公开(公告)号：EP2657225A2

公开(公告)日：2013-10-30

申请号：EP11851231.8

申请日：2011-12-13

申请人： Ivachtchenko, Alexandre Vasilievich ,  Alla Chem, LLC.

发明人： MITKIN, Oleg Dmitrievich ,  KADIEVA, Madina Georgievna

IPC分类号： C07C317/36 ,  C07D263/48 ,  C07D215/38 ,  C07D215/42 ,  C07D213/34 ,  C07D213/38 ,  C07D295/096 ,  C07D471/04 ,  C07D413/04 ,  C07D413/14 ,  C07D211/84 ,  C07D307/64 ,  C07D401/04 ,  C07D409/04 ,  C07D333/34 ,  C07D333/36 ,  C07D317/32 ,  C07D307/66 ,  A61K31/422 ,  A61K31/4706

CPC分类号： C07D471/04 ,  C07C317/36 ,  C07D213/40 ,  C07D215/42 ,  C07D295/135 ,  C07D413/04 ,  C07D413/14

摘要： The present invention relates to novel substituted methyl-amines, serotonin 5-HT 6 receptor antagonists, to active components, pharmaceutical compositions, method for prophylaxis and treatment of CNS diseases and "molecular tools", in which novel substituted methyl-amines represent compounds of the general formula 1 and their crystalline forms and pharmaceutically acceptable salts,

wherein:
W represents benzene, naphthalene, indolizine, quinoline or oxazole cycle;
R1 = H, F, Cl;
R2 represents hydrogen, fluoro, methyl, phenyl, thienyl, furan-2-yl, pyridyl, piperazin-1-yl or 4-methylpiperazin-1-yl; R3 represents cyclopropyl or optionally substituted methyl; with the exception of the compounds in which W simultaneously represents oxazole cycle and R2 = phenyl or pyridyl.

摘要翻译： 本发明涉及新的substituiertem甲基cardamines，血清素5-HT 6受体拮抗剂，至活性成分，药物组合物，用于CNS疾病和“分子工具”的预防和治疗方法，其中，新颖substituiertem甲基cardamines代表的化合物 通式1及其晶体形式及其药学上可接受的盐，worin：W darstellt苯，萘，中氮茚，喹啉或恶唑环; R1 = H，氟，氯; R2 darstellt氢，氟，甲基，苯基，噻吩基，呋喃-2-基，吡啶基，哌嗪-1-基或4-甲基哌嗪-1-基; R3 darstellt环丙基或任选取代的甲基; 与化合物除外，其中W同时darstellt恶唑周期和R2 =苯基或吡啶基。