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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. 发明授权

US07795267B2 Bicyclic piperazine compound having TGR23 antagonistic activity 失效
标题翻译：具有TGR23拮抗活性的双环哌嗪化合物
公开(公告)号：US07795267B2
公开(公告)日：2010-09-14
申请号：US10570270
申请日：2004-08-26
申请人： Kohji Fukatsu , Yutaka Nakayama , Naoki Tarui , Masaaki Mori , Hirokazu Matsumoto , Osamu Kurasawa , Hiroshi Banno
发明人： Kohji Fukatsu , Yutaka Nakayama , Naoki Tarui , Masaaki Mori , Hirokazu Matsumoto , Osamu Kurasawa , Hiroshi Banno
IPC分类号： A61K31/4965
CPC分类号： C07D487/04 , C07D513/04
摘要： The present invention provides a compound represented by the formula: wherein R1 is —(C═O)—NR7R8 or —(C═O)—OR6, R2 is a hydrocarbon group which may be substituted or the like, R3 is a hydrocarbon group which may be substituted or the like, R4 is a hydrocarbon group which may be substituted or the like, n is from 0 to 4, and X is an oxygen atom, or a salt thereof. The invention also provides a compound which has a TGR23 antagonist activity and thus is useful for prevention and treatment of cancer.
摘要翻译：本发明提供由下式表示的化合物：其中R 1为 - （C = O）-NR 7 R 8或 - （C = O）-OR 6，R 2为可被取代的烃基等，R 3为烃基其可以被取代或类似，R 4是可以被取代的烃基等，n是0-4，X是氧原子或其盐。本发明还提供具有TGR23拮抗剂活性的化合物，因此可用于预防和治疗癌症。

3. 发明申请

US20090012093A1 Receptor Function Regulator 有权
标题翻译：受体功能调节器
公开(公告)号：US20090012093A1
公开(公告)日：2009-01-08
申请号：US10534081
申请日：2003-11-06
申请人： Kohji Fukatsu , Shinobu Sasaki , Shuji Hinuma , Yasuaki Ito , Nobuhiro Suzuki , Masataka Harada , Tsuneo Yasuma
发明人： Kohji Fukatsu , Shinobu Sasaki , Shuji Hinuma , Yasuaki Ito , Nobuhiro Suzuki , Masataka Harada , Tsuneo Yasuma
IPC分类号： A61K31/4965 , C07C62/34 , C07D241/18 , C07D277/42 , G01N33/566 , A61K31/427 , A61K31/192
CPC分类号： C07C255/24 , A61K31/192 , A61K31/195 , A61K31/216 , A61K31/343 , A61K31/381 , A61K31/401 , A61K31/404 , A61K31/426 , A61K31/428 , A61K31/437 , C07C59/64 , C07C59/68 , C07C59/72 , C07C59/74 , C07C59/76 , C07C59/90 , C07C65/24 , C07C69/734 , C07C69/736 , C07C217/48 , C07C217/58 , C07C217/76 , C07C235/42 , C07C255/54 , C07C317/28 , C07C323/19 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D209/12 , C07D277/36 , C07D277/42 , C07D277/64 , C07D295/13 , C07D307/91 , C07D333/32 , C07D333/54 , C07D333/62 , C07D333/78 , C07D471/04
摘要： The GPR40 receptor function regulator of the present invention, which comprises a compound having an aromatic ring and a group capable of releasing cation is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.
摘要翻译：本发明的GPR40受体功能调节剂包含具有芳香环的化合物和能释放阳离子的基团，可用作胰岛素促分泌素或预防或治疗糖尿病等的药剂。

