公开(公告)号：US07897792B2

公开(公告)日：2011-03-01

申请号：US12161256

申请日：2007-02-09

申请人： Hitoshi Iikura ,  Ikumi Hyoudoh ,  Toshihiro Aoki ,  Noriyuki Furuichi ,  Masayuki Matsushita ,  Fumio Watanabe ,  Sawako Ozawa ,  Masahiro Sakaitani ,  Pil-Su Ho ,  Yasushi Tomii ,  Kenji Takanashi ,  Naoki Harada

发明人： Hitoshi Iikura ,  Ikumi Hyoudoh ,  Toshihiro Aoki ,  Noriyuki Furuichi ,  Masayuki Matsushita ,  Fumio Watanabe ,  Sawako Ozawa ,  Masahiro Sakaitani ,  Pil-Su Ho ,  Yasushi Tomii ,  Kenji Takanashi ,  Naoki Harada

IPC分类号： C07D311/00

CPC分类号： C07D311/18 ,  C07D405/12 ,  C07D417/12

摘要： The present invention provides a compound represented by general formula (1) below or a pharmaceutically acceptable salt thereof: wherein: X is selected from heteroaryl etc., Y1 and Y2 are selected from —N═ etc., Y3 and Y4 are selected from —CH═ etc., A is selected from sulfamide etc., R1 is selected from hydrogen etc., and R2 is selected from C1-6 alkyl etc. The compound or salt has sufficiently high antitumor activity, and is useful in the treatment of cell proliferative disorders, particularly cancers. The present invention also provides a pharmaceutical composition containing the compound or salt as an active ingredient.

摘要翻译： 本发明提供下述通式（1）表示的化合物或其药学上可接受的盐：其中：X选自杂芳基等，Y1和Y2选自-N =等，Y 3和Y 4选自 - CH等等，A选自磺酰胺等，R1选自氢等，R2选自C1-6烷基等。该化合物或盐具有足够高的抗肿瘤活性，可用于细胞的治疗 增殖性疾病，特别是癌症。 本发明还提供含有作为活性成分的化合物或盐的药物组合物。

公开(公告)号：US08569378B2

公开(公告)日：2013-10-29

申请号：US12669944

申请日：2008-07-18

申请人： Toshiyuki Sakai ,  Hitoshi Iikura ,  Ikumi Hyoudoh ,  Toshihiro Aoki ,  Noriyuki Furuichi ,  Masayuki Matsushita ,  Fumio Watanabe ,  Sawako Ozawa ,  Masahiro Sakaitani ,  Pil-Su Ho ,  Yasushi Tomii ,  Kenji Takanashi ,  Naoki Harada

发明人： Toshiyuki Sakai ,  Hitoshi Iikura ,  Ikumi Hyoudoh ,  Toshihiro Aoki ,  Noriyuki Furuichi ,  Masayuki Matsushita ,  Fumio Watanabe ,  Sawako Ozawa ,  Masahiro Sakaitani ,  Pil-Su Ho ,  Yasushi Tomii ,  Kenji Takanashi ,  Naoki Harada

IPC分类号： A01N41/02 ,  A01N41/06 ,  A01N43/16 ,  A61K31/16 ,  A61K31/18 ,  A61K31/35 ,  C07D311/00 ,  C07C331/00 ,  C07C381/00 ,  C07C303/00 ,  C07C309/00 ,  C07C311/00

CPC分类号： C07D405/14 ,  C07D407/04 ,  C07D409/04 ,  C07D409/12 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D491/052

摘要： The present invention provides a p27 protein inducing agent comprising a compound represented by general formula (11) below or pharmaceutically acceptable salt thereof as an active ingredient: wherein G1, G2, G3 and G8 are each independently selected from —N═ etc., Ring G6 is selected from divalent aryl etc., A is selected from amino etc., G4 is selected from oxygen etc., G5 is selected from oxygen etc., G7 is selected from —CH2— etc., and R2 is selected from C1-6 alkyl etc.

