公开(公告)号：US20060142268A1

公开(公告)日：2006-06-29

申请号：US11353995

申请日：2006-02-15

申请人： Hiroyuki Koshio ,  Akio Kakefuda ,  Ippei Sato ,  Ryutaro Wakayama ,  Masanao Sanagi

发明人： Hiroyuki Koshio ,  Akio Kakefuda ,  Ippei Sato ,  Ryutaro Wakayama ,  Masanao Sanagi

IPC分类号： A61K31/55 ,  C07D487/02

CPC分类号： C07D487/04

摘要： To provide a compound having a superior arginine vasopressin antagonism. A novel 1,4,5,6-tetrahydroimidazo[4,5-d]benzazepine derivative or a pharmaceutically acceptable salt thereof.

摘要翻译： 提供具有优异精氨酸加压素拮抗作用的化合物。 一种新的1,4,5,6-四氢咪唑并[4,5-d]苯并吖庚因衍生物或其药学上可接受的盐。

公开(公告)号：US07056910B2

公开(公告)日：2006-06-06

申请号：US10432732

申请日：2001-11-27

申请人： Hiroyuki Koshio ,  Akio Kakefuda ,  Ippei Sato ,  Ryutaro Wakayama ,  Masanao Sanagi

发明人： Hiroyuki Koshio ,  Akio Kakefuda ,  Ippei Sato ,  Ryutaro Wakayama ,  Masanao Sanagi

IPC分类号： A61P9/00 ,  A61K31/55 ,  A07D487/00

CPC分类号： C07D487/04

摘要： To provide a compound having a superior arginine vasopressin antagonism. A novel 1,4,5,6-tetrahydroimidazo[4,5-d]benzazepine derivative or a pharmaceutically acceptable salt thereof.

摘要翻译： 提供具有优异精氨酸加压素拮抗作用的化合物。 一种新的1,4,5,6-四氢咪唑并[4,5-d]苯并吖庚因衍生物或其药学上可接受的盐。

公开(公告)号：US20110172230A1

公开(公告)日：2011-07-14

申请号：US12377918

申请日：2007-08-22

申请人： Takahiro Ishii ,  Takashi Sugane ,  Akio Kakefuda ,  Tatsuhisa Takahashi ,  Tokatoshi Kanayama ,  Kentaro Sato ,  Ikumi Kuriwaki ,  Chika Kitada ,  Jotaro Suzuki

发明人： Takahiro Ishii ,  Takashi Sugane ,  Akio Kakefuda ,  Tatsuhisa Takahashi ,  Tokatoshi Kanayama ,  Kentaro Sato ,  Ikumi Kuriwaki ,  Chika Kitada ,  Jotaro Suzuki

IPC分类号： A61K31/5377 ,  C07D401/12 ,  A61K31/4545 ,  C07D211/46 ,  A61K31/445 ,  C07D401/06 ,  A61K31/454 ,  A61K31/496 ,  C07D403/06 ,  C07D401/14 ,  A61K31/497 ,  C07D403/12 ,  A61K31/501 ,  A61K31/4725 ,  A61K31/4709 ,  C07D413/14 ,  A61K31/506 ,  A61K31/53 ,  A61P13/00

CPC分类号： C07D209/08 ,  C07D211/44 ,  C07D213/74 ,  C07D235/30 ,  C07D237/22 ,  C07D249/14 ,  C07D251/42 ,  C07D285/135 ,  C07D295/16 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

摘要： [Object] To provide a compound which can be used for the treatment of a disease associated with fatty acid amide hydrolase (FAAH), particularly urinary frequency, urinary incontinence and/or overactive bladder.[Means for solution] It is confirmed that a urea compound chemical-structurally characterized by having a piperidine or piperazine ring or a salt thereof has an excellent FAAH-inhibitory activity, and thus the present invention is completed. The urea compound or its pharmaceutically acceptable salt of the present invention can increase the effective bladder capacity and ameliorate the state of urinary frequency, and is therefore useful as an agent for treating urinary frequency, urinary incontinence and/or overactive bladder.

