公开(公告)号：US20130310419A1

公开(公告)日：2013-11-21

申请号：US13983362

申请日：2012-01-31

申请人： Neelima Sinha ,  Gourhari Jana ,  Navnath Popat Karche ,  Shridhar Keshav Adurkar ,  Girish Dhanraj Hatnapure ,  Venkata P. Palle ,  Rajender Kumar Kamboj

发明人： Neelima Sinha ,  Gourhari Jana ,  Navnath Popat Karche ,  Shridhar Keshav Adurkar ,  Girish Dhanraj Hatnapure ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC分类号： C07D207/333 ,  A61K31/4025 ,  A61K31/4709 ,  A61K31/402 ,  C07D401/04 ,  A61K31/4725 ,  C07D405/04 ,  A61K45/06

CPC分类号： C07D207/333 ,  A61K31/402 ,  A61K31/4025 ,  A61K31/4709 ,  A61K31/4725 ,  A61K45/06 ,  C07D401/04 ,  C07D405/04

摘要： The present invention is related to pyrrole derivatives of formula I as the modulators of nicotinic acetylcholine receptors particularly the α7 subtype. The invention includes pyrrole derivatives, analogues, their prodrugs, their isotopes, their metabolites, pharmaceutically acceptable salts, polymorphs, solvates, optical isomers, clathrates, co-crystals, combinations with suitable medicament and pharmaceutical compositions thereof. The present invention also includes process of preparation of the said compounds and intended use in therapy of them. Owing to the modulatory activity of the pyrrole derivatives on the nicotinic acetylcholine receptors, the invention finds application in the prophylaxis and therapy of disorders encompassing the involvement of cholinergic transmission in the central and peripheral nervous system. The invention relates to the ability of pyrrole derivatives to modulate the cholinergic transmission and efficacy of the endogenous neurotransmitter ACh thorough the nicotinic acetylcholine receptors particularly the α7 subtype.

摘要翻译： 本发明涉及式I的吡咯衍生物作为烟碱乙酰胆碱受体的调节剂，特别是α7亚型。 本发明包括吡咯衍生物，类似物，其前药，其同位素，其代谢物，药学上可接受的盐，多晶型物，溶剂合物，旋光异构体，包合物，共晶体，与合适的药物的组合及其药物组合物。 本发明还包括制备所述化合物的方法和用于治疗它们的预期用途。 由于吡咯衍生物对烟碱乙酰胆碱受体的调节活性，本发明可用于预防和治疗包括胆碱能传递在中枢和周围神经系统中的疾病。 本发明涉及吡咯衍生物通过烟碱乙酰胆碱受体，特别是α7亚型调节内源性神经递质ACh的胆碱能传递和功效的能力。