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.

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.

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。

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。

公开(公告)号：US07173029B2

公开(公告)日：2007-02-06

申请号：US11250782

申请日：2005-10-14

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 ,  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。

公开(公告)号：US20060058321A1

公开(公告)日：2006-03-16

申请号：US11250782

申请日：2005-10-14

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： A61K31/519 ,  C07D491/02 ,  C07D498/02 ,  C07D498/14

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。

公开(公告)号：US20050014771A1

公开(公告)日：2005-01-20

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： A61K31/00 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  C07D471/04 ,  C07D471/14 ,  C07D491/04 ,  C07D491/14 ,  C07D495/04 ,  C07D495/14

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。

公开(公告)号：US06673799B1

公开(公告)日：2004-01-06

申请号：US09787672

申请日：2001-03-21

申请人： Nobuaki Taniguchi ,  Isao Kinoyama ,  Takashi Kamikubo ,  Akira Toyoshima ,  Kiyohiro Samizu ,  Eiji Kawaminami ,  Masakazu Imamura ,  Hiroyuki Moritomo ,  Akira Matsuhisa ,  Masaaki Hirano ,  Yoji Miyazaki ,  Eisuke Nozawa ,  Minoru Okada ,  Hiroshi Koutoku ,  Mitsuaki Ohta

发明人： Nobuaki Taniguchi ,  Isao Kinoyama ,  Takashi Kamikubo ,  Akira Toyoshima ,  Kiyohiro Samizu ,  Eiji Kawaminami ,  Masakazu Imamura ,  Hiroyuki Moritomo ,  Akira Matsuhisa ,  Masaaki Hirano ,  Yoji Miyazaki ,  Eisuke Nozawa ,  Minoru Okada ,  Hiroshi Koutoku ,  Mitsuaki Ohta

IPC分类号： C07D23174

CPC分类号： C07D295/192 ,  C07D213/85 ,  C07D241/08 ,  C07D295/205 ,  C07D295/215 ,  C07D295/26

摘要： This application relates to a piperazino-substituted novel cyanophenyl derivative in which a substituted carbamoyl or substituted sulfamoyl group having an aryl, heterocyclic or the like group that may have a substituent group is bonded to one nitrogen atom on the piperazine ring. The compound of this application has an anti-androgen action and is useful in preventing or treating prostatic cancer, benign prostatic hyperplasia and the like diseases.

摘要翻译： 本申请涉及哌嗪取代的新型氰基苯基衍生物，其中具有可具有取代基的芳基，杂环等基团的取代氨基甲酰基或取代氨磺酰基与哌嗪环上的一个氮原子键合。 本申请的化合物具有抗雄激素作用，可用于预防或治疗前列腺癌，良性前列腺增生等疾病。

公开(公告)号：US06608056B1

公开(公告)日：2003-08-19

申请号：US10243416

申请日：2002-09-13

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： C07D48704

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.