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    2-(cyclic amino)-pyrimidone derivatives
    1.
    发明授权
    2-(cyclic amino)-pyrimidone derivatives 失效
    2-（环状氨基） - 嘧啶酮衍生物

    公开(公告)号：US08569294B2

    公开(公告)日：2013-10-29

    申请号：US12282396

    申请日：2007-03-14

    申请人： Kenji Fukunaga ,  Toshiyuki Kohara ,  Kazutoshi Watanabe ,  Yoshihiro Usui ,  Fumiaki Uehara ,  Satoshi Yokoshima ,  Daiki Sakai ,  Shin-ichi Kusaka ,  Kazuki Nakayama

    发明人： Kenji Fukunaga ,  Toshiyuki Kohara ,  Kazutoshi Watanabe ,  Yoshihiro Usui ,  Fumiaki Uehara ,  Satoshi Yokoshima ,  Daiki Sakai ,  Shin-ichi Kusaka ,  Kazuki Nakayama

    IPC分类号： A61K31/535

    CPC分类号： C07D413/14 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D409/14 ,  C07D453/06 ,  C07D493/04

    摘要： A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R2 represents a hydrogen or the like; R3 represents methyl group or the like; R20 represents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; R4 represents hydrogen or the like; R5 represents hydrogen or the like; R6 represents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH2, oxygen atom, NH, or the like; any one or more of R5 and R6, R5 and R4, R6 and R4, X and R5, X and R4, X and R6, and R6 and R6 may combine to each other to form a ring, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).

    摘要翻译： 由式（I）表示的化合物或其光学活性异构体或其药学上可接受的盐：其中R2表示氢等; R3表示甲基等; R 20表示卤素原子等; q表示0〜3的整数， Z表示氮原子，CH等; R4表示氢等; R5表示氢等; R6表示取代的烷氧基等; p表示0〜3的整数， X表示键，CH2，氧原子，NH等; R 5和R 6，R 5和R 4，R 6和R 4，X和R 5，X和R 4，X和R 6以及R 6和R 6中的任何一个或多个可以彼此结合形成环，其用于预防和/ 或治疗由tau蛋白激酶1多动症如神经变性疾病（例如阿尔茨海默病）引起的疾病。

    Pyrimidone compounds
    4.
    发明授权
    Pyrimidone compounds 有权
    嘧啶酮化合物

    公开(公告)号：US08940738B2

    公开(公告)日：2015-01-27

    申请号：US13389504

    申请日：2010-08-11

    申请人： Daiki Sakai ,  Kazuki Nakayama ,  Kazutoshi Watanabe

    发明人： Daiki Sakai ,  Kazuki Nakayama ,  Kazutoshi Watanabe

    IPC分类号： A61K31/5377 ,  A61P25/28 ,  A61P9/10 ,  C07D413/04 ,  C07D401/04 ,  C07D413/14

    CPC分类号： C07D413/04 ,  C07D401/04 ,  C07D413/14

    摘要： A pyrimidone derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof: wherein X represents hydrogen atom and Y represents hydroxyl group, or X represents fluorine atom and Y represents hydrogen atom; R1 represents a C1-6 alkyl group; R2 represents a morpholin-4-yl group which may be substituted, or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).

    摘要翻译： 由通式（I）表示的嘧啶酮衍生物或其药学上可接受的盐：其中X表示氢原子，Y表示羟基，或X表示氟原子，Y表示氢原子; R1表示C1-6烷基; R2表示可被取代的吗啉-4-基，其用于预防和/或治疗由tau蛋白激酶1多动症如神经变性疾病（例如阿尔茨海默病）引起的疾病。

    INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF
    5.
    发明申请
    INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF 审中-公开
    用于合成药物代理的中间体化合物及其生产方法

    公开(公告)号：US20120059165A1

    公开(公告)日：2012-03-08

    申请号：US13255748

    申请日：2010-03-09

    申请人： Rikizou Furuya ,  Hiroki Ozawa ,  Eiji Toyofuku ,  Shinichi Kusaka ,  Hiroshi Iwamura ,  Daiki Sakai ,  Kazuki Nakayama ,  Kazutoshi Watanabe

    发明人： Rikizou Furuya ,  Hiroki Ozawa ,  Eiji Toyofuku ,  Shinichi Kusaka ,  Hiroshi Iwamura ,  Daiki Sakai ,  Kazuki Nakayama ,  Kazutoshi Watanabe

