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1. 发明申请

WO2014142363A1 SPIRO AZETIDINE ISOXAZOLE DERIVATIVES AND THEIR USE AS SSTR5 ANTAGONISTS 审中-公开
标题翻译： SPIRO AZETIDINE异丙唑衍生物及其作为SSTR5拮抗剂的用途
公开(公告)号：WO2014142363A1
公开(公告)日：2014-09-18
申请号：PCT/JP2014/058144
申请日：2014-03-13
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED
发明人： KASAI, Shizuo , OGINO, Masaki , MIZOJIRI, Ryo , YAMASAKI, Takeshi , HIROSE, Hideki , TAKAKURA, Nobuyuki , YAMASHITA, Tohru , MORIMOTO, Sachie , NAKAHATA, Takashi , KINA, Asato
IPC分类号： C07D498/10 , A61K31/424 , A61P3/00
CPC分类号： C07D498/10
摘要： Provided is a compound represented by the following formula (1) or a salt thereof, which has an SSTR5 antagonistic action: wherein each symbol has the same definition as in the specification.
摘要翻译：提供具有下式（1）表示的化合物或其盐，其具有SSTR5拮抗作用：其中每个符号具有与说明书中相同的定义。

2. 发明申请

WO2015064083A1 HETEROCYCLIC COMPOUND 审中-公开
标题翻译：杂环化合物
公开(公告)号：WO2015064083A1
公开(公告)日：2015-05-07
申请号：PCT/JP2014/005438
申请日：2014-10-28
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED
发明人： KASAI, Shizuo , NAKAHATA, Takashi , KINA, Asato , HIROSE, Hideki , YAMASAKI, Takeshi , YAMASHITA, Tohru , NISHIKAWA, Yoichi
IPC分类号： C07D401/14 , C07D401/04 , A61K31/444 , A61P3/10
CPC分类号： C07D401/12 , C07D211/86 , C07D239/22 , C07D401/04 , C07D401/14
摘要： A compound having an SSTR5 antagonist action and use of the compound as a medicament are provided. Specifically, a compound represented by the following formula: wherein each symbol is as defined herein, or a salt thereof, a medicament comprising the compound or a salt thereof, and use of the compound or a salt thereof as an agent the prophylaxis or treatment of diabetes mellitus are provided.
摘要翻译：提供具有SSTR5拮抗作用的化合物和该化合物作为药物的用途。具体地，由下式表示的化合物或其盐，其中每个符号如本文所定义，或其盐，包含该化合物或其盐的药物，以及该化合物或其盐的用途作为预防或治疗提供糖尿病。

3. 发明申请

WO2015052910A1 ANTAGONISTS OF SOMATOSTATIN RECEPTOR SUBTYPE 5 (SSTR5) 审中-公开
标题翻译： SOMATOSTATIN受体亚型5（SSTR5）的拮抗剂
公开(公告)号：WO2015052910A1
公开(公告)日：2015-04-16
申请号：PCT/JP2014/005075
申请日：2014-10-06
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED
发明人： KASAI, Shizuo , HIROSE, Hideki , YAMASAKI, Takeshi , YAMASHITA, Tohru , KINA, Asato , NISHIKAWA, Yoichi
IPC分类号： C07D471/04 , A61K31/4545 , A61P3/00 , A61P9/00
CPC分类号： C07D471/04
摘要： A compound having an SSTR5 antagonist action and use of the compound as a medicament are provided. Specifically, a compound represented by the following formula: wherein each symbol is as defined herein, or a salt thereof, a medicament comprising the compound or a salt thereof, and use of the compound or a salt thereof as an agent for the prophylaxis or treatment of diabetes mellitus are provided.
摘要翻译：提供具有SSTR5拮抗作用的化合物和该化合物作为药物的用途。具体地，由下式表示的化合物或其盐，其中每个符号如本文所定义，或其盐，包含该化合物或其盐的药物，以及该化合物或其盐作为预防或治疗剂的用途的糖尿病。

4. 发明申请

WO2012074126A9 BICYCLIC COMPOUND 审中-公开
公开(公告)号：WO2012074126A9
公开(公告)日：2012-06-07
申请号：PCT/JP2011/078010
申请日：2011-11-29
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED , YASUMA, Tsuneo , KAMATA, Makoto , YAMASHITA, Tohru , HIROSE, Hideki , MURAKAMI, Masataka , KINA, Asato , YONEMORI, Kazuko , MIZOJIRI, Ryo , FUJIMORI, Ikuo , FUJIMOTO, Takuya , IKEDA, Zenichi
发明人： YASUMA, Tsuneo , KAMATA, Makoto , YAMASHITA, Tohru , HIROSE, Hideki , MURAKAMI, Masataka , KINA, Asato , YONEMORI, Kazuko , MIZOJIRI, Ryo , FUJIMORI, Ikuo , FUJIMOTO, Takuya , IKEDA, Zenichi
IPC分类号： C07D401/04 , C07D405/04 , C07D413/04 , C07D417/04 , A61K31/423 , A61K31/416 , A61P9/00
摘要： The present invention provides a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes and the like, and having superior efficacy. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

