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：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：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：US20130197009A1

公开(公告)日：2013-08-01

申请号：US13877358

申请日：2011-10-21

申请人： Yukitaka Ideyama ,  Sadao Kuromitsu ,  Takashi Furutani ,  Masayoshi Takeda ,  Satoshi Konagai ,  Tomohiro Yamada ,  Nobuaki Taniguchi ,  Yutaka Kondoh ,  Masaaki Hirano ,  Kazushi Watanabe ,  Takashi Sugane ,  Akio Kakefuda

发明人： Yukitaka Ideyama ,  Sadao Kuromitsu ,  Takashi Furutani ,  Masayoshi Takeda ,  Satoshi Konagai ,  Tomohiro Yamada ,  Nobuaki Taniguchi ,  Yutaka Kondoh ,  Masaaki Hirano ,  Kazushi Watanabe ,  Takashi Sugane ,  Akio Kakefuda

IPC分类号： C07D401/02 ,  C07D401/14 ,  C07D403/02

CPC分类号： C07D401/02 ,  A61K31/496 ,  A61K31/506 ,  C07D401/12 ,  C07D401/14 ,  C07D403/02 ,  C07D403/12

摘要： [Problem] An object of the present invention is to provide a novel anticancer drug which is useful for treating prostate cancer accompanying androgen receptor mutation[Means for Solution] The present inventors conducted thorough research on mutant androgen-related diseases for which the traditional anti-androgen drugs become ineffective. As a result, they found that the compound, which is an active ingredient of the pharmaceutical composition of the present invention, exhibits an inhibitory action against transcriptional activation in a human mutant androgen receptor (AR), and has an excellent antitumor action in a human prostate cancer-bearing mouse, thereby completing the present invention. Accordingly, the compound, which is an active ingredient of the pharmaceutical composition of the present invention, is useful for a series of androgen receptor-related diseases including prostate cancer.

摘要翻译： 本发明的目的在于提供一种可用于治疗伴随雄激素受体突变的前列腺癌的新型抗癌药物。本发明人进行了关于雄激素相关疾病的全面研究， 雄激素药物变得无效。 结果发现，作为本发明的药物组合物的活性成分的化合物在人突变型雄激素受体（AR）中表现出对转录活化的抑制作用，并且在人体中具有优异的抗肿瘤作用 前列腺癌的小鼠，从而完成本发明。 因此，作为本发明的药物组合物的活性成分的化合物可用于一系列与前列腺癌有关的雄激素受体相关疾病。

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：US07919494B2

公开(公告)日：2011-04-05

申请号：US12543690

申请日：2009-08-19

申请人： Takahiro Ishii ,  Takashi Sugane ,  Jun Maeda ,  Fumie Narazaki ,  Akio Kakefuda ,  Kentaro Sato ,  Tatsuhisa Takahashi ,  Takatoshi Kanayama ,  Chikashi Saitoh ,  Jotaro Suzuki ,  Chisato Kanai

发明人： Takahiro Ishii ,  Takashi Sugane ,  Jun Maeda ,  Fumie Narazaki ,  Akio Kakefuda ,  Kentaro Sato ,  Tatsuhisa Takahashi ,  Takatoshi Kanayama ,  Chikashi Saitoh ,  Jotaro Suzuki ,  Chisato Kanai

IPC分类号： A61K31/496 ,  A61K31/4545 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

CPC分类号： A61K31/44 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/55 ,  C07D401/12

摘要： 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.

摘要翻译： 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。

公开(公告)号：US20100009971A1

公开(公告)日：2010-01-14

申请号：US12543659

申请日：2009-08-19

申请人： Takahiro Ishii ,  Takashi Sugane ,  Jun Maeda ,  Fumie Narazaki ,  Akio Kakefuda ,  Kentaro Sato ,  Tatsuhisa Takahashi ,  Takatoshi Kanayama ,  Chikashi Saitoh ,  Jotaro Suzuki ,  Chisato Kanai

发明人： Takahiro Ishii ,  Takashi Sugane ,  Jun Maeda ,  Fumie Narazaki ,  Akio Kakefuda ,  Kentaro Sato ,  Tatsuhisa Takahashi ,  Takatoshi Kanayama ,  Chikashi Saitoh ,  Jotaro Suzuki ,  Chisato Kanai

IPC分类号： A61K31/4545 ,  A61K31/551 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/4709 ,  A61K31/444 ,  C07D413/12 ,  C07D401/12 ,  A61P25/00 ,  C07D405/14 ,  A61P13/00

CPC分类号： A61K31/44 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/55 ,  C07D401/12

摘要： 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.

摘要翻译： 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。

公开(公告)号：US07807664B2

公开(公告)日：2010-10-05

申请号：US11598732

申请日：2006-11-14

申请人： Hiroyuki Koshio ,  Issei Tsukamoto ,  Akio Kakefuda ,  Seijiro Akamatsu ,  Chikashi Saitoh

发明人： Hiroyuki Koshio ,  Issei Tsukamoto ,  Akio Kakefuda ,  Seijiro Akamatsu ,  Chikashi Saitoh

IPC分类号： A61P7/12 ,  A61K31/55 ,  C07D223/16

CPC分类号： C07D401/06 ,  C07D223/16

摘要： 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.

摘要翻译： 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 。