摘要翻译： 本发明提供了包含下述通式（11）表示的化合物或其药学上可接受的盐作为活性成分的p27蛋白诱导剂：其中，G1，G2，G3和G8各自独立地选自-N =等，环 G6选自二价芳基等，A选自氨基等，G4选自氧等，G5选自氧等，G7选自-CH2-等，R2选自C1- 6烷基等

公开(公告)号：US20110092700A1

公开(公告)日：2011-04-21

申请号：US12960134

申请日：2010-12-03

申请人： Hitoshi Iikura ,  Ikumi Hyoudoh ,  Toshihiro Aoki ,  Noriyuki Furuichi ,  Masayuki Matsushita ,  Fumio Watanabe ,  Sawako Ozawa ,  Masahiro Sakaitani ,  Pil-Su Ho ,  Yasushi Tomii ,  Kenji Takanashi ,  Naoki Harada

发明人： Hitoshi Iikura ,  Ikumi Hyoudoh ,  Toshihiro Aoki ,  Noriyuki Furuichi ,  Masayuki Matsushita ,  Fumio Watanabe ,  Sawako Ozawa ,  Masahiro Sakaitani ,  Pil-Su Ho ,  Yasushi Tomii ,  Kenji Takanashi ,  Naoki Harada

IPC分类号： C07D265/26 ,  C07D311/16 ,  C07D409/06 ,  C07D403/12 ,  C07D491/14 ,  C07D417/12 ,  C07D401/10 ,  C07D403/10 ,  C07D403/14 ,  C07D413/12

CPC分类号： C07D311/18 ,  C07D405/12 ,  C07D417/12

摘要： The present invention provides a compound represented by general formula (1) below or a pharmaceutically acceptable salt thereof: wherein: X is selected from heteroaryl etc., Y1 and Y2 are selected from —N═ etc., Y3 and Y4 are selected from —CH═ etc., A is selected from sulfamide etc., R1 is selected from hydrogen etc., and R2 is selected from C1-6 alkyl etc. The compound or salt has sufficiently high antitumor activity, and is useful in the treatment of cell proliferative disorders, particularly cancers. The present invention also provides a pharmaceutical composition containing the compound or salt as an active ingredient.

摘要翻译： 本发明提供下述通式（1）表示的化合物或其药学上可接受的盐：其中：X选自杂芳基等，Y1和Y2选自-N =等，Y 3和Y 4选自 - CH等等，A选自磺酰胺等，R1选自氢等，R2选自C1-6烷基等。化合物或盐具有足够高的抗肿瘤活性，可用于细胞的治疗 增殖性疾病，特别是癌症。 本发明还提供含有作为活性成分的化合物或盐的药物组合物。

公开(公告)号：US08278465B2

公开(公告)日：2012-10-02

申请号：US12960134

申请日：2010-12-03

申请人： Hitoshi Iikura ,  Ikumi Hyoudoh ,  Toshihiro Aoki ,  Noriyuki Furuichi ,  Masayuki Matsushita ,  Fumio Watanabe ,  Sawako Ozawa ,  Masahiro Sakaitani ,  Pil-Su Ho ,  Yasushi Tomii ,  Kenji Takanashi ,  Naoki Harada

发明人： Hitoshi Iikura ,  Ikumi Hyoudoh ,  Toshihiro Aoki ,  Noriyuki Furuichi ,  Masayuki Matsushita ,  Fumio Watanabe ,  Sawako Ozawa ,  Masahiro Sakaitani ,  Pil-Su Ho ,  Yasushi Tomii ,  Kenji Takanashi ,  Naoki Harada

IPC分类号： C07D311/00

CPC分类号： C07D311/18 ,  C07D405/12 ,  C07D417/12

摘要： The present invention provides a compound represented by general formula (1) below or a pharmaceutically acceptable salt thereof: wherein: X is selected from heteroaryl etc., Y1 and Y2 are selected from —N═ etc., Y3 and Y4 are selected from —CH═ etc., A is selected from sulfamide etc., R1 is selected from hydrogen etc., and R2 is selected from C1-6 alkyl etc. The compound or salt has sufficiently high antitumor activity, and is useful in the treatment of cell proliferative disorders, particularly cancers. The present invention also provides a pharmaceutical composition containing the compound or salt as an active ingredient.

