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1. 发明授权

US06403588B1 Imidazopyridine derivatives 有权
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.

2. 发明授权

US06608053B2 Fused heteroaryl derivatives 有权
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.

3. 发明申请

US20070037805A1 Fused heteroaryl derivatives 审中-公开
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.

4. 发明申请

US20060142222A1 Novel gene relating to fibrotic conditions 审中-公开
标题翻译：与纤维化病症有关的新基因
公开(公告)号：US20060142222A1
公开(公告)日：2006-06-29
申请号：US10547710
申请日：2004-03-03
申请人： Makoto Ogino , Tomohiro Hirose , Kazumi Hayashi , Tomonobu Koizumi , Toshihide Yokoyama
发明人： Makoto Ogino , Tomohiro Hirose , Kazumi Hayashi , Tomonobu Koizumi , Toshihide Yokoyama
IPC分类号： A61K48/00 , C12Q1/68 , C07H21/04 , A61K38/54 , C12N9/99
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。

5. 发明授权

US07037915B2 Fused heteroaryl derivatives 有权
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.

6. 发明授权

US06838457B2 Fused heteroaryl derivatives 有权
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.

7. 发明授权

US06770641B2 Fused heteroaryl derivatives 有权
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.

8. 发明授权

US06653320B2 Imidazopyridine derivatives 有权
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.

9. 发明授权

US08067586B2 Fused heteroaryl derivatives 有权
标题翻译：稠合杂芳基衍生物
公开(公告)号：US08067586B2
公开(公告)日：2011-11-29
申请号：US12688272
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： C07D413/00
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.
摘要翻译：本发明提供了可用作磷脂酰肌醇3激酶（PI3K）抑制剂和抗肿瘤剂的药物组合物，其提供了具有优异的PI3K抑制活性和癌细胞生长的新型双环或三环稠合杂芳基衍生物或其盐抑制活性。

10. 发明申请

US20100137584A1 FUSED HETEROARYL DERIVATIVES 有权
标题翻译：熔融异丁醇衍生物
公开(公告)号：US20100137584A1
公开(公告)日：2010-06-03
申请号：US12688272
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
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.
摘要翻译：本发明提供了可用作磷脂酰肌醇3激酶（PI3K）抑制剂和抗肿瘤剂的药物组合物，其提供了具有优异的PI3K抑制活性和癌细胞生长的新型双环或三环稠合杂芳基衍生物或其盐抑制活性。

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