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公开(公告)号:US06806266B1
公开(公告)日:2004-10-19
申请号:US10030618
申请日:2002-01-11
申请人: Fumihiko Kanai , Nobuyoshi Amishiro , Yushi Kitamura , Chikara Murakata , Tadakazu Akiyama , Shiro Akinaga , Eiichi Fuse , Takashi Kuwabara , Kenichi Yasoshima
发明人: Fumihiko Kanai , Nobuyoshi Amishiro , Yushi Kitamura , Chikara Murakata , Tadakazu Akiyama , Shiro Akinaga , Eiichi Fuse , Takashi Kuwabara , Kenichi Yasoshima
IPC分类号: C07D49822
CPC分类号: C07D498/22 , A61K31/553
摘要: The present invention provides an antitumor agent comprising a staurosporin derivative or a pharmaceutically acceptable salt thereof, as an active ingredient, which is represented by the general formula (I): wherein R1 represents hydrogen, hydroxy or lower alkoxy, R2 and R3 are the same or different and represent hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted aryl, a substituted or unsubstituted heterocyclic group, halogen, nitro, formyl, etc., R4 represents hydrogen, etc., R5 represents NR11AR12A (wherein R11A and R12A represent hydrogen, substituted or unsubstituted lower alkyl, etc.), provided that R2 and R3 are not simultaneously hydrogen.
摘要翻译: 本发明提供包含星形孢菌素衍生物或其药学上可接受的盐作为活性成分的抗肿瘤剂,其由通式(I)表示:其中R 1表示氢,羟基或低级烷氧基,R 2 和R 3相同或不同,表示氢,取代或未取代的烷基,取代或未取代的低级烯基,取代或未取代的低级炔基,取代或未取代的芳基,取代或未取代的杂环基,卤素,硝基,甲酰基, 等等,R 4表示氢等,R 5表示NR 11A R 12A(其中R 11A和R 12A表示氢,取代或未取代的低级烷基等), 条件是R 2和R 3不同时为氢。
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公开(公告)号:US20110275827A1
公开(公告)日:2011-11-10
申请号:US13188819
申请日:2011-07-22
申请人: Kazuhiko KATO , Yushi KITAMURA
发明人: Kazuhiko KATO , Yushi KITAMURA
IPC分类号: C07D285/135
CPC分类号: C07D285/13 , A61K31/433 , A61K31/4439 , A61K31/506 , A61K31/5377 , C07D285/135
摘要: A mitotic kinesin Eg5 inhibitor which comprises a thiadiazoline derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein R1 represents a hydrogen atom and the like, R2 represents a hydrogen atom, —C(═W)R6 (wherein W represents an oxygen atom or a sulfur atom, and R6 represents substituted or unsubstituted lower alkyl and the like) and the like, R3 represents —C(═Z)R19 (wherein Z represents an oxygen atom or a sulfur atom, and R19 represents substituted or unsubstituted lower alkyl and the like) and the like, R4 represents substituted or unsubstituted lower alkyl and the like, and R5 represents substituted or unsubstituted aryl and the like] and the like are provided.
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公开(公告)号:US20070265268A1
公开(公告)日:2007-11-15
申请号:US11718079
申请日:2005-11-09
申请人: Yushi Kitamura , Yutaka Kanda , Takayuki Nakashima
发明人: Yushi Kitamura , Yutaka Kanda , Takayuki Nakashima
IPC分类号: A61K31/166 , A61K31/235 , A61K31/24 , A61K31/40 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/5375 , C07C229/34 , C07C235/44 , C07C69/84 , C07D207/08 , C07D213/04 , C07D265/30 , C07D295/14
CPC分类号: C07C235/64 , C07C69/88 , C07C235/60 , C07D213/40 , C07D295/192
摘要: The present invention provides Hsp90 family protein inhibitors comprising, as an active ingredient, a benzoic acid derivative represented by General Formula (I): [wherein n represents an integer of 0 to 10; R1 represents substituted or unsubstituted lower alkoxycarbonyl, substituted or unsubstituted aroyl, or the like; R2 represents —NR14R15 (wherein R14 and R15 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl or the like); R3 and R5 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl or the like; and R4 and R6 may be the same or different and each represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl or the like] or a prodrug thereof, or a pharmaceutically acceptable salt of said benzoic acid derivative or said prodrug.