摘要翻译： 本发明提供下述通式（1）表示的化合物或其药学上可接受的盐：其中：X选自杂芳基等，Y1和Y2选自-N =等，Y 3和Y 4选自 - CH等等，A选自磺酰胺等，R1选自氢等，R2选自C1-6烷基等。该化合物或盐具有足够高的抗肿瘤活性，可用于细胞的治疗 增殖性疾病，特别是癌症。 本发明还提供含有作为活性成分的化合物或盐的药物组合物。

公开(公告)号：US20110009398A1

公开(公告)日：2011-01-13

申请号：US12669944

申请日：2008-07-18

申请人： Toshiyuki Sakai ,  Hitoshi Iikura ,  Ikumi Hyoudoh ,  Toshihiro Aoki ,  Noriyuki Furuichi ,  Masayuki Matsushita ,  Fumio Watanabe ,  Sawako Ozawa ,  Masahiro Sakaitani ,  Pil-Su Ho ,  Yasushi Tomii ,  Kenji Takanashi ,  Naoki Harada

发明人： Toshiyuki Sakai ,  Hitoshi Iikura ,  Ikumi Hyoudoh ,  Toshihiro Aoki ,  Noriyuki Furuichi ,  Masayuki Matsushita ,  Fumio Watanabe ,  Sawako Ozawa ,  Masahiro Sakaitani ,  Pil-Su Ho ,  Yasushi Tomii ,  Kenji Takanashi ,  Naoki Harada

IPC分类号： A61K31/536 ,  A61K31/4965 ,  A61K31/506 ,  A61K31/436 ,  A61K31/427 ,  A61K31/366 ,  C07D413/02 ,  C07D405/02 ,  C07D405/14 ,  C07D471/02 ,  C07D417/12 ,  C07D311/06 ,  C07D417/14

CPC分类号： C07D405/14 ,  C07D407/04 ,  C07D409/04 ,  C07D409/12 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D491/052

摘要： The present invention provides a p27 protein inducing agent comprising a compound represented by general formula (11) below or pharmaceutically acceptable salt thereof as an active ingredient: wherein G1, G2, G3 and G8 are each independently selected from —N═ etc., Ring G6 is selected from divalent aryl etc., A is selected from amino etc., G4 is selected from oxygen etc., G5 is selected from oxygen etc., G7 is selected from —CH2— etc., and R2 is selected from C1-6 alkyl etc.

摘要翻译： 本发明提供一种p27蛋白诱导剂，其含有下述通式（11）表示的化合物或其药学上可接受的盐作为活性成分：其中，G1，G2，G3和G8各自独立地选自-N等。环 G6选自二价芳基等，A选自氨基等，G4选自氧等，G5选自氧等，G7选自-CH2-等，R2选自C1- 6烷基等

公开(公告)号：US20100004233A1

公开(公告)日：2010-01-07

申请号：US12161256

申请日：2007-02-09

申请人： Hitoshi Iikura ,  Ikumi Hyoudoh ,  Toshihiro Aoki ,  Noriyuki Furuichi ,  Masayuki Matsushita ,  Fumio Watanabe ,  Sawako Ozawa ,  Masahiro Sakaitani ,  Pil-Su Ho ,  Yasushi Tomii ,  Kenji Takanashi ,  Naoki Harada

发明人： Hitoshi Iikura ,  Ikumi Hyoudoh ,  Toshihiro Aoki ,  Noriyuki Furuichi ,  Masayuki Matsushita ,  Fumio Watanabe ,  Sawako Ozawa ,  Masahiro Sakaitani ,  Pil-Su Ho ,  Yasushi Tomii ,  Kenji Takanashi ,  Naoki Harada

