公开(公告)号：EP1318988A2

公开(公告)日：2003-06-18

申请号：EP01970926.0

申请日：2001-09-12

申请人： Sepracor, Inc.

发明人： AQUILA, Brian, M. ,  BANNISTER, Thomas, D. ,  CUNY, Gregory, D. ,  HAUSKE, James, R. ,  HOLLAND, Joanne, M. ,  PERSONS, Paul, E. ,  RADEKE, Heike ,  WANG, Fengjian ,  SHAO, Liming

IPC分类号： C07D295/16

CPC分类号： C40B40/04 ,  C07B2200/11 ,  C07C255/46 ,  C07C2601/04 ,  C07D205/02 ,  C07D207/06 ,  C07D207/08 ,  C07D207/09 ,  C07D211/12 ,  C07D211/16 ,  C07D211/18 ,  C07D211/20 ,  C07D211/26 ,  C07D211/32 ,  C07D211/40 ,  C07D211/42 ,  C07D211/60 ,  C07D233/04 ,  C07D233/10 ,  C07D265/30 ,  C07D267/10 ,  C07D303/08 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C40B30/04 ,  C40B50/14

摘要： One aspect of the present invention relates to heterocyclic compounds formula A; whereof the substituents are defined in the description. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous aliments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

摘要翻译： 本发明的一个方面涉及杂环化合物。 本发明的第二方面涉及杂环化合物作为各种哺乳动物细胞受体（包括多巴胺，5-羟色胺或去甲肾上腺素转运蛋白）的配体的用途。 本发明的化合物可用于治疗多种疾病，包括但不限于成瘾，焦虑，抑郁，性功能障碍，高血压，偏头痛，阿尔茨海默病，肥胖症，呕吐，精神病， 精神分裂症，帕金森病，炎症性疼痛，神经性疼痛，Lesche-Nyhane病，Wilson氏病和Tourette综合征。 本发明的另一方面涉及杂环化合物的组合文库的合成，以及用于生物活性的那些文库的筛选，例如在基于多巴胺转运蛋白的测定中。