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1. 发明申请

US20090281097A1 NITROGEN-CONTAINING HETEROCYCLIC COMPOUND 审中-公开
标题翻译：含氮杂环化合物
公开(公告)号：US20090281097A1
公开(公告)日：2009-11-12
申请号：US12296874
申请日：2007-04-13
申请人： Kohji Fukatsu , Makoto Kamata , Tohru Yamashita , Satoshi Endo
发明人： Kohji Fukatsu , Makoto Kamata , Tohru Yamashita , Satoshi Endo
IPC分类号： A61K31/5377 , C07D413/14 , A61K31/4535 , C07D409/06 , C07D409/14 , A61K31/4545 , A61P3/10
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，肌肉减少症等，并且具有优异的性质如功效，活性持续时间，特异性，低毒性等。本发明提供由下式表示的化合物，其中环M为5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是氢原子，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独立地是氢原子或取代基，或者T和U与环M一起形成任选取代的双环; 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部分为-N-或-N-时，则U不应为其或其盐。

2. 发明申请

US20100160255A1 SPIRO-CYCLIC COMPOUND 审中-公开
标题翻译：螺旋环化合物
公开(公告)号：US20100160255A1
公开(公告)日：2010-06-24
申请号：US11997021
申请日：2006-07-28
申请人： Makoto Kamata , Kohji Fukatsu , Tohru Yamashita , Naoki Furuyama , Satoshi Endo
发明人： Makoto Kamata , Kohji Fukatsu , Tohru Yamashita , Naoki Furuyama , Satoshi Endo
IPC分类号： A61K31/695 , C07D471/10 , A61K31/4545 , C07D211/06 , A61P3/04 , A61P9/12 , A61P3/06 , A61P9/00 , A61P3/10 , C07D498/10 , A61K31/5386 , C07D487/10 , A61K31/499 , C07F7/02 , C07D413/14 , A61K31/5377
CPC分类号： C07D513/10 , C07D221/20 , C07D401/04 , C07D471/10 , C07D487/10 , C07D491/10 , C07F7/1804
摘要： The present invention provides a compound represented by the formula (I): wherein E is an optionally substituted cyclic group; D is a carbonyl group or a sulfonyl group; A is CH or N; ring P is an optionally further substituted 5- to 7-membered ring; ring Q is an optionally further substituted 5- to 7-membered nonaromatic ring; and ring R is an optionally further substituted and optionally condensed 5- to 7-membered nonaromatic ring, or a salt thereof. The compound of the present invention has an ACC inhibitory activity, 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 in the efficacy, duration of activity, specificity, low toxicity and the like.
摘要翻译：本发明提供由式（I）表示的化合物：其中E为任选取代的环状基团; D是羰基或磺酰基; A是CH或N; 环P是任选进一步取代的5-至7-元环; 环Q是任选进一步取代的5-至7-元非芳族环; 并且环R是任选进一步取代的和任选缩合的5-至7-元非芳族环或其盐。本发明化合物具有ACC抑制活性，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，代谢综合征，肌肉减少症等，并且具有优异的功效特性，活动持续时间，特异性，低毒性等。

3. 发明申请

US20100093777A1 SPIRO-RING COMPOUND 审中-公开
标题翻译：螺环化合物
公开(公告)号：US20100093777A1
公开(公告)日：2010-04-15
申请号：US12449084
申请日：2008-01-24
申请人： Kohji Fukatsu , Makoto Kamata , Tohru Yamashita
发明人： Kohji Fukatsu , Makoto Kamata , Tohru Yamashita
IPC分类号： A61K31/4545 , C07D471/10 , C07D498/10 , C07D513/10 , A61P3/04 , A61P3/10 , A61P9/00 , A61P35/00
CPC分类号： C07D519/00 , C07D495/04 , C07D498/10 , C07F7/1804
摘要： The present invention aims to provide a compound having an acetyl-CoA carboxylase (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 R1 is a hydrogen atom or a substituent; ring P is an optionally substituted 6-membered nitrogen-containing aromatic heterocycle; ring Q is an optionally further substituted 5- to 7-membered nitrogen-containing non-aromatic heterocycle; and ring R is an optionally fused 5- to 7-membered non-aromatic ring, which is further optionally substituted, or a salt thereof.
摘要翻译：本发明旨在提供一种具有乙酰-CoA羧化酶（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，癌症和并具有优越的疗效。本发明提供由式（I）表示的化合物：其中R1是氢原子或取代基; 环P是任选取代的6元含氮芳族杂环; 环Q是任选进一步取代的5-至7-元含氮非芳族杂环; 并且环R是任选稠合的5至7元非芳族环，其进一步任选被取代，或其盐。

