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1. 发明申请

US20080305081A1 Novel aminopyrimidine derivatives as PLK1 inhibitors 有权
标题翻译：新型氨基嘧啶衍生物作为PLK1抑制剂
公开(公告)号：US20080305081A1
公开(公告)日：2008-12-11
申请号：US12002546
申请日：2007-12-18
申请人： Takashi Hashihayata , Mikako Kawamura , Morihiro Mitsuya , Yoshiyuki Sato
发明人： Takashi Hashihayata , Mikako Kawamura , Morihiro Mitsuya , Yoshiyuki Sato
IPC分类号： A61K38/21 , C07D471/04 , A61K39/395 , A61K33/24 , A61K38/50 , A61P35/00 , A61K31/506
CPC分类号： C07D471/04
摘要： The present invention relates to a compound represented by Formula [I]: or a pharmaceutically acceptable salt or ester thereof, wherein R1 and R2, which may be the same or different, are each a hydrogen atom, a lower alkyl group, a cycloalkyl group, or the like; R3 and R4, which may be the same or different, are each a hydrogen atom, a lower alkyl group, NRaRb, a phenyl group, a lower alkyl group substituted with a phenyl group, a 4- to 7-membered aliphatic heterocyclic group, a lower alkyl group substituted with a 4- to 7-membered aliphatic heterocyclic group, a 5- or 6-membered aromatic heterocyclic group, a lower alkyl group substituted with a 5- or 6-membered aromatic heterocyclic group, or the like; and R5 is a hydrogen atom, a cyano group, a halogen atom, or a lower alkyl group.
摘要翻译：本发明涉及由式[I]表示的化合物或其药学上可接受的盐或酯，其中R 1和R 2可以相同或不同，分别为氢原子，低级烷基，环烷基，等等; R 3和R 4可以相同或不同，分别为氢原子，低级烷基，NR a R b，苯基，被苯基取代的低级烷基，4-至7-元脂族杂环基，被4-至7-元脂族杂环基取代的低级烷基，5或6元芳族杂环基，被5或6元芳族杂环基取代的低级烷基等; R5为氢原子，氰基，卤素原子或低级烷基。

2. 发明申请

US20080070894A1 Novel Substituted Imidazole Derivative 有权
标题翻译：新型替代咪唑衍生物
公开(公告)号：US20080070894A1
公开(公告)日：2008-03-20
申请号：US11661486
申请日：2005-08-30
申请人： Mikako Kawamura , Takashi Hashihayata , Satoshi Sunami , Tetsuya Sugimoto , Fuyuki Yamamoto , Yoshiyuki Sato , Kaori Kamijo , Morihiro Mitsuya , Yoshikazu Iwasawa , Hideya Komatani
发明人： Mikako Kawamura , Takashi Hashihayata , Satoshi Sunami , Tetsuya Sugimoto , Fuyuki Yamamoto , Yoshiyuki Sato , Kaori Kamijo , Morihiro Mitsuya , Yoshikazu Iwasawa , Hideya Komatani
IPC分类号： A61K31/397 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/52 , A61K31/5377 , A61K31/5513 , A61P35/00 , C07D237/06 , C07D239/24 , C07D243/14 , C07D295/00 , C07D473/00
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to a compound represented by Formula [I] or a pharmaceutically acceptable salt or ester thereof: wherein: X1, X2, X3, and X4, which may be identical or different, are each C or N, provided that none to two of X1, X2, X3, and X4 is/are N; Y is CH or N; R1, R1′, R2, R2′, R3, R3′, R4, and R4′, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R5 is a hydrogen atom or a methyl group; R6 and R7, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R8 and R8′, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R9 is an aryl group or a heteroaryl group which may be substituted; and n is an integer from 1 to 3, and a PLK1 inhibitor or an anticancer agent containing the same.
摘要翻译：本发明涉及由式[I]表示的化合物或其药学上可接受的盐或酯：其中：X 1，X 2，X 3， / SUB>和X 4可以相同或不同，各自为C或N，条件是X 1，X 2， / SUB>，X 3和X 4是N; Y是CH或N; R 1，R 1，R 2，R 2，R 3，N 3， R 3，R 4，R 4，R 4和R 4可以相同或不同，分别为氢原子，低级烷基等; R 5是氢原子或甲基; R 6和R 7可以相同或不同，分别为氢原子，低级烷基等; R 8和R 8可以相同或不同，分别为氢原子，低级烷基等; R 9是可以被取代的芳基或杂芳基; n为1〜3的整数，PLK1抑制剂或含有该PLK1抑制剂的抗癌剂。

