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    2-PHENYL OR 2-HETARYL IMIDAZOL[1,2-a]PYRIDINE DERIVATIVES
    5.
    发明申请
    2-PHENYL OR 2-HETARYL IMIDAZOL[1,2-a]PYRIDINE DERIVATIVES 审中-公开

    公开(公告)号：US20160244441A1

    公开(公告)日：2016-08-25

    申请号：US14925574

    申请日：2015-10-28

    申请人： Hoffmann-La Roche Inc.

    发明人： Edilio Borroni ,  Luca Gobbi ,  Michael Honer ,  Henner Knust ,  Matthias Koerner ,  Dieter Muri

    IPC分类号： C07D471/04 ,  A61K49/00

    CPC分类号： C07D471/04 ,  A61K49/0002

    摘要： The invention relates to compounds of formulas I and II wherein R1 is hydrogen, lower alkyl, lower alkoxy, halogen, S-lower alkyl, lower alkoxy substituted by halogen, di-lower alkyl amino, C(O)O-lower alkyl, lower alkyl substituted by hydroxy or hydroxy; R2 is hydrogen, lower alkyl, halogen, lower alkoxy, S-lower alkyl, lower alkoxy substituted by halogen, O(CH2)2-lower alkoxy substituted by halogen, di-lower alkyl amino, alkyl amino, NH-lower alkyl substituted by halogen, N(lower alkyl)-benzyl, lower alkyl substituted by hydroxy, heterocycloalkyl optionally substituted by halogen, CH2-lower alkoxy, CH2-lower alkoxy substituted by halogen or hydroxy; or R1 and R2 form together with the carbon atoms to which they are attached a ring containing —OCH2CH2O—, OCH2O—, OCH2CH2CH2O— or —NHC(O)CH2O—; R3 is hydrogen or lower alkoxy; R4 is hydrogen or lower alkyl; R5 is lower alkyl, cycloalkyl, lower alkyl substituted by hydroxy or lower alkyl substituted by halogen; or R4 and R5 form together with the nitrogen atom to which they are attached a ring containing —CH2CH2CHRCH2CH2—, —CH2CHRCH2CH2—, —CH2CH2OCH2CH2—CH2CH2NR′CH2CH2—, CH2CHR— or —CH2CH2CH2—; wherein R is hydrogen, halogen, lower alkyl, lower alkoxy or lower alkyl substituted by halogen; R′ is lower alkyl substituted by halogen; Ra is hydrogen or 3H; Rb is hydrogen, hydroxy or 3H; R6 is hydrogen, halogen or lower alkyl; HetAr is selected from the group consisting of thiophenyl, furanyl, thiozolyl, benzofuranyl, pyrazolyl, benzoimidazolyl or pyridinyl; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The present compounds are suitable as imaging tool, which will improve diagnosis by identifying potential patients with excess of tau aggregates in the brain, which may be likely to develop Alzheimer's disease.

    Dual Modulators of 5HT2A and D3 Receptors
    6.
    发明申请
    Dual Modulators of 5HT2A and D3 Receptors 有权
    5HT2A和D3受体的双重调制器

    公开(公告)号：US20130165432A1

    公开(公告)日：2013-06-27

    申请号：US13772390

    申请日：2013-02-21

    申请人： Hoffmann-La Roche Inc.

    发明人： Luca Gobbi ,  Georg Jaeschke ,  Olivier Roche ,  Rosa Maria Rodriquez Sarmiento ,  Lucinda Steward

    IPC分类号： C07D413/04 ,  C07D417/14 ,  C07D413/14

    CPC分类号： C07D413/04 ,  C07D413/14

    摘要： The present invention relates to compounds of the formula (I) wherein R1, R2, X and n are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.

    摘要翻译： 本发明涉及式（I）化合物，其中R 1，R 2，X和n如说明书中所定义，作为5-羟色胺5-HT2a和多巴胺D3受体的双重调节剂，其制备方法，含有它们的药物组合物及其用途 用于治疗精神病，以及其他疾病如抑郁和焦虑，药物依赖，痴呆和记忆障碍。