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：US20100099658A1

公开(公告)日：2010-04-22

申请号：US12448759

申请日：2008-07-04

申请人： Yutaka Kondoh ,  Kazuhiko Iikubo ,  Sadao Kuromitsu ,  Nobuaki Shindo ,  Takatoshi Soga ,  Takashi Furutani ,  Itsuro Shimada ,  Takahiro Matsuya ,  Kazuo Kurosawa ,  Akio Kamikawa ,  Hiroyuki Mano

发明人： Yutaka Kondoh ,  Kazuhiko Iikubo ,  Sadao Kuromitsu ,  Nobuaki Shindo ,  Takatoshi Soga ,  Takashi Furutani ,  Itsuro Shimada ,  Takahiro Matsuya ,  Kazuo Kurosawa ,  Akio Kamikawa ,  Hiroyuki Mano

IPC分类号： A61K31/397 ,  C07D239/72 ,  A61K31/497 ,  A61K31/517 ,  C07D413/02 ,  A61K31/5377 ,  C07D403/02 ,  A61K31/53 ,  C07D279/12 ,  A61K31/541 ,  A61P35/00

CPC分类号： A61K31/551 ,  A61K31/517 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/541 ,  C07D239/95 ,  C07D251/18 ,  C07D251/48 ,  C07D251/50 ,  C07D251/52 ,  C07D251/70 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/08 ,  C07D491/113 ,  C07D498/10

摘要： The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins.As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention. The compound of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, lung cancer, non-small cell lung cancer, small cell lung cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive lung cancer, or EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive non-small cell lung cancer, etc.

摘要翻译： 本发明提供了可用作抑制EML4-ALK融合蛋白和突变型EGFR蛋白的激酶活性的化合物。 作为对具有对EML4-ALK融合蛋白和突变型EGFR蛋白的激酶活性具有抑制作用的化合物的广泛和深入研究的结果，本发明的发明人已经发现本发明的二（芳基氨基）芳基化合物具有 对EML4-ALK融合蛋白和突变型EGFR蛋白激酶活性的抑制活性。 这一发现导致了本发明的完成。 本发明的化合物可以用作预防和/或治疗癌症，肺癌，非小细胞肺癌，小细胞肺癌，EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸的药物组合物， 阳性癌症，EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸阳性肺癌或EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸阳性非小细胞肺癌等。

公开(公告)号：US20130096100A1

公开(公告)日：2013-04-18

申请号：US13618732

申请日：2012-09-14

申请人： Yutaka KONDOH ,  Kazuhiko Iikubo ,  Sadao Kuromitsu ,  Nobuaki Shindo ,  Takatoshi Soga ,  Takashi Furutani ,  Itsuro Shimada ,  Takahiro Matsuya ,  Kazuo Kurosawa ,  Akio Kamikawa ,  Hiroyuki Mano

发明人： Yutaka KONDOH ,  Kazuhiko Iikubo ,  Sadao Kuromitsu ,  Nobuaki Shindo ,  Takatoshi Soga ,  Takashi Furutani ,  Itsuro Shimada ,  Takahiro Matsuya ,  Kazuo Kurosawa ,  Akio Kamikawa ,  Hiroyuki Mano

IPC分类号： A61K31/551 ,  A61K31/541 ,  A61K31/53 ,  A61K31/517 ,  A61K31/5377

CPC分类号： A61K31/551 ,  A61K31/517 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/541 ,  C07D239/95 ,  C07D251/18 ,  C07D251/48 ,  C07D251/50 ,  C07D251/52 ,  C07D251/70 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/08 ,  C07D491/113 ,  C07D498/10

摘要： The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins.As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention. The compound of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, lung cancer, non-small cell lung cancer, small cell lung cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive lung cancer, or EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive non-small cell lung cancer, etc.

