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    THIENO[2,3-b]PYRIDINE DERIVATIVES
    1.
    发明授权
    THIENO[2,3-b]PYRIDINE DERIVATIVES 有权
    噻吩[2,3-b]吡啶衍生物

    公开(公告)号：EP1963337B1

    公开(公告)日：2010-09-01

    申请号：EP06831522.5

    申请日：2006-12-19

    申请人： Richter Gedeon Nyrt.

    发明人： NÓGRÁDI, Katalin ,  WÁGNER, Gábor ,  KESERÜ, György ,  BIELIK, Attila ,  GÁTI, Tamás ,  HÁDA, Viktor ,  KÓTI, János ,  GÁL, Krisztina ,  VASTAG, Mónika ,  BOBOK, Amrita, Ágnes

    IPC分类号： C07D495/04 ,  A61K31/4365 ,  A61P25/00

    CPC分类号： C07D495/04

    摘要： The present invention relates to new mGluRl and mGluR5 receptor subtype preferring ligands of formula (I) wherein X represents a group selected from SO, SO2; Y represents a group selected from (CH2)n, NH, NHCH2; n is an integer of 0 to 1; Z is H or monosubstituted by alkyl, nitro, halogen, alkoxy, trifluoromethyl, cyano, amino, alkylamino, dialkylamino, aminomethyl, alkylaminomethyl, dialkylaminomethyl, hydroxyl, alkylsulfonylamino; R1 is an optionally substituted alkyl, cycloalkyl, phenyl, biphenyl, heterocyclyl; R2 is an optionally substituted phenyl, heterocyclyl, or NR3R4 group wherein R3 and R4 are independently selected from the group of hydrogen and an optionally substituted alkyl, or R3 and R4 together with the N atom to which they are attached form an optionally substituted C5-7 heterocyclyl group, containing one or more heteroatom(s), or NH-CO-NR5R6 group, wherein R5 and R6 are independently selected from the group of hydrogen and an optionally substituted alkyl, or R5 and R6 together with the N atom to which they are attached form an optionally substituted C5-7 heterocyclyl group, containing one or more heteroatom(s); and/or hydrates and/or solvates and/or pharmaceutically acceptable salts thereof formed with acids or bases, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluRl and mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain, neuromuscular dysfunctions of the lower urinary tract and gastrointestinal disorders.

    NEW COMPOUNDS
    3.
    发明公开
    NEW COMPOUNDS 审中-公开
    新化合物

    公开(公告)号：EP1963338A1

    公开(公告)日：2008-09-03

    申请号：EP06842192.4

    申请日：2006-12-19

    申请人： Richter Gedeon NYRT

    发明人： NÓGRÁDI, Katalin ,  KESERÜ, György ,  BIELIK, Attila ,  GÁTI, Tamás ,  GÁL, Krisztina ,  VASTAG, Mónika ,  BOBOK, Amrita, Ágnes

    IPC分类号： C07D495/04 ,  A61K31/4365 ,  A61P25/00

    CPC分类号： C07D495/04

    摘要： The present invention relates to new mGluR1 and mGluR5 receptor subtype preferring ligands of formula (I); wherein Y represents a subtituent selected from hydrogen, methyl, fluoro, chloro, bromo, methoxy; Z is hydrogen or methyl; R is an optionally substituted heteroaryl, and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluR1 and mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain and neuromuscular dysfunctions of the lower urinary tract.

    摘要翻译： 本发明涉及式（I）的新的mGluR1和mGluR5受体亚型优选配体; 其中Y代表选自氢，甲基，氟，氯，溴，甲氧基的取代基; Z是氢或甲基; R是任选取代的杂芳基，和/或其盐和/或水合物和/或溶剂化物，涉及其制备方法，涉及含有该化合物的药物组合物及其在治疗和/或预防需要 mGluR1和mGluR5受体的调节，例如神经障碍，精神障碍，急性和慢性疼痛以及下尿路的神经肌肉功能障碍。

    NEW COMPOUNDS
    4.
    发明公开
    NEW COMPOUNDS 审中-公开
    新化合物

    公开(公告)号：EP1963336A1

    公开(公告)日：2008-09-03

    申请号：EP06831521.7

    申请日：2006-12-19

    申请人： Richter Gedeon NYRT

    发明人： NÓGRÁDI, Katalin ,  WÁGNER, Gábor ,  KESERÜ, György ,  BIELIK, Attila ,  GÁTI, Tamás ,  HÁDA, Viktor ,  KÓTI, János ,  GÁL, Krisztina ,  VASTAG, Mónika ,  BOBOK, Amrita, Ágnes

    IPC分类号： C07D495/04 ,  A61K31/4365 ,  A61P25/00

    CPC分类号： C07D495/04

    摘要： The present invention relates to new mGluRl and mGluR5 receptor subtype preferring ligands of formula (I) wherein X represents a group selected from CO, SO, SO2; Y represents a group selected from 0, OCH2, (CH2)n, NH, NHCH2; n is an integer of 0 to 2; R1 is an optionally substituted alkyl, cycloalkyl, phenyl, biphenyl, heterocyclyl; R2 is an optionally substituted phenyl, heterocyclyl or NR3R4 group wherein R3 and R4 are independently selected from the group of hydrogen, alkyl, or R3 and R4 together with the N atom to which they are attached can form an optionally substituted C5-7 heterocyclyl group, containing one or more heteroatom(s) selected from the group of N, O, S, and/or tautomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluRl and mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain, neuromuscular dysfunctions of the lower urinary tract and gastrointestinal disorders.