4. 发明授权

US06218429B1 Tricyclic compounds, their production and use 有权
标题翻译：三环化合物，其生产和使用
公开(公告)号：US06218429B1
公开(公告)日：2001-04-17
申请号：US09309519
申请日：1999-05-10
申请人： Shigenori Ohkawa , Osamu Uchikawa , Kohji Fukatsu , Masaomi Miyamoto
发明人： Shigenori Ohkawa , Osamu Uchikawa , Kohji Fukatsu , Masaomi Miyamoto
IPC分类号： A01N34308
CPC分类号： C07D263/52 , C07D265/34 , C07D307/93 , C07D311/94 , C07D317/70 , C07D319/14 , C07D491/04 , Y10S514/923
摘要： A compound of the formula: wherein R1 is an optionally substituted hydrocarbon, amino or heterocyclic group; R2 is H or an optionally substituted hydrocarbon group; R3 is H or an optionally substituted hydrocarbon or heterocyclic group; X is CHR4, NR4, O or S in which R4 is H or an optionally substituted hydrocarbon group; Y is C, CH or N; ring A is optionally substituted 5- to 7-membered ring; ring B is an optionally substituted benzene ring; and m is 1 to 4, or a salt thereof, a process for producing it, an intermediate for the production and a pharmaceutical composition comprising it are provided.
摘要翻译：下式的化合物：其中R 1是任选取代的烃，氨基或杂环基; R2是H或任选取代的烃基; R3是H或任选取代的烃或杂环基; X是CHR 4，NR 4，O或S，其中R 4是H或任选取代的烃基; Y为C，CH或N; 环A为任选取代的5-至7-元环; 环B是任选取代的苯环; 和m为1至4，或其盐，其制备方法，制备中间体和包含其的药物组合物。

5. 发明授权

US6034239A Tricyclic compounds, their production and use 失效
标题翻译：三环化合物，其生产和使用
公开(公告)号：US6034239A
公开(公告)日：2000-03-07
申请号：US812168
申请日：1997-03-06
申请人： Shigenori Ohkawa , Osamu Uchikawa , Kohji Fukatsu , Masaomi Miyamoto
发明人： Shigenori Ohkawa , Osamu Uchikawa , Kohji Fukatsu , Masaomi Miyamoto
IPC分类号： C07C233/00 , C07D307/92 , C07D413/00 , C07D493/00
CPC分类号： C07D307/77 , C07D263/62 , C07D311/94 , C07D317/70 , C07D319/14 , C07D491/04
摘要： A compound of the formula: ##STR1## wherein R.sup.1 is an optionally substituted hydrocarbon, amino or heterocyclic group; R.sup.2 is H or an optionally substituted hydrocarbon group; R.sup.3 is H or an optionally substituted hydrocarbon or heterocyclic group; X is CHR.sup.4, NR.sup.4, O or S in which R.sup.4 is H or an optionally substituted hydrocarbon group; Y is C, CH or N; ring A is optionally substituted 5- to 7-membered ring; ring B is an optionally substituted benzene ring; and m is 1 to 4, or a salt thereof, a process for producing it, an intermediate for the production and a pharmaceutical composition comprising it are provided.
摘要翻译：下式的化合物：其中R 1是任选取代的烃，氨基或杂环基; R2是H或任选取代的烃基; R3是H或任选取代的烃或杂环基; X是CHR 4，NR 4，O或S，其中R 4是H或任选取代的烃基; Y为C，CH或N; 环A为任选取代的5-至7-元环; 环B是任选取代的苯环; 和m为1至4，或其盐，其制备方法，制备中间体和包含其的药物组合物。

6. 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。

7. 发明授权

US07553867B2 Furan or thiophene derivative and medicinal use thereof 失效
标题翻译：呋喃或噻吩衍生物及其医药用途
公开(公告)号：US07553867B2
公开(公告)日：2009-06-30
申请号：US10526507
申请日：2003-09-04
申请人： Kazumasa Hamamura , Shigekazu Sasaki , Yuichiro Amano , Junichi Sakamoto , Kohji Fukatsu
发明人： Kazumasa Hamamura , Shigekazu Sasaki , Yuichiro Amano , Junichi Sakamoto , Kohji Fukatsu
IPC分类号： A61K31/341 , A61K31/381 , C07D307/40 , C07D333/14 , C07D333/18
CPC分类号： C07D307/42 , C07D307/38 , C07D307/54 , C07D307/68 , C07D307/79 , C07D405/12 , C07D409/12 , C07D413/06 , C07D417/06 , C07D417/12
摘要： The present invention provides a compound represented by the formula (I): [wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, p is 0, 1 or 2, and when p is 2, each R may be the same or different, R1 is a hydrogen atom or an optionally substituted hydrocarbon group, R2 is an optionally substituted aromatic group, Ring A is an optionally substituted monocyclic aromatic ring or optionally substituted bicyclic aromatic fused ring, X1 is an oxygen atom or a sulfur atom, X2 is a bond, an oxygen atom or —S(O)n— (wherein n is 0, 1 or 2), Y is a bond, an oxygen atom, —S(O)m—, —C(═O)—N(R3)— or —N(R3)—C(═O)— (R3 is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, and m is 0, 1 or 2), M1, M2 and M3 may be the same or different and are each independently a bond or an optionally substituted divalent aliphatic hydrocarbon group, and M4 is an optionally substituted divalent aliphatic hydrocarbon group] or a salt thereof, which is useful as a prophylactic and/or therapeutic agent for lipid metabolism abnormality, arteriosclerotic disease and sequelae thereof, diabetes mellitus and the like.
摘要翻译：本发明提供由式（I）表示的化合物：[其中R是任选取代的烃基或任选取代的杂环基，p是0,1或2，当p是2时，每个R可以相同或不同的，R 1是氢原子或任选取代的烃基，R 2是任选取代的芳族基团，环A是任选取代的单环芳族环或任选取代的双环芳族稠环，X 1是氧原子或硫原子， X 2是键，氧原子或-S（O）n - （其中n是0,1或2），Y是键，氧原子，-S（O）m - ， - C（-O） -N（R3） - 或-N（R3）-C（-O） - （R3是氢原子，任选取代的烃基或任选取代的杂环基，m是0,1或2），M1， M2和M3可以相同或不同，并且各自独立地为键或任选取代的二价脂族烃基，M4是任选取代的二价脂族氢羰基]或其盐，其可用作脂质代谢异常的预防和/或治疗剂，动脉硬化疾病及其后遗症，糖尿病等。