    IPC分类号： C07D413/10 ,  C07D413/14

    CPC分类号： C07D413/10 ,  C07D413/14

    摘要： A production method of an optically active 2-{4-(5-substituted-oxadiazolyl) phenyl}morpholine which is useful as an intermediate for synthesizing a pharmaceutical agent is provided and the method comprises the following steps 1) to 4): 1) reacting a bromophenylmorpholine with a hexacyanoferrate(II) or a hydrate thereof at a temperature of from 110° C. to 140° C. in a reaction mixture comprising a Na2CO3, an organophosphorus compound, and a palladium catalyst in a polar aprotic solvent alone or combination of a polar aprotic solvent and other polar aprotic solvent or hydrocarbon solvent to give a cyanophenylmorpholine; 2) reacting the cyanophenylmorpholine with hydroxylamine or hydroxylamine hydrochloride at a temperature of from 10° C. to 40° C. in an aprotic polar solvent to give a hydroxylamine derivative; 3) reacting the hydroxylamine derivative with an acylation reagent selected from the group consisting of aliphatic acyl halides, aromatic acyl halides, aliphatic acyl anhydrides and aromatic anhydrides; and 4) keeping the mixture obtained after step 3) at a temperature of from 60° C. to 140° C. to give a 2-{4-(5-substituted-oxadiazolyl) phenyl}morpholine.

    摘要翻译： 提供了可用作合成药剂的中间体的光学活性2- {4-（5-取代 - 恶二唑基）苯基}吗啉的制备方法，该方法包括以下步骤1）至4）：1） 在包含Na 2 CO 3，有机磷化合物和钯催化剂的反应混合物中，在单极极性非质子溶剂中使溴苯基吗啉与​​六氰基铁酸盐（II）或其水合物在110℃至140℃的温度下反应，或 极性非质子溶剂和其他极性非质子溶剂或烃溶剂的组合，得到氰基苯基吗啉; 2）使氰基苯基吗啉与​​羟胺或羟胺盐酸盐在非质子极性溶剂中在10℃至40℃的温度下反应，得到羟胺衍生物; 3）使羟胺衍生物与选自脂族酰基卤，芳族酰基卤，脂族酰基酸酐和芳族酸酐的酰化试剂反应; 和4）将步骤3）后获得的混合物保持在60℃至140℃的温度下，得到2- {4-（5-取代 - 恶二唑基）苯基}吗啉。

    3-[1,4]oxazepane-4-pyrimidone derivatives
    7.
    发明授权
    3-[1,4]oxazepane-4-pyrimidone derivatives 有权
    3- [1,4]氧氮杂环庚烷-4-嘧啶酮衍生物

    公开(公告)号：US09108957B2

    公开(公告)日：2015-08-18

    申请号：US13262396

    申请日：2010-04-01

    申请人： Kazutoshi Watanabe ,  Kazuki Nakayama ,  Daiki Sakai

    发明人： Kazutoshi Watanabe ,  Kazuki Nakayama ,  Daiki Sakai

    IPC分类号： A61K31/553 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14

    CPC分类号： C07D413/14 ,  C07D401/14 ,  C07D403/14

    摘要： A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom, C—F or the like; R1 represents a C1-C3 alkyl group; Y represents oxygen atom or N—R7; R2, R3, R4, R5, R6 and R7 each independently represents hydrogen atom, a C1-C6 alkyl group, or a group represented by the formula (II): which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).

    摘要翻译： 由式（I）表示的化合物或其药学上可接受的盐：其中Z表示氮原子，C-F等; R1表示C1-C3烷基; Y表示氧原子或N-R7; R2，R3，R4，R5，R6和R7各自独立地表示氢原子，C1-C6烷基或由式（II）表示的基团：其用于预防和/或治疗由 tau蛋白激酶1多动症如神经变性疾病（如阿兹海默症）。

    3-[1,4]OXAZEPANE-4-PYRIMIDONE DERIVATIVES
    10.
    发明申请
    3-[1,4]OXAZEPANE-4-PYRIMIDONE DERIVATIVES 有权
    3- [1,4]氧杂环丁烷-4-吡啶酮衍生物

    公开(公告)号：US20120095216A1

    公开(公告)日：2012-04-19

    申请号：US13262396

    申请日：2010-04-01

    申请人： Kazutoshi Watanabe ,  Kazuki Nakayama ,  Daiki Sakai

    发明人： Kazutoshi Watanabe ,  Kazuki Nakayama ,  Daiki Sakai

    IPC分类号： C07D413/14

    CPC分类号： C07D413/14 ,  C07D401/14 ,  C07D403/14

    摘要： A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom, C—F or the like; R1 represents a C1-C3 alkyl group; Y represents oxygen atom or N—R7; R2, R3, R4, R5, R6 and R7 each independently represents hydrogen atom, a C1-C6 alkyl group, or a group represented by the formula (II): which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).

    摘要翻译： 由式（I）表示的化合物或其药学上可接受的盐：其中Z表示氮原子，C-F等; R1表示C1-C3烷基; Y表示氧原子或N-R7; R2，R3，R4，R5，R6和R7各自独立地表示氢原子，C1-C6烷基或由式（II）表示的基团：其用于预防和/或治疗由 tau蛋白激酶1多动症如神经变性疾病（如阿兹海默症）。