公开(公告)号：US20100292288A1

公开(公告)日：2010-11-18

申请号：US12663415

申请日：2008-06-06

申请人： Anthony C. Blackburn ,  John A. DeMattei ,  Ryan M. Hart ,  Young Mi Khulman ,  Michael Mesleh ,  Jeffrey Smith

发明人： Anthony C. Blackburn ,  John A. DeMattei ,  Ryan M. Hart ,  Young Mi Khulman ,  Michael Mesleh ,  Jeffrey Smith

IPC分类号： A61K31/40 ,  C07D207/04 ,  A61P25/28 ,  A61P25/08 ,  A61P25/00 ,  A61P25/24 ,  A61P3/04 ,  A61P25/20 ,  A61P25/18 ,  A61P11/00 ,  A61P29/00

CPC分类号： C07D207/06

摘要： The present invention is directed to novel salts of (R)-1-{2-[4′-(3-methoxy-propane-1-sulfonyl)-biphenyl-4-yl]-ethyl}-2-methyl-pyrrolidine, and crystalline forms, and compositions thereof that modulate the activity of the histamine H3-receptor and are useful in the treatment of histamine H3-receptor associated disorders, such as, cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as narcolepsy, shift-work syndrome, drowsiness as a side effect from a medication, maintenance of vigilance to aid in completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, pain, dementia, Alzheimer's disease and the like.

摘要翻译： 本发明涉及（R）-1- {2- [4' - （3-甲氧基 - 丙磺酰基） - 联苯-4-基] - 乙基} -2-甲基 - 吡咯烷的新型盐， 调节组胺H3受体活性的结晶形式及其组合物，可用于治疗组胺H3受体相关疾病，例如认知障碍，癫痫，脑创伤，抑郁症，肥胖症，睡眠障碍和 觉醒，如发作性睡病，转移综合征，嗜睡作为药物的副作用，维持警惕以帮助完成任务等，猝死，睡眠过多，嗜睡综合征，时差，睡眠呼吸暂停等，注意力缺陷 过敏性疾病（ADHD），精神分裂症，过敏反应，上呼吸道过敏反应，过敏性鼻炎，鼻充血，疼痛，痴呆，阿尔茨海默氏病等。