摘要翻译： 提供可用于治疗与脂肪酰胺水解酶（FAAH）相关疾病，特别是尿频，尿失禁和/或膀胱过度活动症的化合物。 [解决方法]确认化学结构特征在于具有哌啶或哌嗪环或其盐的脲化合物具有优异的FAAH抑制活性，从而完成了本发明。 本发明的尿素化合物或其药学上可接受的盐可以增加膀胱的有效性并改善尿频的状态，因此可用作治疗尿频，尿失禁和/或膀胱过度活动症的药剂。

公开(公告)号：US08513422B2

公开(公告)日：2013-08-20

申请号：US12675744

申请日：2008-08-28

申请人： Akio Kakefuda ,  Kazushi Watanabe ,  Akio Kamikawa ,  Kentaro Enjo ,  Takashi Furutani ,  Minoru Yasuda

发明人： Akio Kakefuda ,  Kazushi Watanabe ,  Akio Kamikawa ,  Kentaro Enjo ,  Takashi Furutani ,  Minoru Yasuda

IPC分类号： A61K31/445 ,  C07D211/32

CPC分类号： C07D401/06

摘要： As a result of studies on compounds having a selective inhibitory activity against 17βHSD type 5, the present inventors have confirmed that a {1-[(indol-2-yl)carbonyl]piperidyl}alkanol derivative has a potent selective inhibitory activity against 17βHSD type 5. The invention has been completed based on these findings. The compound of the present invention can be used as an agent for treating and/or an agent for preventing diseases associated with 17βHSD type 5, such as benign prostatic hyperplasia and prostate cancer, without accompanying adverse effects due to a decrease in testosterone.

摘要翻译： 作为对具有针对17βHSD5型选择性抑制活性的化合物的研究结果，本发明人已证实{1 - [（吲哚-2-基）羰基]哌啶基}链烷醇衍生物对17βHSD型具有有效的选择性抑制活性 基于这些发现完成了本发明。 本发明的化合物可以用作治疗剂和/或用于预防与17βHSD5型相关的疾病，如良性前列腺增生和前列腺癌，而不伴随睾丸激素降低引起的不良反应。

公开(公告)号：US20090181960A1

公开(公告)日：2009-07-16

申请号：US12281416

申请日：2007-03-01

申请人： Tatsuya Niimi ,  Akio Kamikawa ,  Yasushi Amano ,  Tomohiko Yamaguchi ,  Kenichi Suzumura ,  Kentaro Enjo ,  Takashi Furutani ,  Akio Kakefuda ,  Yutaka Kondoh ,  Masaaki Hirano

发明人： Tatsuya Niimi ,  Akio Kamikawa ,  Yasushi Amano ,  Tomohiko Yamaguchi ,  Kenichi Suzumura ,  Kentaro Enjo ,  Takashi Furutani ,  Akio Kakefuda ,  Yutaka Kondoh ,  Masaaki Hirano

IPC分类号： A61K31/404 ,  C07D209/42 ,  C07D413/12 ,  A61K31/538 ,  A61P35/00

CPC分类号： C07D209/08 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04

摘要： To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selective inhibitory activity against 17βHSD type 5.It was found that an N-sulfonylindole derivative, where the indole ring is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group at its carbon atom, has potent selective inhibitory activity against 17βHSD type 5 and may become a therapeutic agent and/or preventive agent for benign prostatic hyperplasia, prostatic cancer and the like without accompanying adverse drug reactions due to a decrease in testosterone, and the present invention has thus been completed.

摘要翻译： 提供治疗和/或预防前列腺癌，良性前列腺增生，痤疮，皮脂溢，多毛症，秃发，脱发，早熟青春期，肾上腺肥大，多囊卵巢综合征，乳腺癌，肺癌，子宫内膜异位症，平滑肌瘤和 其基于对17βHSD型5的选择性抑制活性。发现其吲哚环被羧基取代的N-磺基吲哚衍生物，羧基取代的低级烷基或羧基取代的低级烯基 碳原子对17betaHSD型5具有有效的选择性抑制活性，并且可能成为由于睾丸激素降低引起的伴随不良药物反应的良性前列腺增生，前列腺癌等的治疗剂和/或预防剂，本发明具有 从而完成。

公开(公告)号：US20060084807A1

公开(公告)日：2006-04-20

申请号：US10540421

申请日：2003-12-24

申请人： Shinya Yoshida ,  Toshihiro Watanabe ,  Kiyotaka Marumo ,  Akio Kakefuda

发明人： Shinya Yoshida ,  Toshihiro Watanabe ,  Kiyotaka Marumo ,  Akio Kakefuda

IPC分类号： C07D401/02

CPC分类号： C07D401/06 ,  C07D211/60

摘要： There are provided a novel process for the production of an isoquinoline derivative having an inhibitory action for If current; a novel benzamide derivative or a salt thereof used for the production process; and a process for the production of the benzamide derivative or a salt thereof.