摘要翻译: 本发明提供Hsp90家族蛋白抑制剂,其包含通式(I)表示的苯甲酸衍生物作为活性成分:[其中,n表示0〜10的整数, R 1表示取代或未取代的低级烷氧基羰基,取代或未取代的芳酰基等; R 2表示-NR 14 R 15(其中R 14和R 15) 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,取代或未取代的芳烷基等); R 3和R 5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; R 4和R 6可以相同或不同,各自表示氢原子,卤素,取代或未取代的低级烷基等]或其前药,或 所述苯甲酸衍生物或所述前药的药学上可接受的盐。
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公开(公告)号:US08273738B2
公开(公告)日:2012-09-25
申请号:US12440237
申请日:2007-09-05
申请人: Naoto Osakada , Mariko Osakada , Takashi Sawada , Satoshi Kaneko , Atsuko Mizutani , Noriaki Uesaka , Yoshisuke Nakasato , Keishi Katayama , Masamori Sugawara , Yushi Kitamura
发明人: Naoto Osakada , Mariko Osakada , Takashi Sawada , Satoshi Kaneko , Atsuko Mizutani , Noriaki Uesaka , Yoshisuke Nakasato , Keishi Katayama , Masamori Sugawara , Yushi Kitamura
IPC分类号: A61K31/535 , A61K31/4965
CPC分类号: C07D233/64 , C07D401/04 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要: A CB2 receptor modulator comprising an imidazole derivative represented by the general formula (I): [wherein, R1 represents optionally substituted lower alkyl or the like; R2 represents optionally substituted cycloalkyl or the like; R3 represents optionally substituted aryl or the like; and n represents an integer of 0 to 3] or a pharmaceutically acceptable salt thereof as an active ingredient, and the like are provided.
摘要翻译: 包含由通式(I)表示的咪唑衍生物的CB2受体调节剂:[其中,R 1表示任选取代的低级烷基等; R2代表任选取代的环烷基等; R3表示任选取代的芳基等; 和n表示0〜3的整数]或其药学上可接受的盐作为活性成分,等。
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公开(公告)号:US20110004000A1
公开(公告)日:2011-01-06
申请号:US12883338
申请日:2010-09-16
申请人: Chikara MURAKATA , Yoshinori YAMASHITA , Ryuichiro NAKAI , Kazuhito AKASAKA , Yoji INO , Kazuhiko KATO , Yushi KITAMURA
发明人: Chikara MURAKATA , Yoshinori YAMASHITA , Ryuichiro NAKAI , Kazuhito AKASAKA , Yoji INO , Kazuhiko KATO , Yushi KITAMURA
IPC分类号: C07D285/135
CPC分类号: C07D285/13 , A61K31/433 , A61K31/4439 , A61K31/506 , A61K31/5377 , C07D285/135
摘要: A mitotic kinesin Eg5 inhibitor which comprises a thiadiazoline derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein R1 represents a hydrogen atom and the like, R2 represents a hydrogen atom, —C(═W)R6 (wherein W represents an oxygen atom or a sulfur atom, and R6 represents substituted or unsubstituted lower alkyl and the like) and the like, R3 represents —C(═Z)R19 (wherein Z represents an oxygen atom or a sulfur atom, and R19 represents substituted or unsubstituted lower alkyl and the like) and the like, R4 represents substituted or unsubstituted lower alkyl and the like, and R5 represents substituted or unsubstituted aryl and the like] and the like are provided.
摘要翻译: 一种有丝分裂驱动蛋白Eg5抑制剂,其包含由通式(I)表示的噻二唑啉衍生物或其药理学上可接受的盐作为活性成分:[其中R 1表示氢原子等,R 2表示氢原子,-C(= W)R6(其中W表示氧原子或硫原子,R6表示取代或未取代的低级烷基等)等,R3表示-C(= Z)R19(其中Z表示氧原子或硫原子 原子,R 19表示取代或未取代的低级烷基等)等,R 4表示取代或未取代的低级烷基等,R 5表示取代或未取代的芳基等〕等。
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公开(公告)号:US20100152178A1
公开(公告)日:2010-06-17
申请号:US12440237
申请日:2007-09-05
申请人: Naoto Osakada , Mariko Osakada , Takashi Sawada , Satoshi Kaneko , Atsuko Mizutani , Noriaki Uesaka , Yoshisuke Nakasato , Keishi Katayama , Masamori Sugawara , Yushi Kitamura
发明人: Naoto Osakada , Mariko Osakada , Takashi Sawada , Satoshi Kaneko , Atsuko Mizutani , Noriaki Uesaka , Yoshisuke Nakasato , Keishi Katayama , Masamori Sugawara , Yushi Kitamura
IPC分类号: A61K31/5377 , C07D233/64 , A61K31/4174 , C07D401/04 , A61K31/4439 , C07D401/10 , A61K31/454 , C07D413/10 , C07D471/04 , A61K31/519 , C07D401/14 , A61K31/497 , C07D413/14 , A61P29/00 , A61P25/06 , A61P25/00 , A61P37/08 , A61P37/00 , A61P19/02 , A61P1/00 , A61P25/28 , A61P11/06 , A61P11/00 , A61P17/00 , A61P9/10 , A61P3/04 , A61P19/10 , A61P27/06
CPC分类号: C07D233/64 , C07D401/04 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要: A CB2 receptor modulator comprising an imidazole derivative represented by the general formula (I): [wherein, R1 represents optionally substituted lower alkyl or the like; R2 represents optionally substituted cycloalkyl or the like; R3 represents optionally substituted aryl or the like; and n represents an integer of 0 to 3] or a pharmaceutically acceptable salt thereof as an active ingredient, and the like are provided.
