公开(公告)号：US20080214543A1

公开(公告)日：2008-09-04

申请号：US11861327

申请日：2007-09-26

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

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

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

CPC classification number: C07D213/75 ,  C07D213/84 ,  C07D239/42 ,  C07D295/215

Abstract: 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.

Abstract translation: 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：US06403588B1

公开(公告)日：2002-06-11

申请号：US09843610

申请日：2001-04-26

Applicant: Masahiko Hayakawa ,  Hiroyuki Kaizawa ,  Ken-Ichi Kawaguchi ,  Koyo Matsuda ,  Noriko Ishikawa ,  Tomonobu Koizumi ,  Mayumi Yamano ,  Minoru Okada ,  Mitsuaki Ohta

Inventor： Masahiko Hayakawa ,  Hiroyuki Kaizawa ,  Ken-Ichi Kawaguchi ,  Koyo Matsuda ,  Noriko Ishikawa ,  Tomonobu Koizumi ,  Mayumi Yamano ,  Minoru Okada ,  Mitsuaki Ohta

IPC: A61K31435

CPC classification number: C07D471/04 ,  A61K31/435 ,  C07D487/04

Abstract: 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：US20110319385A1

公开(公告)日：2011-12-29

申请号：US13254368

申请日：2010-03-04

Applicant: Hiroyuki Kaizawa ,  Mari Sugita ,  Hidenori Azami ,  Ryushi Seo ,  Takaho Nomura ,  Satoshi Yamamoto ,  Hirofumi Yamamoto ,  Kazuyuki Tsuchiya ,  Hideki Kubota ,  Kazunori Kamijo

Inventor： Hiroyuki Kaizawa ,  Mari Sugita ,  Hidenori Azami ,  Ryushi Seo ,  Takaho Nomura ,  Satoshi Yamamoto ,  Hirofumi Yamamoto ,  Kazuyuki Tsuchiya ,  Hideki Kubota ,  Kazunori Kamijo

IPC: A61K31/4985 ,  C07D413/14 ,  A61P13/00 ,  A61K31/5377 ,  A61K31/55 ,  C07D487/04 ,  C07D403/14

CPC classification number: C07D498/04 ,  C07D487/04 ,  C07D491/107 ,  C07D519/00

Abstract: [Problem]Provided is a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like.[Means for Solution]The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like, and thus, have found that an imidazoquinoxaline compound or a triazoloquinoxaline compound has a PDE9-inhibiting action, thereby completing the present invention. The imidazoquinoxaline compound or the triazoloquinoxaline compound of the present invention has a PDE9-inhibiting action and can be used as an agent for preventing and/or treating storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like.

Abstract translation: [问题]提供具有PDE9抑制作用并可用作治疗和/或预防储存功能障碍，排尿功能障碍和膀胱/尿道疾病的药剂的活性成分的化合物等。 [解决方案]本发明人已经研究了具有PDE9抑制作用并可用作治疗和/或预防储存功能障碍，排尿功能障碍和膀胱/尿道疾病等的活性成分的化合物 ，因此已经发现咪唑并喹喔啉化合物或三唑并喹喔啉化合物具有抑制PDE9的作用，从而完成了本发明。 本发明的咪唑并喹喔啉化合物或三唑并喹喔啉化合物具有PDE9抑制作用，可用作预防和/或治疗储存功能障碍，排尿功能障碍和膀胱/尿道疾病等的药剂。

公开(公告)号：US06608053B2

公开(公告)日：2003-08-19

申请号：US09843615

申请日：2001-04-26

Applicant: Masahiko Hayakawa ,  Hiroyuki Kaizawa ,  Hiroyuki Moritomo ,  Ken-Ichi Kawaguchi ,  Tomonobu Koizumi ,  Mayumi Yamano ,  Koyo Matsuda ,  Minoru Okada ,  Mitsuaki Ohta