摘要翻译： 提供了一种制备具有对I电流的抑制作用的异喹啉衍生物的新方法; 用于生产过程的新型苯甲酰胺衍生物或其盐; 以及生产苯甲酰胺衍生物或其盐的方法。

公开(公告)号：US20110071146A1

公开(公告)日：2011-03-24

申请号：US12943435

申请日：2010-11-10

申请人： Tatsuya Niimi ,  Akio Kamikawa ,  Yasushi Amano ,  Tomohiko Yamaguchi ,  Kenichi Suzumura ,  Kentaro Enjo ,  Takashi Furutani ,  Akio Kakefuda ,  Yutaka Kondoh ,  Masaaki Hirano

发明人： Tatsuya Niimi ,  Akio Kamikawa ,  Yasushi Amano ,  Tomohiko Yamaguchi ,  Kenichi Suzumura ,  Kentaro Enjo ,  Takashi Furutani ,  Akio Kakefuda ,  Yutaka Kondoh ,  Masaaki Hirano

IPC分类号： A61K31/536 ,  A61K31/40 ,  A61K31/415 ,  A61K31/44 ,  A61K31/41 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/42 ,  A61P13/08

CPC分类号： C07D209/08 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04

摘要： To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selective inhibitory activity against 17βHSD type 5.It was found that an N-sulfonylindole derivative, where the indole ring is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group at its carbon atom, has potent selective inhibitory activity against 17βHSD type 5 and may become a therapeutic agent and/or preventive agent for benign prostatic hyperplasia, prostatic cancer and the like without accompanying adverse drug reactions due to a decrease in testosterone, and the present invention has thus been completed.

摘要翻译： 提供治疗和/或预防前列腺癌，良性前列腺增生，痤疮，皮脂溢，多毛症，秃发，脱发，早熟青春期，肾上腺肥大，多囊卵巢综合征，乳腺癌，肺癌，子宫内膜异位症，平滑肌瘤和 基于针对17＆amp; HSD型5的选择性抑制活性的类似物。已经发现，吲哚环被羧基取代的N-磺基吲哚衍生物，羧基取代的低级烷基或羧基取代的低级烯基 在其碳原子上具有对17和HSD 5型的有效的选择性抑制活性，并且可能成为由于睾丸激素降低引起的伴有不良药物反应的良性前列腺增生，前列腺癌等的治疗剂和/或预防剂， 从而完成了本发明。

公开(公告)号：US07855225B2

公开(公告)日：2010-12-21

申请号：US12281416

申请日：2007-03-01

申请人： Tatsuya Niimi ,  Akio Kamikawa ,  Yasushi Amano ,  Tomohiko Yamaguchi ,  Kenichi Suzumura ,  Kentaro Enjo ,  Takashi Furutani ,  Akio Kakefuda ,  Yutaka Kondoh ,  Masaaki Hirano

发明人： Tatsuya Niimi ,  Akio Kamikawa ,  Yasushi Amano ,  Tomohiko Yamaguchi ,  Kenichi Suzumura ,  Kentaro Enjo ,  Takashi Furutani ,  Akio Kakefuda ,  Yutaka Kondoh ,  Masaaki Hirano

IPC分类号： C07D209/42 ,  A61K31/404

CPC分类号： C07D209/08 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04

摘要： To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selective inhibitory activity against 17βHSD type 5.It was found that an N-sulfonylindole derivative, where the indole ring is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group at its carbon atom, has potent selective inhibitory activity against 17βHSD type 5 and may become a therapeutic agent and/or preventive agent for benign prostatic hyperplasia, prostatic cancer and the like without accompanying adverse drug reactions due to a decrease in testosterone, and the present invention has thus been completed.

