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公开(公告)号：US20110172230A1
公开(公告)日：2011-07-14
申请号：US12377918
申请日：2007-08-22
Applicant: Takahiro Ishii , Takashi Sugane , Akio Kakefuda , Tatsuhisa Takahashi , Tokatoshi Kanayama , Kentaro Sato , Ikumi Kuriwaki , Chika Kitada , Jotaro Suzuki
Inventor： Takahiro Ishii , Takashi Sugane , Akio Kakefuda , Tatsuhisa Takahashi , Tokatoshi Kanayama , Kentaro Sato , Ikumi Kuriwaki , Chika Kitada , Jotaro Suzuki
IPC: 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 classification number: 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
Abstract: [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.
Abstract translation: 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。
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公开(公告)号：US08513422B2
公开(公告)日：2013-08-20
申请号：US12675744
申请日：2008-08-28
Applicant: Akio Kakefuda , Kazushi Watanabe , Akio Kamikawa , Kentaro Enjo , Takashi Furutani , Minoru Yasuda
Inventor： Akio Kakefuda , Kazushi Watanabe , Akio Kamikawa , Kentaro Enjo , Takashi Furutani , Minoru Yasuda
IPC: A61K31/445 , C07D211/32
CPC classification number: C07D401/06
Abstract: 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.
Abstract translation: 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。
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3.发明授权公开(公告)号：US07919494B2
公开(公告)日：2011-04-05
申请号：US12543690
申请日：2009-08-19
Applicant: Takahiro Ishii , Takashi Sugane , Jun Maeda , Fumie Narazaki , Akio Kakefuda , Kentaro Sato , Tatsuhisa Takahashi , Takatoshi Kanayama , Chikashi Saitoh , Jotaro Suzuki , Chisato Kanai
Inventor： Takahiro Ishii , Takashi Sugane , Jun Maeda , Fumie Narazaki , Akio Kakefuda , Kentaro Sato , Tatsuhisa Takahashi , Takatoshi Kanayama , Chikashi Saitoh , Jotaro Suzuki , Chisato Kanai
IPC: A61K31/496 , A61K31/4545 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/14
CPC classification number: A61K31/44 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/55 , C07D401/12
Abstract: A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.
Abstract translation: 新型吡啶基非芳族含氮杂环-1-羧酸酯化合物及其药学上可接受的盐具有有效的FAAH抑制活性。 此外，本公开的吡啶基非芳族含氮杂环-1-羧酸酯化合物也可用于治疗尿频和尿失禁，膀胱过度活动和/或疼痛。
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4.发明申请Pyridyl Non-Aromatic Nitrogen-Containing Heterocyclic-1-Carboxylate Compound 有权含吡啶基非芳香族氮的杂环-1-羧酸酯化合物公开(公告)号：US20100009971A1
公开(公告)日：2010-01-14
申请号：US12543659
申请日：2009-08-19
Applicant: Takahiro Ishii , Takashi Sugane , Jun Maeda , Fumie Narazaki , Akio Kakefuda , Kentaro Sato , Tatsuhisa Takahashi , Takatoshi Kanayama , Chikashi Saitoh , Jotaro Suzuki , Chisato Kanai
Inventor： Takahiro Ishii , Takashi Sugane , Jun Maeda , Fumie Narazaki , Akio Kakefuda , Kentaro Sato , Tatsuhisa Takahashi , Takatoshi Kanayama , Chikashi Saitoh , Jotaro Suzuki , Chisato Kanai
IPC: A61K31/4545 , A61K31/551 , A61K31/5377 , A61K31/496 , A61K31/4709 , A61K31/444 , C07D413/12 , C07D401/12 , A61P25/00 , C07D405/14 , A61P13/00
CPC classification number: A61K31/44 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/55 , C07D401/12
Abstract: A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound or its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.
Abstract translation: 新型吡啶基非芳族含氮杂环-1-羧酸盐化合物或其药学上可接受的盐具有有效的FAAH抑制活性。 此外，本公开的吡啶基非芳族含氮杂环-1-羧酸酯化合物也可用于治疗尿频和尿失禁，膀胱过度活动和/或疼痛。
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公开(公告)号：US20090181960A1
公开(公告)日：2009-07-16
申请号：US12281416
申请日：2007-03-01
Applicant: Tatsuya Niimi , Akio Kamikawa , Yasushi Amano , Tomohiko Yamaguchi , Kenichi Suzumura , Kentaro Enjo , Takashi Furutani , Akio Kakefuda , Yutaka Kondoh , Masaaki Hirano
Inventor： Tatsuya Niimi , Akio Kamikawa , Yasushi Amano , Tomohiko Yamaguchi , Kenichi Suzumura , Kentaro Enjo , Takashi Furutani , Akio Kakefuda , Yutaka Kondoh , Masaaki Hirano
IPC: A61K31/404 , C07D209/42 , C07D413/12 , A61K31/538 , A61P35/00
CPC classification number: C07D209/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D513/04
Abstract: 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.
