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1. 发明授权

US06734203B2 Fused imidazolium derivatives 有权
标题翻译：熔融咪唑鎓衍生物
公开(公告)号：US06734203B2
公开(公告)日：2004-05-11
申请号：US10169409
申请日：2002-07-01
申请人： Akira Matsuhisa , Isao Kinoyama , Akira Toyoshima , Takahito Nakahara , Masahiro Takeuchi , Minoru Okada
发明人： Akira Matsuhisa , Isao Kinoyama , Akira Toyoshima , Takahito Nakahara , Masahiro Takeuchi , Minoru Okada
IPC分类号： A61K314184
CPC分类号： C07D213/64 , A61K31/36 , A61K31/416 , A61K31/4188 , A61K31/424 , A61K31/4245 , A61K31/427 , A61K31/429 , A61K31/437 , A61K31/4453 , A61K31/4468 , A61K31/454 , A61K31/47 , A61K31/4709 , A61K31/497 , A61K31/4985 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/519 , A61K31/5375 , A61K31/551 , C07C233/41 , C07C235/14 , C07C237/04 , C07C255/24 , C07C255/25 , C07C255/58 , C07C259/06 , C07C271/28 , C07C311/37 , C07C317/28 , C07C323/25 , C07C2601/02 , C07C2601/14 , C07C2602/10 , C07C2603/74 , C07D209/16 , C07D211/58 , C07D213/38 , C07D213/74 , C07D213/89 , C07D215/12 , C07D233/64 , C07D235/02 , C07D235/14 , C07D239/26 , C07D241/12 , C07D241/20 , C07D295/13 , C07D307/14 , C07D317/58 , C07D333/68 , C07D335/06 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/06 , C07D471/04 , C07D495/04
摘要： This invention relates to medicaments, particularly novel fused imidazolium derivatives useful for the treatment of cancers and novel synthetic intermediate compounds thereof. The novel imidazolium derivatives fused with an aryl or heteroaryl ring, characterized in that the 1- and/or 3-position is substituted by an alkyl group etc. having a substituent selected from the group consisting of —ORa, —SRa and the like, have excellent anti-tumor activity and low toxicity and are useful as anticancer agents having wide margins of safety.
摘要翻译：本发明涉及药物，特别是可用于治疗癌症的新型稠合咪唑衍生物及其新型合成中间体化合物。与芳基或杂芳基环稠合的新型咪唑衍生物，其特征在于1-和/或3-位被取代通过具有选自-OR，-SRa等的取代基的烷基等具有优异的抗肿瘤活性和低毒性，并且可用作具有宽的安全边缘的抗癌剂。

2. 发明授权

US06673799B1 Cyanophenyl derivative 失效
标题翻译：氰基苯基衍生物
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。

3. 发明申请

US20050090498A1 3-Quinolin-2(1h)-ylideneindolin-2-one derivative 审中-公开
标题翻译： 3-喹啉-2（1h） - 亚基二氢吲哚-2-酮衍生物
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。

4. 发明申请

US20060223831A1 Bromide and its crystal 审中-公开
标题翻译：溴化物及其水晶
公开(公告)号：US20060223831A1
公开(公告)日：2006-10-05
申请号：US10553151
申请日：2004-04-14
申请人： Isao Kinoyama , Kenichirou Sakamoto , Hiroki Okui , Noritaka Hamada , Akira Matsuhisa
发明人： Isao Kinoyama , Kenichirou Sakamoto , Hiroki Okui , Noritaka Hamada , Akira Matsuhisa
IPC分类号： A61K31/497 , C07D403/02
CPC分类号： C07D403/06
摘要： The 1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(pyrazin-2-ylmethyl)-4,9-dihydro-1H-naphtho[2,3-d]imidazol-3-ium bromide of the invention and its crystals, particularly α- and β- form Crystals, have no hygroscopic property, have excellent stability and therefore are useful as production materials of medicines. Particularly, the β- form Crystal is most stable and markedly useful as a bulk for medicines.
摘要翻译：将1-（2-甲氧基乙基）-2-甲基-4,9-二氧代-3-（吡嗪-2-基甲基）-4,9-二氢-1H-萘并[2,3-d]咪唑-3-酮本发明的溴化物及其晶体，特别是α-和β-晶体，不具有吸湿性，具有优异的稳定性，因此可用作药物的生产材料。特别地，晶体晶体是最稳定的并且显着地用作药物的主体。

5. 发明授权

US07666873B2 N-phenyl-(2R,5S)dimethylpiperazine derivative 有权
标题翻译： N-苯基 - （2R，5S）二甲基哌嗪衍生物
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。

6. 发明申请

US20080214543A1 N-Phenyl-(2R,5S)Dimethylpiperazine Derivative 有权
标题翻译： N-苯基 - （2R，5S）二甲基哌嗪衍生物
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。

