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公开(公告)号:US20060142222A1
公开(公告)日:2006-06-29
申请号:US10547710
申请日:2004-03-03
CPC分类号: C07K14/47 , A61K38/00 , C07K14/4712 , G01N2500/10
摘要: This discloses a novel human or rat polypeptide useful in improving and/or preventing organ fibrosis and a polynucleotide encoding the aforementioned polypeptide, an expression vector containing the aforementioned polynucleotide, and a cell transfected with the aforementioned expression vector. The aforementioned polynucleotide shows a remarkable decrease in the expression dose in the kidney of a chronic renal insufficiency model rat and in the bladder of a rat suffering from the induction of fibrotic conditions in the bladder, compared with a normal individual. Also, the production of extracellular matrix is suppressed by overexpression of the aforementioned polypeptide. Also disclosed are the promoter region of the aforementioned polypeptide, a method for screening a remedy for fibrotic conditions, and a process for producing a medicinal composition for improving fibrotic conditions which contains a substance obtained by the aforementioned screening method as the active ingredient.
摘要翻译: 这公开了可用于改善和/或预防器官纤维化的新型人或大鼠多肽和编码上述多肽的多核苷酸,含有上述多核苷酸的表达载体和用上述表达载体转染的细胞。 与正常个体相比,上述多核苷酸表现出慢性肾功能不全模型大鼠肾脏和膀胱中诱导纤维化病症的大鼠膀胱中的表达剂量显着降低。 此外,通过上述多肽的过表达来抑制细胞外基质的产生。 还公开了上述多肽的启动子区域,筛选纤维化病症的治疗方法,以及生产用于改善纤维化病症的药物组合物的方法,其含有通过上述筛选方法获得的物质作为活性成分。
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公开(公告)号:US06403588B1
公开(公告)日:2002-06-11
申请号:US09843610
申请日:2001-04-26
申请人: Masahiko Hayakawa , Hiroyuki Kaizawa , Ken-Ichi Kawaguchi , Koyo Matsuda , Noriko Ishikawa , Tomonobu Koizumi , Mayumi Yamano , Minoru Okada , Mitsuaki Ohta
发明人: Masahiko Hayakawa , Hiroyuki Kaizawa , Ken-Ichi Kawaguchi , Koyo Matsuda , Noriko Ishikawa , Tomonobu Koizumi , Mayumi Yamano , Minoru Okada , Mitsuaki Ohta
IPC分类号: A61K31435
CPC分类号: C07D471/04 , A61K31/435 , C07D487/04
摘要: The present invention relates to novel compounds having a phosphatidylinositol 3 kinase (PI3K) inhibiting activity which are useful as medicaments, more particularly as antitumor agent. Novel 3-(imidazo[1,2-a]pyridin-3-yl) derivatives or salts thereof exhibit an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity, and are thus useful as medicaments, especially as PI3K inhibitors and antitumor agents.
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公开(公告)号:US06608053B2
公开(公告)日:2003-08-19
申请号:US09843615
申请日:2001-04-26
申请人: Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
发明人: Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
IPC分类号: C07D41304
CPC分类号: C07D471/04 , A61K31/00 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D471/14 , C07D491/04 , C07D491/14 , C07D495/04 , C07D495/14
摘要: The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.
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公开(公告)号:US20100137585A1
公开(公告)日:2010-06-03
申请号:US12688273
申请日:2010-01-15
申请人: Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
发明人: Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
IPC分类号: C07D487/04 , C07D491/048 , C07D495/04
CPC分类号: C07D471/04 , A61K31/00 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D471/14 , C07D491/04 , C07D491/14 , C07D495/04 , C07D495/14
摘要: The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.
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公开(公告)号:US20050191612A1
公开(公告)日:2005-09-01
申请号:US10511549
申请日:2003-09-10
申请人: Takahide Ohishi , Tomonobu Koizumi
发明人: Takahide Ohishi , Tomonobu Koizumi
CPC分类号: G01N33/5008 , C07K14/723 , G01N33/502 , G01N33/5023 , G01N33/507 , G01N2333/726
摘要: A screening tool for an agent for promoting insulin production and/or an agent for increasing insulin content, wherein the tool is a G protein-coupled receptor exhibiting an activity of promoting insulin production by activation, or a cell expressing the polypeptide, is disclosed. Further, a method for screening an agent for promoting insulin production and/or an agent for increasing insulin content, comprising the steps of bringing the cell or a cell membrane thereof into contact with a substance to be tested, and analyzing whether or not the polypeptide is activated, is disclosed. The screening tool and the screening method are useful in screening a substance which increases insulin content and prevents and/or treats diabetes. Furthermore, a novel agent for increasing insulin content comprising as an active ingredient a substance obtained by the screening, is disclosed.