Abstract translation: 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。
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Patent Agency Ranking
公开(公告)号：US20100256189A1
公开(公告)日：2010-10-07
申请号：US12675744
申请日：2008-08-28
Applicant: Akio KAKEFUDA
Inventor： Akio KAKEFUDA
IPC: A61K31/454 , C07D401/06 , C07D211/22 , A61K31/4525 , A61P35/00 , A61P17/08 , A61P17/10
CPC classification number: C07D401/06
Abstract: 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.
Abstract translation: 作为对17和HSD 5型选择性抑制活性的化合物的研究结果，本发明人证实{1 - [（吲哚-2-基）羰基]哌啶基}链烷醇衍生物具有强烈的选择性抑制活性， 17＆bgr; HSD型5.根据这些发现完成了本发明。 本发明的化合物可以用作治疗和/或用于预防与17型和HSD 5型相关的疾病的药物，例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。
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7.发明授权4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivative or salt thereof 有权4,4-二氟-1,2,3,4-四氢-5H-1-苯并氮杂衍生物或其盐公开(公告)号：US07807664B2
公开(公告)日：2010-10-05
申请号：US11598732
申请日：2006-11-14
Applicant: Hiroyuki Koshio , Issei Tsukamoto , Akio Kakefuda , Seijiro Akamatsu , Chikashi Saitoh
Inventor： Hiroyuki Koshio , Issei Tsukamoto , Akio Kakefuda , Seijiro Akamatsu , Chikashi Saitoh
IPC: A61P7/12 , A61K31/55 , C07D223/16
CPC classification number: C07D401/06 , C07D223/16
Abstract: A novel 4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivative or a pharmaceutically acceptable salt thereof, which is useful as an agent for treating or preventing nocturia and/or diabetes insipidus, is provided.
Abstract translation: 提供了可用作治疗或预防夜尿和/或尿崩症的药剂的新型的4,4-二氟-1,2,3,4-四氢-5H-1-苯并吖庚因衍生物或其药学上可接受的盐 。
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8.发明申请Pyridyl Non-Aromatic Nitrogen-Containing Heterocyclic-1-Carboxylate Compound 有权含吡啶基非芳香族氮的杂环-1-羧酸酯化合物公开(公告)号：US20100009972A1
公开(公告)日：2010-01-14
申请号：US12543690
申请日：2009-08-19
Applicant: Takahiro Ishii , Takashi Sugane , Jun Maeda , Fumie Narazaki , Akio Kakefuda , Kentaro Sato , Tatsuhisa Takahashi , Takatoshi Kanayama , Chikashi Saitoh , Jotaro Suzuki , Chisato Kanai
Inventor： Takahiro Ishii , Takashi Sugane , Jun Maeda , Fumie Narazaki , Akio Kakefuda , Kentaro Sato , Tatsuhisa Takahashi , Takatoshi Kanayama , Chikashi Saitoh , Jotaro Suzuki , Chisato Kanai
IPC: A61K31/4545 , C07D401/12 , C07D405/14 , A61K31/506 , A61K31/551 , A61K31/4725 , A61P13/00
CPC classification number: A61K31/44 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/55 , C07D401/12
Abstract: A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.
Abstract translation: 新型吡啶基非芳族含氮杂环-1-羧酸酯化合物及其药学上可接受的盐具有有效的FAAH抑制活性。 此外，本公开的吡啶基非芳族含氮杂环-1-羧酸酯化合物也可用于治疗尿频和尿失禁，膀胱过度活动和/或疼痛。
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公开(公告)号：US20060084807A1
公开(公告)日：2006-04-20
申请号：US10540421
申请日：2003-12-24
Applicant: Shinya Yoshida , Toshihiro Watanabe , Kiyotaka Marumo , Akio Kakefuda
Inventor： Shinya Yoshida , Toshihiro Watanabe , Kiyotaka Marumo , Akio Kakefuda
IPC: C07D401/02
CPC classification number: C07D401/06 , C07D211/60
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US20110071146A1
公开(公告)日：2011-03-24
申请号：US12943435
申请日：2010-11-10
Applicant: Tatsuya Niimi , Akio Kamikawa , Yasushi Amano , Tomohiko Yamaguchi , Kenichi Suzumura , Kentaro Enjo , Takashi Furutani , Akio Kakefuda , Yutaka Kondoh , Masaaki Hirano
Inventor： Tatsuya Niimi , Akio Kamikawa , Yasushi Amano , Tomohiko Yamaguchi , Kenichi Suzumura , Kentaro Enjo , Takashi Furutani , Akio Kakefuda , Yutaka Kondoh , Masaaki Hirano
IPC: A61K31/536 , A61K31/40 , A61K31/415 , A61K31/44 , A61K31/41 , A61K31/4965 , A61K31/505 , A61K31/42 , A61P13/08
CPC classification number: C07D209/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D513/04
Abstract: 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.
Abstract translation: 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。
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