3. 发明申请

US20060258701A1 Novel 2-pyridinecarboxamide derivatives 有权
标题翻译：新型2-吡啶甲酰胺衍生物
公开(公告)号：US20060258701A1
公开(公告)日：2006-11-16
申请号：US10545424
申请日：2004-02-13
申请人： Morihiro Mitsuya , Makoto Bamba , Fumio Sakai , Hitomi Watanabe , Yasuhiro Sasaki , Teruyuki Nishimura , Jun-ichi Eiki
发明人： Morihiro Mitsuya , Makoto Bamba , Fumio Sakai , Hitomi Watanabe , Yasuhiro Sasaki , Teruyuki Nishimura , Jun-ichi Eiki
IPC分类号： A61K31/4745 , A61K31/444 , A61K31/4439 , C07D498/02 , C07D417/14
CPC分类号： C07D471/04 , C07D417/14
摘要： The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen atom or the like; R1 represents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; R and R3 are the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II) represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III) represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及具有葡糖激酶活化作用并可用作糖尿病治疗剂的化合物，其由式（I）表示：其中X 1表示氮原子，硫原子，氧原子等; R 1表示6至10元芳基，5至7元杂芳基等; D表示氧原子或硫原子; R和R 3相同或不同，各自表示氢原子，低级烷基等; 式（II）表示任选取代的5〜7元杂芳基等; 式（III）表示单环或双环杂芳基]或其药学上可接受的盐。

4. 发明申请

US20130102605A1 INHIBITORS OF AKT ACTIVITY 审中-公开
标题翻译： AKT活动的抑制剂
公开(公告)号：US20130102605A1
公开(公告)日：2013-04-25
申请号：US13642958
申请日：2011-04-21
申请人： Peng Liang , Morihiro Mitsuya , Yoshio Ogino , Changhe Qi , Hidekazu Takahashi , Paul Tempest , Jiabing Wang , Yuguang Wang , Zhenzhen Wang , Shaohua Zhang , Nanyan Zhou , Jiuxiang Zhu
发明人： Peng Liang , Morihiro Mitsuya , Yoshio Ogino , Changhe Qi , Hidekazu Takahashi , Paul Tempest , Jiabing Wang , Yuguang Wang , Zhenzhen Wang , Shaohua Zhang , Nanyan Zhou , Jiuxiang Zhu
IPC分类号： C07D417/04 , C07D417/14
CPC分类号： C07D417/04 , C07D277/28 , C07D417/14 , C07D487/08
摘要： The instant invention provides for substituted thiazoles that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译：本发明提供抑制Akt活性的取代的噻唑。特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。

