公开(公告)号：US07449456B2

公开(公告)日：2008-11-11

申请号：US10518043

申请日：2003-06-26

申请人： Shinya Nagashima ,  Hiroshi Nagata ,  Masahiro Iwata ,  Masaki Yokota ,  Hiroyuki Moritomo ,  Eiichi Nakai ,  Sadao Kuromitsu ,  Keiko Ohga ,  Makoto Takeuchi

发明人： Shinya Nagashima ,  Hiroshi Nagata ,  Masahiro Iwata ,  Masaki Yokota ,  Hiroyuki Moritomo ,  Eiichi Nakai ,  Sadao Kuromitsu ,  Keiko Ohga ,  Makoto Takeuchi

IPC分类号： C07D239/48 ,  A61K31/506

CPC分类号： C07D403/12 ,  C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/04 ,  C07D453/02 ,  C07D471/10 ,  C07D487/08

摘要： A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided.A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.

摘要翻译： 提供了可用于预防或治疗其中涉及STAT6的呼吸系统疾病的化合物，特别是哮喘，慢性阻塞性肺病等。 具有可以被特定取代基取代的芳基氨基或芳基乙氨基的嘧啶衍生物或其盐在2-位被苄基取代的氨基或4-位上的氨基甲酰基和氨基甲酰基， 可以在5位被提供。

公开(公告)号：US20050272753A1

公开(公告)日：2005-12-08

申请号：US10518043

申请日：2003-06-26

申请人： Shinya Nagashima ,  Hiroshi Nagata ,  Masahiro Iwata ,  Masaki Yokota ,  Hiroyuki Moritomo ,  Eiichi Nakai ,  Sadao Kuromitsu ,  Keiko Ohga ,  Makoto Takeuchi

发明人： Shinya Nagashima ,  Hiroshi Nagata ,  Masahiro Iwata ,  Masaki Yokota ,  Hiroyuki Moritomo ,  Eiichi Nakai ,  Sadao Kuromitsu ,  Keiko Ohga ,  Makoto Takeuchi

IPC分类号： A61P11/00 ,  A61P11/06 ,  A61P43/00 ,  C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/04 ,  C07D453/02 ,  C07D471/08 ,  C07D471/10 ,  C07D487/08 ,  A61K31/506 ,  A61K31/505 ,  C07D43/02

CPC分类号： C07D403/12 ,  C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/04 ,  C07D453/02 ,  C07D471/10 ,  C07D487/08

摘要： A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.

摘要翻译： 提供了可用于预防或治疗其中涉及STAT6的呼吸系统疾病的化合物，特别是哮喘，慢性阻塞性肺病等。 具有可以被特定取代基取代的芳基氨基或芳基乙氨基的嘧啶衍生物或其盐在2-位被苄基取代的氨基或4-位上的氨基甲酰基和氨基甲酰基， 可以在5位被提供。

公开(公告)号：US20110294749A1

公开(公告)日：2011-12-01

申请号：US13171411

申请日：2011-06-28

申请人： Shinya Nagashima ,  Hiroshi Nagata ,  Masahiro Iwata ,  Masaki Yokota ,  Hiroyuki Moritomo ,  Eiichi Nakai ,  Sadao Kuromitsu ,  Keiko Ohga ,  Makoto Takeuchi

发明人： Shinya Nagashima ,  Hiroshi Nagata ,  Masahiro Iwata ,  Masaki Yokota ,  Hiroyuki Moritomo ,  Eiichi Nakai ,  Sadao Kuromitsu ,  Keiko Ohga ,  Makoto Takeuchi

IPC分类号： A61K31/505 ,  C07D413/12 ,  A61K31/5377 ,  C07D413/14 ,  C07D417/12 ,  A61K31/541 ,  C07H15/26 ,  A61K31/7064 ,  C07D403/12 ,  A61K31/551 ,  A61K31/553 ,  A61P11/06 ,  A61P11/00 ,  A61K31/506 ,  C07D239/48

CPC分类号： C07D403/12 ,  C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/04 ,  C07D453/02 ,  C07D471/10 ,  C07D487/08

摘要： A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided.A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.

摘要翻译： 提供了可用于预防或治疗其中涉及STAT6的呼吸系统疾病的化合物，特别是哮喘，慢性阻塞性肺病等。 具有可以被特定取代基取代的芳基氨基或芳基乙氨基的嘧啶衍生物或其盐在2-位被苄基取代的4-氨基甲酰基和氨基甲酰基上， 可以在5位被提供。

公开(公告)号：US08012959B2

公开(公告)日：2011-09-06

申请号：US12235189

申请日：2008-09-22

申请人： Shinya Nagashima ,  Hiroshi Nagata ,  Masashiro Iwata ,  Masaki Yokota ,  Hiroyuki Moritomo ,  Eiichi Nakai ,  Sadao Kuromitsu ,  Keiko Ohga ,  Makoto Takeuchi

发明人： Shinya Nagashima ,  Hiroshi Nagata ,  Masashiro Iwata ,  Masaki Yokota ,  Hiroyuki Moritomo ,  Eiichi Nakai ,  Sadao Kuromitsu ,  Keiko Ohga ,  Makoto Takeuchi

IPC分类号： C07D239/48 ,  A61K31/506

CPC分类号： C07D403/12 ,  C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/04 ,  C07D453/02 ,  C07D471/10 ,  C07D487/08

摘要： A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided.A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.