5. 发明申请

WO2011136385A1 BICYCLIC COMPOUND DERIVATIVES AND THEIR USE AS ACC INHIBITORS. 审中-公开
标题翻译：双相化合物衍生物及其作为ACC抑制剂的用途。
公开(公告)号：WO2011136385A1
公开(公告)日：2011-11-03
申请号：PCT/JP2011/060616
申请日：2011-04-26
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED , YAMASHITA, Tohru , KAMATA, Makoto , HIROSE, Hideki , MURAKAMI, Masataka , FUJIMOTO, Takuya , IKEDA, Zenichi , YASUMA, Tsuneo , FUJIMORI, Ikuo , MIZOJIRI, Ryo , YUKAWA, Tomoya
发明人： YAMASHITA, Tohru , KAMATA, Makoto , HIROSE, Hideki , MURAKAMI, Masataka , FUJIMOTO, Takuya , IKEDA, Zenichi , YASUMA, Tsuneo , FUJIMORI, Ikuo , MIZOJIRI, Ryo , YUKAWA, Tomoya
IPC分类号： C07D231/54 , C07D263/56 , C07D263/58 , C07D307/81 , C07D413/04 , C07D417/04 , C07D487/08 , C07D498/04 , A61K31/416 , A61K31/496 , A61K31/4355 , A61K31/4365 , A61P3/00 , A61P9/00
CPC分类号： C07D413/14 , A61K31/41 , A61K31/415 , A61K31/439 , A61K31/4439 , A61K31/444 , C07D231/54 , C07D263/56 , C07D263/58 , C07D307/81 , C07D401/02 , C07D401/14 , C07D403/02 , C07D405/02 , C07D413/04 , C07D417/04 , C07D487/08 , C07D491/048 , C07D498/04
摘要： The present invention provides to a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification.
摘要翻译：本发明提供具有ACC抑制作用的化合物，其可用作预防或治疗肥胖症，糖尿病，高血压，高脂血症，心力衰竭，糖尿病并发症，代谢综合征，肌肉减少症，癌症等的药剂，以及具有优越的疗效。本发明涉及由式（I）表示的化合物：其中每个符号如说明书中所定义。

6. 发明公开

EP2009011A1 NITROGEN-CONTAINING HETEROCYCLIC COMPOUND 审中-公开
标题翻译：含氮的杂环化合物
公开(公告)号：EP2009011A1
公开(公告)日：2008-12-31
申请号：EP07741635.2
申请日：2007-04-13
申请人： Takeda Pharmaceutical Company Limited
发明人： FUKATSU, Kohji , KAMATA, Makoto , YAMASHITA, Tohru , ENDO, Satoshi
IPC分类号： C07D409/06 , A61K31/4535 , A61K31/5377 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/04 , A61P9/12 , A61P21/00 , A61P43/00 , C07D409/14 , C07D413/14 , C07D417/14 , C12N9/99 , C12N15/09
CPC分类号： C07D401/04 , C07D409/06 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The object of the present invention is to provide a compound having an ACC inhibitory action, which is useful for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and has superior properties such as efficacy, duration of activity, specificity, low toxicity and the like.
The present invention provides a compound represented by the following formula

wherein
ring M is a 5- or 6-membered aromatic ring;
W is C or N;
K is an optionally substituted methylene group or an optionally substituted imino group;
R is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted hydroxy group or an optionally substituted heterocyclic group;
T and U are independently a hydrogen atom or a substituent or, T and U form, together with ring M, an optionally substituted bicyclic ring;
D and G are independently a carbonyl group or a sulfonyl group; ring P is an optionally substituted piperidine or an optionally substituted piperazine;
B is CH or N;
ring Q is an optionally substituted monocyclic ring;
A is C, CH or N; and
J is an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted amino group,
provided that when the W moiety of ring M is =N- or -N=, then U should be absent,
or a salt thereof.
摘要翻译：本发明的目的是提供可用于预防或治疗肥胖症，糖尿病，高血压，高脂血症，心力衰竭，糖尿病并发症，代谢综合症，肌肉减少症等的具有ACC抑制作用的化合物，诸如功效，活性持续时间，特异性，低毒性等优越特性。本发明提供由下式表示的化合物，其中环M为5元或6元芳环; W是C或N; K是任选取代的亚甲基或任选取代的亚氨基; R为氢原子，任选取代的烃基，任选取代的羟基或任选取代的杂环基; T和U独立地为氢原子或取代基，或者T和U形式与环M一起为任选取代的双环; D和G独立地为羰基或磺酰基; 环P是任选取代的哌啶或任选取代的哌嗪; B是CH或N; 环Q是任选取代的单环; A是C，CH或N; 并且J是任选取代的烃基，任选取代的杂环基或任选取代的氨基，条件是当环M的W部分是= N-或-N =时，则U应当不存在或其盐。

