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    Substituted pyrimidines and [1,2, 4] triazoles and the use thereof for treating prophylaxis, cardiovascular diseases, metabolic diseases and/or central nervous system diseases
    1.
    发明授权
    Substituted pyrimidines and [1,2, 4] triazoles and the use thereof for treating prophylaxis, cardiovascular diseases, metabolic diseases and/or central nervous system diseases 失效
    取代的嘧啶和[1,2,4]三唑及其用于治疗预防，心血管疾病，代谢疾病和/或中枢神经系统疾病的用途

    公开(公告)号：US07998968B2

    公开(公告)日：2011-08-16

    申请号：US12625622

    申请日：2009-11-25

    申请人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa ,  Koji Fuji

    发明人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa ,  Koji Fuji

    IPC分类号： A61K31/505

    CPC分类号： C07D413/10 ,  C07D413/14 ,  C07D417/14

    摘要： A compound represented by the formula (I): wherein R1 is an oxo group, ═N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: R3 and R4 are each H, or C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkylamino, di(C1-C6)alkylamino or C1-C6 alkylthio, each of which is optionally substituted; and R5 is H, or C1-C6 alkyl, C2-C6 alkenyl, cyclic group, each of which is optionally substituted, —CO—R8 or —O—R8′, or a salt thereof. For example, the compound may be substituted pyrimidines and pharmaceutical compositions of the formula (I) where X=—CR3; X1=—CR2 or —NR2; and X2=—CR5 or —NR5. The compound of the present invention is useful as a drug for the prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases.

    摘要翻译： 由式（I）表示的化合物：其中R 1是氧代基，或= N-R等; 由下式表示的基团是由下式表示的基团：R 2是由下式表示的基团：R 3和R 4各自为H或C 1 -C 6烷基，C 3 -C 6环烷基，C 1 -C 6烷氧基，C 1 -C 6 烷基氨基，二（C 1 -C 6）烷基氨基或C 1 -C 6烷硫基，其各自任选被取代; 和R 5为H或C 1 -C 6烷基，C 2 -C 6烯基，环状基团，各自为任选取代的-CO-R 8或-O-R 8'或其盐。 例如，化合物可以是取代的嘧啶和式（I）的药物组合物，其中X = -CR 3; X1 = -CR2或-NR2; X2 = -CR5或-NR5。 本发明的化合物可用作预防或治疗心血管疾病，代谢疾病和/或中枢神经系统疾病的药物。

    HETEROMONOCYCLIC COMPOUND AND USE THEREOF
    2.
    发明申请
    HETEROMONOCYCLIC COMPOUND AND USE THEREOF 失效
    异环化合物及其用途

    公开(公告)号：US20100105709A1

    公开(公告)日：2010-04-29

    申请号：US12625622

    申请日：2009-11-25

    申请人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa ,  Koji Fuji

    发明人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa ,  Koji Fuji

    IPC分类号： A61K31/506 ,  C07D413/10 ,  C07D413/14 ,  A61P25/00 ,  A61P9/00 ,  A61P3/00

    CPC分类号： C07D413/10 ,  C07D413/14 ,  C07D417/14

    摘要： A compound represented by the formula (I): wherein R1 is an oxo group, ═N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: R3 and R4 are each H, or C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkylamino, di(C1-C6)alkylamino or C1-C6 alkylthio, each of which is optionally substituted; and R5 is H, or C1-C6 alkyl, C2-C6 alkenyl, cyclic group, each of which is optionally substituted, —CO—R8 or —O—R8′, or a salt thereof. The compound of the present invention is useful as a drug for the prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases.

