchuk ,  Sergey Yevgenievich Tkachenko ,  Alexander Viktorovich Khvat ,  Alexander Vasilievich Ivaschenko

发明人： Andrey Alexandrovich Ivaschenko ,  Yan Vadimovich Lavrovsky ,  Sergey Viktorovich Malyarchuk ,  Ilya Matusovich Okun ,  Nikolay Filippovich Savchuk ,  Sergey Yevgenievich Tkachenko ,  Alexander Viktorovich Khvat ,  Alexander Vasilievich Ivaschenko

IPC分类号： A61K31/55 ,  A61K31/5025 ,  C07D487/04 ,  A61K31/5377 ,  A61K31/542 ,  C07D513/04 ,  A61P35/00 ,  A61K31/437 ,  C07D471/04 ,  A61K31/519 ,  C07D495/04 ,  A61K31/454 ,  A61K31/496 ,  A61K31/438 ,  A61K31/4545 ,  C07D401/04 ,  C07D215/58 ,  A61K31/47 ,  A61K31/4365

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信号系统的生物化学特征的用途，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。