公开(公告)号：US20060217420A1

公开(公告)日：2006-09-28

申请号：US10552107

申请日：2004-03-30

申请人： Nicholas Cosford ,  Dehua Huang ,  Nicholas Smith ,  Essa Hsinyi Hu

发明人： Nicholas Cosford ,  Dehua Huang ,  Nicholas Smith ,  Essa Hsinyi Hu

IPC分类号： A61K31/444 ,  C07D403/14

CPC分类号： C07D233/64 ,  C07D401/04 ,  C07D401/14 ,  C07D471/04

摘要： Imidazole compounds of Formula (I): (where A, B, R11, R12, W, X, Y and Z are as defined herein) wherein the imidazole is substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ring, which are MgluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorders, and panic, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm and sleep disorders—such as shift-work induced sleep disorder and jet-lag, drug addiction, drug abuse, drug withdrawal, obesity and other diseases, and pharmaceutical compositions and methods of treating these diseases.

摘要翻译： 式（I）的咪唑化合物（其中A，B，R 11，R 12，W，X，Y和Z如本文所定义），其中咪唑是 直接或桥接，其中i）杂芳基部分，其含有与杂芳基的连接点相邻的N，和ii）另一杂芳基或芳基环，其中至少一个环进一步被另一个环取代， 用于治疗精神病和情绪障碍（例如精神分裂症，焦虑症，抑郁症，双相性精神障碍和恐慌）以及治疗疼痛，帕金森病，认知功能障碍，癫痫，昼夜节律和睡眠的MgluR5调节剂 疾病 - 如转移工作诱导的睡眠障碍和时滞，药物成瘾，药物滥用，药物戒断，肥胖症等疾病，以及治疗这些疾病的药物组合物和方法。

公开(公告)号：US5786472A

公开(公告)日：1998-07-28

申请号：US766400

申请日：1996-12-12

申请人： Essa Hsinyi Hu ,  Daniel R. Sidler ,  Ulf H. Dolling ,  Michael A. Patane

发明人： Essa Hsinyi Hu ,  Daniel R. Sidler ,  Ulf H. Dolling ,  Michael A. Patane

IPC分类号： C07D239/22 ,  C07D239/36

CPC分类号： C07D239/22

摘要： The present invention provides a process for forming 5-(alkyl or alkoxy)carbonyl-6-alkyl-4-(aryl or alkyl)-3,4-2(1H)-dihydropyrimidinones by combining a .beta.-keto ester or diketone, an aldehyde and urea in the presence of a boron reagent, a metal salt (e.g., Cu.sub.2 O) and a catalyst (e.g., acid). The reaction is typically run in one pot in a solvent to afford dihydropyrimidinones in higher yields and with easier work up than previously known methods.

摘要翻译： 本发明提供了通过将β-酮酯或二酮组合形成5-（烷基或烷氧基）羰基-6-烷基-4-（芳基或烷基）-3,4-2（1H） - 二氢嘧啶酮的方法， 醛和尿素在硼试剂，金属盐（例如Cu 2 O）和催化剂（例如酸）​​的存在下进行。 反应通常在溶剂中在一锅中进行，以更高的产率提供二氢嘧啶酮，并且比以前已知的方法更容易处理。