2. Academic Validation
  3. Novel quinuclidinyl heteroarylcarbamate derivatives as muscarinic receptor antagonists

Novel quinuclidinyl heteroarylcarbamate derivatives as muscarinic receptor antagonists

  • Bioorg Med Chem. 2014 Jul 1;22(13):3478-87. doi: 10.1016/j.bmc.2014.04.031.
Shinya Nagashima 1,  Yuji Matsushima 2,  Hisao Hamaguchi 2,  Hiroshi Nagata 2,  Toru Kontani 2,  Ayako Moritomo 2,  Tadatsura Koshika 2,  Makoto Takeuchi 2
Affiliations

Affiliations

  • 1 Drug Discovery Research, Astellas Pharma Inc, 21, Miyukigaoka, Tsukuba, Ibaraki 305-8585, Japan. Electronic address: shinya.nagashima@astellas.com.
  • 2 Drug Discovery Research, Astellas Pharma Inc, 21, Miyukigaoka, Tsukuba, Ibaraki 305-8585, Japan.
PMID: 24837158 DOI: 10.1016/j.bmc.2014.04.031
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.

Keywords

ASP9133; COPD; In vivo selectivity; Long acting muscarinic receptor antagonist.

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