5. 发明授权

US08030327B2 Fused imidazole derivative 有权
标题翻译：熔融咪唑衍生物
公开(公告)号：US08030327B2
公开(公告)日：2011-10-04
申请号：US11667282
申请日：2005-11-07
申请人： Yoshiyuki Sato , Hideki Kurihara , Kaori Kamijo , Yu Onozaki , Toshiaki Tsujino , Tetsuya Sugimoto , Akiko Watanabe , Morihiro Mitsuya , Hideya Komatani
发明人： Yoshiyuki Sato , Hideki Kurihara , Kaori Kamijo , Yu Onozaki , Toshiaki Tsujino , Tetsuya Sugimoto , Akiko Watanabe , Morihiro Mitsuya , Hideya Komatani
IPC分类号： A01N43/42 , A01N43/38 , A01N43/06 , A61K31/44 , A61K31/40 , A61K31/38 , C07D513/02 , C07D515/02 , C07D333/02 , C07D333/34 , C07D333/22
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to a compound represented by the Formula [I]: Wherein: the A ring is a 5-membered aromatic heterocyclic group containing at least one hetero atom selected from a nitrogen atom, and the like; A1 and A2, are each a nitrogen atom, and the like; X2, X3, X4, and X5 are all carbon atoms, or alternatively any one of X2, X3, X4, and X5 is a nitrogen atom and the rest are all carbon atoms; R1 is a hydrogen atom, or the like; R2, R3, R4, and R5, are each a hydrogen atom, or the like; R6 and R6′, are each a hydrogen atom, and the like; R7 is an aryl group and the like; and R8 is an amino group or a hydroxy group, or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：本发明涉及由式[I]表示的化合物：其中：A环是含有至少一个选自氮原子的杂原子的5元芳族杂环基等; A1和A2各自为氮原子等; X2，X3，X4和X5都是碳原子，或者X2，X3，X4和X5中的任何一个是氮原子，其余全部是碳原子; R1是氢原子等; R2，R3，R4和R5各自为氢原子等; R6和R6'各自为氢原子等; R7是芳基等; 并且R 8是氨基或羟基，或其药学上可接受的盐或酯。

6. 发明授权

US07718801B2 Substituted imidazole derivative 有权
标题翻译：取代的咪唑衍生物
公开(公告)号：US07718801B2
公开(公告)日：2010-05-18
申请号：US11661486
申请日：2005-08-30
申请人： Mikako Kawamura , Takashi Hashihayata , Satoshi Sunami , Tetsuya Sugimoto , Fuyuki Yamamoto , Yoshiyuki Sato , Kaori Kamijo , Morihiro Mitsuya , Yoshikazu Iwasawa , Hideya Komatani
发明人： Mikako Kawamura , Takashi Hashihayata , Satoshi Sunami , Tetsuya Sugimoto , Fuyuki Yamamoto , Yoshiyuki Sato , Kaori Kamijo , Morihiro Mitsuya , Yoshikazu Iwasawa , Hideya Komatani
IPC分类号： C07D239/00 , C07D239/02
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to a compound represented by Formula [I] or a pharmaceutically acceptable salt or ester thereof: wherein: X1, X2, X3, and X4, which may be identical or different, are each C or N, provided that none to two of X1, X2, X3, and X4 is/are N; Y is CH or N; R1, R1′, R2, R2′, R3, R3′, R4, and R4′, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R5 is a hydrogen atom or a methyl group; R6 and R7, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R8 and R8′, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R9 is an aryl group or a heteroaryl group which may be substituted; and n is an integer from 1 to 3, and a PLK1 inhibitor or an anticancer agent containing the same.
摘要翻译：本发明涉及由式[I]表示的化合物或其药学上可接受的盐或酯：其中：X 1，X 2，X 3和X 4可以相同或不同，各自为C或N，条件是 X1，X2，X3和X4中的两个为N; Y是CH或N; R1，R1'，R2，R2'，R3，R3'，R4和R4'可以相同或不同，分别为氢原子，低级烷基等; R5是氢原子或甲基; R 6和R 7可以相同或不同，分别为氢原子，低级烷基等; R 8和R 8'可以相同或不同，分别为氢原子，低级烷基等; R9是可以被取代的芳基或杂芳基; n为1〜3的整数，PLK1抑制剂或含有该PLK1抑制剂的抗癌剂。

7. 发明授权

US07629362B2 2-pyridine carboxamide derivatives 有权
标题翻译： 2-吡啶甲酰胺衍生物
公开(公告)号：US07629362B2
公开(公告)日：2009-12-08
申请号：US10545424
申请日：2004-02-13
申请人： Morihiro Mitsuya , Makoto Bamba , Fumiko Sakai , Hitomi Watanabe , Yasuhiro Sasaki , Teruyuki Nishimura , Jun-ichi Eiki
发明人： Morihiro Mitsuya , Makoto Bamba , Fumiko Sakai , Hitomi Watanabe , Yasuhiro Sasaki , Teruyuki Nishimura , Jun-ichi Eiki
IPC分类号： A61K31/4436 , C07D417/14 , C07D401/14
CPC分类号： C07D471/04 , C07D417/14
摘要： The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen atom or the like; R1 represents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; R2 and R3 are the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II) represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III) represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及具有葡糖激酶活化作用并可用作糖尿病治疗剂的化合物，其由式（I）表示：[其中X1表示氮原子，硫原子，氧原子等 ; R1表示6-至10-元芳基，5-至7-元杂芳基等; D表示氧原子或硫原子; R2和R3相同或不同，各自表示氢原子，低级烷基等; 式（II）表示任选取代的5〜7元杂芳基等; 式（III）表示单环或双环杂芳基]或其药学上可接受的盐。