4. 发明申请

US20100113418A1 HETEROCYCLIC COMPOUND 审中-公开
标题翻译：杂环化合物
公开(公告)号：US20100113418A1
公开(公告)日：2010-05-06
申请号：US12449680
申请日：2008-02-19
申请人： Kohji Fukatsu , Makoto Kamata , Tohru Yamashita
发明人： Kohji Fukatsu , Makoto Kamata , Tohru Yamashita
IPC分类号： A61K31/55 , C07D491/10 , A61K31/438 , C07D265/04 , A61K31/537 , A61P3/04 , A61P3/10 , A61P9/00 , A61P35/00
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。

5. 发明申请

US20110263562A1 BICYCLIC COMPOUND 失效
标题翻译：双相化合物
公开(公告)号：US20110263562A1
公开(公告)日：2011-10-27
申请号：US13094015
申请日：2011-04-26
申请人： Tohru Yamashita , Makoto Kamata , Hideki Hirose , Masataka Murakami , Takuya Fujimoto , Zenichi Ikeda , Tsuneo Yasuma , Ikuo Fujimori , Ryo Mizojiri , Tomoya Yukawa
发明人： Tohru Yamashita , Makoto Kamata , Hideki Hirose , Masataka Murakami , Takuya Fujimoto , Zenichi Ikeda , Tsuneo Yasuma , Ikuo Fujimori , Ryo Mizojiri , Tomoya Yukawa
IPC分类号： A61K31/423 , A61K31/438 , A61K31/439 , C07D417/04 , A61K31/454 , A61K31/416 , A61K31/34 , C07D498/04 , C07D413/14 , C07D413/04 , C07D263/56 , C07D231/56 , C07D307/87 , A61P35/04 , A61P3/04 , A61P3/06 , A61P9/12 , A61P9/00 , A61P3/10 , A61P3/00 , A61K31/497
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. 发明授权

US08703758B2 Bicyclic compound 失效
标题翻译：双环化合物
公开(公告)号：US08703758B2
公开(公告)日：2014-04-22
申请号：US13094015
申请日：2011-04-26
申请人： Tohru Yamashita , Makoto Kamata , Hideki Hirose , Masataka Murakami , Takuya Fujimoto , Zenichi Ikeda , Tsuneo Yasuma , Ikuo Fujimori , Ryo Mizojiri , Tomoya Yukawa
发明人： Tohru Yamashita , Makoto Kamata , Hideki Hirose , Masataka Murakami , Takuya Fujimoto , Zenichi Ikeda , Tsuneo Yasuma , Ikuo Fujimori , Ryo Mizojiri , Tomoya Yukawa
IPC分类号： A01N43/00 , A61K31/00 , A01N43/42 , A61K31/44 , A01N43/76 , A61K31/42 , A01N43/56 , A61K31/415 , A01N43/08 , A61K31/34 , C07D413/14 , C07D405/02 , C07D401/02 , C07D401/14 , C07D403/02 , C07D491/048 , A61K31/41 , A61K31/439 , A61K31/444 , A61K31/4439
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。

7. 发明授权

US08501804B2 Bicyclic compound 失效
标题翻译：双环化合物
公开(公告)号：US08501804B2
公开(公告)日：2013-08-06
申请号：US13126103
申请日：2009-10-26
申请人： Makoto Kamata , Tohru Yamashita , Asato Kina , Michiko Amano
发明人： Makoto Kamata , Tohru Yamashita , Asato Kina , Michiko Amano
IPC分类号： A61K31/343 , C07D307/83
CPC分类号： C07D235/14 , C07D261/20 , C07D263/56 , C07D277/64 , C07D307/81 , C07D333/58 , C07D405/06 , C07D405/12 , C07D407/06 , C07D407/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D491/04 , C07D491/048
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, 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, 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，并且具有优越的疗效。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，或其盐。

8. 发明申请

US20120010247A1 BICYCLIC COMPOUND 失效
标题翻译：双相化合物
公开(公告)号：US20120010247A1
公开(公告)日：2012-01-12
申请号：US13126103
申请日：2009-10-26
申请人： Makoto Kamata , Tohru Yamashita , Asato Kina , Michiko Amano
发明人： Makoto Kamata , Tohru Yamashita , Asato Kina , Michiko Amano
IPC分类号： A61K31/343 , C07D405/12 , A61K31/443 , A61P3/04 , A61P35/00 , A61P9/12 , A61P3/06 , A61P9/04 , A61P3/00 , C07D307/81 , A61P3/10
CPC分类号： C07D235/14 , C07D261/20 , C07D263/56 , C07D277/64 , C07D307/81 , C07D333/58 , C07D405/06 , C07D405/12 , C07D407/06 , C07D407/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D491/04 , C07D491/048
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, 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, 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，并且具有优越的疗效。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，或其盐。

