公开(公告)号：US07820663B2

公开(公告)日：2010-10-26

申请号：US11455228

申请日：2006-06-15

申请人： Derk J. Hogenkamp ,  Timothy B. C. Johnstone ,  Kelvin W. Gee

发明人： Derk J. Hogenkamp ,  Timothy B. C. Johnstone ,  Kelvin W. Gee

IPC分类号： C07D401/02 ,  A61K31/47

CPC分类号： C07D213/50 ,  C07C237/16 ,  C07D213/56 ,  C07D257/04 ,  C07D261/08 ,  C07D261/18 ,  C07D413/04 ,  C07D413/12

摘要： The present invention is related substituted enaminones represented by a compound of Formula I that are novel allosteric modulators of α7 nAChRs. The invention also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on α7 nAChRs in a mammal by administering an effective amount of a compound of Formula I.

摘要翻译： 本发明涉及作为α7nAChRs的新型变构调节剂的式I化合物所代表的相关取代的烯胺基。 本发明还公开了通过施用有效量的式I化合物来治疗对哺乳动物中对α7nAChRs的乙酰胆碱作用增强有作用的病症的治疗。

公开(公告)号：US06780853B1

公开(公告)日：2004-08-24

申请号：US09321882

申请日：1999-05-28

申请人： Ravindra B. Upasani ,  David B. Fick ,  Derk J. Hogenkamp ,  Nancy C. Lan

发明人： Ravindra B. Upasani ,  David B. Fick ,  Derk J. Hogenkamp ,  Nancy C. Lan

IPC分类号： A61K3158

CPC分类号： C07J1/0029 ,  C07J1/0007 ,  C07J1/0055 ,  C07J1/0077 ,  C07J17/00 ,  C07J21/00 ,  C07J31/006 ,  C07J41/0005 ,  C07J41/005 ,  C07J43/003

摘要： The invention relates to 3&agr;-hydroxy, 17-(un)substituted derivatives of the androstane series and 3&agr;-hydroxy, 21-substituted derivatives of the pregnane series. These derivatives are capable of acting at a recently identified site on the GRC, thereby modulating brain excitability in a manner that will alleviate stress, anxiety, insomnia, mood disorders that are amenable to GRC-active agents (such as depression) and seizure activity. The steroid derivatives of this invention are those having the general structural Formula: wherein R, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are farther defined herein and the dotted lines are single or double bonds. The structure includes androstanes, pregnanes (R4=methyl), 19-norandrostanes, and norpregnanes (R4=H).

摘要翻译： 本发明涉及雄甾烷基系列的3α-羟基，17-（未）取代的衍生物和孕烷系列的3α-羟基，21-取代的衍生物。 这些衍生物能够在最近确定的GRC位点起作用，从而以减轻压力，焦虑，失眠，舒适于GRC活性剂（如抑郁症）和癫痫发作活动的情绪障碍的方式调节脑兴奋性。 本发明的类固醇衍生物是具有以下结构式的化合物：其中R，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10在本文中进一步定义，虚线是单键或双键。 该结构包括雄甾烷，孕烷（R4 =甲基），19-去雄孕烷和诺孕烷（R4 = H）。

公开(公告)号：US06335354B2

公开(公告)日：2002-01-01

申请号：US09819693

申请日：2001-03-29

申请人： Derk J. Hogenkamp

发明人： Derk J. Hogenkamp

IPC分类号： C07D21302

CPC分类号： C07D213/74

摘要： This invention relates to aminopyridines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein R1-R8, X and m are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

摘要翻译： 本发明涉及式I的氨基吡啶或其药学上可接受的盐，前药或溶剂化物，其中R1-R8，X和m在说明书中设定。 本发明还涉及式I化合物用于治疗全身和局部缺血后的神经元损伤，用于治疗或预防神经变性疾病如肌萎缩性侧索硬化（ALS）以及治疗，预防或改善的用途 作为抗惊厥剂，作为抗惊厥剂，作为抗躁狂抑制剂，作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病变。