Art

J-GLOBAL ID：201702224184814463   Reference number：17A0746992

Pharmacological evaluation of novel (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives as TRPV4 antagonists for the treatment of pain

痛みの治療のためのTRPV4アンタゴニストとしての新規(6-アミノピリジン-3-イル)(4-(ピリジン-2-イル)ピペラジン-1-イル)メタノン誘導体の薬理学的評価

Author (25)： Tsuno Naoki (Medicinal Chemistry Research Laboratory, Shionogi & Co., Ltd, Japan) ,  Yukimasa Akira (Medicinal Chemistry Research Laboratory, Shionogi & Co., Ltd, Japan) ,  Yoshida Osamu (Medicinal Chemistry Research Laboratory, Shionogi & Co., Ltd, Japan) ,  Suzuki Shinji (Medicinal Chemistry Research Laboratory, Shionogi & Co., Ltd, Japan) ,  Nakai Hiromi (Medicinal Chemistry Research Laboratory, Shionogi & Co., Ltd, Japan) ,  Ogawa Tomoyuki (Medicinal Chemistry Research Laboratory, Shionogi & Co., Ltd, Japan) ,  Fujiu Motohiro (Medicinal Chemistry Research Laboratory, Shionogi & Co., Ltd, Japan) ,  Takaya Kenji (Medicinal Chemistry Research Laboratory, Shionogi & Co., Ltd, Japan) ,  Nozu Azusa (Medicinal Chemistry Research Laboratory, Shionogi & Co., Ltd, Japan) ,  Yamaguchi Hiroki (Medicinal Chemistry Research Laboratory, Shionogi & Co., Ltd, Japan) ,  Matsuda Hidetoshi (Shionogi Techno Advance Research Co., Ltd, Japan) ,  Funaki Satoko (Research Laboratory for Development, Shionogi & Co., Ltd, Japan) ,  Yamanada Natsue (Drug Discovery & Disease Research Laboratory, Shionogi & Co., Ltd, Japan) ,  Tanimura Miki (Drug Discovery & Disease Research Laboratory, Shionogi & Co., Ltd, Japan) ,  Nagamatsu Daiki (Research Laboratory for Development, Shionogi & Co., Ltd, Japan) ,  Asaki Toshiyuki (Drug Discovery & Disease Research Laboratory, Shionogi & Co., Ltd, Japan) ,  Horita Narumi (Shionogi Techno Advance Research Co., Ltd, Japan) ,  Yamamoto Miyuki (Drug Discovery & Disease Research Laboratory, Shionogi & Co., Ltd, Japan) ,  Hinata Mikie (Drug Discovery & Disease Research Laboratory, Shionogi & Co., Ltd, Japan) ,  Soga Masahiko (Drug Discovery & Disease Research Laboratory, Shionogi & Co., Ltd, Japan) ,  Imai Masayuki (Global Innovation Office, Shionogi & Co., Ltd, Japan) ,  Morioka Yasuhide (Drug Discovery & Disease Research Laboratory, Shionogi & Co., Ltd, Japan) ,  Kanemasa Toshiyuki (Drug Discovery & Disease Research Laboratory, Shionogi & Co., Ltd, Japan) ,  Sakaguchi Gaku (Global Innovation Office, Shionogi & Co., Ltd, Japan) ,  Iso Yasuyoshi (IMP Manufacturing Center, CMC R&D Division, Shionogi & Co., Ltd, Japan)
Material： Bioorganic & Medicinal Chemistry  (Bioorganic and Medicinal Chemistry)
Volume： 25  Issue： 7  Page： 2177-2190  Publication year： Apr. 01, 2017 
JST Material Number： W0556A  ISSN： 0968-0896  Document type： Article
Article type： 原著論文  Country of issue： Netherlands (NLD)  Language： ENGLISH (EN)

Thesaurus term： *ion channel ,  *drug ,  amine ,  *nitrogen heterocyclic compound ,  pharmacology ,  guinea pig ,  rat ,  *adjuvant ,  pain ,  experimental disease ,  *analgesic action ,  structure-activity relationship ,  *drug receptor ,  proton magnetic resonance ,  Electrospray Ionization Mass Spectrometry
Semi thesaurus term： 1H-NMR ,  ESI-MS ,  *Freund's Adjuvant ,  *TRPV4 ,  Aminopyridines ,  *vanilloid receptor ,  animal models of human disease ,  Piperazines ,  Mechanical hyperalgesia ,  *Receptor antagonist ,  *analgesic effect

Author keywords (5)： Transient receptor potential vanilloid 4 ,  TRPV4 antagonist ,  Ion channel ,  Vanilloid receptor ,  Pain

JST classification (6)： Biological function  (EB03040U) ,  Transport of cell membrane  (EF04020R) ,  Nitrogen heterocycles in general  (CF07040G) ,  Synthesis of drugs  (GV01030F) ,  Structure-activity relationship of drugs  (GV01050B) ,  Basic research of antipyretic analgesics  (GW03040H)

Substance index (2)： 2-(2′,4′-Dimethyl-4,5′-bithiazole-2-ylamino)-5-[3-[5-(trifluoromethyl)-2-pyrimidinyl]-3,8-diazabicyclo[3.2.1]octane-8-ylcarbonyl]pyridine ,  2-(2′,4′-Dimethyl-4,5′-bithiazole-2-ylamino)-5-[2,6-diethyl-4-[5-(trifluoromethyl)-2-pyrimidinyl]piperazinocarbonyl]pyridine

Terms in the title (11)： 痛み ,  治療 ,  TRPV4 ,  アンタゴニスト ,  アミノピリジン ,  ピリジン ,  ピペラジン ,  メタノン ,  誘導体 ,  薬理学 ,  評価