摘要翻译： 提供治疗和/或预防前列腺癌，良性前列腺增生，痤疮，皮脂溢，多毛症，秃发，脱发，早熟性青春期，肾上腺肥大，多囊卵巢综合征，乳腺癌，肺癌，子宫内膜异位症，平滑肌瘤和 基于针对17＆amp; HSD型5的选择性抑制活性的类似物。已经发现，吲哚环被羧基取代的N-磺基吲哚衍生物，羧基取代的低级烷基或羧基取代的低级烯基 在其碳原子上具有对17和HSD 5型的有效的选择性抑制活性，并且可能成为由于睾丸激素降低引起的伴有不良药物反应的良性前列腺增生，前列腺癌等的治疗剂和/或预防剂， 从而完成了本发明。

公开(公告)号：US20100190826A1

公开(公告)日：2010-07-29

申请号：US12670384

申请日：2008-07-23

申请人： Akio Kakefuda ,  Yutaka Kondoh ,  Masaaki Hirano ,  Akio Kamikawa ,  Kentaro Enjo ,  Takashi Furutani

发明人： Akio Kakefuda ,  Yutaka Kondoh ,  Masaaki Hirano ,  Akio Kamikawa ,  Kentaro Enjo ,  Takashi Furutani

IPC分类号： A61K31/4184 ,  C07D209/04 ,  C07D235/18 ,  C07D403/04 ,  A61K31/404 ,  A61K31/454 ,  A61P35/00 ,  A61P17/10

CPC分类号： C07D209/08 ,  C07D209/12 ,  C07D235/06 ,  C07D235/08 ,  C07D235/10 ,  C07D235/12 ,  C07D235/18 ,  C07D235/26 ,  C07D401/04 ,  C07D401/06 ,  C07D405/04

摘要： Provided is a novel and excellent method for treating and/or preventing benign prostatic hyperplasia, prostate cancer, and the like based on selective inhibitory activity against 17βHSD type 5. It was found that an indole or benzimidazole derivative, where a nitrogen atom of the indole ring or benzimidazole ring is substituted with a phenyl group substituted with COOH, has a potent selective inhibitory activity against 17βHSD type 5 and may become an agent for treating and/or an agent for preventing a disease associated with 17βHSD type 5, such as benign prostatic hyperplasia, prostate cancer and the like, without accompanying adverse effects due to a decrease in testosterone; and the present invention has thus been completed.

摘要翻译： 本发明提供了一种用于治疗和/或预防良性前列腺增生症，前列腺癌等的基于17＆amp; HSD型5的选择性抑制活性的新颖且优异的方法。发现吲哚或苯并咪唑衍生物，其中氮 吲哚环或苯并咪唑环被用COOH取代的苯基取代，对17和HSD 5型具有有效的选择性抑制活性，并且可以成为用于治疗和/或用于预防与17型糖尿病相关的疾病的药物 5，如良性前列腺增生，前列腺癌等，不伴随睾丸激素降低引起的不良反应; 从而完成了本发明。

公开(公告)号：US06573279B1

公开(公告)日：2003-06-03

申请号：US09980402

申请日：2001-12-03

申请人： Toshihiro Watanabe ,  Akio Kakefuda ,  Toshio Okazaki ,  Noriyuki Masuda ,  Koichi Wada

发明人： Toshihiro Watanabe ,  Akio Kakefuda ,  Toshio Okazaki ,  Noriyuki Masuda ,  Koichi Wada

IPC分类号： A61K3147

CPC分类号： C07D401/06 ,  C07D405/14

摘要： The compound of the present invention relates to a drug, particularly to a novel isoquinoline derivative or its salt having an If current inhibitory effect without serious side effects such as convulsion and also to a drug, particularly a cardiac rate lowering agent, containing the compound as the active ingredient. Namely, the compound has a current If inhibitory effect and is particularly useful as a cardiac rate lowering agent for preventing ischemic heart diseases such as angina and cardiac infarction and circulatory diseases such as congestive cardiac insufficiency and arrhythmia (supraventricular arrhythmia). The present invention relates to dialkoxy-1,2,3,4-tetrahydroquinoline-2-carbonylpiperidino-3,4-dialkoxypropaneanilide derivatives, etc.

摘要翻译： 本发明的化合物涉及一种药物，特别是涉及一种新颖的异喹啉衍生物或其盐，其具有无剧烈反应的If电流抑制作用，还涉及含有化合物的药物，特别是心率降低剂 活性成分。 也就是说，该化合物具有电流If抑制作用，并且特别可用作用于预防心绞痛和心肌梗死以及诸如充血性心功能不全和心律失常（室上性心律不齐）的循环系统疾病的心脏病降低剂。 本发明涉及二烷氧基-1,2,3,4-四氢喹啉-2-羰基哌啶子基-3,4-二烷氧基丙酰苯胺衍生物等