    摘要翻译： 由式（I）表示的化合物：其中R 1是氧代基，或= N-R等; 由下式表示的基团是由下式表示的基团：R 2是由下式表示的基团：R 3和R 4各自为H或C 1 -C 6烷基，C 3 -C 6环烷基，C 1 -C 6烷氧基，C 1 -C 6 烷基氨基，二（C 1 -C 6）烷基氨基或C 1 -C 6烷硫基，其各自任选被取代; 和R 5为H或C 1 -C 6烷基，C 2 -C 6烯基，环状基团，各自为任选取代的-CO-R 8或-O-R 8'或其盐。 本发明的化合物可用作预防或治疗心血管疾病，代谢疾病和/或中枢神经系统疾病的药物。

    HETEROMONOCYCLIC COMPOUND AND USE THEREOF
    3.
    发明申请
    HETEROMONOCYCLIC COMPOUND AND USE THEREOF 审中-公开
    异环化合物及其用途

    公开(公告)号：US20080207654A1

    公开(公告)日：2008-08-28

    申请号：US11943910

    申请日：2007-11-21

    申请人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa

    发明人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa

    IPC分类号： A61K31/506 ,  C07D239/22 ,  A61P3/10 ,  A61P3/04

    CPC分类号： C07D413/14 ,  C07D413/10 ,  C07D417/14

    摘要： A compound represented by the formula (I): wherein R1 is an oxo group, ═N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: R3 and R4 are each H, or C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkylamino, di(C1-C6)alkylamino or C1-C6 alkylthio, each of which is optionally substituted; and R5 is H, or C1-C6 alkyl, C2-C6 alkenyl, cyclic group, each of which is optionally substituted, —CO—R8 or —O—R8′, or a salt thereof. The compound of the present invention is useful as a drug for the prophylaxis or treatment of circulatory diseases, metabolic diseases and/or central nervous system diseases.

    摘要翻译： 由式（I）表示的化合物：其中R1是氧代基，-N-R等; 由下式表示的基团是由下式表示的基团：R 2是由下式表示的基团：R 3和R 4各自为H或C 1 -C 6烷基，C 3 -C 6环烷基，C 1 -C 6烷氧基，C 1 -C 6 烷基氨基，二（C 1 -C 6）烷基氨基或C 1 -C 6烷硫基，其各自任选被取代; 和R 5为H或C 1 -C 6烷基，C 2 -C 6烯基，环状基团，各自为任选取代的-CO-R 8或-O-R 8'或其盐。 本发明的化合物可用作预防或治疗循环系统疾病，代谢疾病和/或中枢神经系统疾病的药物。

    HETEROMONOCYCLIC COMPOUND AND USE THEREOF
    6.
    发明申请
    HETEROMONOCYCLIC COMPOUND AND USE THEREOF 失效
    异环化合物及其用途

    公开(公告)号：US20090176812A1

    公开(公告)日：2009-07-09

    申请号：US12114048

    申请日：2008-05-02

    申请人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa ,  Koji Fuji

    发明人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa ,  Koji Fuji

    IPC分类号： A61K31/505 ,  C07D239/54 ,  C07D413/08 ,  A61P9/10

    CPC分类号： C07D413/10 ,  C07D413/14 ,  C07D417/14

    摘要： A compound represented by the formula (I): wherein R1 is an oxo group, ═N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: R3 and R4 are each H, or C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkylamino, di(C1-C6)alkylamino or C1-C6 alkylthio, each of which is optionally substituted; and R5 is H, or C1-C6 alkyl, C2-C6 alkenyl, cyclic group, each of which is optionally substituted, —CO—R8 or —O—R8′, or a salt thereof. The compound of the present invention is useful as a drug for the prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases.

    摘要翻译： 由式（I）表示的化合物：其中R1是氧代基，-N-R等; 由下式表示的基团是由下式表示的基团：R 2是由下式表示的基团：R 3和R 4各自为H或C 1 -C 6烷基，C 3 -C 6环烷基，C 1 -C 6烷氧基，C 1 -C 6 烷基氨基，二（C 1 -C 6）烷基氨基或C 1 -C 6烷硫基，其各自任选被取代; 和R 5为H或C 1 -C 6烷基，C 2 -C 6烯基，环状基团，各自为任选取代的-CO-R 8或-O-R 8'或其盐。 本发明的化合物可用作预防或治疗心血管疾病，代谢疾病和/或中枢神经系统疾病的药物。

