Discovery of the Oral Leukotriene C4 Synthase Inhibitor (1<i>S</i>,2<i>S</i>)-2-({5-[(5-Chloro-2,4-difluorophenyl)(2-fluoro-2-methylpropyl)amino]-3-methoxypyrazin-2-yl}carbonyl)cyclopropanecarboxylic Acid (AZD9898) as a New Treatment for Asthma.

Munck Af Rosenschöld, Magnus; Johannesson, Petra; Nikitidis, Antonios; Tyrchan, Christian; Chang, Hui-Fang; Rönn, Robert; Chapman, Dave; Ullah, Victoria; Nikitidis, Grigorios; Glader, Pernilla; Käck, Helena; Bonn, Britta; Wågberg, Fredrik; Björkstrand, Eva; Andersson, Ulf; Swedin, Linda; Rohman, Mattias; Andreasson, Theresa; Bergström, Eva Lamm; Jiang, Fanyi; Zhou, Xiao-Hong; Lundqvist, Anders J; Malmberg, Anna; Ek, Margareta; Gordon, Euan; Pettersen, Anna; Ripa, Lena; Davis, Andrew M

Discovery of the Oral Leukotriene C4 Synthase Inhibitor (1S,2S)-2-({5-[(5-Chloro-2,4-difluorophenyl)(2-fluoro-2-methylpropyl)amino]-3-methoxypyrazin-2-yl}carbonyl)cyclopropanecarboxylic Acid (AZD9898) as a New Treatment for Asthma.

Munck Af Rosenschöld, Magnus; Johannesson, Petra; Nikitidis, Antonios; Tyrchan, Christian; Chang, Hui-Fang; Rönn, Robert; Chapman, Dave; Ullah, Victoria; Nikitidis, Grigorios; Glader, Pernilla; Käck, Helena; Bonn, Britta; Wågberg, Fredrik; Björkstrand, Eva; Andersson, Ulf; Swedin, Linda; Rohman, Mattias; Andreasson, Theresa; Bergström, Eva Lamm; Jiang, Fanyi; Zhou, Xiao-Hong; Lundqvist, Anders J; Malmberg, Anna; Ek, Margareta; Gordon, Euan; Pettersen, Anna; Ripa, Lena; Davis, Andrew M.

Affiliation

Rönn R; Orexo AB , Virdings allé 32A , SE-75450 Uppsala , Sweden.
Björkstrand E; Orexo AB , Virdings allé 32A , SE-75450 Uppsala , Sweden.

J Med Chem ; 62(17): 7769-7787, 2019 09 12.

Article in En | MEDLINE | ID: mdl-31415176

Subject(s)

Anti-Asthmatic Agents/pharmacology; Asthma/drug therapy; Drug Discovery; Enzyme Inhibitors/pharmacology; Glutathione Transferase/antagonists & inhibitors; Pyrazines/pharmacology; Administration, Oral; Animals; Anti-Asthmatic Agents/administration & dosage; Anti-Asthmatic Agents/chemistry; Asthma/metabolism; Disease Models, Animal; Dose-Response Relationship, Drug; Enzyme Inhibitors/administration & dosage; Enzyme Inhibitors/chemistry; Glutathione Transferase/metabolism; Humans; Molecular Structure; Pyrazines/chemical synthesis; Pyrazines/chemistry; Rats; Structure-Activity Relationship

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Full text: 1 Database: MEDLINE Main subject: Pyrazines / Asthma / Anti-Asthmatic Agents / Enzyme Inhibitors / Drug Discovery / Glutathione Transferase Type of study: Prognostic_studies Language: En Journal: J Med Chem Year: 2019 Type: Article

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