7. 发明授权

US07297698B2 N-phenyl-(2R,5S) dimethylpiperazine derivative 有权
标题翻译： N-苯基 - （2R，5S）二甲基哌嗪衍生物
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。

8. 发明申请

US20050261303A1 N-phenyl-(2r,5s) dimethylpiperadine derivative 有权
标题翻译： N-苯基 - （2r，5s）二甲基哌啶衍生物
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。

9. 发明授权

US08076367B2 Benzimidazolylidene propane-1,3-dione derivative or salt thereof 失效
标题翻译：苯并咪唑基丙烷-1,3-二酮衍生物或其盐
公开(公告)号：US08076367B2
公开(公告)日：2011-12-13
申请号：US12726506
申请日：2010-03-18
申请人： Masaaki Hirano , Eiji Kawaminami , Isao Kinoyama , Shunichiro Matsumoto , Kei Ohnuki , Kazuyoshi Obitsu , Toshiyuki Kusayama
发明人： Masaaki Hirano , Eiji Kawaminami , Isao Kinoyama , Shunichiro Matsumoto , Kei Ohnuki , Kazuyoshi Obitsu , Toshiyuki Kusayama
IPC分类号： A01N43/52
CPC分类号： C07D401/06
摘要： Compounds useful as GnRH receptor antagonists are provided. The present inventors have further examined propane-1,3-dione derivatives and confirmed as a result that a propane-1,3-dione having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene), or a compound which has benzene or thiophene ring substituted with a group derived from 1-hydroxymethyl, shows excellent availability, in addition to its excellent GnRH receptor antagonism, thereby accomplishing the invention. Since the compound of the invention shows excellent availability, in addition to its strong GnRH receptor antagonism, it can be expected that it exerts superior drug effect in the living body, and it is useful for the treatment of sex hormone dependent diseases such as prostate cancer, breast cancer, endometriosis, uterine leiomyoma, benign prostatic hypertrophy and the like. In addition, since the compound of the invention is excellent in metabolic stability in human and also is less in drug interaction, it has more desirable properties as a medicament to be used for the aforementioned diseases.
摘要翻译：提供了可用作GnRH受体拮抗剂的化合物。本发明人进一步研究了丙-1,3-二酮衍生物，结果确认了具有2-（1,3-二氢-2H-苯并咪唑-2-亚基）的丙-1,3-二酮或化合物其具有被衍生自1-羟甲基的基团取代的苯或噻吩环，除了其优异的GnRH受体拮抗作用外，显示出优异的可利用性，从而完成本发明。由于本发明的化合物显示出优异的可利用性，除了其强的GnRH受体拮抗作用外，可以预期其在生物体中具有优异的药物作用，并且可用于治疗性激素依赖性疾病如前列腺癌，乳腺癌，子宫内膜异位症，子宫平滑肌瘤，良性前列腺肥大等。此外，由于本发明的化合物在人体中的代谢稳定性优异，药物相互作用也较少，因此作为上述疾病的药物具有更优选的特性。

10. 发明授权

US07960562B2 Propane-1,3-dione derivative or salt thereof 有权
标题翻译：丙烷-1,3-二酮衍生物或其盐
公开(公告)号：US07960562B2
公开(公告)日：2011-06-14
申请号：US11887384
申请日：2006-03-30
申请人： Masaaki Hirano , Isao Kinoyama , Shunichiro Matsumoto , Eiji Kawaminami , Kei Ohnuki , Hirofumi Yamamoto , Kazuhiko Osoda , Tatsuhisa Takahashi , Takashi Shin , Takanori Koike , Itsuro Shimada , Hiroyuki Hisamichi , Toshiyuki Kusayama
发明人： Masaaki Hirano , Isao Kinoyama , Shunichiro Matsumoto , Eiji Kawaminami , Kei Ohnuki , Hirofumi Yamamoto , Kazuhiko Osoda , Tatsuhisa Takahashi , Takashi Shin , Takanori Koike , Itsuro Shimada , Hiroyuki Hisamichi , Toshiyuki Kusayama
IPC分类号： A61K31/4184 , C07D235/12
CPC分类号： C07D235/12 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/10 , C07D413/12 , C07D417/06 , C07D417/12 , C07D417/14
摘要： It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by —SO2—R3 in a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.
摘要翻译：旨在提供可用作GnRH受体拮抗剂的化合物。本发明人进一步研究了丙烷-1,3-二酮衍生物。结果证实，在具有2-（1,3-二氢-2H-苯并咪唑）的丙烷-1,3-二酮衍生物中具有被-SO 2 -R 3表示的基团取代的苯环或噻吩环的化合物 -2-亚基）具有优异的GnRH受体拮抗作用，完成了本发明。因为本发明的化合物具有强的GnRH受体拮抗作用，因此可用于治疗性激素依赖性疾病，特别是GnRH相关疾病。此外，由于本发明的化合物在人体中具有优异的代谢稳定性，药物相互作用少，因此作为上述疾病的药物具有优选的特性。

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