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    Novel aminopyrimidine derivatives as PLK1 inhibitors
    1.
    发明申请
    Novel aminopyrimidine derivatives as PLK1 inhibitors 有权
    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。

    Substituted imidazole derivative
    3.
    发明授权
    Substituted imidazole derivative 有权
    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。

    Aminopyrimidine derivatives as PLK1 inhibitors
    4.
    发明授权
    Aminopyrimidine derivatives as PLK1 inhibitors 有权
    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。

    Novel 2-pyridinecarboxamide derivatives
    7.
    发明申请
    Novel 2-pyridinecarboxamide derivatives 有权
    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。

    Substituted piperidine derivatives as muscarinic M.sub.3 receptor antagonists
    10.
    发明授权
    Substituted piperidine derivatives as muscarinic M.sub.3 receptor antagonists 失效
    取代的哌啶衍生物作为毒蕈碱M3受体拮抗剂

    公开(公告)号：US6130232A

    公开(公告)日：2000-10-10

    申请号：US51287

    申请日：1998-04-09

    申请人： Toshiaki Mase ,  Morihiro Mitsuya ,  Kensuke Kobayashi ,  Kazuhito Noguchi

    发明人： Toshiaki Mase ,  Morihiro Mitsuya ,  Kensuke Kobayashi ,  Kazuhito Noguchi

    IPC分类号： C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  A61K31/445

    CPC分类号： C07D401/06 ,  C07D405/06 ,  C07D409/06

    摘要： This invention provides substituted heteroaromatic ring derivatives which are represented by a general formula [I] below: ##STR1## [in the formula, R.sup.1 and R.sup.2 may be same or different and each signifies hydrogen, halogen or lower alkyl; R.sup.3 signifies C.sub.3 -C.sub.6 cycloalkyl or cycloalkenyl; R.sup.4 signifies a heteroaromatic ring group which may be condensed with a benzene ring and which has 1 or 2 hetero atoms selected from a group consisting of nitrogen, oxygen and sulfur atoms (said heteroaromatic ring group being optionally substituted with lower alkyl, halogen, lower alkoxy, amino or hydroxymethyl); and X stands for O or NH]or their pharmaceutically acceptable salts.The substituted heteroaromatic ring derivatives of the present invention have selective M.sub.3 muscarinic receptor antagonist activity, and hence they are useful as therapeutic or prophylactic agents which are safe and efficacious with little side effects, of respiratory diseases such as asthma, chronic airway obstruction and pulmonary fibrosis, etc.; urinary diseases which induce such urination disorders as pollakiurea, urgency and urinary incontinence, etc.; and gastrointestinal diseases such as irritable bowel syndrome, spasm of gastrointestinal tract and gastrointestinal hyperkinesis.

    摘要翻译： PCT No.PCT / JP96 / 02904 Sec。 371日期：1998年4月9日 102（e）1998年4月9日PCT 1996年10月7日PCT公布。 公开号WO97 / 13766 日期：1997年04月17日本发明提供由以下通式[I]表示的取代杂芳环衍生物：[式中，R 1和R 2可以相同或不同，表示氢，卤素或低级烷基; R3表示C3-C6环烷基或环烯基; R4表示可以与苯环稠合并且具有1或2个选自氮，氧和硫原子的杂原子的杂芳族环基（所述杂芳环基团任选被低级烷基，卤素，低级烷氧基 ，氨基或羟甲基）; 和X代表O或NH]或其药学上可接受的盐。 本发明的取代杂芳环衍生物具有选择性的M3毒蕈碱受体拮抗剂活性，因此它们可用作安全有效的副作用少，呼吸系统疾病如哮喘，慢性气道阻塞和肺纤维化的治疗或预防剂 等等 引起排尿障碍的尿路疾病如呼吸窘迫综合征，紧急性尿失禁等; 胃肠道疾病如肠易激综合征，胃肠道痉挛和胃肠蠕动过多。