摘要翻译: 包含由通式(I)表示的咪唑衍生物的CB2受体调节剂:[其中,R 1表示任选取代的低级烷基等; R2代表任选取代的环烷基等; R3表示任选取代的芳基等; 和n表示0〜3的整数]或其药学上可接受的盐作为活性成分,等。
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公开(公告)号:US20080194653A1
公开(公告)日:2008-08-14
申请号:US11909289
申请日:2006-03-22
申请人: Chikara Murakata , Kazuhiko Kato , Junichiro Yamamoto , Ryuichiro Nakai , Seiho Okamoto , Yoji Ino , Yushi Kitamura , Toshikazu Saitoh , Takeshi Katsuhira
发明人: Chikara Murakata , Kazuhiko Kato , Junichiro Yamamoto , Ryuichiro Nakai , Seiho Okamoto , Yoji Ino , Yushi Kitamura , Toshikazu Saitoh , Takeshi Katsuhira
IPC分类号: A61K31/433 , C07D285/08 , A61P35/00
CPC分类号: A61K31/433 , A61K31/454 , C07D285/135 , C07D417/04
摘要: A therapeutic and/or prophylactic agent for a solid tumor, which comprises a thiadiazoline derivative represented by the general formula (I), or a pharmaceutically acceptable salt thereof: [wherein, n represents an integer of 1 to 3, R1 represents a hydrogen atom, R2 represents lower alkyl, or R1 and R2 are combined together to represent alkylene, R3 represents lower alkyl, R4 represents NHSO2R6 (wherein R6 represents hydroxy or the like) or the like, and R5 represents aryl or the like] and the like are provided.
摘要翻译: 含有通式(I)表示的噻二唑啉衍生物或其药学上可接受的盐的固体肿瘤治疗剂和/或预防剂,其中n表示1〜3的整数,R 1 R 2表示氢原子,R 2表示低级烷基,或R 1和R 2结合在一起代表亚烷基,R 低级烷基表示低级烷基,R 4表示NHSO 2 R 6(其中R 6或以上) >表示羟基等)等,R 5表示芳基等]等。
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公开(公告)号:US20070155813A1
公开(公告)日:2007-07-05
申请号:US10584234
申请日:2004-12-24
申请人: Yushi Kitamura , Shinji Nara , Hiroshi Nakagawa , Rieko Nakatsu , Takayuki Nakashima , Shiro Soga , Jiro Kajita , Yukimasa Shiotsu , Yutaka Kanda
发明人: Yushi Kitamura , Shinji Nara , Hiroshi Nakagawa , Rieko Nakatsu , Takayuki Nakashima , Shiro Soga , Jiro Kajita , Yukimasa Shiotsu , Yutaka Kanda
IPC分类号: A61K31/4152 , A61K31/277 , A61K31/138
CPC分类号: C07C311/21 , C07C39/367 , C07C43/178 , C07C43/21 , C07C43/23 , C07C49/245 , C07C49/248 , C07C49/83 , C07C59/56 , C07C65/105 , C07C69/732 , C07C69/734 , C07C69/736 , C07C215/52 , C07C217/08 , C07C217/76 , C07C233/25 , C07C233/75 , C07C235/06 , C07C235/08 , C07C235/16 , C07C235/34 , C07C235/36 , C07C235/38 , C07C235/42 , C07C235/44 , C07C235/46 , C07C235/80 , C07C251/40 , C07C251/48 , C07C275/32 , C07C307/02 , C07C309/65 , C07C311/08 , C07C2601/14 , C07D203/10 , C07D207/27 , C07D211/16 , C07D211/58 , C07D213/30 , C07D213/36 , C07D213/40 , C07D213/85 , C07D217/04 , C07D217/06 , C07D231/56 , C07D235/18 , C07D263/32 , C07D263/34 , C07D271/113 , C07D277/24 , C07D295/108 , C07D295/155 , C07D295/185 , C07D307/12 , C07D307/42 , C07D307/52 , C07D307/54 , C07D307/68 , C07D307/91 , C07D309/06 , C07D317/20 , C07D317/54 , C07D333/16 , C07D405/12
摘要: wherein n is an integer of 0 to 10; R1 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, substituted or unsubstituted cycloalkyl, substituted or unsubstituted lower alkoxycarbonyl, substituted or unsubstituted heterocyclic-alkyl, substituted or unsubstituted aryl, —CONR7R8, —NR9R10, etc.; R2 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; R3 and R5 may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, etc.; R4 and R6 may be the same or different, each represent a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, etc.) Provided are an Hsp90 family protein inhibitor comprising, as an active ingredient, a benzene derivative of formula (I) or a prodrug thereof or a pharmaceutically-acceptable salt thereof, etc.
