Novel quinuclidinyl heteroarylcarbamate derivatives as muscarinic receptor antagonists

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• 作者：Shinya Nagashima ; ^{shinya.nagashima@astellas.com" class="auth_mail} ; Yuji Matsushima ; Hisao Hamaguchi ; Hiroshi Nagata^&dagger ; ; Toru Kontani^&Dagger ; ; Ayako Moritomo ; Tadatsura Koshika ; Makoto Takeuchi
• 关键词：COPD ; Long acting muscarinic receptor antagonist ; In vivo selectivity ; ASP9133
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：1 July 2014
• 年：2014
• 卷：22
• 期：13
• 页码：3478-3487
• 全文大小：1097 K

文摘

Herein, we describe the synthesis and pharmacological profiles of novel quinuclidinyl heteroarylcarbamate derivatives. Among them, the quinuclidin-4-yl thiazolylcarbamate derivative ASP9133 was identified as a promising long-acting muscarinic antagonist (LAMA) showing more selective inhibition of bronchoconstriction against salivation and more rapid onset of action in a rat model than tiotropium bromide.