8. 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。

9. 发明申请

US20080167378A1 Receptor Function Regulation Agent 有权
标题翻译：受体功能调节剂
公开(公告)号：US20080167378A1
公开(公告)日：2008-07-10
申请号：US10580906
申请日：2004-11-26
申请人： Kohji Fukatsu , Ryo Fujii , Makoto Kobayashi , Jinichi Yonemori , Toshio Tanaka
发明人： Kohji Fukatsu , Ryo Fujii , Makoto Kobayashi , Jinichi Yonemori , Toshio Tanaka
IPC分类号： A61K31/192 , C07K14/705 , G01N33/566 , A61P3/04 , A61P3/10 , C07C57/03
CPC分类号： C07D213/643 , A61K31/192 , A61K31/216 , A61K31/341 , A61K31/4453 , A61K31/5375 , C07C45/68 , C07C45/71 , C07C59/68 , C07C69/734 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D213/64 , C07D277/34 , C07D295/088 , C07D295/096 , C07D307/12 , C07D317/54 , C07D333/32 , C07F7/1804 , C07C49/697 , C07C49/67 , C07C49/84 , C07C49/755 , C07C47/575
摘要： An agent for regulating 14273 receptor function, which is useful as a preventing or treating drug for diabetes mellitus, hyperlipidemia or the like, is provided. An agent for regulating 14273 receptor function comprising a compound containing an aromatic ring and a group capable of releasing a cation.
摘要翻译：提供了调节14273受体功能的药剂，其可用作预防或治疗糖尿病，高脂血症等药物。用于调节14273受体功能的试剂，其包含含有芳环的化合物和能释放阳离子的基团。

10. 发明申请

US20070072865A1 Bicyclic piperazine compound and use thereof 失效
标题翻译：双环哌嗪化合物及其用途
公开(公告)号：US20070072865A1
公开(公告)日：2007-03-29
申请号：US10570270
申请日：2004-08-26
申请人： Kohji Fukatsu , Yutaka Nakayama , Naoki Tarui , Masaaki Mori , Hirokazu Matsumoto , Osamu Kurasawa , Hiroshi Banno
发明人： Kohji Fukatsu , Yutaka Nakayama , Naoki Tarui , Masaaki Mori , Hirokazu Matsumoto , Osamu Kurasawa , Hiroshi Banno
IPC分类号： A61K31/498 , C07D498/04 , C07D491/04 , C07D487/04
CPC分类号： C07D487/04 , C07D513/04
摘要： The present invention provides a compound represented by the formula: wherein R1 is an acyl group, R2 is a hydrocarbon group which may be substituted or the like, R3 is a hydrocarbon group which may be substituted or the like, R4 is a hydrocarbon group which may be substituted or the like, n is from 0 to 4, and X is an oxygen atom, a sulfur atom or the like, or a salt thereof. The invention also provides a compound which has a TGR23 antagonist activity and thus is useful for prevention and treatment of cancer.
摘要翻译：本发明提供由下式表示的化合物：其中R 1是酰基，R 2是可以被取代的烃基，等等，R SUP > 3为可以被取代的烃基等，R 4为可以被取代的烃基等，n为0〜4，X为氧原子，硫原子等，或其盐。本发明还提供具有TGR23拮抗剂活性的化合物，因此可用于预防和治疗癌症。

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