IPC分类号： A61K31/536 ,  C07D311/06 ,  A61K31/352 ,  C07D405/12 ,  A61K31/506 ,  C07D413/12

CPC分类号： C07D311/18 ,  C07D405/12 ,  C07D417/12

摘要： The present invention provides a compound represented by general formula (1) below or a pharmaceutically acceptable salt thereof: wherein: X is selected from heteroaryl etc., Y1 and Y2 are selected from —N═ etc., Y3 and Y4 are selected from —CH═ etc., A is selected from sulfamide etc., R1 is selected from hydrogen etc., and R2 is selected from C1-6 alkyl etc. The compound or salt has sufficiently high antitumor activity, and is useful in the treatment of cell proliferative disorders, particularly cancers. The present invention also provides a pharmaceutical composition containing the compound or salt as an active ingredient.

摘要翻译： 本发明提供下述通式（1）表示的化合物或其药学上可接受的盐：其中：X选自杂芳基等，Y1和Y2选自-N-等，Y3和Y4选自 - CH-等，A选自磺酰胺等，R1选自氢等，R2选自C1-6烷基等。化合物或盐具有足够高的抗肿瘤活性，可用于治疗细胞 增殖性疾病，特别是癌症。 本发明还提供含有作为活性成分的化合物或盐的药物组合物。

公开(公告)号：US07189858B2

公开(公告)日：2007-03-13

申请号：US10933577

申请日：2004-09-03

申请人： Hiroshi Fukuda ,  Tadakatsu Hayase ,  Eisaku Mizuguchi ,  Nobuo Shimma ,  Jun Ohwada ,  Nobuhiro Oikawa ,  Masahiro Sakaitani ,  Masao Tsukazaki ,  Isao Umeda

发明人： Hiroshi Fukuda ,  Tadakatsu Hayase ,  Eisaku Mizuguchi ,  Nobuo Shimma ,  Jun Ohwada ,  Nobuhiro Oikawa ,  Masahiro Sakaitani ,  Masao Tsukazaki ,  Isao Umeda

IPC分类号： C07D417/06

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D417/06 ,  C07D417/14

摘要： N-substituted carbamoyloxyalkyl-azolium derivatives Which have antifungal activity and are useful for the treatment of fungal diseases.

摘要翻译： N-取代氨基甲酰氧基烷基 - 唑类衍生物具有抗真菌活性，可用于治疗真菌病。

公开(公告)号：US06489440B1

公开(公告)日：2002-12-03

申请号：US09360476

申请日：1999-07-23

申请人： Masahiro Aoki ,  Masami Kohchi ,  Kazunao Masubuchi ,  Eisaku Mizuguchi ,  Takeshi Murata ,  Hiroaki Ohkuma ,  Takehiro Okada ,  Masahiro Sakaitani ,  Nobuo Shimma ,  Takahide Watanabe ,  Mieko Yanagisawa ,  Yuri Yasuda

发明人： Masahiro Aoki ,  Masami Kohchi ,  Kazunao Masubuchi ,  Eisaku Mizuguchi ,  Takeshi Murata ,  Hiroaki Ohkuma ,  Takehiro Okada ,  Masahiro Sakaitani ,  Nobuo Shimma ,  Takahide Watanabe ,  Mieko Yanagisawa ,  Yuri Yasuda

IPC分类号： C07K750

CPC分类号： C07K7/08 ,  A61K38/00 ,  C07K7/56

摘要： The present invention relates to novel Aerothricins represented by the Formula (I), wherein R1, R2, R3, R4, R5, X, Y, Z, and m are as defined in Claim 1; and pharmaceutically acceptable salts thereof. The present invention also relates to a pharmaceutical composition comprising an Aerothricin of the Formula (I) and a pharmaceutically acceptable carrier. Furthermore, the present invention relates to the use of such Aerothricins for the preparation of medicaments, as well as to processes and intermediates for the preparation of the Aerothricins of the Formula (I).

