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    2-ANILINE-4-ARYL SUBSTITUTED THIAZOLE DERIVATIVES
    3.
    发明申请
    2-ANILINE-4-ARYL SUBSTITUTED THIAZOLE DERIVATIVES 审中-公开
    2-苯胺-4-芳基取代的噻唑衍生物

    公开(公告)号：WO2007031440A3

    公开(公告)日：2007-08-02

    申请号：PCT/EP2006066015

    申请日：2006-09-05

    Applicant: JANSSEN PHARMACEUTICA NV ,  THURING JOHANNES WILHELMUS JOH ,  MACDONALD GREGOR JAMES ,  GRANTHAM CHRISTOPHER JAMES ,  DINKLO THEODORUS ,  LESAGE ANNE SIMONE JOSEPHINE

    Inventor： THURING JOHANNES WILHELMUS JOH ,  MACDONALD GREGOR JAMES ,  GRANTHAM CHRISTOPHER JAMES ,  DINKLO THEODORUS ,  LESAGE ANNE SIMONE JOSEPHINE

    IPC: C07D277/42 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4436 ,  A61P25/18 ,  A61P25/28 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

    CPC classification number: C07D471/04 ,  C07D277/42 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D513/04

    Abstract: This invention concerns the use of a compound of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is hydrogen, halo, C 1-6 alkyl, Het 1 , HO-C 1-6 alkyl-, cyano-C 1-6 alkyl-, amino-C(=O)-C 1-6 alkyl-, formylamino-C 1-6 alkyl-, C 1-6 alkyl-C(=O)-NH-C 1-6 alkyl-, mono- or di(C 1-6 alkyl)amino-C(=O)-C 1-6 alkyl-, phenyl-C 1-6 alkyl-, or He 4 -C 1-6 alkyl-; Q is phenyl, pyridyl, benzofuranyl, 2,3-dihydro-benzofuranyl, pyrazolyl, isoxazolyl or indazolyl wherein each of said ring systems is optionally being substituted with up to three substituents each independently selected from halo, cyano, C 1-6 alkyl, C 1-6 alkyl -O-, C 1-6 alkyl, Ar or polyhaloC 1-6 alkyl; L is phenyl, pyridyl, pyrimidazolyl, 8-Azapyrimidazolyl, pyridazinyl, imidazothiazolyl or furanyl wherein each of said ring systems may optionally be substituted with one or two or more substituents, each substituent independently being selected from halo, hydroxy, amino, cyano, C 1-6 alkyl or C 1-6 alkyl-O-; Het 1 represents morpholinyl; pyrazolyl or imidazolyl; Het 4 represents morpholinyl, pyrazolyl or imidazolyl; Ar represents phenyl optionally substituted with halo, C 1-6 alkyl, C 1-6 alkyl-O- or polyhaloC 1-6 alkyl; for the manufacture of a medicament for the prevention or the treatment or prophylaxis of psychotic disorders, intellectual impairment disorders or diseases or conditions in which modulation of the a7 nicotinic receptor is beneficial.

    Abstract translation: 本发明涉及式（I）化合物，其N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式的用途，其中Z是氢，卤素，C 1-6 - 烷基，Het 1，HO-C 1-6烷基 - ，氰基-C 1-6烷基 - ，氨基-C （= O）-C 1-6烷基 - ，甲酰氨基-C 1-6烷基 - ，C 1-6烷基-C（C 1 -C 6烷基） = O）-NH-C 1-6烷基 - ，单 - 或二（C 1-6烷基）氨基-C（= O）-C≡N 1-6烷基 - ，苯基-C 1-6烷基 - 或He + 4 -C 1-6烷基 - ; Q是苯基，吡啶基，苯并呋喃基，2,3-二氢 - 苯并呋喃基，吡唑基，异恶唑基或吲唑基，其中每个所述环系统任选被至多三个各自独立地选自卤素，氰基，C1- C 1-6烷基，C 1-6烷基-O-，C 1-6烷基，Ar或多卤代C 1-6烷基 ; L是苯基，吡啶基，嘧啶基，8-氮杂嘧啶基，哒嗪基，咪唑并噻唑基或呋喃基，其中每个所述环系可以任选被一个或两个或多个取代基取代，每个取代基独立地选自卤素，羟基，氨基，氰基，C 1-6烷基或C 1-6烷基-O-; Het 1表示吗啉基; 吡唑基或咪唑基; Het 4表示吗啉基，吡唑基或咪唑基; Ar代表任选被卤素取代的苯基，C 1-6烷基，C 1-6烷基-O-或多卤代C 1-6烷基; 用于制造用于预防或治疗或预防精神障碍，智力损伤障碍或调节α7烟碱受体有益的疾病或病症的药物。

    3-CYANO-4-(4-TETRAHYDROPYRAN-PHENYL)-PYRIDIN-2-ONE DERIVATIVES
    4.
    发明申请
    3-CYANO-4-(4-TETRAHYDROPYRAN-PHENYL)-PYRIDIN-2-ONE DERIVATIVES 审中-公开
    3-氰基-4-（4-四氢吡喃-2-基） - 吡啶-2-酮衍生物

    公开(公告)号：WO2008107481A8

    公开(公告)日：2008-12-24

    申请号：PCT/EP2008052768

    申请日：2008-03-07

    Applicant: JANSSEN PHARMACEUTICA NV ,  ADDEX PHARMACEUTICALS SA ,  CID-NUNEZ JOSE MARIA ,  TRABANCO-SUAREZ ANDRES AVELINO ,  MACDONALD GREGOR JAMES ,  DUVEY GUILLAUME ALBERT JACQUES

    Inventor： CID-NUNEZ JOSE MARIA ,  TRABANCO-SUAREZ ANDRES AVELINO ,  MACDONALD GREGOR JAMES ,  DUVEY GUILLAUME ALBERT JACQUES

    IPC: C07D405/12 ,  A61K31/4545 ,  A61P25/28

    CPC classification number: C07D405/12

    Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 ( mGluR2 ) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are centralnervous system disorders selected from the group of anxiety,schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and such compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

    Abstract translation: 本发明涉及新化合物，特别是包括其任何立体化学异构形式的式（I）的新型吡啶酮衍生物或其药学上可接受的盐或其溶剂合物，其中所有基团在申请和权利要求书中定义。 根据本发明的化合物是代谢型谷氨酸受体亚型2（mGluR2）的正性变构调节剂，其可用于治疗或预防与谷氨酸功能障碍相关的神经和精神障碍以及涉及代谢型受体的mGluR2亚型的疾病。 特别地，这些疾病是选自焦虑，精神分裂症，偏头痛，抑郁症和癫痫组的中枢神经系统疾病。 本发明还涉及药物组合物和制备这些化合物和这些组合物的方法，以及这些化合物用于预防和治疗其中涉及mGluR2的疾病的用途。

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