7. 发明授权

EP3063139B1 HETEROCYCLIC COMPOUND 有权转让
公开(公告)号：EP3063139B1
公开(公告)日：2018-11-21
申请号：EP14800152.2
申请日：2014-10-28
申请人： Takeda Pharmaceutical Company Limited
发明人： KASAI, Shizuo , NAKAHATA, Takashi , KINA, Asato , HIROSE, Hideki , YAMASAKI, Takeshi , YAMASHITA, Tohru , NISHIKAWA, Yoichi
IPC分类号： C07D401/14 , C07D401/04 , A61K31/444 , A61P3/10
CPC分类号： C07D401/12 , C07D211/86 , C07D239/22 , C07D401/04 , C07D401/14
摘要： A compound having an SSTR5 antagonist action and use of the compound as a medicament are provided. Specifically, a compound represented by the following formula: wherein each symbol is as defined herein, or a salt thereof, a medicament comprising the compound or a salt thereof, and use of the compound or a salt thereof as an agent the prophylaxis or treatment of diabetes mellitus are provided.

8. 发明授权

EP2649062B1 BICYCLIC COMPOUNDS AS INHIBITORS OF ACETYL-COA CARBOXYLASE (ACC) 有权
标题翻译：双环化合物乙酰辅酶A羧化酶（ACC）
公开(公告)号：EP2649062B1
公开(公告)日：2015-04-08
申请号：EP11802168.2
申请日：2011-11-29
申请人： Takeda Pharmaceutical Company Limited
发明人： YASUMA, Tsuneo , KAMATA, Makoto , YAMASHITA, Tohru , HIROSE, Hideki , MURAKAMI, Masataka , KINA, Asato , YONEMORI, Kazuko , MIZOJIRI, Ryo , FUJIMORI, Ikuo , FUJIMOTO, Takuya , IKEDA, Zenichi
IPC分类号： C07D401/04 , C07D405/04 , C07D413/04 , C07D417/04 , A61K31/423 , A61K31/416 , A61P9/00
CPC分类号： C07D413/04 , C07D401/04 , C07D405/04 , C07D417/04

9. 发明公开

EP2123652A1 HETEROCYCLIC COMPOUND 审中-公开
标题翻译：杂志VERBINDUNG
公开(公告)号：EP2123652A1
公开(公告)日：2009-11-25
申请号：EP08711532.5
申请日：2008-02-19
申请人： Takeda Pharmaceutical Company Limited
发明人： FUKATSU, Kohji , KAMATA, Makoto , YAMASHITA, Tohru
IPC分类号： C07D471/10 , A61K31/438 , A61K31/537 , A61P1/00 , A61P1/12 , A61P1/16 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/48 , A61P7/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12 , A61P15/00 , A61P19/10 , A61P21/04 , A61P25/16
CPC分类号： C07D471/10 , C07D491/107 , C07D495/10 , C07D498/10 , C07D519/00
摘要： The present invention provides a compound having an ACC inhibitory action, which is useful for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy.
The present invention provides a compound represented by the formula (I):

wherein each symbol is as in the specification, or a salt thereof.
摘要翻译：本发明提供具有ACC抑制作用的化合物，其可用于预防或治疗肥胖，糖尿病，高血压，高脂血症，心力衰竭，糖尿病并发症，代谢综合征，肌肉减少症，癌症等，并且具有优异的疗效。本发明提供由式（I）表示的化合物：其中每个符号如说明书中所述，或其盐。

10. 发明授权

EP3055309B1 ANTAGONISTS OF SOMATOSTATIN RECEPTOR SUBTYPE 5 (SSTR5) 有权
公开(公告)号：EP3055309B1
公开(公告)日：2018-06-13
申请号：EP14790746.3
申请日：2014-10-06
申请人： Takeda Pharmaceutical Company Limited
发明人： KASAI, Shizuo , HIROSE, Hideki , YAMASAKI, Takeshi , YAMASHITA, Tohru , KINA, Asato , NISHIKAWA, Yoichi
IPC分类号： C07D471/04 , A61K31/4545 , A61P3/00 , A61P9/00
CPC分类号： C07D471/04
摘要： A compound having an SSTR5 antagonist action and use of the compound as a medicament are provided. Specifically, a compound represented by the following formula: wherein each symbol is as defined herein, or a salt thereof, a medicament comprising the compound or a salt thereof, and use of the compound or a salt thereof as an agent for the prophylaxis or treatment of diabetes mellitus are provided.

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