9. 发明授权

US08822699B2 Heterocyclic compound and use thereof 有权
标题翻译：杂环化合物及其用途
公开(公告)号：US08822699B2
公开(公告)日：2014-09-02
申请号：US13223455
申请日：2011-09-01
申请人： Tatsuki Koike , Minoru Nakamura , Yoshihide Tomata , Takafumi Takai , Yasutaka Hoashi , Yuichi Kajita , Tetsuya Tsukamoto , Makoto Kamata
发明人： Tatsuki Koike , Minoru Nakamura , Yoshihide Tomata , Takafumi Takai , Yasutaka Hoashi , Yuichi Kajita , Tetsuya Tsukamoto , Makoto Kamata
IPC分类号： A61K31/42 , C07D263/30 , C07D413/02
CPC分类号： C07D471/04
摘要： The present invention provides a heterocycle derivative having a superior amyloid β production inhibitory activity and/or a superior γ-secretase modulation activity, and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
摘要翻译：本发明提供具有优异淀粉样蛋白的杂环衍生物; 生产抑制活性和/或优异的γ-分泌酶调节活性及其用途。由式（I）表示的化合物或其盐，其中每个符号如本说明书中所定义。

10. 发明申请

US20060128690A1 Amine derivative 失效
标题翻译：胺衍生物
公开(公告)号：US20060128690A1
公开(公告)日：2006-06-15
申请号：US10545120
申请日：2004-02-12
申请人： Yuji Ishihara , Makoto Kamata , Shiro Takekawa
发明人： Yuji Ishihara , Makoto Kamata , Shiro Takekawa
IPC分类号： A61K31/55 , A61K31/401 , A61K31/445
CPC分类号： C07D211/16 , A61K31/55 , C07C233/73 , C07C235/42 , C07D207/09 , C07D207/12 , C07D211/14 , C07D213/82 , C07D233/24 , C07D295/135
摘要： The present invention provides a compound represented by the formula wherein Ar1 is a cyclic group optionally having substituent(s); R is a hydrogen atom, an optionally halogenated C1-6 alkyl, a phenyl optionally having substituent(s) or a pyridyl optionally having substituent(s); Ra1, Ra2, Ra3 and Ra4 are the same or different and each is a hydrogen atom, an optionally halogenated C1-6 alkyl or the like; Ar is a monocyclic aromatic ring optionally having substituent(s); Y is an optionally halogenated alkylene group; and R1 and R2 are (1) the same or different and each is a hydrogen atom or a C1-6 alkyl, (2) R1 and R2 form a nitrogen-containing heterocycle optionally having substituent(s) together with the adjacent nitrogen atom, or (3) R1 and Y form a nitrogen-containing heterocycle optionally having substituent(s) together with the adjacent nitrogen atom, and R2 is a hydrogen atom or a C1-6 alkyl; provided that when the nitrogen-containing heterocycle formed by R1 and R2 together with the adjacent nitrogen atom is a piperazine, or when R is a C1-4 alkyl, Ar1 is a cyclic group having substituent(s), or a salt thereof, having a melanin-concentrating hormone antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like.
摘要翻译：本发明提供由下式表示的化合物：其中Ar 1是任选具有取代基的环状基团; R是氢原子，任选卤代的C 1-6烷基，任选具有取代基的苯基或任选具有取代基的吡啶基; Ra 1，R 2，R 3，R 3和R 4相同或不同，各自为氢原子，任选卤代的C 1-6烷基等; Ar是任选具有取代基的单环芳环; Y是任选卤代的亚烷基; 且R 1和R 2均为（1）相同或不同，并且各自为氢原子或C 1-6烷基，（ 2）R 1和R 2 2形成任选具有取代基的氮杂环与相邻的氮原子，或（3）R 1， Y和Y形成任选具有取代基的氮杂环与相邻的氮原子一起形成，R 2是氢原子或C 1-6 烷基; 条件是当由R 1和R 2与相邻氮原子一起形成的含氮杂环是哌嗪时，或当R是C 1〜 4个烷基，Ar 1是具有取代基的环状基团或其盐，其具有黑色素浓缩激素拮抗作用并且可用作预防或治疗的药剂肥胖等。

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