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公开(公告)号:US20120184521A1
公开(公告)日:2012-07-19
申请号:US13498159
申请日:2010-09-24
申请人: Eiji Kawaminami , Tatsuhisa Takahashi , Takatoshi Kanayama , Yuta Fukuda , Hiroyuki Kaizawa , Yutaka Kondoh , Ryushi Seo , Kazuyuki Kuramoto , Kazuhiko Take , Kazuyuki Sakamoto
发明人: Eiji Kawaminami , Tatsuhisa Takahashi , Takatoshi Kanayama , Yuta Fukuda , Hiroyuki Kaizawa , Yutaka Kondoh , Ryushi Seo , Kazuyuki Kuramoto , Kazuhiko Take , Kazuyuki Sakamoto
IPC分类号: A61K31/426 , C07D417/12 , A61K31/427 , A61K31/496 , A61P43/00 , A61K31/513 , A61K31/538 , A61K31/454 , A61K31/541 , C07D277/56 , A61K31/4439
CPC分类号: A61K31/426 , A61K31/341 , A61K31/381 , A61K31/401 , A61K31/415 , A61K31/42 , A61K31/427 , A61K31/44 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/4965 , C07D207/34 , C07D213/81 , C07D263/34 , C07D277/56 , C07D307/68 , C07D333/38 , C07D417/12
摘要: A substituted amide compound is useful as an active ingredient of a pharmaceutical composition, in particular a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA). The compound is of a formula: In this formula, A is an optionally substituted aryl, etc.; B is an optionally substituted 5-membered aromatic hetero ring group; X is a single bond or —(CRX1RX2)n—; n is 1, 2, 3, or 4; RX1 and RX2 are hydrogen, etc.; Y1 to Y5 are each CRY or N; each RY is hydrogen, etc.; R1 and R2 are hydrogen, etc.; m is 1, 2, or 3; R3 is hydrogen, etc.; and R4 is an optionally substituted lower alkyl, etc.
摘要翻译: 取代的酰胺化合物可用作药物组合物的活性成分,特别是用于治疗由溶血磷脂酸(LPA)引起的疾病的药物组合物。 该化合物具有下式:在该式中,A是任选取代的芳基等; B是任选取代的5元芳族杂环基团; X是单键或 - (CRX1RX2)n-; n为1,2,3或4; RX1和RX2是氢等; Y1〜Y5分别为CRY或N; 每个RY是氢等; R1和R2是氢等; m为1,2或3; R3是氢等; 并且R 4是任选取代的低级烷基等。
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公开(公告)号:US08669246B2
公开(公告)日:2014-03-11
申请号:US13498159
申请日:2010-09-24
申请人: Eiji Kawaminami , Tatsuhisa Takahashi , Takatoshi Kanayama , Yuta Fukuda , Hiroyuki Kaizawa , Yutaka Kondoh , Ryushi Seo , Kazuyuki Kuramoto , Kazuhiko Take , Kazuyuki Sakamoto
发明人: Eiji Kawaminami , Tatsuhisa Takahashi , Takatoshi Kanayama , Yuta Fukuda , Hiroyuki Kaizawa , Yutaka Kondoh , Ryushi Seo , Kazuyuki Kuramoto , Kazuhiko Take , Kazuyuki Sakamoto
IPC分类号: A61K31/341 , A61K31/381 , A61K31/401 , A61K31/415 , C07D207/34 , C07D213/81 , C07D263/34 , C07D277/56 , C07D307/68 , C07D333/38 , C07D417/12
CPC分类号: A61K31/426 , A61K31/341 , A61K31/381 , A61K31/401 , A61K31/415 , A61K31/42 , A61K31/427 , A61K31/44 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/4965 , C07D207/34 , C07D213/81 , C07D263/34 , C07D277/56 , C07D307/68 , C07D333/38 , C07D417/12
摘要: A substituted amide compound is useful as an active ingredient of a pharmaceutical composition, in particular a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA). The compound is of a formula: In this formula, A is an optionally substituted aryl, etc.; B is an optionally substituted 5-membered aromatic hetero ring group; X is a single bond or —(CRX1RX2)n—; n is 1, 2, 3, or 4; RX1 and RX2 are hydrogen, etc.; Y1 to Y5 are each CRY or N; each RY is hydrogen, etc.; R1 and R2 are hydrogen, etc.; m is 1, 2, or 3; R3 is hydrogen, etc.; and R4 is an optionally substituted lower alkyl, etc.
