公开(公告)号：US08829009B2

公开(公告)日：2014-09-09

申请号：US13573818

申请日：2012-10-09

申请人： Alexander Vasillevich Ivashtchenko ,  Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk

发明人： Alexander Vasillevich Ivashtchenko ,  Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The present invention relates to novel substituted 2-amino-3-(arylsulfonyl)pyrazolo[1,5-a]pyrimidines of general formula 1, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions, to medicaments, methods for preparation thereof, and to methods for prophylaxis and treatment of various CNS diseases, pathogenesis of which is associated with disturbance of monoaminergic signaling pathways, more specifically over- or hypo-activation of serotonin 5-HT6 receptors.In general formula 1 R1 and R3 independently of each other represent C1-C3 alkyl or phenyl; R2 represents hydrogen or C1-C3 alkyl; R41, R42 independently of each other represent hydrogen, optionally substituted C1-C3 alkyl or optionally substituted phenyl, or R41 and R42 together with the nitrogen atom they are attached to form optionally substituted heterocyclyl; Ar is aryl selected from phenyl, optionally substituted with Ri5 that is one or two optionally identical substituents selected from hydrogen, lower alkyl, trifluoromethyl or halogen; or optionally substituted 5-6-membered heteroaryl, containing as the heteroatom nitrogen or sulfur atom.

摘要翻译： 本发明涉及通式1的新的取代的2-氨基-3-（芳基磺酰基）吡唑并[1,5-a]嘧啶，5-羟色胺5-HT 6受体拮抗剂，新药物和药物组合物，药物，方法 以及用于预防和治疗各种CNS疾病的方法，其发病机制与单胺能信号通路的紊乱相关，更具体地说是5-羟色胺5-HT 6受体的过激活或低激活。 在通式1中，R 1和R 3彼此独立地表示C 1 -C 3烷基或苯基; R2代表氢或C1-C3烷基; R 41，R 42彼此独立地表示氢，任选取代的C 1 -C 3烷基或任选取代的苯基，或R 41和R 42与它们连接的氮原子一起形成任选取代的杂环基; Ar是选自苯基的芳基，任选被R 15取代，R 15是选自氢，低级烷基，三氟甲基或卤素的一个或两个任选相同的取代基; 或含有杂原子氮或硫原子的任选取代的5-6元杂芳基。