摘要翻译： 提供了可用于预防或治疗其中涉及STAT6的呼吸系统疾病的化合物，特别是哮喘，慢性阻塞性肺病等。 具有可以被特定取代基取代的芳基氨基或芳基乙氨基的嘧啶衍生物或其盐在2-位被苄基取代的氨基或4-位上的氨基甲酰基和氨基甲酰基， 可以在5位被提供。

公开(公告)号：US20090281072A1

公开(公告)日：2009-11-12

申请号：US12235189

申请日：2008-09-22

申请人： Shinya Nagashima ,  Hiroshi Nagata ,  Masashiro Iwata ,  Masaki Yokota ,  Hiroyuki Moritomo ,  Eiichi Nakai ,  Sadao Kuromitsu ,  Keiko Ohga ,  Makoto Takeuchi

发明人： Shinya Nagashima ,  Hiroshi Nagata ,  Masashiro Iwata ,  Masaki Yokota ,  Hiroyuki Moritomo ,  Eiichi Nakai ,  Sadao Kuromitsu ,  Keiko Ohga ,  Makoto Takeuchi

IPC分类号： A61K31/5377 ,  A61K31/551 ,  A61K31/397 ,  A61P11/06

CPC分类号： C07D403/12 ,  C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/04 ,  C07D453/02 ,  C07D471/10 ,  C07D487/08

摘要： A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided.A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.

摘要翻译： 提供了可用于预防或治疗其中涉及STAT6的呼吸系统疾病的化合物，特别是哮喘，慢性阻塞性肺病等。 具有可以被特定取代基取代的芳基氨基或芳基乙氨基的嘧啶衍生物或其盐在2-位被苄基取代的氨基或4-位上的氨基甲酰基和氨基甲酰基， 可以在5位被提供。

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

公开(公告)号：US07728120B2

公开(公告)日：2010-06-01

申请号：US11845498

申请日：2007-08-27

申请人： Hiroyuki Mano ,  Sadao Kuromitsu ,  Nobuaki Shindo ,  Takatoshi Soga ,  Takashi Furutani

发明人： Hiroyuki Mano ,  Sadao Kuromitsu ,  Nobuaki Shindo ,  Takatoshi Soga ,  Takashi Furutani

IPC分类号： C07H21/04

CPC分类号： C12N15/1137 ,  A61K31/506 ,  C07K14/47 ,  C07K2319/00 ,  C12N9/1205 ,  C12N2310/14 ,  C12Q1/485 ,  C12Q1/6886

摘要： The present inventors found that a fusion gene present in some cancer patients is an oncogene. The present invention relates to a polypeptide as a novel fusion protein, a polynucleotide encoding the polypeptide, a vector comprising the polynucleotide, a transformed cell comprising the vector, a method for detecting the fusion protein or polynucleotide, a method for screening a therapeutic agent for cancer, and a method for treating cancer that is shown to be positive for the fusion gene. Further, the present invention relates kit, primer set, and probe useful in the detection of cancer that is shown to be positive for the fusion gene.

摘要翻译： 本发明人发现存在于某些癌症患者中的融合基因是癌基因。 本发明涉及作为新型融合蛋白的多肽，编码多肽的多核苷酸，包含多核苷酸的载体，包含载体的转化细胞，检测融合蛋白或多核苷酸的方法，用于筛选治疗剂的方法 癌症和治疗癌症的方法，所述方法显示为融合基因呈阳性。 此外，本发明涉及可用于检测癌症的试剂盒，引物组和探针，其对于融合基因显示为阳性。

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：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：US20080213800A1

公开(公告)日：2008-09-04

申请号：US11596867

申请日：2005-05-19

申请人： Tetsuo Yamada ,  Haruhisa Mita ,  Sadao Kuromitsu ,  Hiroyuki Yokota ,  Shuji Morita ,  Masashi Hiramoto ,  Masatoshi Yuri

发明人： Tetsuo Yamada ,  Haruhisa Mita ,  Sadao Kuromitsu ,  Hiroyuki Yokota ,  Shuji Morita ,  Masashi Hiramoto ,  Masatoshi Yuri

IPC分类号： G01N33/573 ,  C12Q1/37 ,  C12Q1/28

CPC分类号： G01N33/573 ,  C12Q1/28 ,  C12Q1/37 ,  G01N2333/908 ,  G01N2333/966 ,  G01N2800/34

摘要： It has been found that the urine from an IC patient shows a high value in amount and the existence of activity of an azurophilic granular substance, thereby to establish a method for examining IC. The present invention relates to a method for examining interstitial cystitis using the kinetics of an azurophilic granular substance in urine as a marker. Also, the present invention relates to a kit for examining interstitial cystitis for use in the examination method, a use of an azurophilic granular substance as a test marker for examining interstitial cystitis or evaluating pharmacological effects of a drug, and a method for examining therapeutic effects on a patient with interstitial cystitis using an azurophilic granular substance as a marker.

摘要翻译： 已经发现，来自IC患者的尿液显示出高的值和存在的氮氧自由基颗粒物质的活性，从而建立了用于检查IC的方法。 本发明涉及使用尿液中的氮氧自由基粒状物质作为标记物的动力学来检查间质性膀胱炎的方法。 此外，本发明涉及一种用于检查用于检查方法的间质性膀胱炎的试剂盒，使用氮氧自由基粒状物质作为检查间质性膀胱炎或评价药物的药理作用的检查标记物，以及用于检查治疗效果的方法 对患有间质性膀胱炎的患者使用氮氧自由基粒状物质作为标记物。