摘要翻译: 取代的酰胺化合物可用作药物组合物的活性成分,特别是用于治疗由溶血磷脂酸(LPA)引起的疾病的药物组合物。 该化合物具有下式:在该式中,A是任选取代的芳基等; B是任选取代的5元芳族杂环基团; X是单键或 - (CRX1RX2)n-; n为1,2,3或4; RX1和RX2是氢等; Y1〜Y5分别为CRY或N; 每个RY是氢等; R1和R2是氢等; m为1,2或3; R3是氢等; 并且R 4是任选取代的低级烷基等。
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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。
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公开(公告)号:US20120040968A1
公开(公告)日:2012-02-16
申请号:US13266164
申请日:2010-05-06
申请人: Itsuro Shimada , Kazuo Kurosawa , Takahiro Matsuya , Kazuhiko Iikubo , Yutaka Kondoh , Akio Kamikawa , Hiroshi Tomiyama , Yoshinori Iwai
发明人: Itsuro Shimada , Kazuo Kurosawa , Takahiro Matsuya , Kazuhiko Iikubo , Yutaka Kondoh , Akio Kamikawa , Hiroshi Tomiyama , Yoshinori Iwai
IPC分类号: A61K31/497 , C07D405/14 , C07D401/14 , C07D491/113 , C07D403/12 , A61K31/551 , A61K31/538 , C07D409/14 , C07D417/12 , A61K31/55 , A61K31/541 , C07D471/08 , C07D241/28 , C07D401/12 , A61K31/513 , C07D239/48 , A61P35/00 , A61K31/5377
CPC分类号: C07D239/48 , C07D241/26 , C07D241/28 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/08 , C07D491/113
摘要: Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein.As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.
摘要翻译: 提供了可用作抑制EML4-ALK融合蛋白的激酶活性的化合物。 作为对具有针对EML4-ALK融合蛋白的激酶活性的抑制活性的化合物进行了深入和广泛的研究的结果,本发明人发现本发明的二氨基杂环羧酰胺化合物对EML4-ALK融合体的激酶活性具有抑制活性 蛋白。 通过这一发现,完成了本发明。 本发明的化合物可以用作预防和/或治疗癌症的药物组合物,例如肺癌,非小细胞肺癌和小细胞肺癌。
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公开(公告)号:US5541182A
公开(公告)日:1996-07-30
申请号:US391835
申请日:1995-02-16
申请人: Masato Satoh , Yutaka Kondoh , Yoshinori Okamoto , Akito Nishida , Kazuo Honda , Masayuki Saito
发明人: Masato Satoh , Yutaka Kondoh , Yoshinori Okamoto , Akito Nishida , Kazuo Honda , Masayuki Saito
IPC分类号: A61K31/55 , B65D25/52 , B65D83/08 , B65H35/10 , C07D243/24 , C07D243/26 , C07D401/06 , C07D403/04 , C07D403/06 , C07D409/06
CPC分类号: C07D401/06 , B65D83/0847 , B65H35/10 , C07D243/24 , C07D403/04 , C07D409/06 , B65H2701/11231
摘要: This invention relates to novel benzodiazepine derivatives represented by the following general formula (I) or pharmaceutically acceptable salts thereof, ##STR1## (wherein R.sup.1 is an aryl group, or an aromatic heterocyclic radical of 5-membered monocyclic, 6-membered monocyclic or 5- and 6-membered bicyclic structure, which may optionally be substituted; and R.sup.2 is an aryl group which may optionally be substituted), to medicinal compositions comprising the same, and to a process for producing the same. The compounds of formula (I) shown above exhibit antagonism for the CCK-B receptor and the action of depressing the gastric acid secretion caused by the stimulus of pentagastrin, and are therefore useful as a drug for the relief of diseases related to the CCK-B receptor and the gastrin receptor.
摘要翻译: 本发明涉及由以下通式(I)表示的新型苯并二氮杂衍生物或其药学上可接受的盐,其中R 1为芳基或5元单环,6元环的芳族杂环基 单环或5-和6-元双环结构,其可任选被取代;和R 2是可任选被取代的芳基),包含它们的药用组合物及其制备方法。 上述式(I)的化合物对CCK-B受体表现出拮抗作用,并且抑制由五肽胃泌素刺激引起的胃酸分泌的作用,因此可用作缓解与CCK- B受体和胃泌素受体。
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公开(公告)号:US5357816A
公开(公告)日:1994-10-25
申请号:US14248
申请日:1993-02-05
CPC分类号: B60R21/33 , G01P15/036 , Y10T74/11
摘要: An impact sensing apparatus includes a housing having a wall portion which is parallel with the applied direction of an outside shock and a hole which is formed in the wall portion, a weight disposed in the housing and moved by an outside shock which is more than a predetermined value, an output member rotatably disposed in the housing and rotated in response to the movement of the weight and an urging member interposed between the housing and the output member for urging the output member so as to project from the hole. According to this improved impact sensing apparatus, it is possible to lengthen the stroke of the rotational motion of the output member and therefore it is possible to effectively utilize the urging force of the urging member as a kinetic energy of the output member. Thus, it is possible to improve the reliability for igniting the ignition element such as a primer due to a striking operation of the output member.
摘要翻译: 冲击感测装置包括壳体,该壳体具有与外部冲击的施加方向平行的壁部和形成在壁部中的孔,设置在壳体中并由外部冲击移动的重物, 预定值,可旋转地设置在壳体中并且响应于重物的移动而旋转的输出构件和插入壳体和输出构件之间的推动构件,用于推压输出构件以从孔突出。 根据该改进的冲击感测装置,可以延长输出部件的旋转运动的行程,因此能够有效地利用推动部件的作用力作为输出部件的动能。 因此,可以提高由于输出构件的打击操作而引燃诸如底漆的点火元件的可靠性。
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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。
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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。
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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。
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10.
公开(公告)号:US5849062A
公开(公告)日:1998-12-15
申请号:US836409
申请日:1997-05-02
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。
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