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11. 发明授权

US07956060B2 Pyrimidine derivative compound 失效
标题翻译：嘧啶衍生物化合物
公开(公告)号：US07956060B2
公开(公告)日：2011-06-07
申请号：US10594369
申请日：2005-03-30
申请人： Hitoshi Arai , Tsutomu Matsumura , Syoichi Isami , Hiroshi Ishida , Koji Hagihara , Hiroshi Umehara , Yoshinori Yamashita , Nana Oiwa , Yukimasa Shiotsu , Tomoki Naoe , Hitoshi Kiyoi
发明人： Hitoshi Arai , Tsutomu Matsumura , Syoichi Isami , Hiroshi Ishida , Koji Hagihara , Hiroshi Umehara , Yoshinori Yamashita , Nana Oiwa , Yukimasa Shiotsu , Tomoki Naoe , Hitoshi Kiyoi
IPC分类号： C07D471/04 , C07D471/22 , C07D487/04 , C07D239/70 , C07D471/00 , C07D487/00 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , A61K31/505 , A01N43/56
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention provides an antitumor agent and the like, which comprises as an active ingredient, a pyrimidine derivative represented by Formula (I): [wherein —X—Y—Z— represents —O—CR3═N— (wherein R3 represents a hydrogen atom, a substituted or unsubstituted aromatic heterocyclic group and the like) and the like, R1 represents —NR10R11 (wherein R10 and R11 may be the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl and the like) and the like, R2 represents —NR13R14 (wherein R13 and R14 may be the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl and the like)] or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了包含作为活性成分的式（I）所示的嘧啶衍生物的抗肿瘤剂等：[其中-X-Y-Z-表示-O-CR 3 = N-（其中R 3表示氢原子，取代或未取代的芳族杂环基等）等，R 1表示-NR 10 R 11（其中R 10和R 11可以相同或不同，各自表示氢原子，取代或未取代的低级烷基等）等等，R 2表示-NR 13 R 14（其中R 13和R 14可以相同或不同，各自表示氢原子，取代或未取代的低级烷基等）]或其药学上可接受的盐。

12. 发明授权

US07858333B2 Method for screening candidate compounds for antitumor drug 失效
标题翻译：筛选抗肿瘤药物候选化合物的方法
公开(公告)号：US07858333B2
公开(公告)日：2010-12-28
申请号：US11521372
申请日：2006-09-15
申请人： Hitoshi Kiyoi , Tomoki Naoe , Masayuki Towatari , Toshio Kitamura
发明人： Hitoshi Kiyoi , Tomoki Naoe , Masayuki Towatari , Toshio Kitamura
IPC分类号： C12Q1/50
CPC分类号： G01N33/57426 , G01N33/5011
摘要： Investigation on the frequency of FLT3/ITD found in various blood cancers has revealed that the frequency is high in acute myeloblastic leukemia in particular. Studies on the effects of FLT3/ITD in the blood cell lines revealed that the tyrosine residues in FLT3/ITD is constitutively phosphorylated in these cell lines and that blood cells into which FLT3/ITD is introduced show IL-3 independent proliferation. Moreover, the blood cells into which FLT3/ITD is introduced are found to be capable of forming tumors and inhibit cell differentiation. The inventors have found that it is possible to screen for pharmaceutical compounds against tumors by using inhibition of these FLT3/ITD functions as an index.
摘要翻译：对各种血液中FLT3 / ITD频率的调查显示，特别是急性成髓细胞白血病的频率高。关于FLT3 / ITD在血细胞系中的作用的研究表明，FLT3 / ITD中的酪氨酸残基在这些细胞系中被组成型磷酸化，并且引入了FLT3 / ITD的血细胞显示IL-3不依赖的增殖。此外，发现引入FLT3 / ITD的血细胞能够形成肿瘤并抑制细胞分化。本发明人已经发现，通过使用这些FLT3 / ITD功能的抑制作为指标，可以筛选针对肿瘤的药物化合物。

13. 发明申请

US20090082348A1 INDAZOLE DERIVATIVES 失效
标题翻译：吲哚衍生物
公开(公告)号：US20090082348A1
公开(公告)日：2009-03-26
申请号：US12275614
申请日：2008-11-21
申请人： Yoshihisa Ohta , Fumihiko Kanai , Shinji Nara , Yutaka Kanda , Hiroshi Umehara , Yukimasa Shiotsu , Tomoki Naoe , Hitoshi Kiyoi , Keiko Kawashima , Hiromi Ando , Motoki Miyama
发明人： Yoshihisa Ohta , Fumihiko Kanai , Shinji Nara , Yutaka Kanda , Hiroshi Umehara , Yukimasa Shiotsu , Tomoki Naoe , Hitoshi Kiyoi , Keiko Kawashima , Hiromi Ando , Motoki Miyama
IPC分类号： A61K31/5377 , A61K31/416 , A61K31/496 , A61K31/454 , A61K31/506 , A61K31/4439 , A61P35/00
CPC分类号： C07D231/56
摘要： The present invention provides a compound represented by Formula (I): [wherein R1 represents CONR1aR1b (wherein R1a and R1b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R1a and R1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group) or the like, R2 represents a hydrogen atom, CONR2aR2b (wherein R2a and R2b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R2a and R2b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group), NR2cR2d (wherein R2c and R2d may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkanoyl, substituted or unsubstituted aroyl, substituted or unsubstituted heteroaroyl, substituted or unsubstituted ararkyl, substituted or unsubstituted lower alkylsulfonyl or substituted or unsubstituted lower arylsulfonyl) or the like].
摘要翻译：本发明提供由式（I）表示的化合物：[其中R1表示CONR1aR1b（其中R1a和R1b可以相同或不同，各自表示氢原子，取代或未取代的低级烷基，取代或未取代的芳基，取代或未取代的芳基或取代或未取代的杂环基，或者R1a和R1b与相邻的氮原子一起形成取代或未取代的杂环基）等，R2表示氢原子，CONR2aR2b（其中R2a和R2b可以是各自表示氢原子，取代或未取代的低级烷基，取代或未取代的芳基，取代或未取代的芳基或取代或未取代的杂环基，或者R 2a和R 2b与相邻的氮原子一起形成取代基或未取代的杂环基），NR2cR2d（其中R2c和R2d可以相同或不同取代或未取代的芳酰基，取代或未取代的芳酰基，取代或未取代的低级烷基磺酰基或取代或未取代的低级芳基磺酰基）等。。

