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1. 发明申请

US20120029004A1 NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION 有权
标题翻译：具有选择性抑制作用的新型氨基吡啶衍生物
公开(公告)号：US20120029004A1
公开(公告)日：2012-02-02
申请号：US13258748
申请日：2010-03-12
申请人： Hayley Binch , Masaya Hashimoto , Toshiharu Iwama , Nobuhiko Kawanishi , Michael Mortimore , Mitsuru Ohkubo , Tomoko Sunami
发明人： Hayley Binch , Masaya Hashimoto , Toshiharu Iwama , Nobuhiko Kawanishi , Michael Mortimore , Mitsuru Ohkubo , Tomoko Sunami
IPC分类号： A61K31/506 , A61P35/00 , C07D403/14
CPC分类号： C07D403/14
摘要： The present invention relates to a compound of Formula (I): wherein: R1 is H or C1-2 alkyl; R2 is H or C1-3 alkyl; R3 and R4 are each independently H or C1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from R10; R5 is H, hydroxy, C1-2 alkyl, or OCH3; and R10 is F or Cl, or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：本发明涉及式（I）的化合物：其中：R 1是H或C 1-2烷基; R2是H或C1-3烷基; R 3和R 4各自独立地为H或C 1-2烷基，其中烷基可以被一至三个相同或不同的选自R 10的取代基取代; R5是H，羟基，C1-2烷基或OCH3; R 10为F或Cl，或其药学上可接受的盐或酯。

2. 发明授权

US08492397B2 Aminopyridine derivatives having Aurora A selective inhibitory action 有权
标题翻译：具有极光A的氨基吡啶衍生物选择性抑制作用
公开(公告)号：US08492397B2
公开(公告)日：2013-07-23
申请号：US13258748
申请日：2010-03-12
申请人： Hayley Binch , Masaya Hashimoto , Toshiharu Iwama , Nobuhiko Kawanishi , Michael Mortimore , Mitsuru Ohkubo , Tomoko Sunami
发明人： Hayley Binch , Masaya Hashimoto , Toshiharu Iwama , Nobuhiko Kawanishi , Michael Mortimore , Mitsuru Ohkubo , Tomoko Sunami
IPC分类号： C07D403/14 , A61K31/535
CPC分类号： C07D403/14
摘要： The present invention relates to a compound of Formula (I): wherein R1 is H or C1-2 alkyl; R2 is H or C1-3 alkyl; R3 and R4 are each independently H or C1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from R10; R5 is H, hydroxy, C1-2 alkyl, or OCH3; and R10 is F or Cl, or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：本发明涉及式（I）的化合物：其中R 1是H或C 1-2烷基; R2是H或C1-3烷基; R 3和R 4各自独立地为H或C 1-2烷基，其中烷基可以被一至三个相同或不同的选自R 10的取代基取代; R5是H，羟基，C1-2烷基或OCH3; R 10为F或Cl，或其药学上可接受的盐或酯。

