Novel Aminopyridine Derivatives Having Aurora a Selective Inhibitory Action
    5.
    发明申请
    Novel Aminopyridine Derivatives Having Aurora a Selective Inhibitory Action 有权
    具有极光选择性抑制作用的新型氨基吡啶衍生物

    公开(公告)号:US20090192174A1

    公开(公告)日:2009-07-30

    申请号:US12226639

    申请日:2007-04-25

    IPC分类号: A61K31/506 C07D487/04

    CPC分类号: C07D487/08

    摘要: The present invention relates to a compound of general formula I: wherein: n1 and n2 are the same or different, and are 0 or 1; R is aryl, heteroaryl, etc.; Re is hydrogen atom or lower alkyl; two groups selected from four groups consisting of (i) either one of Ra1 and Ra1′, (ii) either one of Ra2 and Ra2′, (iii) either one of Rb1 and Rb1′, and (iv) either one of Rb2 and Rb2′, are combined to form —(CH2)n— where n is 1, 2 or 3; and among Ra1, Ra1′, Ra2, Ra2′, Rb1, Rb1′, Rb2 and Rb2′, the groups which do not form —(CH2)n— are each independently hydrogen atom, etc.; X1, X2, X3 and X4 are each independently CH, N, etc.; Y1, Y2, Y3 and Y4 are the same or different and are CH or N, etc.; W is a 5-membered aromatic heterocyclic group, or a pharmaceutically acceptable salt or ester thereof.

    摘要翻译: 本发明涉及通式I的化合物:其中:n1和n2相同或不同,为0或1; R是芳基,杂芳基等; Re为氢原子或低级烷基; 选自由(i)Ra1和Ra1'中的任一个组成的四组中的两个基团,(ii)Ra2和Ra2'中的任一个,(iii)Rb1和Rb1'中的任一个,以及(iv)Rb2和 Rb2'组合形成 - (CH 2)n - ,其中n为1,2或3; 在Ra1,Ra1',Ra2,Ra2',Rb1,Rb1',Rb2和Rb2'之间,不形成 - (CH2)n-的基团各自独立地为氢原子等; X1,X2,X3和X4各自独立地为CH,N等; Y1,Y2,Y3和Y4相同或不同,为CH或N等; W是5元芳杂环基或其药学上可接受的盐或酯。

    Aminopyridine derivatives having aurora a selective inhibitory action
    6.
    发明授权
    Aminopyridine derivatives having aurora a selective inhibitory action 有权
    具有极光选择性抑制作用的氨基吡啶衍生物

    公开(公告)号:US08101621B2

    公开(公告)日:2012-01-24

    申请号:US12226639

    申请日:2007-04-25

    CPC分类号: C07D487/08

    摘要: The present invention relates to a compound of general formula I: wherein: n1 and n2 are the same or different, and are 0 or 1; R is aryl, heteroaryl, etc.; Re is hydrogen atom or lower alkyl; two groups selected from four groups consisting of (i) either one of Ra1 and Ra1′, (ii) either one of Ra2 and Ra2′, (iii) either one of Rb1 and Rb1′, and (iv) either one of Rb2 and Rb2′, are combined to form —(CH2)n— where n is 1, 2 or 3; and among Ra1, Ra1′, Ra2, Ra2′, Rb1, Rb1′, Rb2 and Rb2′, the groups which do not form —(CH2)n— are each independently hydrogen atom, etc.; X1, X2, X3 and X4 are each independently CH, N, etc.; Y1, Y2, Y3 and Y4 are the same or different and are CH or N, etc.; W is a 5-membered aromatic heterocyclic group, or a pharmaceutically acceptable salt or ester thereof.

    摘要翻译: 本发明涉及通式I的化合物:其中:n1和n2相同或不同,为0或1; R是芳基,杂芳基等; Re为氢原子或低级烷基; 选自由(i)Ra1和Ra1'中的任一个组成的四组中的两个基团,(ii)Ra2和Ra2'中的任一个,(iii)Rb1和Rb1'中的任一个,以及(iv)Rb2和 Rb2'组合形成 - (CH 2)n - ,其中n为1,2或3; 在Ra1,Ra1',Ra2,Ra2',Rb1,Rb1',Rb2和Rb2'之间,不形成 - (CH2)n-的基团各自独立地为氢原子等; X1,X2,X3和X4各自独立地为CH,N等; Y1,Y2,Y3和Y4相同或不同,为CH或N等; W是5元芳杂环基或其药学上可接受的盐或酯。

    Spiro compounds
    10.
    发明授权
    Spiro compounds 失效
    螺环化合物

    公开(公告)号:US07205417B2

    公开(公告)日:2007-04-17

    申请号:US10485955

    申请日:2002-08-02

    摘要: Compounds of the formula (I): (wherein A is an optionally substituted straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally intervened by oxygen or nitrogen atom; Ar1 is aryl or heteroaryl, any of which is optionally substituted; n is 0 or 1; R0 is hydrogen, or lower alkylene attached to an arbitrary, bondable position of A; T, U, V and W are independently nitrogen atom or optionally substituted methine, and at least two of T, U, V and W are said methine group; X is —N(SO2R1)—, —N(COR2)— or —CO—; Y is —C(R3)(R4)—, —O— or —N(R5)—; Z is methine or nitrogen atom) exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as hypertension, nephropathy, heart disease, vasospasm, arteriosclerosis, etc., central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia, etc., sexual and reproductive dysfunctions, and gastro-intestinal motility disorder.

    摘要翻译: 式(I)的化合物: