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1. 发明授权

EP2900675B1 PRODUCTION METHOD OF THIENOPYRIMIDINE DERIVATIVE 有权
公开(公告)号：EP2900675B1
公开(公告)日：2019-03-06
申请号：EP13779938.3
申请日：2013-09-27
申请人： Takeda Pharmaceutical Company Limited
发明人： FUKUOKA, Koichiro , MIWA, Kazuhiro , SASAKI, Tsuyoshi , KOMURA, Fumiya
IPC分类号： C07D495/04 , C07D333/38 , C07D409/12

2. 发明授权

EP1591446B1 Thienopyrimidine compounds and use thereof 有权转让
标题翻译：噻吩并嘧啶化合物及其用途
公开(公告)号：EP1591446B1
公开(公告)日：2013-03-06
申请号：EP04705950.6
申请日：2004-01-28
申请人： Takeda Pharmaceutical Company Limited
发明人： CHO, Nobuo , IMADA, Takashi , HITAKA, Takenori , MIWA, Kazuhiro , KUSAKA, Masami , SUZUKI, Nobuhiro
IPC分类号： C07D495/04 , A61K31/519 , A61P1/04 , A61P5/04 , A61P5/24 , A61P13/08 , A61P15/00 , A61P15/08 , A61P15/18 , A61P17/10 , A61P17/14 , A61P25/28 , A61P35/00 , A61P43/00
CPC分类号： C07D495/04 , A61K31/519

3. 发明公开

EP2900675A2 PRODUCTION METHOD OF THIENOPYRIMIDINE DERIVATIVE 有权
标题翻译：噻吩并嘧啶衍生物的生产方法
公开(公告)号：EP2900675A2
公开(公告)日：2015-08-05
申请号：EP13779938.3
申请日：2013-09-27
申请人： Takeda Pharmaceutical Company Limited
发明人： FUKUOKA, Koichiro , MIWA, Kazuhiro , SASAKI, Tsuyoshi , KOMURA, Fumiya
IPC分类号： C07D495/04 , C07D333/38
CPC分类号： C07D495/04 , C07D333/38 , C07D409/12
摘要： 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.
摘要翻译：本发明提供高产率地高质量地具有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制造方法。本发明提供了制备噻吩并嘧啶衍生物的方法，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。

4. 发明公开

EP4119564A1 PRODUCTION METHOD OF THIENOPYRIMIDINE DERIVATIVE 审中-实审
公开(公告)号：EP4119564A1
公开(公告)日：2023-01-18
申请号：EP22168256.0
申请日：2013-09-27
申请人： Takeda Pharmaceutical Company Limited
发明人： MIWA, Kazuhiro
IPC分类号： C07D495/04
摘要： The present invention relates to a crystalline form of 1-{4-[1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea that exhibits an X-ray powder diffraction pattern having 2-theta (2θ) peaks at approximately 8.932°, 16.607°, and 17.328° or peaks expressed in d values (Å) at approximately 9.893, 5.334, and 5.114.

5. 发明公开

EP3130581A1 METHOD FOR PRODUCING HETEROCYCLIC COMPOUND 审中-公开
标题翻译： VERFAHREN ZUR HERSTELLUNG EINER HETEROCYCLISCHEN VERBINDUNG
公开(公告)号：EP3130581A1
公开(公告)日：2017-02-15
申请号：EP15777381.3
申请日：2015-04-09
申请人： Takeda Pharmaceutical Company Limited
发明人： YAMASHITA, Hironori , MIWA, Kazuhiro
IPC分类号： C07C231/02 , C07C231/18 , C07C233/58 , C07D211/60 , C07B61/00
CPC分类号： C07D211/60 , C07C231/02 , C07C231/08 , C07C2101/02 , C07C2101/08 , C07C2101/16 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07D401/06 , C07C233/58
摘要： 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.
摘要翻译：提供具有肾素抑制活性的杂环化合物的合成中间体的制造方法，可用作糖尿病性肾病，高血压等的预防或治疗药物。由式（III-1a），式（III-1b），式（III-1c）和/或式（III-1d）表示的化合物的制备方法; 其中每个符号如描述中所述，或其盐，包括使由式（Ia）或（Ib）表示的化合物：其中每个符号如描述中所述，或其盐与式（II）：其中每个符号如描述中所述，或其盐，在铝化合物和手性胺化合物的存在下。

6. 发明公开

EP1957495A1 FUSED HETEROCYCLIC COMPOUND 审中-公开
标题翻译：熔合杂环化合物
公开(公告)号：EP1957495A1
公开(公告)日：2008-08-20
申请号：EP06834254.2
申请日：2006-12-01
申请人： Takeda Pharmaceutical Company Limited
发明人： ISHIKAWA, Tomoyasu , MIWA, Kazuhiro , SETO, Masaki , BANNO, Hiroshi , KAWAKITA, Youichi
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： The present invention provides a compound represented by the formula: wherein R1a is a hydrogen atom, R2a is a C1-6 alkyl group substituted by a group represented by-NR6a-CO-(CH2) n -SO2 -optionally halogenated C1-4 alkyl wherein n is an integer of 1 to 4, R6a is a hydrogen atom or a C 1-4 alkyl group, and -(CH2) n - is optionally substituted by C 1-4 alkyl, R3a is a hydrogen atom or a C 1-6 alkyl group, R4a is a halogen atom or a C 1-6 alkyl group, R5a is a halogen atom or a C 1-6 alkyl group, and Xa is a hydrogen atom or a halogen atom, or a salt thereof. The compound of the present invention has a superior tyrosine kinase inhibitory action, is highly safe, and is sufficiently satisfactory as a pharmaceutical product.
摘要翻译：本发明提供由下式表示的化合物：其中R 1a是氢原子，R 2a是被-NR 6 a -CO-（CH 2）n -SO 2 - 表示的基团取代的C 1-6烷基 - 任选卤代的C 1-4烷基其中n是1至4的整数，R 6a是氢原子或C 1-4烷基，并且 - （CH 2）n - 任选被C 1-4烷基取代，R 3a是氢原子或C 1 -6烷基，R 4a是卤素原子或C 1-6烷基，R 5a是卤素原子或C 1-6烷基，X a是氢原子或卤素原子。本发明的化合物具有优异的酪氨酸激酶抑制作用，安全性高，作为医药品充分令人满意。

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