公开(公告)号：US07666873B2

公开(公告)日：2010-02-23

申请号：US11861327

申请日：2007-09-26

申请人： Nobuaki Taniguchi ,  Masakazu Imamura ,  Masahiko Hayakawa ,  Kenichi Kawaguchi ,  Takenori Kimura ,  Isao Kinoyama ,  Hiroyuki Kaizawa ,  Minoru Okada ,  Takashi Furutani

发明人： Nobuaki Taniguchi ,  Masakazu Imamura ,  Masahiko Hayakawa ,  Kenichi Kawaguchi ,  Takenori Kimura ,  Isao Kinoyama ,  Hiroyuki Kaizawa ,  Minoru Okada ,  Takashi Furutani

IPC分类号： A61K31/497 ,  C07D401/00

CPC分类号： C07D213/75 ,  C07D213/84 ,  C07D239/42 ,  C07D295/215

摘要： The present invention relates to a novel N-phenyl-(2R,5S)dimethylpiperazine derivatives useful as antiandrogenic agent which exhibits a sufficient prostate gland reducing effect as compared with conventional compounds and are excellent in oral activity. The compound of the present application is useful in preventing or treating prostate cancer, benign prostatic hyperplasia, and the like. The present invention also provides a novel intermediate useful in producing the compound of the present invention.

摘要翻译： 本发明涉及用作抗雄激素剂的新型N-苯基 - （2R，5S）二甲基哌嗪衍生物，其与常规化合物相比表现出足够的前列腺减少效果，口服活性优异。 本申请的化合物可用于预防或治疗前列腺癌，良性前列腺增生等。 本发明还提供了可用于制备本发明化合物的新型中间体。

公开(公告)号：US07297698B2

公开(公告)日：2007-11-20

申请号：US10521119

申请日：2003-07-11

申请人： Nobuaki Taniguchi ,  Masakazu Imamura ,  Masahiko Hayakawa ,  Kenichi Kawaguchi ,  Takenori Kimura ,  Isao Kinoyama ,  Hiroyuki Kaizawa ,  Minoru Okada ,  Takashi Furutani

发明人： Nobuaki Taniguchi ,  Masakazu Imamura ,  Masahiko Hayakawa ,  Kenichi Kawaguchi ,  Takenori Kimura ,  Isao Kinoyama ,  Hiroyuki Kaizawa ,  Minoru Okada ,  Takashi Furutani

IPC分类号： A61K31/4965 ,  C07D403/00

CPC分类号： C07D213/75 ,  C07D213/84 ,  C07D239/42 ,  C07D295/215

摘要： The present invention relates to a novel N-phenyl-(2R,5S)dimethylpiperazine derivatives useful as antiandrogenic agent which exhibits a sufficient prostate gland reducing effect as compared with conventional compounds and are excellent in oral activity. The compound of the present application is useful in preventing or treating prostate cancer, benign prostatic hyperplasia, and the like. The present invention also provides a novel intermediate useful in producing the compound of the present invention.

摘要翻译： 本发明涉及用作抗雄激素剂的新型N-苯基 - （2R，5S）二甲基哌嗪衍生物，其与常规化合物相比表现出足够的前列腺减少效果，口服活性优异。 本申请的化合物可用于预防或治疗前列腺癌，良性前列腺增生等。 本发明还提供了可用于制备本发明化合物的新型中间体。

公开(公告)号：US20050261303A1

公开(公告)日：2005-11-24

申请号：US10521119

申请日：2003-07-11

申请人： Nobuaki Taniguchi ,  Masakazu Imamura ,  Masahiko Hayakawa ,  Kenichi Kawaguchi ,  Takenori Kimura ,  Isao Kinoyama ,  Hiroyuki Kaizawa ,  Minoru Okada ,  Takashi Furutani

发明人： Nobuaki Taniguchi ,  Masakazu Imamura ,  Masahiko Hayakawa ,  Kenichi Kawaguchi ,  Takenori Kimura ,  Isao Kinoyama ,  Hiroyuki Kaizawa ,  Minoru Okada ,  Takashi Furutani

IPC分类号： A61P5/28 ,  A61P13/08 ,  A61P17/08 ,  A61P17/14 ,  A61P35/00 ,  C07D213/75 ,  C07D213/84 ,  C07D239/42 ,  C07D295/215 ,  A61K31/496 ,  A61K31/506 ,  C07D43/02

CPC分类号： C07D213/75 ,  C07D213/84 ,  C07D239/42 ,  C07D295/215

摘要： The present invention relates to a novel N-phenyl-(2R,5S)dimethylpiperazine derivatives useful as antiandrogenic agent which exhibits a sufficient prostate gland reducing effect as compared with conventional compounds and are excellent in oral activity. The compound of the present application is useful in preventing or treating prostate cancer, benign prostatic hyperplasia, and the like. The present invention also provides a novel intermediate useful in producing the compound of the present invention.