    摘要翻译： 本发明涉及新的式（I）的mGluR1和mGluR5受体亚型优选配体，其中X代表选自CO，SO，SO2的基团; Y代表选自O，OCH 2，（CH 2）n，NH，NHCH 2的基团; n是0至2的整数; R1是任选取代的烷基，环烷基，苯基，联苯基，杂环基; R 2为任选取代的苯基，杂环基或NR 3 R 4基团，其中R 3和R 4独立地选自氢，烷基或R 3和R 4与它们所连接的N原子一起可形成任选取代的C 5-7杂环基 ，其含有一种或多种选自N，O，S和/或互变异构体和/或盐和/或水合物和/或溶剂合物的杂原子，涉及其制备方法，涉及药物组合物 以及它们在治疗和/或预防需要调节mGluR1和mGluR5受体如神经障碍，精神障碍，急性和慢性疼痛，下尿路神经肌肉功能障碍和胃肠病症的病理状况中的用途。

    NEW COMPOUNDS
    6.
    发明公开
    NEW COMPOUNDS 有权
    噻吩并[2,3-b]吡啶衍生物

    公开(公告)号：EP1963337A1

    公开(公告)日：2008-09-03

    申请号：EP06831522.5

    申请日：2006-12-19

    申请人： Richter Gedeon NYRT

    发明人： NÓGRÁDI, Katalin ,  WÁGNER, Gábor ,  KESERÜ, György ,  BIELIK, Attila ,  GÁTI, Tamás ,  HÁDA, Viktor ,  KÓTI, János ,  GÁL, Krisztina ,  VASTAG, Mónika ,  BOBOK, Amrita, Ágnes

    IPC分类号： C07D495/04 ,  A61K31/4365 ,  A61P25/00

    CPC分类号： C07D495/04

    摘要： The present invention relates to new mGluRl and mGluR5 receptor subtype preferring ligands of formula (I) wherein X represents a group selected from SO, SO2; Y represents a group selected from (CH2)n, NH, NHCH2; n is an integer of 0 to 1; Z is H or monosubstituted by alkyl, nitro, halogen, alkoxy, trifluoromethyl, cyano, amino, alkylamino, dialkylamino, aminomethyl, alkylaminomethyl, dialkylaminomethyl, hydroxyl, alkylsulfonylamino; R1 is an optionally substituted alkyl, cycloalkyl, phenyl, biphenyl, heterocyclyl; R2 is an optionally substituted phenyl, heterocyclyl, or NR3R4 group wherein R3 and R4 are independently selected from the group of hydrogen and an optionally substituted alkyl, or R3 and R4 together with the N atom to which they are attached form an optionally substituted C5-7 heterocyclyl group, containing one or more heteroatom(s), or NH-CO-NR5R6 group, wherein R5 and R6 are independently selected from the group of hydrogen and an optionally substituted alkyl, or R5 and R6 together with the N atom to which they are attached form an optionally substituted C5-7 heterocyclyl group, containing one or more heteroatom(s); and/or hydrates and/or solvates and/or pharmaceutically acceptable salts thereof formed with acids or bases, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluRl and mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain, neuromuscular dysfunctions of the lower urinary tract and gastrointestinal disorders.

    PROCESS FOR THE PREPARATION OF PIPERAZINE DERIVATIVES
    9.
    发明公开
    PROCESS FOR THE PREPARATION OF PIPERAZINE DERIVATIVES 有权
    用于生产哌嗪衍生物

    公开(公告)号：EP2367807A1

    公开(公告)日：2011-09-28

    申请号：EP09797147.7

    申请日：2009-12-18

    申请人： Richter Gedeon Nyrt.

    发明人： ÁGAINÉ CSONGOR, Éva ,  CZIBULE, László ,  SEBÖK, Ferenc ,  JUHÁSZ, Bálint ,  GALAMBOS, János ,  NÓGRÁDI, Katalin

    IPC分类号： C07D295/135

    CPC分类号： C07D295/135

    摘要： The invention relates to a process for the preparation of the trans
    N-{ 4-{2-[4-(2,3- dichlorophenyl)-piperazine-1-yl]-ethyl}-cyclohexyl}-carbamide derivatives of formula (I) by reacting the compound of formula (III) with a carbamoylchloride of formula (II) which comprises carrying out the reaction in a mixture of a solvent and concentrated aqueous solution of an alkali hydroxide at a temperature between 40-100 °C in the presence of a phase transfer catalyst, separating the phases and washing the organic layer then removing the solvent and drying the compound of formula (I) obtained until its weight is constant.