公开(公告)号：US20100075975A1

公开(公告)日：2010-03-25

申请号：US12307385

申请日：2007-07-03

申请人： István Gacsalyi ,  Gábor Gigler ,  Márta Agoston ,  Hajnalka Kompagne ,  Szabolcs Kertesz ,  Krisztina Moricz ,  György Levay ,  Gábor Szenas ,  László Gábor Harsing ,  József Barcoczy ,  Gyula Simig

发明人： István Gacsalyi ,  Gábor Gigler ,  Márta Agoston ,  Hajnalka Kompagne ,  Szabolcs Kertesz ,  Krisztina Moricz ,  György Levay ,  Gábor Szenas ,  László Gábor Harsing ,  József Barcoczy ,  Gyula Simig

IPC分类号： A61K31/501 ,  A61P25/00 ,  A61P37/00 ,  A61P25/16

CPC分类号： A61K31/501

摘要： The invention relates the use of 4-chloro-5-{2-[4-(6-fluoro-1,2-benz[d]isoxazole-3-yl)piperidin-1-yl]ethyl-amino}-2-methyl-3-(2H) pyridazinone of the Formula (I) or pharmaceutically acceptable salts thereof for the preparation of medicaments suitable for the improvement of cognitive function or obtaining neuroprotective effect. The medicaments containing 4-chloro-5-{2-[4-(6-fluoro-1,2-benz[d]isoxazol-3-yl)piperidin-1-yl]ethyl-amino}-2-methyl-3-(2H) pyridazinone of the Formula (I) or therapeutically acceptable salt thereof can be used for the treatment or prevention of neuronal death, mental decline, sclerosis multiplex, Creuzfeld-Jacobs disease, Huntington-syndrome, amyotrophic lateral sclerosis, Parkinson-disease, memory disturbance, loss of memory, amnesia, stroke or for the improvement of memory function or learning ability.

摘要翻译： 本发明涉及4-氯-5- {2- [4-（6-氟-1,2-苯并[d]异恶唑-3-基）哌啶-1-基]乙基 - 氨基} -2- （I）的3-甲基-3-（2H）哒嗪酮或其药学上可接受的盐，用于制备适于改善认知功能或获得神经保护作用的药物。 含有4-氯-5- {2- [4-（6-氟-1,2-苯并[d]异恶唑-3-基）哌啶-1-基]乙基 - 氨基} -2-甲基-3 - （2H）哒嗪酮或其治疗上可接受的盐可用于治疗或预防神经元死亡，精神衰退，硬化多发性，克鲁兹菲尔德 - 雅各布氏病，亨廷顿综合症，肌萎缩性侧索硬化，帕金森病 ，记忆障碍，记忆丧失，遗忘，中风或改善记忆功能或学习能力。

公开(公告)号：US07053082B1

公开(公告)日：2006-05-30

申请号：US10030436

申请日：2000-07-04

申请人： Zoltan Greff ,  Geza Szabo ,  Jozsef Barkoczy ,  Zoltan Ratkai ,  Gabor Blasko ,  Gyula Simig ,  Gabor Gigler ,  Bernadett Martonné Marko ,  György Levay ,  Karoly Tihanyi ,  Andras Egyed ,  Annamaria Simo

发明人： Zoltan Greff ,  Geza Szabo ,  Jozsef Barkoczy ,  Zoltan Ratkai ,  Gabor Blasko ,  Gyula Simig ,  Gabor Gigler ,  Bernadett Martonné Marko ,  György Levay ,  Karoly Tihanyi ,  Andras Egyed ,  Annamaria Simo

IPC分类号： A61P25/00 ,  A61K31/551 ,  C07D491/04

CPC分类号： C07D491/04

摘要： The invention relates to new 2,3-benzodiazepine derivatives of general Formula (I), (wherein R1 stands for methyl, formyl, carboxy, cyano, —CH═NOH, —CH═NNHCONH2 or —NR5R6, wherein R5 and R6 independently from each other represent hydrogen or lower alkyl or together with the nitrogen atom, they are attached to, form a 5- or 6-membered, saturated or unsaturated heterocyclic ring optionally containing one or more further nitrogen, sulfur and/or oxygen atom(s); R2 is nitro or amino; R3 stands for hydrogen, lower alkanoyl or CO—NR7R8, wherein R7 and R8 independently from each other stand for hydrogen, lower alkoxy, lower alkyl or lower cycloalkyl or together with the nitrogen atom, they are attached to, form a 5- or 6-membered, saturated or unsaturated heterocyclic ring optionally containing one or more further nitrogen, sulfur and/or oxygen atom(s); R4 is hydrogen or lower alkyl; the dotted lines have the following meaning: if R3 and R4 are not present, the bond between positions C8 and C9 is a single bond and the bond between positions C8 and N7 is a double bond; if R3 and R4 are present, the bonds between positions C8 and C9 and between position C8 and N7 are single bonds; and if R3 is present and R4 is missing, the bond between positions C8 and C9 is a double bond and the bond between positions C8 and N7 is a single bond) and salts thereof. The invention compounds have neuroprotective effect.