公开(公告)号：EP4249077A1

公开(公告)日：2023-09-27

申请号：EP21894629.1

申请日：2021-11-16

申请人： Shionogi & Co., Ltd ,  Shionogi Pharma Co., Ltd.

发明人： MAJIMA, Shohei

IPC分类号： A61P43/00 ,  B01J35/02 ,  C07B53/00 ,  C07D219/02 ,  C07D219/04 ,  C07D219/06 ,  C07D219/08 ,  C07F5/02 ,  C07B61/00 ,  C07D498/14 ,  B01J31/02 ,  A61K31/5383

摘要： The present invention provides novel aclidinium salt of the formula (I) and a process for the production of the aclidinium salt.

wherein R 1 is C1-C6 alkyl or C1-C6 alkyloxy; R 2 is hydrogen or C1-C6 alkyloxy; R 3 is hydrogen, halogen, C1-C6 alkyl or C1-C6 alkyloxy; R 4 is hydrogen, C1-C6 alkyloxy, halo C1-C6 alkyloxy or C1-C6 alkylamino; R 5 is C1-C3 alkyl; and X - is an anion.

公开(公告)号：EP3693373A1

公开(公告)日：2020-08-12

申请号：EP18865221.8

申请日：2018-10-05

申请人： Shionogi & Co., Ltd.

发明人： OKAMOTO, Kazuya ,  UENO, Tatsuhiko ,  HATO, Yoshio ,  HAKOGI, Toshikazu ,  MAJIMA, Shohei

IPC分类号： C07D498/14 ,  C07D213/89 ,  C07D401/12

摘要： The present invention provides industrially suitable processes for preparing intermediates in the production of substituted polycyclic pyridone derivatives having a cap-dependent endonuclease inhibitory activity.
In the process as shown below, wherein each symbol is as defined in the specification, an optically active substituted tricyclic pyridone derivative of the formula (VII) is obtained in high yield and high enantioselectivity by subjecting a compound of the formula (III) or (VI) to intramolecular cyclization with controlling stereochemistry to obtain a compound of the formula (IV) having a removable functional group on an asymmetric carbon, and then removing the functional group thereof.