摘要翻译: 公开了用于促进胰岛素生成的试剂和/或增加胰岛素含量的试剂的筛选工具,其中该工具是表现出通过活化促进胰岛素产生的活性的G蛋白偶联受体或表达该多肽的细胞。 另外,用于筛选促进胰岛素生成的试剂的方法和/或用于增加胰岛素含量的试剂的方法,包括使细胞或其细胞膜与被检物质接触的步骤,以及分析多肽 被激活。 筛选工具和筛选方法可用于筛选增加胰岛素含量并预防和/或治疗糖尿病的物质。 此外,公开了一种用于增加胰岛素含量的新型药剂,其包含通过筛选获得的物质作为活性成分。
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公开(公告)号:US20070037805A1
公开(公告)日:2007-02-15
申请号:US11544144
申请日:2006-10-06
申请人: Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
发明人: Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
IPC分类号: A61K31/5377
CPC分类号: C07D471/04 , A61K31/00 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D471/14 , C07D491/04 , C07D491/14 , C07D495/04 , C07D495/14
摘要: The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.
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公开(公告)号:US07037915B2
公开(公告)日:2006-05-02
申请号:US10918094
申请日:2004-08-13
申请人: Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
发明人: Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
IPC分类号: C07D495/04 , A61K31/519
CPC分类号: C07D471/04 , A61K31/00 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D471/14 , C07D491/04 , C07D491/14 , C07D495/04 , C07D495/14
摘要: The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.
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公开(公告)号:US06838457B2
公开(公告)日:2005-01-04
申请号:US10459002
申请日:2003-06-10
申请人: Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
发明人: Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
IPC分类号: A61K31/00 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D471/04 , C07D471/14 , C07D491/04 , C07D491/14 , C07D495/04 , C07D495/14 , C07D487/04 , A61K31/381
CPC分类号: C07D471/04 , A61K31/00 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D471/14 , C07D491/04 , C07D491/14 , C07D495/04 , C07D495/14
摘要: The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.
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公开(公告)号:US06770641B2
公开(公告)日:2004-08-03
申请号:US10459220
申请日:2003-06-10
申请人: Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
发明人: Masahiko Hayakawa , Hiroyuki Kaizawa , Hiroyuki Moritomo , Ken-Ichi Kawaguchi , Tomonobu Koizumi , Mayumi Yamano , Koyo Matsuda , Minoru Okada , Mitsuaki Ohta
IPC分类号: C07D41304
CPC分类号: C07D471/04 , A61K31/00 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D471/14 , C07D491/04 , C07D491/14 , C07D495/04 , C07D495/14
摘要: The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.
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公开(公告)号:US06653320B2
公开(公告)日:2003-11-25
申请号:US10087717
申请日:2002-03-01
申请人: Masahiko Hayakawa , Hiroyuki Kaizawa , Ken-Ichi Kawaguchi , Koyo Matsuda , Noriko Ishikawa , Tomonobu Koizumi , Mayumi Yamano , Minoru Okada , Mitsuaki Ohta
发明人: Masahiko Hayakawa , Hiroyuki Kaizawa , Ken-Ichi Kawaguchi , Koyo Matsuda , Noriko Ishikawa , Tomonobu Koizumi , Mayumi Yamano , Minoru Okada , Mitsuaki Ohta
IPC分类号: A61K31437
CPC分类号: C07D471/04 , A61K31/435 , C07D487/04
摘要: The present invention relates to novel compounds having a phosphatidylinositol 3 kinase (PI3K) inhibiting activity which are useful as medicaments, more particularly as antitumor agent. Novel 3-(imidazo[1,2-a]pyridin-3-yl) derivatives or salts thereof exhibit an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity, and are thus useful as medicaments, especially as PI3K inhibitors and antitumor agents.
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