摘要翻译： 本发明涉及用作抗雄激素剂的新型N-苯基 - （2R，5S）二甲基哌嗪衍生物，其与常规化合物相比表现出足够的前列腺减少效果，口服活性优异。 本申请的化合物可用于预防或治疗前列腺癌，良性前列腺增生等。 本发明还提供了可用于制备本发明化合物的新型中间体。

公开(公告)号：US20080214543A1

公开(公告)日：2008-09-04

申请号：US11861327

申请日：2007-09-26

申请人： Nobuaki Taniguchi ,  Masakazu Imamura ,  Masahiko Hayakawa ,  Kenichi Kawaguchi ,  Isao Kinoyama ,  Hiroyuki Kaizawa ,  Minoru Okada ,  Takashi Furutani

发明人： Nobuaki Taniguchi ,  Masakazu Imamura ,  Masahiko Hayakawa ,  Kenichi Kawaguchi ,  Isao Kinoyama ,  Hiroyuki Kaizawa ,  Minoru Okada ,  Takashi Furutani

IPC分类号： A61K31/5355 ,  C07D413/14 ,  A61K31/497 ,  C07D401/14

CPC分类号： C07D213/75 ,  C07D213/84 ,  C07D239/42 ,  C07D295/215

摘要： The present invention relates to a novel N-phenyl-(2R,5S)dimethylpiperazine derivatives useful as antiandrogenic agent which exhibits a sufficient prostate gland reducing effect as compared with conventional compounds and are excellent in oral activity. The compound of the present application is useful in preventing or treating prostate cancer, benign prostatic hyperplasia, and the like. The present invention also provides a novel intermediate useful in producing the compound of the present invention.

摘要翻译： 本发明涉及用作抗雄激素剂的新型N-苯基 - （2R，5S）二甲基哌嗪衍生物，其与常规化合物相比表现出足够的前列腺减少效果，口服活性优异。 本申请的化合物可用于预防或治疗前列腺癌，良性前列腺增生等。 本发明还提供了可用于制备本发明化合物的新型中间体。

公开(公告)号：US20050090498A1

公开(公告)日：2005-04-28

申请号：US10478504

申请日：2002-05-23

申请人： Kiyohiro Samizu ,  Hiroyuki Hisamichi ,  Akira Matsuhisa ,  Isao Kinoyama ,  Masahiko Hayakawa ,  Nobuaki Taniguchi ,  Yukitaka Ideyama ,  Sadao Kuromitsu ,  Kiyoshi Yahiro ,  Minoru Okada

发明人： Kiyohiro Samizu ,  Hiroyuki Hisamichi ,  Akira Matsuhisa ,  Isao Kinoyama ,  Masahiko Hayakawa ,  Nobuaki Taniguchi ,  Yukitaka Ideyama ,  Sadao Kuromitsu ,  Kiyoshi Yahiro ,  Minoru Okada

IPC分类号： A61P27/02 ,  A61P35/00 ,  A61P43/00 ,  C07D209/34 ,  C07D211/22 ,  C07D215/12 ,  C07D215/60 ,  C07D263/10 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/10 ,  C07D491/113 ,  C07D493/04 ,  C07D471/02 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/498 ,  A61K31/519

CPC分类号： C07D263/10 ,  C07D209/34 ,  C07D211/22 ,  C07D215/12 ,  C07D215/60 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/10 ,  C07D493/04

摘要： There is provided medicaments, particularly a vascular endothelial growth factor (VEGF) inhibitor which is useful as a therapeutic drug for solid tumors, diabetic retinopathy and the like diseases in which angiogenesis is taking a role. That is, since a novel 3-quinolin-2(1H)-ylideneindolin-2-one derivative or a salt thereof has good VEGF inhibitory action, angiogenesis inhibitory action and anti-tumor action, it is useful as ideal VEGF inhibitor, angiogenesis inhibitor and anti-tumor agent.

摘要翻译： 提供了药物，特别是血管内皮生长因子（VEGF）抑制剂，其可用作实体瘤的治疗药物，糖尿病性视网膜病变等血管生成正在起作用的疾病。 也就是说，由于新型3-喹啉-2（1H） - 亚基二氢吲哚-2-酮衍生物或其盐具有良好的VEGF抑制作用，血管生成抑制作用和抗肿瘤作用，因此可用作理想的VEGF抑制剂，血管生成抑制剂 和抗肿瘤剂。

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.

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.

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.

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.

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.