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    2-aniline-4-aryl substituted thiazole derivatives
    3.
    发明授权
    2-aniline-4-aryl substituted thiazole derivatives 有权
    2-苯胺-4-芳基取代的噻唑衍生物

    公开(公告)号：US09388175B2

    公开(公告)日：2016-07-12

    申请号：US12063689

    申请日：2008-02-13

    申请人： Johannes Wilhelmus John F. Thuring ,  Gregor James MacDonald ,  Christopher James Grantham ,  Theodorus Dinklo ,  Anne Simone Josephine Lesage

    发明人： Johannes Wilhelmus John F. Thuring ,  Gregor James MacDonald ,  Christopher James Grantham ,  Theodorus Dinklo ,  Anne Simone Josephine Lesage

    IPC分类号： C07D471/04 ,  C07D277/42 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D513/04

    CPC分类号： C07D471/04 ,  C07D277/42 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D513/04

    摘要： 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, C1-6alkyl, Het1, HO—C1-6alkyl-, cyano-C1-6alkyl-, amino-C(═O)—C1-6alkyl-, formylamino-C1-6alkyl-, C1-6alkyl-C(═O)—NH—C1-6alkyl-, mono- or di(C1-6alkyl)amino-C(═O)—C1-6alkyl-, phenyl-C1-6alkyl-, or Het4-C1-6alkyl-; 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, C1-6alkyl, C1-6alkyl-O—, C1-6alkylthio, Ar or polyhaloC1-6alkyl; 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, C1-6alkyl or C1-6alkyl-O—; Het1 represents morpholinyl; pyrazolyl or imidazolyl; Het4 represents morpholinyl, pyrazolyl or imidazolyl; Ar represents phenyl optionally substituted with halo, C1-6alkyl, C1-6alkyl-O— or polyhaloC1-6alkyl; 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 α7 nicotinic receptor is beneficial.

    摘要翻译： 本发明涉及式（I）化合物的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 氰基-C 1-6烷基 - ，氨基-C（= O）-C 1-6烷基 - ，甲酰基氨基-C 1-6烷基 - ，C 1-6烷基-C（= O）-NH-C 1-6烷基 - 或二（C 1-6烷基）氨基-C（= O）-C 1-6烷基 - ，苯基-C 1-6烷基 - 或Het 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独立地选自卤素，氰基，C 1-6烷基， C 1-6烷基-O-，C 1-6烷硫基，Ar或多卤代C 1-6烷基; L是苯基，吡啶基，嘧唑基，8-氮杂唑基，哒嗪基，咪唑并噻唑基或呋喃基，其中每个所述环体系可以任选地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-; Het1表示吗啉基; 吡唑基或咪唑基; Het4表示吗啉基，吡唑基或咪唑基; Ar表示任选被卤素，C 1-6烷基，C 1-6烷基-O-或多卤代C 1-6烷基取代的苯基; 用于制备用于预防或治疗或预防精神病，智力障碍或其中α7烟碱受体的调节有益的疾病或病症的药物。

    3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
    5.
    发明授权
    3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives 有权
    3-氰基-4-（4-四氢吡喃 - 苯基） - 吡啶-2-酮衍生物

    公开(公告)号：US08906939B2

    公开(公告)日：2014-12-09

    申请号：US12529568

    申请日：2008-03-07

    申请人： Jose Maria Cid-Nunez ,  Andres Avelino Trabanco-Suarez ,  Gregor James MacDonald ,  Guillaume Albert Jacques Duvey

    发明人： Jose Maria Cid-Nunez ,  Andres Avelino Trabanco-Suarez ,  Gregor James MacDonald ,  Guillaume Albert Jacques Duvey

    IPC分类号： C07D405/12 ,  A61K31/4433

    CPC分类号： C07D405/12

    摘要： 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 central nervous 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.

    摘要翻译： 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化物，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病学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。

    4-alkoxypyridazine derivatives as fast dissociating dopamine 2 receptor antagonists
    6.
    发明授权
    4-alkoxypyridazine derivatives as fast dissociating dopamine 2 receptor antagonists 有权
    4-烷氧基哒嗪衍生物作为快速解离的多巴胺2受体拮抗剂

    公开(公告)号：US08906921B2

    公开(公告)日：2014-12-09

    申请号：US12597166

    申请日：2008-04-18

    申请人： Gregor James MacDonald ,  José Manuel Bartolomé-Nebreda

    发明人： Gregor James MacDonald ,  José Manuel Bartolomé-Nebreda

    IPC分类号： A61K31/50 ,  C07D237/02

    CPC分类号： C07D401/12

    摘要： The present invention relates to (1-benzyl-piperidin-4-yl)-(4-alkoxy-pyridazin-3-y1)-amines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.

    摘要翻译： 本发明涉及快速解离多巴胺2受体拮抗剂的（1-苄基 - 哌啶-4-基） - （4-烷氧基 - 哒嗪-3-基） - 胺，制备这些化合物的方法，包含这些化合物的药物组合物 作为活性成分。 该化合物可用作治疗或预防中枢神经系统疾病（例如精神分裂症）的药物，通过发挥抗精神病作用而没有运动副作用。