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发明申请
US20140018366A1 BITOPIC MUSCARINIC AGONISTS AND ANTAGONISTS AND METHODS OF SYNTHESIS AND USE THEREOF 有权
双极肌肉激素和拮抗剂及其合成和使用方法

  • 专利标题： BITOPIC MUSCARINIC AGONISTS AND ANTAGONISTS AND METHODS OF SYNTHESIS AND USE THEREOF
  • 专利标题（中）： 双极肌肉激素和拮抗剂及其合成和使用方法
  • 申请号： US13937350
    申请日： 2013-07-09
  • 公开(公告)号： US20140018366A1
    公开(公告)日： 2014-01-16
  • 发明人: John BOULOS
  • 申请人： BARRY UNIVERSITY, INC.
  • 主分类号： C07D417/06
  • IPC分类号： C07D417/06 ;  C07D405/06 ;  C07D295/14
BITOPIC MUSCARINIC AGONISTS AND ANTAGONISTS AND METHODS OF SYNTHESIS AND USE THEREOF
摘要：
Compositions for treating a condition associated with activity of a muscarinic receptor (e.g., one or more of M1, M2, M3, M4, M5) and for anesthetizing a subject include a bitopic muscarinic antagonist or agonist. A bitopic muscarinic antagonist named JB-D4 was discovered. This bitopic ligand and its structural analogs, as well as bitopic muscarinic agonists, may be used as neuromuscular blocking agents (e.g., for use in compositions for anesthetizing a subject) and for the treatment of central nervous system disorders (e.g., Parkinson's disease, Schizophrenia, etc.), Overactive Bladder Syndrome, Chronic Obstructive Pulmonary Disease, asthma, and many other diseases associated with the activation or inhibition of M1-M5 acetylcholine receptors.
摘要（中）：

用于治疗与毒蕈碱受体（例如，M1，M2，M3，M4，M5中的一种或多种）的活性相关的病症的组合物和用于麻醉受试者的组合物包括苦味毒蕈碱性拮抗剂或激动剂。 发现了一种名为JB-D4的苦涩毒蕈碱拮抗剂。 这种比特配位体及其结构类似物以及苦味碱激动剂可用作神经肌肉阻滞剂（例如用于麻醉受试者的组合物）和治疗中枢神经系统疾病（例如，帕金森病，精神分裂症 等），过度活动性膀胱综合征，慢性阻塞性肺疾病，哮喘和许多其他与M1-M5乙酰胆碱受体活化或抑制相关的疾病。

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