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    Cyclic Amine Compound and Use Thereof for the Prophylaxis or Treatment of Hypertension
    1.
    发明申请
    Cyclic Amine Compound and Use Thereof for the Prophylaxis or Treatment of Hypertension 审中-公开
    环胺化合物及其用途用于预防或治疗高血压

    公开(公告)号：US20100121048A1

    公开(公告)日：2010-05-13

    申请号：US12224046

    申请日：2007-02-15

    申请人： Takanobu Kuroita ,  Yasuhiro Imaeda ,  Naohiro Taya ,  Tsuneo Oda ,  Kouichi Iwanaga ,  Yasutomi Asano

    发明人： Takanobu Kuroita ,  Yasuhiro Imaeda ,  Naohiro Taya ,  Tsuneo Oda ,  Kouichi Iwanaga ,  Yasutomi Asano

    IPC分类号： C07D403/12 ,  C07D417/14 ,  C07D401/14 ,  C07D403/06 ,  C07D413/14 ,  C07D409/06 ,  C07D403/14

    CPC分类号： C07D403/06 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

    摘要： The present invention relates to a compound represented by the formula: (I) wherein ring A is a 5- or 6-membered aromatic heterocycle optionally having substituent (s); U, V and W are each independently C or N, provided that when any one of U, V and W is N, then the others should be C; Ra and Rb are each independently a cyclic group optionally having substituent(s), a C1-10alkyl group optionally having substituent(s), a C2-10 alkenyl group optionally having substituent(s), or a C2-10alkynyl group optionally having substituent(s); X is a bond, or a spacer having 1 to 6 atoms in the main chain; Y is a spacer having 1 to 6 atoms in the main chain; Rc is a hydrocarbon group optionally containing heteroatom(s) as the constituting atom(s), which optionally has substituent(s); m and n are each independently 1 or 2; and ring B optionally further has substituent(s), or a salt thereof. The compound of the present invention has excellent renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension, and the like.

    摘要翻译： 本发明涉及式（I）表示的化合物，其中环A是任选具有取代基的5-或6-元芳族杂环; U，V和W各自独立为C或N，条件是当U，V和W中的任何一个为N时，其他应为C; Ra和Rb各自独立地为任选具有取代基的环状基团，任选具有取代基的C 1-10烷基，任选具有取代基的C 2-10烯基或任选具有取代基的C 2-10炔基， （s）; X是键或在主链中具有1至6个原子的间隔基; Y是主链中具有1至6个原子的间隔基; Rc是任选地含有杂原子作为构成原子的烃基，其任选具有取代基; m和n各自独立地为1或2; 任选地，环B还具有取代基或其盐。 本发明的化合物具有优异的肾素抑制活性，因此可用作预防或治疗高血压，各种高血压器官损害等的药剂。

    Method for producing optically active compound
    9.
    发明授权
    Method for producing optically active compound 失效
    光学活性化合物的制造方法

    公开(公告)号：US07629472B2

    公开(公告)日：2009-12-08

    申请号：US11812052

    申请日：2007-06-14

    申请人： Toru Yamano ,  Naohiro Taya ,  Akio Ojida

    发明人： Toru Yamano ,  Naohiro Taya ,  Akio Ojida

    IPC分类号： C07D233/54 ,  C07D211/80

    CPC分类号： C07D233/64 ,  C07D213/55

    摘要： The present invention provides a method for producing an optically active β-hydroxy ester compound represented by the general formula: wherein R1 represents an optionally substituted hydrocarbon group and the like, R2 represents a nitrogen-containing heterocyclic group different from R1, which is represented by the general formula: wherein the ring may be substituted and the like, R3 represents an optionally substituted hydrocarbon group and the like, R4 and R5 represent, the same or different, a hydrogen atom, a halogen atom and the like, the symbol “*” represents an optically active center, which comprises reacting in the presence of a cinchona alkaloid and the like a compound represented by the general formula: wherein R1 and R2 are as defined above with a compound represented by the general formula: wherein R3, R4 and R5 are as defined above, and X is a halogen atom.

    摘要翻译： 本发明提供一种制备由以下通式表示的光学活性β-羟基酯化合物的方法：其中R 1表示任选取代的烃基等，R 2表示与R 1不同的含氮杂环基，其表示为 通式：其中环可以被取代等，R 3表示任选取代的烃基等，R 4和R 5表示相同或不同的氢原子，卤素原子等，符号“* “表示光学活性中心，其包括在cinchona生物碱等存在下反应，由通式表示的化合物：其中R 1和R 2如上所定义，与通式表示的化合物反应：其中R 3，R 4和 R5如上所定义，X为卤素原子。

    Process for production of optically active compounds
    10.
    发明授权
    Process for production of optically active compounds 失效
    光学活性化合物的制造方法

    公开(公告)号：US07084278B2

    公开(公告)日：2006-08-01

    申请号：US10506309

    申请日：2003-03-05

    申请人： Toru Yamano ,  Naohiro Taya ,  Akio Ojida

    发明人： Toru Yamano ,  Naohiro Taya ,  Akio Ojida

    IPC分类号： C07D213/16 ,  C07D213/28 ,  C07D233/64

    CPC分类号： C07D233/64 ,  C07D213/55

    摘要： The present invention provides a method for producing an optically active β-hydroxy ester compound represented by the general formula: wherein R1 represents an optionally substituted hydrocarbon group and the like, R2 represents a nitrogen-containing heterocyclic group different from R1, which is represented by the general formula: wherein the ring may be substituted and the like, R3 represents an optionally substituted hydrocarbon group and the like, R4 and R5 represent, the same or different, a hydrogen atom, a halogen atom and the like, the symbol “*” represents an optically active center, which comprises reacting in the presence of a cinchona alkaloid and the like a compound represented by the general formula: wherein R1 and R2 are as defined above with a compound represented by the general formula: wherein R3, R4 and R5 are as defined above, and X is a halogen atom.

    摘要翻译： 本发明提供一种制备由以下通式表示的光学活性β-羟基酯化合物的方法：其中R 1表示任选取代的烃基等，R 2 O >表示不同于R 1的含氮杂环基，其由以下通式表示：其中该环可以被取代等，R 3表示任选地 取代烃基等，R 4和R 5表示相同或不同的氢原子，卤素原子等，符号“*”表示 光学活性中心，其包括在cinchona生物碱等存在下反应，由通式表示的化合物：其中R 1和R 2如上定义 与下列通式表示的化合物：其中R 3，R 4和R 5如上所定义，X是卤代基 n原子。