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    4-ALKOXYPYRIDAZINE DERIVATIVES AS FAST DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS
    2.
    发明申请
    4-ALKOXYPYRIDAZINE DERIVATIVES AS FAST DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS 审中-公开
    4-烷氧基吡啶衍生物作为快速分解多巴胺2受体拮抗剂

    公开(公告)号：WO2008128995A1

    公开(公告)日：2008-10-30

    申请号：PCT/EP2008/054731

    申请日：2008-04-18

    申请人： JANSSEN PHARMACEUTICA N.V. ,  MACDONALD, Gregor, James ,  BARTOLOMÉ-NEBREDA, José Manuel

    发明人： MACDONALD, Gregor, James ,  BARTOLOMÉ-NEBREDA, José Manuel

    IPC分类号： C07D401/12 ,  A61K31/501 ,  A61P25/18

    CPC分类号： C07D401/12

    摘要： The present invention relates to (1-benzyl-piperidin-4-yl) - (4-alkoxy-pyridazin-3-yl) - amines of formula (I) 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受体拮抗剂的式（I）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， 包含这些化合物作为活性成分的药物组合物。 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。

    ANTIBACTERIAL QUINOLINE DERIVATIVES
    4.
    发明申请
    ANTIBACTERIAL QUINOLINE DERIVATIVES 审中-公开
    抗生素喹啉衍生物

    公开(公告)号：WO2008068269A1

    公开(公告)日：2008-06-12

    申请号：PCT/EP2007/063315

    申请日：2007-12-04

    申请人： JANSSEN PHARMACEUTICA N.V. ,  GUILLEMONT, Jérôme, Emile, Georges ,  MOTTE, Magali, Madeleine, Simone ,  ANDRIES, Koenraad, Jozef, Lodewijk, Marcel ,  KOUL, Anil

    发明人： GUILLEMONT, Jérôme, Emile, Georges ,  MOTTE, Magali, Madeleine, Simone ,  ANDRIES, Koenraad, Jozef, Lodewijk, Marcel ,  KOUL, Anil

    IPC分类号： C07D215/22 ,  A61K31/465 ,  A61P31/06

    CPC分类号： C07D215/227

    摘要： The present invention relates to novel substituted quinoline derivatives according to the general formula (Ia) or formula (Ib): including any stereochemically isomeric form thereof, a pharmaceutically acceptable salt thereof, a N -oxide form thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or composit ions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.

    摘要翻译： 本发明涉及根据通式（Ia）或式（Ib）的新的取代喹啉衍生物：包括其任何立体化学异构形式，其药学上可接受的盐，其N-氧化物形式或其溶剂合物。 所要求保护的化合物可用于治疗细菌感染。 还要求保护的是包含药学上可接受的载体和作为活性成分的治疗有效量的所要求保护的化合物的组合物，所要求保护的化合物或复合离子在制备用于治疗细菌感染和方法的药物中的用途 用于制备所要求保护的化合物。

    COMBINATIONS OF 4-BROMO-2-(4-CHLOROPHENYL)-5-(TRIFLUOROMETHYL)-1H-PYRROLE-3-CARBONITRILE AND METAL COMPOUNDS
    6.
    发明申请
    COMBINATIONS OF 4-BROMO-2-(4-CHLOROPHENYL)-5-(TRIFLUOROMETHYL)-1H-PYRROLE-3-CARBONITRILE AND METAL COMPOUNDS 审中-公开
    4-溴-2-（4-氯苯基）-5-（三氟甲基）-1H-吡咯并 - 碳二烯和金属化合物的组合