8. 发明申请

US20080032996A1 Substituted Quinazoline or Pyridopyrimidine Derivative 失效
标题翻译：取代喹唑啉或吡啶并嘧啶衍生物
公开(公告)号：US20080032996A1
公开(公告)日：2008-02-07
申请号：US10593540
申请日：2005-03-23
申请人： Morihiro Mitsuya , Makoto Bamba , Yasuhiro Sasaki , Teruyuki Nishimura , Jun-ichi Eiki , Keisuke Arakawa
发明人： Morihiro Mitsuya , Makoto Bamba , Yasuhiro Sasaki , Teruyuki Nishimura , Jun-ichi Eiki , Keisuke Arakawa
IPC分类号： A61K31/519 , A61K31/517 , A61K38/28 , A61P3/04 , A61P3/10 , C07D403/12 , C07D413/12 , C07D417/14 , C07D471/04 , C07D513/04
CPC分类号： A61K31/513 , A61K31/517 , A61K31/519 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D513/04
摘要： The present invention provides a compound having a glucokinase activating action being useful for prevention or treatment of diabetes mellitus, etc. being represented by the formula (I): X is nitrogen atom, etc.; Y is oxygen atom, etc.; R1 is an optionally substituted five to six-membered heteroaryl group, etc.; R2 is hydrogen atom or fluorine atom; and ring A is a monocyclic or bicyclic heteroaryl group which may have a substituent represented by the formula (II)] or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有葡糖激酶活化作用的化合物，其可用于预防或治疗由式（I）表示的糖尿病等：X为氮原子等; Y是氧原子等; R 1是任选取代的五至六元杂芳基等; R 2是氢原子或氟原子; 环A是可以具有式（II）表示的取代基的单环或双环杂芳基]或其药学上可接受的盐。