摘要翻译： 本发明提供了可用作抑制EML4-ALK融合蛋白和突变型EGFR蛋白的激酶活性的化合物。 作为对具有对EML4-ALK融合蛋白和突变型EGFR蛋白的激酶活性具有抑制作用的化合物的广泛和深入研究的结果，本发明的发明人已经发现本发明的二（芳基氨基）芳基化合物具有 对EML4-ALK融合蛋白和突变型EGFR蛋白激酶活性的抑制活性。 这一发现导致了本发明的完成。 本发明的化合物可以用作预防和/或治疗癌症，肺癌，非小细胞肺癌，小细胞肺癌，EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸的药物组合物， 阳性癌症，EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸阳性肺癌或EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸阳性非小细胞肺癌等。

公开(公告)号：US08318702B2

公开(公告)日：2012-11-27

申请号：US12448759

申请日：2008-07-04

申请人： Yutaka Kondoh ,  Kazuhiko Iikubo ,  Sadao Kuromitsu ,  Nobuaki Shindo ,  Takatoshi Soga ,  Takashi Furutani ,  Itsuro Shimada ,  Takahiro Matsuya ,  Kazuo Kurosawa ,  Akio Kamikawa ,  Hiroyuki Mano

发明人： Yutaka Kondoh ,  Kazuhiko Iikubo ,  Sadao Kuromitsu ,  Nobuaki Shindo ,  Takatoshi Soga ,  Takashi Furutani ,  Itsuro Shimada ,  Takahiro Matsuya ,  Kazuo Kurosawa ,  Akio Kamikawa ,  Hiroyuki Mano

IPC分类号： A01N57/00 ,  A01N43/00 ,  A01N43/66 ,  A61K31/675 ,  A61K31/00 ,  A61K31/53 ,  C07D251/00 ,  C07D253/00 ,  C07D251/40 ,  C07D251/18 ,  C07D251/48

CPC分类号： A61K31/551 ,  A61K31/517 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/541 ,  C07D239/95 ,  C07D251/18 ,  C07D251/48 ,  C07D251/50 ,  C07D251/52 ,  C07D251/70 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/08 ,  C07D491/113 ,  C07D498/10

摘要： The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins.As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention. The compound of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, lung cancer, non-small cell lung cancer, small cell lung cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive lung cancer, or EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive non-small cell lung cancer, etc.

摘要翻译： 本发明提供了可用作抑制EML4-ALK融合蛋白和突变型EGFR蛋白的激酶活性的化合物。 作为对具有对EML4-ALK融合蛋白和突变型EGFR蛋白的激酶活性具有抑制作用的化合物的广泛和深入研究的结果，本发明的发明人已经发现本发明的二（芳基氨基）芳基化合物具有 对EML4-ALK融合蛋白和突变型EGFR蛋白激酶活性的抑制活性。 这一发现导致了本发明的完成。 本发明的化合物可以用作预防和/或治疗癌症，肺癌，非小细胞肺癌，小细胞肺癌，EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸的药物组合物， 阳性癌症，EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸阳性肺癌或EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸阳性非小细胞肺癌等。

公开(公告)号：US20110282066A1

公开(公告)日：2011-11-17

申请号：US13146434

申请日：2010-01-26

申请人： Takashi Furutani ,  Kentaro Enjo ,  Aya Kikuchi ,  Sadao Kuromitsu ,  Yukitaka Ideyama ,  Tomoyuki Suzuki ,  Ryoko Kurihara

发明人： Takashi Furutani ,  Kentaro Enjo ,  Aya Kikuchi ,  Sadao Kuromitsu ,  Yukitaka Ideyama ,  Tomoyuki Suzuki ,  Ryoko Kurihara

IPC分类号： C07D211/32 ,  C07D209/04 ,  G01N33/53 ,  C07D235/12 ,  C07D401/04 ,  G01N33/535 ,  C07D235/06

CPC分类号： G01N33/5017 ,  G01N33/57434 ,  G01N2333/904 ,  Y10T436/200833

摘要： [Object] A screening method for a compound which is useful as an agent for treating 17βHSD type 5-related diseases and/or an agent for treating 17βHSD type 5-related cancer such as prostate cancer is provided.[Means for Solution] The present invention has been completed by establishing a screening method for a compound which is useful for treating 17βHSD type 5-related diseases, by manifesting a tumor by transplanting tumor cells to, for example, an immunodeficient mouse, topically administering a steroid which is a biosynthetic substance for a hormone into the tumor, and measuring the level of a hormone produced in the tumor.[Selected Figure] None

摘要翻译： [目的]提供可用作治疗17型和HSD5型相关疾病的药剂和/或用于治疗诸如前列腺癌之类的HSD5型相关癌症的药物的化合物的筛选方法。 [解决方案]本发明是通过建立一种可用于治疗17bb HSD5型相关疾病的化合物的筛选方法，通过将肿瘤细胞移植至例如免疫缺陷小鼠， 局部施用作为激素进入肿瘤的生物合成物质的类固醇，并测量肿瘤中产生的激素的水平。 [已选图]无