    公开(公告)号：WO2007088172A2

    公开(公告)日：2007-08-09

    申请号：PCT/EP2007/050927

    申请日：2007-01-31

    申请人： JANSSEN PHARMACEUTICA N.V. ,  KEMPEN, Tony Mathilde Jozef

    发明人： KEMPEN, Tony Mathilde Jozef

    IPC分类号： A01N43/36 ,  A01N59/20 ,  A01N59/16 ,  A01P9/00 ,  A01P13/00 ,  C09D5/16 ,  B27K3/52 ,  C02F1/50

    CPC分类号： A01N43/36 ,  A01N55/02 ,  A01N59/16 ,  A01N59/24 ,  A01N59/20 ,  A01N47/14 ,  A01N43/40 ,  A01N2300/00

    摘要： The present invention relates to combinations of 4-bromo-2-(4-chloro-phenyl)-5-(trifluoromethyl)-1 H -pyrrole-3-carbonitrile, or a salt thereof, and copper or zinc compounds which provide an improved protecting effect against fouling organisms. More particularly, the present invention relates to compositions comprising a combination of 4-bromo-2-(4-chlorophenyl)-5-(trifluoromethyl)-1 H -pyrrole-3-carbonitrile, or a salt thereof, together with one or more copper or zinc compounds selected from Cu 2 O, Cu(OH) 2 , CuSO 4 , copper pyrithione, CuSCN, CuCO 3 , ZnO, ZnCl 2 , ZnSO 4 , zineb, and zinc pyrithione; in respective proportions to provide a synergistic effect against fouling organisms and the use of these compositions for protecting materials against fouling organisms. This invention thus relates to the field of protection of materials, such as underwater objects, protection of wood, wood products, biodegradable materials and coatings.

    摘要翻译： 本发明涉及4-溴-2-（4-氯 - 苯基）-5-（三氟甲基）-1H-吡咯-3-甲腈或其盐与铜或锌化合物的组合，其提供改进的保护 对污染生物的作用。 更具体地说，本发明涉及包含4-溴-2-（4-氯苯基）-5-（三氟甲基）-1H-吡咯-3-甲腈或其盐与一种或多种铜 或选自Cu 2 O，Cu（OH）2，CuSO 4，锌吡啶硫酮，CuSCN，CuCO 3， ZnO，ZnCl 2，ZnSO 4，zineb和吡啶硫酮锌; 以提供对结垢生物的协同作用，以及使用这些组合物来保护材料免受污染生物的影响。 因此，本发明涉及诸如水下物体，保护木材，木制品，可生物降解的材料和涂层等材料的保护领域。

    2-ANILINE-4-ARYL SUBSTITUTED THIAZOLE DERIVATIVES
    8.
    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：WO2007031440A2

    公开(公告)日：2007-03-22

    申请号：PCT/EP2006/066015

    申请日：2006-09-05

    申请人： JANSSEN PHARMACEUTICA N.V. ,  THURING, Johannes, Wilhelmus, John, F. ,  MACDONALD, Gregor, James ,  GRANTHAM, Christopher, James ,  DINKLO, Theodorus ,  LESAGE, Anne, Simone, Josephine

    发明人： THURING, Johannes, Wilhelmus, John, F. ,  MACDONALD, Gregor, James ,  GRANTHAM, Christopher, James ,  DINKLO, Theodorus ,  LESAGE, Anne, Simone, Josephine

    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, 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 α7 nicotinic receptor is beneficial.

    摘要翻译： 本发明涉及式（I）化合物，N-氧化物，药学上可接受的加成盐，季胺及其立体异构体形式的用途，其中Z为氢，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（C 1 -C 6）烷基，C 1 -C 6烷基， （= O）-C 1-6烷基 - ，甲酰氨基-C 1-6烷基 - ，C 1-6 - 烷基-C（ =（O）-NH-C 1-6烷基 - ，单 - 或二（C 1-6烷基）氨基-C（= O）-C 1-6烷基 - ，苯基-C 1-6烷基 - 或者H 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 -C 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，其中每个所述环系可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 C 1-6烷基或C 1-6烷基-O-; Het 表示吗啉基; 吡唑基或咪唑基; Het 4代表吗啉基，吡唑基或咪唑基; Ar表示任选被卤素取代的苯基，C 1-6烷基，C 1-6烷基-O-或多卤C 1-6烷基; 用于制备用于预防或治疗或预防精神病，智力障碍或其中调节a7烟碱样受体有益的疾病或病症的药物。