3. 发明申请

US20120015969A1 NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION 有权
标题翻译：具有选择性抑制作用的新型氨基吡啶衍生物
公开(公告)号：US20120015969A1
公开(公告)日：2012-01-19
申请号：US13259620
申请日：2010-03-15
申请人： Hayley Binch , Masaya Hashimoto , Michael Mortimore , Mitsuru Ohkubo , Tomoko Sunami
发明人： Hayley Binch , Masaya Hashimoto , Michael Mortimore , Mitsuru Ohkubo , Tomoko Sunami
IPC分类号： A61K31/506 , C07D401/14 , A61P35/00 , C07D417/14
CPC分类号： A61K31/535 , C07D401/14 , C07D417/14
摘要： The present invention relates to a compound of Formula (I): wherein: R1 is H, —NHCOOR1a, C5-6 cycloalkyl, or phenyl; where the cycloalkyl and phenyl each independently may be substituted with one to three of the same or different substituents selected from R10; R1a is C1-3 alkyl which may be substituted with one to three of the same or different substituents selected from F and Cl; R2 is H, —COOH, —CH2 COOH, —COOR2a, or —CH2COOR2a; R2a is C1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from halogen atoms; R3 is H, C1-6 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from R11; R10 is F, Cl, CF3, or C1-2 alkyl; R11 is halogen atom, hydroxy, or cyano; W is selected from: W2a is H, halogen atom, cyano, C1-2 alkyl, or C3-5 cycloalkyl, or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：本发明涉及式（I）的化合物：其中：R1是H，-NHCOOR1a，C5-6环烷基或苯基; 其中环烷基和苯基各自独立地可以被一至三个相同或不同的选自R 10的取代基取代; R 1a是可以被一至三个相同或不同的选自F和Cl的取代基取代的C 1-3烷基; R2是H，-COOH，-CH2COOH，-COOR2a或-CH2COOR2a; R2a是C1-2烷基，其中烷基可以被一至三个相同或不同的选自卤素原子的取代基取代; R3是H，C1-6烷基，其中烷基可以被一至三个相同或不同的选自R11的取代基取代; R 10是F，Cl，CF 3或C 1-2烷基; R11是卤素原子，羟基或氰基; W选自：W2a是H，卤素原子，氰基，C1-2烷基或C3-5环烷基，或其药学上可接受的盐或酯。

4. 发明授权

US08367690B2 Aminopyridine derivatives having aurora a selective inhibitory action 有权
标题翻译：具有极光选择性抑制作用的氨基吡啶衍生物
公开(公告)号：US08367690B2
公开(公告)日：2013-02-05
申请号：US13259620
申请日：2010-03-15
申请人： Hayley Binch , Masaya Hashimoto , Michael Mortimore , Mitsuru Ohkubo , Tomoko Sunami
发明人： Hayley Binch , Masaya Hashimoto , Michael Mortimore , Mitsuru Ohkubo , Tomoko Sunami
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： A61K31/535 , C07D401/14 , C07D417/14
摘要： The present invention relates to a compound of Formula (I): wherein: R1 is H, —NHCOOR1a, C5-6 cycloalkyl, or phenyl; where the cycloalkyl and phenyl each independently may be substituted with one to three of the same or different substituents selected from R10; R1a is C1-3 alkyl which may be substituted with one to three of the same or different substituents selected from F and Cl; R2 is H, —COOH, —CH2 COOH, —COOR2a, or —CH2COOR2a; R2a is C1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from halogen atoms; R3 is H, C1-6 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from R11; R10 is F, Cl, CF3, or C1-2 alkyl; R11 is halogen atom, hydroxy, or cyano; W is selected from: W2a is H, halogen atom, cyano, C1-2 alkyl, or C3-5 cycloalkyl, or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：本发明涉及式（I）的化合物：其中：R1是H，-NHCOOR1a，C5-6环烷基或苯基; 其中环烷基和苯基各自独立地可以被一至三个相同或不同的选自R 10的取代基取代; R 1a是可以被一至三个相同或不同的选自F和Cl的取代基取代的C 1-3烷基; R2是H，-COOH，-CH2COOH，-COOR2a或-CH2COOR2a; R2a是C1-2烷基，其中烷基可以被一至三个相同或不同的选自卤素原子的取代基取代; R3是H，C1-6烷基，其中烷基可以被一至三个相同或不同的选自R11的取代基取代; R 10是F，Cl，CF 3或C 1-2烷基; R11是卤素原子，羟基或氰基; W选自：W2a是H，卤素原子，氰基，C1-2烷基或C3-5环烷基，或其药学上可接受的盐或酯。

