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：US07989634B2

公开(公告)日：2011-08-02

申请号：US10579042

申请日：2004-11-12

申请人： Koo Lee ,  Heui-Sul Park ,  In-Ae Ahn ,  Hyun-Ju Yoo ,  Jong-Yup Kim ,  Deog-Young Choi ,  Hyeon-Joo Yim ,  Kyung-Ha Chung ,  Dong-Sup Shim ,  Sang-Kyun Lee ,  Yutaka Kondoh ,  Ryoji Hirabayashi ,  Shugo Honda ,  Hidetaka Kaku ,  Jun-ichi Shishikura ,  Hiroyuki Ito ,  Takeshi Kurama

发明人： Koo Lee ,  Heui-Sul Park ,  In-Ae Ahn ,  Hyun-Ju Yoo ,  Jong-Yup Kim ,  Deog-Young Choi ,  Hyeon-Joo Yim ,  Kyung-Ha Chung ,  Dong-Sup Shim ,  Sang-Kyun Lee ,  Yutaka Kondoh ,  Ryoji Hirabayashi ,  Shugo Honda ,  Hidetaka Kaku ,  Jun-ichi Shishikura ,  Hiroyuki Ito ,  Takeshi Kurama

IPC分类号： C07D213/46 ,  C07D211/70 ,  C07D401/00

CPC分类号： C04B35/632 ,  C07D205/04 ,  C07D207/14 ,  C07D211/58 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

摘要： The present invention relates a compound of formula 1, and pharmaceutically acceptable salt, hydrate, solvate, or isomer thereof effective as agonist of melanocortin receptor, and an agonistic composition of melanocortin receptor comprising the same as active ingredient.

摘要翻译： 本发明涉及有效作为黑皮质素受体激动剂的式1化合物及其药学上可接受的盐，水合物，溶剂化物或异构体，以及包含与活性成分相同的黑皮质素受体激动剂组合物。

公开(公告)号：US07606672B2

公开(公告)日：2009-10-20

申请号：US10396687

申请日：2003-03-26

申请人： Yutaka Kondoh ,  Masahiko Kamiyama ,  Hiroshi Nishikawa ,  Hiroshi Sakamoto ,  Teruji Tarumi ,  Akira Yunoki ,  Yoshimi Maekawa ,  Katuya Kondoh ,  Mikio Izumi

发明人： Yutaka Kondoh ,  Masahiko Kamiyama ,  Hiroshi Nishikawa ,  Hiroshi Sakamoto ,  Teruji Tarumi ,  Akira Yunoki ,  Yoshimi Maekawa ,  Katuya Kondoh ,  Mikio Izumi

IPC分类号： G01B5/28

CPC分类号： G05B9/02

摘要： A plant protection instrumentation equipment, comprises, a sensor that detects a process signal indicating a quantity of a state of a plant, a plurality of A/D converters, each of the A/D converters converts the process signal into a digital signal and outputs a value corresponding to the digital signal, a plurality of instrumentation circuits, each of the instrumentation circuits receives the value corresponding to the process signal and performs a logical operation using the value, and a judgment circuit that judges the state of the plant based on outputs of the plurality of instrumentation circuits and outputs an operation signal based on the process signal, wherein each of the instrumentation circuits comprises a logical integrated circuit including a set value comparator that compares the value corresponding to the process signal with a predetermined set value, and outputs a signal when the value corresponding to the process signal exceeds the set value.

摘要翻译： 一种植物保护仪表设备，包括：检测表示植物状态量的处理信号的传感器，多个A / D转换器，每个A / D转换器将处理信号转换为数字信号并输出 与数字信号相对应的值，多个仪表电路，每个仪表电路接收与处理信号相对应的值，并使用该值执行逻辑运算，以及判断电路，其基于输出判断工厂的状态 并输出基于过程信号的操作信号，其中每个仪表电路包括逻辑集成电路，其包括将对应于处理信号的值与预定设定值进行比较的设定值比较器，并输出 当与处理信号相对应的值超过设定值时的信号。

公开(公告)号：US5849062A

公开(公告)日：1998-12-15

申请号：US836409

申请日：1997-05-02

申请人： Mitsuhiko Fukabori ,  Yuzaburo Nakazato ,  Osamu Fujimoto ,  Yutaka Kondoh ,  Masahiro Miyaji

发明人： Mitsuhiko Fukabori ,  Yuzaburo Nakazato ,  Osamu Fujimoto ,  Yutaka Kondoh ,  Masahiro Miyaji

IPC分类号： B09B5/00 ,  B60R21/26 ,  B60R21/264 ,  C22B1/00 ,  C22B7/00 ,  C22B9/20

CPC分类号： C22B7/001 ,  B09B5/00 ,  B60R21/26 ,  C22B1/005 ,  C22B7/003 ,  C22B7/005 ,  F23G2900/7001 ,  Y02P10/214

摘要： To provide a method for taking out gas generators readily from waste vehicles and then recovering metallic materials of gas generators taken out efficiently. The method is comprised by a) crushing waste vehicles in which air bag apparatuses are installed by a crushing means so that the crushed pieces have approximately the same size as that of the gas generators themselves and the gas generators themselves can be separated from the air bag apparatuses as single bodies without being substantially crushed; b) taking the gas generators out of the crushed pieces of the waste vehicles; c) charging the gas generators thus taken out into a melting furnace; and d) recovering the metallic materials of the gas generator from the melting furnace.

