Novel quinuclidinyl heteroarylcarbamate derivatives as muscarinic receptor antagonists

S Nagashima, Y Matsushima, H Hamaguchi…

Index: Nagashima, Shinya; Matsushima, Yuji; Hamaguchi, Hisao; Nagata, Hiroshi; Kontani, Toru; Moritomo, Ayako; Koshika, Tadatsura; Takeuchi, Makoto Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 13 p. 3478 - 3487

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Abstract

Abstract 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.