14. 发明授权

US07470717B2 Indazole derivatives 失效
标题翻译：吲唑衍生物
公开(公告)号：US07470717B2
公开(公告)日：2008-12-30
申请号：US10548475
申请日：2004-07-30
申请人： Yoshihisa Ohta , Fumihiko Kanai , Shinji Nara , Yutaka Kanda , Hiroshi Umehara , Yukimasa Shiotsu , Tomoki Naoe , Hitoshi Kiyoi , Keiko Kawashima , Hiromi Ando , Motoki Miyama
发明人： Yoshihisa Ohta , Fumihiko Kanai , Shinji Nara , Yutaka Kanda , Hiroshi Umehara , Yukimasa Shiotsu , Tomoki Naoe , Hitoshi Kiyoi , Keiko Kawashima , Hiromi Ando , Motoki Miyama
IPC分类号： A61K31/416 , C07D231/56
CPC分类号： C07D231/56
摘要： The present invention provides a compound represented by Formula (I): [wherein R1 represents CONR1aR1b (wherein R1a and R1b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R1a and R1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group) or the like, R2 represents a hydrogen atom, CONR2aR2b (wherein R2a and R2b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R2a and R2b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group), NR2cR2d (wherein R2c and R2d may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkanoyl, substituted or unsubstituted aroyl, substituted or unsubstituted heteroaroyl, substituted or unsubstituted ararkyl, substituted or unsubstituted lower alkylsulfonyl or substituted or unsubstituted lower arylsulfonyl) or the like].
摘要翻译：本发明提供由式（I）表示的化合物：[其中R1表示CONR1aR1b（其中R1a和R1b可以相同或不同，各自表示氢原子，取代或未取代的低级烷基，取代或未取代的芳基，取代或未取代的芳烷基或取代或未取代的杂环基，或者R1a和R1b与相邻的氮原子一起形成取代或未取代的杂环基）等，R2表示氢原子，CONR2aR2b（其中R2a和R2b可以是各自表示氢原子，取代或未取代的低级烷基，取代或未取代的芳基，取代或未取代的芳烷基或取代或未取代的杂环基，或R 2a和R 2b与相邻的氮原子一起形成取代基或未取代的杂环基），NR2cR2d（其中R2c和R2d可以相同或不同取代或未取代的杂芳酰基，取代或未取代的芳烷基，取代或未取代的低级烷基磺酰基或取代或未取代的低级芳基磺酰基）等，其中R 1代表氢原子，取代或未取代的低级烷基，取代或未取代的低级烷酰基，取代或未取代的芳酰基，。

15. 发明申请

US20070009973A1 Method for screening candidate compounds for antitumor drug 失效
标题翻译：筛选抗肿瘤药物候选化合物的方法
公开(公告)号：US20070009973A1
公开(公告)日：2007-01-11
申请号：US11521372
申请日：2006-09-15
申请人： Hitoshi Kiyoi , Tomoki Naoe , Masayuki Towatari , Toshio Kitamura
发明人： Hitoshi Kiyoi , Tomoki Naoe , Masayuki Towatari , Toshio Kitamura
IPC分类号： G01N33/574
CPC分类号： G01N33/57426 , G01N33/5011
摘要： Investigation on the frequency of FLT3/ITD found in various blood cancers has revealed that the frequency is high in acute myeloblastic leukemia in particular. Studies on the effects of FLT3/ITD in the blood cell lines revealed that the tyrosine residues in FLT3/ITD is constitutively phosphorylated in these cell lines and that blood cells into which FLT3/ITD is introduced show IL-3 independent proliferation. Moreover, the blood cells into which FLT3/ITD is introduced are found to be capable of forming tumors and inhibit cell differentiation. The inventors have found that it is possible to screen for pharmaceutical compounds against tumors by using inhibition of these FLT3/ITD functions as an index.
摘要翻译：对各种血液中FLT3 / ITD频率的调查显示，特别是急性成髓细胞白血病的频率高。关于FLT3 / ITD在血细胞系中的作用的研究表明，FLT3 / ITD中的酪氨酸残基在这些细胞系中被组成型磷酸化，并且引入了FLT3 / ITD的血细胞显示IL-3不依赖的增殖。此外，发现引入FLT3 / ITD的血细胞能够形成肿瘤并抑制细胞分化。本发明人已经发现，通过使用这些FLT3 / ITD功能的抑制作为指标，可以筛选针对肿瘤的药物化合物。

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