摘要翻译： 本发明涉及由式（I）表示的新型气丝菌素，其中R1，R2，R3，R4，R5，X，Y，Z和m如权利要求1所定义; 本发明还涉及包含式（I）的气丝菌素和药学上可接受的载体的药物组合物。 此外，本发明涉及这种气丝菌素用于制备药物的用途，以及制备式（I）的气丝菌素的方法和中间体。

公开(公告)号：US20090275623A1

公开(公告)日：2009-11-05

申请号：US12306901

申请日：2007-06-29

申请人： Kazuhiko Ohrai ,  Michiaki Adachi ,  Koji Toyama ,  Takanori Shimizu ,  Keishi Hayashi ,  Masataka Minami ,  Yoshiyuki Suzuki ,  Masakazu Sugiyama ,  Masateru Ohta ,  Shojiro Kadono ,  Takuya Shiraishi ,  Haruhiko Sato ,  Yoshiaki Watanabe ,  Nobuya Ishii ,  Masahiro Sakaitani ,  Masami Hasegawa

发明人： Kazuhiko Ohrai ,  Michiaki Adachi ,  Koji Toyama ,  Takanori Shimizu ,  Keishi Hayashi ,  Masataka Minami ,  Yoshiyuki Suzuki ,  Masakazu Sugiyama ,  Masateru Ohta ,  Shojiro Kadono ,  Takuya Shiraishi ,  Haruhiko Sato ,  Yoshiaki Watanabe ,  Nobuya Ishii ,  Masahiro Sakaitani ,  Masami Hasegawa

IPC分类号： A61K31/429 ,  C07D513/04 ,  A61P9/04 ,  A61P35/00

CPC分类号： C07D513/04

摘要： The present invention provides novel α-amino acid derivatives of formula (1): (wherein, R1, R2, R3, R4, X and Y are as defined in the claims) or pharmaceutically acceptable salts, prodrugs or solvates thereof. The derivatives of formula (1) have βARK1 inhibitory activity and are useful for preventing or treating heart failure. Moreover, the derivatives of formula (1) also have antitumor activity, particularly dual inhibitory activity on Aurora kinase and CDK, and are useful for cell proliferative diseases such as cancer.

摘要翻译： 本发明提供新的式（1）的α-氨基酸衍生物：（其中，R 1，R 2，R 3，R 4，X和Y如权利要求中所定义）或其药学上可接受的盐，前药或溶剂合物。 式（1）的衍生物具有βARK1抑制活性，可用于预防或治疗心力衰竭。 此外，式（1）的衍生物还具有抗肿瘤活性，特别是对Aurora激酶和CDK的双重抑制活性，并且可用于细胞增殖性疾病如癌症。

公开(公告)号：US07459561B2

公开(公告)日：2008-12-02

申请号：US11504299

申请日：2006-08-15

申请人： Hiroshi Fukuda ,  Tadakatsu Hayase ,  Eisaku Mizuguchi ,  Nobuo Shimma ,  Jun Ohwada ,  Nobuhiro Oikawa ,  Masahiro Sakaitani ,  Masao Tsukazaki ,  Isao Umeda

发明人： Hiroshi Fukuda ,  Tadakatsu Hayase ,  Eisaku Mizuguchi ,  Nobuo Shimma ,  Jun Ohwada ,  Nobuhiro Oikawa ,  Masahiro Sakaitani ,  Masao Tsukazaki ,  Isao Umeda

IPC分类号： C07D401/14

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D417/06 ,  C07D417/14

摘要： N-substituted carbamoyloxyalkyl-azolium derivatives which have antifungal activity and are useful for the treatment of fungal diseases.

摘要翻译： 具有抗真菌活性并可用于治疗真菌疾病的N-取代氨基甲酰氧基烷基 - 唑鎓衍生物。