    HETEROMONOCYCLIC COMPOUND AND USE THEREOF
    7.
    发明申请
    HETEROMONOCYCLIC COMPOUND AND USE THEREOF 失效
    异环化合物及其用途

    公开(公告)号：US20110112120A9

    公开(公告)日：2011-05-12

    申请号：US12625622

    申请日：2009-11-25

    申请人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa ,  Koji Fuji

    发明人： Takanobu Kuroita ,  Hiroki Sakamoto ,  Hideyuki Igawa ,  Minoru Sasaki ,  Kouhei Asano ,  Tsuyoshi Maekawa ,  Koji Fuji

    IPC分类号： A61K31/506 ,  C07D413/10 ,  C07D413/14 ,  A61P25/00 ,  A61P9/00 ,  A61P3/00

    CPC分类号： C07D413/10 ,  C07D413/14 ,  C07D417/14

    摘要： A compound represented by the formula (I): wherein R1 is an oxo group, ═N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: R3 and R4 are each H, or C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkylamino, di(C1-C6)alkylamino or C1-C6 alkylthio, each of which is optionally substituted; and R5 is H, or C1-C6 alkyl, C2-C6 alkenyl, cyclic group, each of which is optionally substituted, —CO—R8 or —O—R8′, or a salt thereof. The compound of the present invention is useful as a drug for the prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases.

    摘要翻译： 由式（I）表示的化合物：其中R 1是氧代基，或= N-R等; 由下式表示的基团是由下式表示的基团：R 2是由下式表示的基团：R 3和R 4各自为H或C 1 -C 6烷基，C 3 -C 6环烷基，C 1 -C 6烷氧基，C 1 -C 6 烷基氨基，二（C 1 -C 6）烷基氨基或C 1 -C 6烷硫基，其各自任选被取代; 和R 5为H或C 1 -C 6烷基，C 2 -C 6烯基，环状基团，各自为任选取代的-CO-R 8或-O-R 8'或其盐。 本发明的化合物可用作预防或治疗心血管疾病，代谢疾病和/或中枢神经系统疾病的药物。

    HETEROCYCLIC COMPOUND AND USE THEREOF
    10.
    发明申请
    HETEROCYCLIC COMPOUND AND USE THEREOF 失效
    杂环化合物及其用途

    公开(公告)号：US20100137281A1

    公开(公告)日：2010-06-03

    申请号：US12451602

    申请日：2008-05-20

    申请人： Takanobu Kuroita ,  Hideyuki Igawa ,  Hiroki Sakamoto ,  Kouhei Asano ,  Minoru Sasaki

    发明人： Takanobu Kuroita ,  Hideyuki Igawa ,  Hiroki Sakamoto ,  Kouhei Asano ,  Minoru Sasaki

    IPC分类号： A61K31/519 ,  C07D495/04 ,  A61K31/5377 ,  A61K31/551 ,  A61P9/00

    CPC分类号： C07D413/10 ,  C07D495/04 ,  C07D495/14 ,  C07D513/04

    摘要： The present invention aims to provide a compound having superior pharmacological action, physicochemical properties and the like, which is useful for the prophylaxis or treatment s of circulatory diseases such as hypertension, cardiac diseases, arteriosclerosis, renal diseases, cerebral apoplexy and the like and/or metabolic diseases such as hyperlipidemia, obesity, diabetes and the like, central nervous disorders such as cerebral infarction and the like, mental diseases such as dementia, depression and the like, and the like.A compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

    摘要翻译： 本发明的目的在于提供具有优异的药理作用，理化特性等的化合物，其可用于预防或治疗诸如高血压，心脏病，动脉硬化，肾脏疾病，脑中风等的循环系统疾病和/ 或代谢性疾病如高脂血症，肥胖症，糖尿病等，中枢神经障碍如脑梗塞等，精神疾病如痴呆，抑郁症等。 由式（I）表示的化合物或其盐，其中每个符号如说明书中所定义。