9. 发明授权

US5777150A Substituted amic acid derivatives 失效
标题翻译：取代的酰胺酸衍生物
公开(公告)号：US5777150A
公开(公告)日：1998-07-07
申请号：US696152
申请日：1996-08-13
申请人： Takashi Nomoto , Masahiro Hayashi , Jun Shibata , Yoshikazu Iwasawa , Morihiro Mitsuya , Yoshiaki Iida , Katsumasa Nonoshita , Yasufumi Nagata
发明人： Takashi Nomoto , Masahiro Hayashi , Jun Shibata , Yoshikazu Iwasawa , Morihiro Mitsuya , Yoshiaki Iida , Katsumasa Nonoshita , Yasufumi Nagata
IPC分类号： C07C69/34 , C07C211/27 , C07C211/29 , C07C215/52 , C07C217/60 , C07C233/05 , C07C233/13 , C07C233/18 , C07C235/06 , C07D213/38 , C07D213/40 , C07D215/12 , C07D215/48 , C07D263/32 , C07D307/14 , C07D307/52 , C07D307/81 , C07D317/58 , C07D333/20 , C07D333/28 , C07D333/54 , C07D333/58 , C07C69/78 , C07C69/767 , C07C69/773 , C07D317/34
CPC分类号： C07D213/40 , C07C211/27 , C07C211/29 , C07C215/52 , C07C217/60 , C07C233/05 , C07C233/13 , C07C233/18 , C07C235/06 , C07C69/34 , C07D213/38 , C07D215/12 , C07D215/48 , C07D263/32 , C07D307/14 , C07D307/52 , C07D307/81 , C07D317/58 , C07D333/20 , C07D333/28 , C07D333/54 , C07D333/58
摘要： A compound of the formula (I) or its pharmaceutically acceptable salt or ester: ##STR1## wherein each of ##STR2## which are the same or different, is an aryl group or a heteroaromatic ring group; A is a C.sub.3-8 linear saturated or unsaturated aliphatic hydrocarbon group which may have substituent(s) selected from the group consisting of a lower alkyl group, a hydroxyl group, a lower alkoxy group, a carboxyl group, an aryl group and an aralkyl group; Q is a single bond or a group of the formula --CO--O--, --O--CO--, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --OCH.sub.2 --, --SCH.sub.2 --, --CH.sub.2 O-- or --CH.sub.2 S--; each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 which are the same or different, is a hydrogen atom, a halogen atom, a lower alkyl group, a hydroxyl group, a lower alkoxy group, or an aryl or heteroaromatic ring group which may have substituent(s) selected from the group consisting of a halogen atom, a lower alkyl group and a lower alkoxy group; each of R.sup.5, R.sup.6 and R.sup.7 which are the same or different, is a hydrogen atom or a lower alkyl group; and R.sup.8 is a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group or an aralkyl group, provided that when Q is a single bond, ##STR3## are not simultaneously 4-chlorophenyl groups.
摘要翻译：式（I）化合物或其药学上可接受的盐或酯：其中每个相同或不同的芳基是芳基或杂芳环; A是可以具有选自低级烷基，羟基，低级烷氧基，羧基，芳基和芳烷基的取代基的C3-8直链饱和或不饱和脂族烃基组; Q是单键或式-CO-O-，-O-CO-，-CH 2 CH 2 - ， - CH = CH - ， - OCH 2 - ， - CH 2 - ， - CH 2 O-或-CH 2 S--的基团; R 1，R 2，R 3和R 4相同或不同的是氢原子，卤素原子，低级烷基，羟基，低级烷氧基或可具有取代基的芳基或杂芳族环基选自卤素原子，低级烷基和低级烷氧基的基团; R 5，R 6和R 7各自相同或不同，为氢原子或低级烷基; 并且R8是氢原子，低级烷基，低级烯基，低级炔基或芳烷基，条件是当Q为单键时，＆lt; IMAGE＆gt;不同时为4-氯苯基。

10. 发明授权

US07977336B2 Aminopyrimidine derivatives as PLK1 inhibitors 有权
标题翻译：氨基嘧啶衍生物作为PLK1抑制剂
公开(公告)号：US07977336B2
公开(公告)日：2011-07-12
申请号：US12002546
申请日：2007-12-18
申请人： Takashi Hashihayata , Mikako Kawamura , Morihiro Mitsuya , Yoshiyuki Sato
发明人： Takashi Hashihayata , Mikako Kawamura , Morihiro Mitsuya , Yoshiyuki Sato
IPC分类号： C07D403/04 , A61K31/506
CPC分类号： C07D471/04
摘要： The present invention relates to a compound represented by Formula [I]: or a pharmaceutically acceptable salt or ester thereof, wherein R1 and R2, which may be the same or different, are each a hydrogen atom, a lower alkyl group, a cycloalkyl group, or the like; R3 and R4, which may be the same or different, are each a hydrogen atom, a lower alkyl group, NRaRb, a phenyl group, a lower alkyl group substituted with a phenyl group, a 4-to 7-membered aliphatic heterocyclic group, a lower alkyl group substituted with a 4- to 7-membered aliphatic heterocyclic group, a 5-or 6-membered aromatic heterocyclic group, a lower alkyl group substituted with a 5-or 6-membered aromatic heterocyclic group, or the like; and R5 is a hydrogen atom, a cyano group, a halogen atom, or a lower alkyl group.
摘要翻译：本发明涉及由式[I]表示的化合物或其药学上可接受的盐或酯，其中R 1和R 2可以相同或不同，分别为氢原子，低级烷基，环烷基，等等; R 3和R 4可以相同或不同，分别为氢原子，低级烷基，NR a R b，苯基，被苯基取代的低级烷基，4-至7-元脂族杂环基，被4〜7元脂肪族杂环基取代的低级烷基，5元或6元芳族杂环基，被5元或6元芳族杂环基取代的低级烷基等。 R5为氢原子，氰基，卤素原子或低级烷基。

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