5. 发明授权

US08263632B2 Aminopyridine derivatives having Aurora A selective inhibitory action 有权
标题翻译：具有极光A的氨基吡啶衍生物选择性抑制作用
公开(公告)号：US08263632B2
公开(公告)日：2012-09-11
申请号：US13258782
申请日：2010-03-15
申请人： Toshiharu Iwama , Nobuhiko Kawanishi , Michael Mortimore , Mitsuru Ohkubo , Tomoko Sunami
发明人： Toshiharu Iwama , Nobuhiko Kawanishi , Michael Mortimore , Mitsuru Ohkubo , Tomoko Sunami
IPC分类号： C07D401/04 , A61K31/535
CPC分类号： C07D471/04 , C07D498/04
摘要： The present invention relates to a compound of Formula (I): wherein: n is 0 or 1; X is 0 or CH2; R1 is H or C1-2 alkyl; R2 is H or C1-3 alkyl; R3 and R4 are each independently H or C1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from R10; R5 is H or OCH3; R10 is F or Cl; or a pharmaceutically acceptable salt or ester thereof
摘要翻译：本发明涉及式（I）的化合物：其中：n为0或1; X为0或CH2; R1是H或C1-2烷基; R2是H或C1-3烷基; R 3和R 4各自独立地为H或C 1-2烷基，其中烷基可以被一至三个相同或不同的选自R 10的取代基取代; R5是H或OCH3; R10为F或Cl; 或其药学上可接受的盐或酯

6. 发明申请

US20120015940A1 NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION 有权
标题翻译：具有选择性抑制作用的新型氨基吡啶衍生物
公开(公告)号：US20120015940A1
公开(公告)日：2012-01-19
申请号：US13258782
申请日：2010-03-15
申请人： Toshiharu Iwama , Nobuhiko Kawanishi , Michael Mortimore , Mitsuru Ohkubo , Tomoko Sunami
发明人： Toshiharu Iwama , Nobuhiko Kawanishi , Michael Mortimore , Mitsuru Ohkubo , Tomoko Sunami
IPC分类号： A61K31/5383 , A61P35/00 , A61K31/506 , C07D487/04 , C07D498/04
CPC分类号： C07D471/04 , C07D498/04
摘要： The present invention relates to a compound of Formula (I): wherein: n is 0 or 1; X is O or CH2; R1 is H or C1-2 alkyl; R2 is H or C1-3 alkyl; R3 and R4 are each independently H or C1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from R10 R5 is H or OCH3; R10 is F or Cl; or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：本发明涉及式（I）的化合物：其中：n为0或1; X是O或CH2; R1是H或C1-2烷基; R2是H或C1-3烷基; R 3和R 4各自独立地为H或C 1-2烷基，其中烷基可被一至三个相同或不同的选自R 10的取代基取代，R 5为H或OCH 3; R10为F或Cl; 或其药学上可接受的盐或酯。

7. 发明申请

US20090317850A1 Crystal Structure of Human 70KD Ribosomal Protein S6 Kinase 1 Kinase Domain 审中-公开
标题翻译：人类70KD核糖体蛋白S6激酶1激酶结构域的晶体结构
公开(公告)号：US20090317850A1
公开(公告)日：2009-12-24
申请号：US12481103
申请日：2009-06-09
申请人： Tomoko Sunami , Mari Machida , Sanjeev K. Munshi , Sujata Sharma
发明人： Tomoko Sunami , Mari Machida , Sanjeev K. Munshi , Sujata Sharma
IPC分类号： C12Q1/48 , C12N9/12
CPC分类号： C12N9/1205
摘要： Crystallization of the 70 kDa ribosomal protein S6 kinase polypeptide 1 (p70S6K1) kinase domain for X-ray crystallography analysis to generate the three-dimensional structure of the p70S6K1 kinase domain is described. Further described is the use of the three 5 dimensional structure of p70S6K1 kinase domain for identifying and designing ligands or low molecular weight molecules that specifically bind to and modulate (inhibit) the kinase activity of p70S6K1. These ligands or molecules can be used for the treatment of metabolic disorders such as diabetes and for the treatment of various cancers.
摘要翻译：描述了70kDa核糖体蛋白S6激酶多肽1（p70S6K1）激酶结构域的结晶，用于X射线晶体学分析以产生p70S6K1激酶结构域的三维结构。进一步描述了p70S6K1激酶结构域的三维结构用于鉴定和设计与p70S6K1的激酶活性特异性结合并调节（抑制）p70S6K1激酶活性的配体或低分子量分子。这些配体或分子可用于治疗代谢性疾病如糖尿病和各种癌症的治疗。

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