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公开(公告)号:US11731983B2
公开(公告)日:2023-08-22
申请号:US17349584
申请日:2021-06-16
Applicant: Takeda Pharmaceutical Company Limited
Inventor: Kazuhiro Miwa
IPC: C07D495/04 , C07D333/38 , C07D409/12
CPC classification number: C07D495/04 , C07D333/38 , C07D409/12
Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.
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公开(公告)号:US10544160B2
公开(公告)日:2020-01-28
申请号:US16116804
申请日:2018-08-29
Applicant: Takeda Pharmaceutical Company Limited
Inventor: Kazuhiro Miwa
IPC: C07D495/04 , C07D333/38 , C07D409/12
Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.
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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.
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公开(公告)号:US12180224B2
公开(公告)日:2024-12-31
申请号:US18121886
申请日:2023-03-15
Applicant: Takeda Pharmaceutical Company Limited
Inventor: Koichiro Fukuoka , Kazuhiro Miwa
IPC: C07D495/04 , C07D333/38 , C07D409/12
Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.
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公开(公告)号:US11795178B2
公开(公告)日:2023-10-24
申请号:US17694635
申请日:2022-03-14
Applicant: Takeda Pharmaceutical Company Limited
Inventor: Koichiro Fukuoka , Kazuhiro Miwa , Tsuyoshi Sasaki , Fumiya Komura
IPC: C07D495/04 , C07D333/38 , C07D409/12
CPC classification number: C07D495/04 , C07D333/38 , C07D409/12
Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrirnidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.
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公开(公告)号:US10464945B2
公开(公告)日:2019-11-05
申请号:US16034002
申请日:2018-07-12
Applicant: Takeda Pharmaceutical Company Limited
Inventor: Kazuhiro Miwa
IPC: C07D495/04 , C07D333/38 , C07D409/12
Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl) -5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine -2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.
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公开(公告)号:US10150778B2
公开(公告)日:2018-12-11
申请号:US15481505
申请日:2017-04-07
Applicant: Takeda Pharmaceutical Company Limited
Inventor: Kazuhiro Miwa
IPC: C07D495/04 , C07D333/38 , C07D409/12
Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.
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公开(公告)号:US20150266891A1
公开(公告)日:2015-09-24
申请号:US14432188
申请日:2013-09-27
Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
Inventor: Koichiro Fukuoka , Kazuhiro Miwa , Tsuyoshi Sasaki , Fumiya Komura
IPC: C07D495/04 , C07D409/12
CPC classification number: C07D495/04 , C07D333/38 , C07D409/12
Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethyl aminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.
Abstract translation: 本发明提供具有促进促性腺激素释放激素(GnRH)拮抗作用的噻吩并嘧啶衍生物或其盐的高产率的制造方法。 本发明提供一种噻吩并嘧啶衍生物的制备方法,其包括使6-(4-氨基苯基)-1-(2,6-二氟苄基)-5-二甲基氨基甲基-3-(6-甲氧基哒嗪-3-基)噻吩并 [2,3-d]嘧啶-2,4(1H,3H) - 二酮或其盐,1,1'-羰基二咪唑或其盐和甲氧胺或其盐等。
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公开(公告)号:US11053257B2
公开(公告)日:2021-07-06
申请号:US16710390
申请日:2019-12-11
Applicant: Takeda Pharmaceutical Company Limited
Inventor: Kazuhiro Miwa
IPC: C07D495/04 , C07D333/38 , C07D409/12
Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.
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公开(公告)号:US09758528B2
公开(公告)日:2017-09-12
申请号:US14432188
申请日:2013-09-27
Applicant: Takeda Pharmaceutical Company Limited
Inventor: Koichiro Fukuoka , Kazuhiro Miwa , Tsuyoshi Sasaki , Fumiya Komura
IPC: C07D495/04 , C07D333/38 , C07D409/12
CPC classification number: C07D495/04 , C07D333/38 , C07D409/12
Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethyl aminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.
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