5-QUINOLINONE DERIVATIVES AS 5HT1A RECEPTOR MODULATORS FOR TREATING SEXUAL DYSFUNCTION, COGNITION IMPAIRMENT, PSYCHOTIC DISORDERS, ANXIETY, DEPRESSION, ETC.
    9.
    发明申请
    5-QUINOLINONE DERIVATIVES AS 5HT1A RECEPTOR MODULATORS FOR TREATING SEXUAL DYSFUNCTION, COGNITION IMPAIRMENT, PSYCHOTIC DISORDERS, ANXIETY, DEPRESSION, ETC. 审中-公开
    5-Quinolinone衍生物作为5HT1A受体调节剂,用于治疗性功能障碍,认知障碍,心理障碍,异常,呕吐等。

    公开(公告)号:US20100004452A1

    公开(公告)日:2010-01-07

    申请号:US12442148

    申请日:2007-09-24

    IPC分类号: C07D401/14

    摘要: Disclosed are compounds of formula (I) wherein R1 is C1-6alkyl, halo or haloC1-6alkyl; R2 is hydrogen or C1-6alkyl; is a single or double bond; each R3 and R4, which may be the same or different, are hydrogen, C1-6alkyl or haloC1-6alkyl; wherein i) when is a double bond p and q are 1, and ii) when is a single bond, p and q are 2, and one of R3 and one of R4, together with their interconnecting atoms, forms a cyclopropane ring which may be substituted by one or two halo or methyl groups, which groups may be the same or different; X is CH or N; when present each R5, which may be the same or different, is C1-6alkyl or halo; or two R5 groups may join to form a bridge, which bridge contains one or two atoms; n is 0, 1, 2 or 3; when present each R6 which may be the same or different, is C1-6alkyl or halo; and m is 0, 1, 2 or 3.

    摘要翻译: 公开了式(I)的化合物,其中R 1是C 1-6烷基,卤素或卤代C 1-6烷基; R2是氢或C1-6烷基; “img id =”CUSTOM-CHARACTER-00001“he =”2.79mm“wi =”6.35mm“file =”US20100004452A1-20100107-P00001.TIF“img-content =”character“img-format =”tif“/> 是单键或双键; 每个R 3和R 4可以相同或不同,是氢,C 1-6烷基或卤代C 1-6烷基; 其中i)当是双键p,q是1,ii)当是单键,p和q是2,R 3和R 4中的一个连同它们的互连原子一起形成环丙烷环, 被一个或两个卤素或甲基取代,这些基团可以相同或不同; X是CH或N; 当存在时,每个可以相同或不同的R 5是C 1-6烷基或卤素; 或两个R5基团可以连接形成桥,该桥包含一个或两个原子; n为0,1,2或3; 当存在每个可以相同或不同的R 6是C 1-6烷基或卤素时; m为0,1,2或3。

    Compounds
    10.
    发明授权
    Compounds 失效
    化合物

    公开(公告)号:US06548504B1

    公开(公告)日:2003-04-15

    申请号:US09600558

    申请日:2000-07-19

    IPC分类号: A61K31495

    CPC分类号: C07D295/096

    摘要: The present invention therefore provides, in a first aspect, a compound of formula (I) or a salt thereof: in which the group D is selected from a group of formula (A), (B) or (C) below: in which P is a monocyclic, bicyclic or tricyclic alicyclic ring containing up to 20 carbon atoms in the ring(s); A is a single bond, a C1-6alkylene or a C2-6alkenylene group; R1 is halogen, C1-6alkyl optionally substituted by one or more fluorine atoms, C3-6cycloalkyl, C1-6alkoxy, OCF3, hydroxy, hydroxyC1-6alkyl, hydroxyC1-6alkoxy, C1-6alkoxyC1-6alkoxy, C1-6alkanoyl, amino, alkylamino or dialkylamino, SR11 where R11 is hydrogen or C1-6alkyl or R1 is aryl, arylC1-6alkyl, a bicyclic heterocyclic ring or is a 5 to 7-membered heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulfur; n is 0, 1, 2 or 3; and R2 is hydrogen, C1-6alkyl, aryl, arylC1-6alkyl or C3-6cycloalkyl; or in which Ra is an alkyl group containing 1 to 20 carbon atoms or is an arylC1-6alkyl group, and Rb is hydrogen or C1-6alkyl;

    摘要翻译: 因此,本发明在第一方面提供式(I)化合物或其盐:其中基团D选自下式(A),(B)或(C)中的基团:其中P 是环中含有至多20个碳原子的单环,双环或三环脂环; A是单键,C 1-6亚烷基或C 2-6亚烯基; R 1是卤素,任选地被一个 或更多个氟原子,C 3-6环烷基,C 1-6烷氧基,OCF 3,羟基,羟基C 1-6烷基,羟基C 1-6烷氧基,C 1-6烷氧基C 1-6烷氧基,C 1-6烷酰基,氨基,烷基氨基或二烷基氨基,SR 11,其中R 11是氢或C 1-6烷基 或R 1为芳基,芳基C 1-6烷基,双环杂环或为各自含有1至4个选自氧,氮或硫的杂原子的5至7元杂环; n为0,1,2或3; 和R 2是氢,C 1-6烷基,芳基,芳基C 1-6烷基或C 3-6环烷基; 其中R a是含有1至20个碳原子的烷基或芳基C 1-6烷基,R b是氢或C 1-6烷基;