Inventor： Masahiko Hayakawa ,  Hiroyuki Kaizawa ,  Hiroyuki Moritomo ,  Ken-Ichi Kawaguchi ,  Tomonobu Koizumi ,  Mayumi Yamano ,  Koyo Matsuda ,  Minoru Okada ,  Mitsuaki Ohta

IPC: C07D41304

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

Abstract: 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：US20120184521A1

公开(公告)日：2012-07-19

申请号：US13498159

申请日：2010-09-24

Applicant: Eiji Kawaminami ,  Tatsuhisa Takahashi ,  Takatoshi Kanayama ,  Yuta Fukuda ,  Hiroyuki Kaizawa ,  Yutaka Kondoh ,  Ryushi Seo ,  Kazuyuki Kuramoto ,  Kazuhiko Take ,  Kazuyuki Sakamoto

Inventor： Eiji Kawaminami ,  Tatsuhisa Takahashi ,  Takatoshi Kanayama ,  Yuta Fukuda ,  Hiroyuki Kaizawa ,  Yutaka Kondoh ,  Ryushi Seo ,  Kazuyuki Kuramoto ,  Kazuhiko Take ,  Kazuyuki Sakamoto

IPC: A61K31/426 ,  C07D417/12 ,  A61K31/427 ,  A61K31/496 ,  A61P43/00 ,  A61K31/513 ,  A61K31/538 ,  A61K31/454 ,  A61K31/541 ,  C07D277/56 ,  A61K31/4439

CPC classification number: A61K31/426 ,  A61K31/341 ,  A61K31/381 ,  A61K31/401 ,  A61K31/415 ,  A61K31/42 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/4965 ,  C07D207/34 ,  C07D213/81 ,  C07D263/34 ,  C07D277/56 ,  C07D307/68 ,  C07D333/38 ,  C07D417/12

Abstract: A substituted amide compound is useful as an active ingredient of a pharmaceutical composition, in particular a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA). The compound is of a formula: In this formula, A is an optionally substituted aryl, etc.; B is an optionally substituted 5-membered aromatic hetero ring group; X is a single bond or —(CRX1RX2)n—; n is 1, 2, 3, or 4; RX1 and RX2 are hydrogen, etc.; Y1 to Y5 are each CRY or N; each RY is hydrogen, etc.; R1 and R2 are hydrogen, etc.; m is 1, 2, or 3; R3 is hydrogen, etc.; and R4 is an optionally substituted lower alkyl, etc.

Abstract translation: 取代的酰胺化合物可用作药物组合物的活性成分，特别是用于治疗由溶血磷脂酸（LPA）引起的疾病的药物组合物。 该化合物具有下式：在该式中，A是任选取代的芳基等; B是任选取代的5元芳族杂环基团; X是单键或 - （CRX1RX2）n-; n为1,2,3或4; RX1和RX2是氢等; Y1〜Y5分别为CRY或N; 每个RY是氢等; R1和R2是氢等; m为1,2或3; R3是氢等; 并且R 4是任选取代的低级烷基等。

公开(公告)号：US20100137585A1

公开(公告)日：2010-06-03

申请号：US12688273

申请日：2010-01-15

Applicant: Masahiko Hayakawa ,  Hiroyuki Kaizawa ,  Hiroyuki Moritomo ,  Ken-Ichi Kawaguchi ,  Tomonobu Koizumi ,  Mayumi Yamano ,  Koyo Matsuda ,  Minoru Okada ,  Mitsuaki Ohta

Inventor： Masahiko Hayakawa ,  Hiroyuki Kaizawa ,  Hiroyuki Moritomo ,  Ken-Ichi Kawaguchi ,  Tomonobu Koizumi ,  Mayumi Yamano ,  Koyo Matsuda ,  Minoru Okada ,  Mitsuaki Ohta

IPC: C07D487/04 ,  C07D491/048 ,  C07D495/04

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

Abstract: 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：US07666873B2

公开(公告)日：2010-02-23

申请号：US11861327

申请日：2007-09-26

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

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

IPC: A61K31/497 ,  C07D401/00

CPC classification number: C07D213/75 ,  C07D213/84 ,  C07D239/42 ,  C07D295/215

Abstract: 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.

Abstract translation: 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：US08357688B2

公开(公告)日：2013-01-22

申请号：US13254368

申请日：2010-03-04

Applicant: Hiroyuki Kaizawa ,  Mari Sugita ,  Hidenori Azami ,  Ryushi Seo ,  Takaho Nomura ,  Satoshi Yamamoto ,  Hirofumi Yamamoto ,  Kazuyuki Tsuchiya ,  Hideki Kubota ,  Kazunori Kamijo

Inventor： Hiroyuki Kaizawa ,  Mari Sugita ,  Hidenori Azami ,  Ryushi Seo ,  Takaho Nomura ,  Satoshi Yamamoto ,  Hirofumi Yamamoto ,  Kazuyuki Tsuchiya ,  Hideki Kubota ,  Kazunori Kamijo

IPC: A61K31/495

CPC classification number: C07D498/04 ,  C07D487/04 ,  C07D491/107 ,  C07D519/00

Abstract: Substituted imidazo[1,5-a]quinoxalin-4(5H)-ones are useful as PDE9 inhibitors.

Abstract translation: 取代的咪唑并[1,5-a]喹喔啉-4（5H） - 酮可用作PDE9抑制剂。

公开(公告)号：US07196080B2

公开(公告)日：2007-03-27

申请号：US10480543

申请日：2002-06-13

Applicant: Masahiro Iwata ,  Noriyuki Kawano ,  Hiroyuki Kaizawa ,  Tomofumi Takuwa ,  Issei Tsukamoto ,  Ryushi Seo ,  Kiyoshi Yahiro ,  Miki Kobayashi ,  Makoto Takeuchi

Inventor： Masahiro Iwata ,  Noriyuki Kawano ,  Hiroyuki Kaizawa ,  Tomofumi Takuwa ,  Issei Tsukamoto ,  Ryushi Seo ,  Kiyoshi Yahiro ,  Miki Kobayashi ,  Makoto Takeuchi

IPC: A61K31/496 ,  C07D401/06 ,  C07D401/14 ,  C07D413/14 ,  C07D213/79

CPC classification number: C07D213/79 ,  A61K31/439 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/55 ,  C07D213/81 ,  C07D213/89 ,  C07D401/12 ,  C07D405/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08

Abstract: The present invention relates to a compound which is represented by the following general formula and has type 4 phosphodiesterase inhibitory action, and uses and an intermediate compound thereof. (wherein R1, R2: hydrogen, a halogen, a lower alkyl, a lower alkoxy, or the like, R3, R4: hydrogen, a (substituted) lower alkyl, a halogen, or the like, R5: hydrogen, a lower alkyl, a lower alkoxycarbonyl, or the like, and n: 0 or 1).

Abstract translation: 本发明涉及由以下通式表示的具有4型磷酸二酯酶抑制作用的化合物及其用途及其中间体化合物。

公开(公告)号：US20070037805A1

公开(公告)日：2007-02-15

申请号：US11544144

申请日：2006-10-06

Applicant: Masahiko Hayakawa ,  Hiroyuki Kaizawa ,  Hiroyuki Moritomo ,  Ken-Ichi Kawaguchi ,  Tomonobu Koizumi ,  Mayumi Yamano ,  Koyo Matsuda ,  Minoru Okada ,  Mitsuaki Ohta

Inventor： Masahiko Hayakawa ,  Hiroyuki Kaizawa ,  Hiroyuki Moritomo ,  Ken-Ichi Kawaguchi ,  Tomonobu Koizumi ,  Mayumi Yamano ,  Koyo Matsuda ,  Minoru Okada ,  Mitsuaki Ohta

IPC: A61K31/5377

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

Abstract: 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.