摘要翻译: 其中n为0至10的整数; R 1表示取代或未取代的低级烷基,取代或未取代的低级烷氧基,取代或未取代的环烷基,取代或未取代的低级烷氧基羰基,取代或未取代的杂环 - 烷基,取代或未取代的芳基,-CONR R 8,R 9,R 10等; R 2表示取代或未取代的芳基或取代或未取代的杂环基等; R 3和R 5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; R 4和R 6可以相同或不同,各自表示氢原子,卤素,取代或未取代的低级烷基等)。提供的是Hsp90家族蛋白抑制剂 包含作为活性成分的式(I)的苯衍生物或其前药或其药学上可接受的盐等。
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公开(公告)号:US20120289502A1
公开(公告)日:2012-11-15
申请号:US13558325
申请日:2012-07-25
申请人: Naoto Osakada , Mariko Osakada , Takashi Sawada , Satoshi Kaneko , Atsuko Mizutani , Noriaki Uesaka , Yoshisuke Nakasato , Keishi Katayama , Masamori Sugawara , Yushi Kitamura
发明人: Naoto Osakada , Mariko Osakada , Takashi Sawada , Satoshi Kaneko , Atsuko Mizutani , Noriaki Uesaka , Yoshisuke Nakasato , Keishi Katayama , Masamori Sugawara , Yushi Kitamura
IPC分类号: A61K31/4164 , A61P25/00 , A61K31/5377 , A61K31/4439 , A61K31/454
CPC分类号: C07D233/64 , C07D401/04 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要: A CB2 receptor modulator comprising an imidazole derivative represented by the general formula (I): [wherein, R1 represents optionally substituted lower alkyl or the like; R2 represents optionally substituted cycloalkyl or the like; R3 represents optionally substituted aryl or the like; and n represents an integer of 0 to 3] or a pharmaceutically acceptable salt thereof as an active ingredient, and the like are provided.
摘要翻译: 包含由通式(I)表示的咪唑衍生物的CB2受体调节剂:[其中,R 1表示任选取代的低级烷基等; R2代表任选取代的环烷基等; R3表示任选取代的芳基等; 和n表示0〜3的整数]或其药学上可接受的盐作为活性成分,等。
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公开(公告)号:US20070276017A1
公开(公告)日:2007-11-29
申请号:US10560230
申请日:2004-06-09
申请人: Chikara Murakata , Yoji Ino , Kazuhiko Kato , Junichiro Yamamoto , Yushi Kitamura , Ryuichiro Nakai , Tomohisa Nakano , Tetsuya Tsujita
发明人: Chikara Murakata , Yoji Ino , Kazuhiko Kato , Junichiro Yamamoto , Yushi Kitamura , Ryuichiro Nakai , Tomohisa Nakano , Tetsuya Tsujita
IPC分类号: A61K31/454 , C07D285/12 , A61K31/433 , C07D417/02
CPC分类号: C07D285/135
摘要: A thiadiazoline derivative represented by the general formula (I), or a pharmacologically acceptable salt thereof: [wherein R1 represents a hydrogen atom and the like, R2 represents a hydrogen atom, —COR5 (wherein R5 represents lower alkyl and the like) and the like, R3 represents lower alkyl and the like, R4 represents aryl and the like, A represents —(CH2)n— (wherein n represents an integer of 1 to 6) and the like, and B represents —NR6R7 (wherein R6 and R7 are the same or different and represent a hydrogen atom, lower alkyl and the like) and the like] is provided.
摘要翻译: 由通式(I)表示的噻二唑啉衍生物或其药理学上可接受的盐:[其中R 1表示氢原子等,R 2表示氢 原子,-COR 5(其中R 5表示低级烷基等)等,R 3表示低级烷基等, R 4表示芳基等,A表示 - (CH 2 CH 2)n - (其中n表示1至6的整数)和 和B代表-NR 6 R 7(其中R 6和R 7和R 7相同或不同) 不同,表示氢原子,低级烷基等)等。
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