摘要翻译： PCT No.PCT / JP95 / 02251 Sec。 371日期：1997年5月2日 102（e）日期1997年5月2日PCT提交1995年11月6日PCT公布。 WO96 / 14173 PCT出版物 日期1996年5月17日提供从废弃车辆中轻松取出气体发生器的方法，然后回收有效取出的气体发生器的金属材料。 该方法包括：a）通过破碎装置破碎安装气囊装置的废弃车辆，使得碎片具有与气体发生器本身大致相同的尺寸，并且气体发生器本身可与气囊分离 设备作为单体而不被基本上压碎; b）将废气发生器从废弃车辆的碎片中取出; c）将如此取出的气体发生器装入熔炉; 和d）从熔化炉中回收气体发生器的金属材料。

公开(公告)号：US5193407A

公开(公告)日：1993-03-16

申请号：US802530

申请日：1991-12-05

申请人： Kazunori Sakamoto ,  Masanobu Ishikawa ,  Yutaka Kondoh

发明人： Kazunori Sakamoto ,  Masanobu Ishikawa ,  Yutaka Kondoh

IPC分类号： B60R21/16 ,  B60R21/33

CPC分类号： B60R21/33 ,  Y10T74/11

摘要： A hole 13 though which a firing pin 6a of a firing lever 6 is projected outside a housing 1 is formed in a wall 1c of the housing which is in parallel with a direction of an external shock applied to the housing 1. This structure ensures the rotational angle of the firing lever 6 and a biasing force of a spring 9 which urges the firing lever 6 can be used effectively as kinetic energy thereof.

摘要翻译： 在外壳1的壁1c上形成有与外壳1的外部冲击方向平行的孔13，通过该孔13将击发杆6的击发销6a突出到外壳1的外侧。 击发杆6的旋转角度和推动击发杆6的弹簧9的作用力能够被有效地用作其动能。

公开(公告)号：US20130338358A1

公开(公告)日：2013-12-19

申请号：US13981118

申请日：2012-01-27

申请人： Kazuyoshi Obitsu ,  Takahiro Akiba ,  Koji Kobayashi ,  Shun Hirasawa ,  Yutaka Kondoh ,  Kazuhiro Takeguchi ,  Vuji Takahama ,  Ryoki Orii

发明人： Kazuyoshi Obitsu ,  Takahiro Akiba ,  Koji Kobayashi ,  Shun Hirasawa ,  Yutaka Kondoh ,  Kazuhiro Takeguchi ,  Vuji Takahama ,  Ryoki Orii

IPC分类号： C07D401/12 ,  C07D211/44

CPC分类号： C07D401/12 ,  C07D211/44

摘要： Provided is a method for producing a di(arylamino)aryl compound that has superior inhibitory activity against the kinase activities of EML4-ALK fusion protein and mutant EGFR protein and is useful as an active ingredient in pharmaceutical compositions for cancer treatment. The production method includes no purification step using silica gel column chromatography or no step possibly producing a mutagenic mesylate ester as a by-product, greatly improves overall yield, and is high yield and low cost and suitable for the industrial production of pharmaceutical products. Also provided is a synthetic intermediate that is useful in the production method.

摘要翻译： 提供了对于EML4-ALK融合蛋白和突变型EGFR蛋白的激酶活性具有优异抑制活性的二（芳基氨基）芳基化合物的制造方法，可用作癌症治疗用药物组合物中的有效成分。 制造方法不包括使用硅胶柱色谱法的纯化步骤，或者没有可能产生作为副产物的诱变甲磺酸酯的步骤，大大提高了总产率，并且产率高，成本低，适合于药品的工业化生产。 还提供了在生产方法中有用的合成中间体。

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：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：US20070129346A1

公开(公告)日：2007-06-07

申请号：US10579042

申请日：2004-11-12

申请人： Koo Lee ,  Heui-Sul Park ,  In-Ae Ahn ,  Hyun-Ju Yoo ,  Jong-Yup Kim ,  Deog-Young Choi ,  Hyeon-Joo Yim ,  Kyung-Ha Chung ,  Dong-Sup Shim ,  Sang-Kyun Lee ,  Yutaka Kondoh ,  Ryoji Hirabayashi ,  Shugo Honda ,  Hidetaka Kaku ,  Jun-ichi Shishikura ,  Hiroyuki Ito ,  Takeshi Kurama

发明人： Koo Lee ,  Heui-Sul Park ,  In-Ae Ahn ,  Hyun-Ju Yoo ,  Jong-Yup Kim ,  Deog-Young Choi ,  Hyeon-Joo Yim ,  Kyung-Ha Chung ,  Dong-Sup Shim ,  Sang-Kyun Lee ,  Yutaka Kondoh ,  Ryoji Hirabayashi ,  Shugo Honda ,  Hidetaka Kaku ,  Jun-ichi Shishikura ,  Hiroyuki Ito ,  Takeshi Kurama

IPC分类号： A61K31/397 ,  A61K31/401 ,  A61K31/445 ,  C07D211/06

CPC分类号： C04B35/632 ,  C07D205/04 ,  C07D207/14 ,  C07D211/58 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

摘要： The present invention relates a compound of formula 1, and pharmaceutically acceptable salt, hydrate, solvate, or isomer thereof effective as agonist of melanocortin receptor, and an agonistic composition of melanocortin receptor comprising the same as active ingredient.

摘要翻译： 本发明涉及有效作为黑皮质素受体激动剂的式1化合物及其药学上可接受的盐，水合物，溶剂化物或异构体，以及包含与活性成分相同的黑皮质素受体激动剂组合物。