公开(公告)号：US09878981B2

公开(公告)日：2018-01-30

申请号：US15301525

申请日：2015-04-09

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Hironori Yamashita ,  Kazuhiro Miwa

IPC: C07D211/60 ,  C07C231/02 ,  C07D401/06

CPC classification number: C07D211/60 ,  C07C231/02 ,  C07C231/08 ,  C07C2101/02 ,  C07C2101/08 ,  C07C2101/16 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07D401/06 ,  C07C233/58

Abstract: Provided is a production method of a synthetic intermediate for a heterocyclic compound having a renin inhibitory activity and useful as a prophylactic or therapeutic drug for diabetic nephropathy, hypertension and the like. A production method of a compound represented by the formula (III-1a), the formula (III-1b), the formula (III-1c) and/or the formula (III-1d); wherein each symbol is as described in DESCRIPTION, or a salt thereof, including reacting a compound represented by the formula (Ia) or (Ib): wherein each symbol is as described in DESCRIPTION, or a salt thereof with a compound represented by the formula (II): wherein each symbol is as described in DESCRIPTION, or a salt thereof, in the presence of an aluminum compound and a chiral amine compound.

公开(公告)号：US09630971B2

公开(公告)日：2017-04-25

申请号：US14900589

申请日：2014-06-20

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  INTRA-CELLULAR THERAPIES, INC.

Inventor： Takashi Abe ,  Graham Buckton ,  Robert Davis ,  Mark Hooper ,  Peng Li ,  Hideaki Maruyama ,  Masahiro Takasuga ,  Lawrence P. Wennogle ,  Yuhei Yamamoto ,  Hironori Yamashita

IPC: A61K31/519 ,  C07D487/14

CPC classification number: C07D487/14

Abstract: The present invention relates to crystals of (6aR,9aS)-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-2-((4-(6-fluoropyridin-2-yl)phenyl)methyl)-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one, and methods of making and using such crystals.