公开(公告)号：EP1509489A1

公开(公告)日：2005-03-02

申请号：EP03736639.0

申请日：2003-05-15

申请人： Sepracor, Inc.

发明人： AQUILA, Brian, A. ,  HOPKINS, Seth ,  LOCKSHIN, Curtis, A. ,  WANG, Fengjiang

IPC分类号： C07C215/00 ,  C07C211/00

CPC分类号： C40B40/04 ,  C07C217/58 ,  C07C2601/02 ,  C07D307/14 ,  C40B20/08 ,  C40B30/04 ,  C40B40/00 ,  C40B50/14

摘要： One aspect of the present invention relates to amines. A second aspect of the present invention relates to the use of the amines as inhibitors of a mammalian anandamide transporter. The compounds of the present invention will also find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to asthma, neuropathic pain, persistent pain, inflammatory pain, hyperactivity, hypertension, brain ischemia, Parkinson’s disease, spasticity. Tourette’s syndrome, schizophrenia, hemorrhagic shock, septic shock, cardiac shock, migrane, Horton’s headache, multiple sclerosis, anorexia, AIDS wasting syndrome, organ rejection, autoimmune diseases, allergy, arthritis, Crohn’s disease, malignant gliomas, neurodegenerative diseases, Huntington’s chorea, glaucoma, nausea, anxiety, psychosis, attention deficit hyperactivity disorder, premature ejaculation, and stroke. Another aspect of the present invention relates to combinatorial libraries of amines, and methods for preparing the libraries.

摘要翻译： 本发明的一个方面涉及胺。 本发明的第二方面涉及胺作为哺乳动物花生四烯酸转运蛋白抑制剂的用途。 本发明的化合物还可用于治疗哺乳动物患病，包括但不限于哮喘，神经性疼痛，持续性疼痛，炎性疼痛，活动过度，高血压，脑缺血，帕金森病， 痉挛。 抽动秽语综合征，精神分裂症，失血性休克，败血性休克，心脏休克，偏头痛，霍顿氏头痛，多发性硬化症， 青光眼，恶心，焦虑症，精神病，注意力缺陷多动症，早泄和中风。 本发明的另一方面涉及胺的组合文库，以及制备文库的方法。