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    NOVEL N-ARYL AND N-HETEROARYL SUBSTITUTED PYRIDINONE DERIVATIVES FOR USE IN MCH-1 MEDIATED DISEASES
    1.
    发明申请
    NOVEL N-ARYL AND N-HETEROARYL SUBSTITUTED PYRIDINONE DERIVATIVES FOR USE IN MCH-1 MEDIATED DISEASES 审中-公开
    用于MCH-1介导的疾病的新型N-亚胺基和N-取代的取代的吡啶酮衍生物

    公开(公告)号：WO2007141200A8

    公开(公告)日：2008-03-27

    申请号：PCT/EP2007055376

    申请日：2007-06-01

    Applicant: JANSSEN PHARMACEUTICA NV ,  ALCAZAR-VACA MANUEL JESUS ,  ANDRES-GIL JOSE IGNACIO ,  DAUTZENBERG FRANK MATTHIAS ,  MACRITCHIE JACQUELINE ,  OYARZABAL SANTAMARINA JULEN

    Inventor： ALCAZAR-VACA MANUEL JESUS ,  ANDRES-GIL JOSE IGNACIO ,  DAUTZENBERG FRANK MATTHIAS ,  MACRITCHIE JACQUELINE ,  OYARZABAL SANTAMARINA JULEN

    IPC: C07D213/69 ,  A61K31/4412 ,  A61P3/04 ,  C07D401/10

    CPC classification number: C07D213/69 ,  C07D401/10

    Abstract: The present invention concerns N-aryl and N-heteroaryl substituted pyridinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-1 activity according to the general Formula (I), a pharmaceutically acceptable acid or base addition salt thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of psychiatric disorders, including but not limited to anxiety, eating disorders, mood disorders, such as bipolar disorders and depression, psychoses, such as schizophrenia, and sleeping disorders; obesity; diabetes; sexual disorders and neurological disorders.

    Abstract translation: 本发明涉及具有拮抗性黑色素浓缩激素（MCH）活性，特别是根据通式（I）的MCH-1活性的N-芳基和N-杂芳基取代的吡啶酮衍生物，其药学上可接受的酸或碱加成盐， 其N-氧化物形式或其季铵盐，其中变量在权利要求1中定义。它还涉及它们的制备方法，包含它们的组合物及其作为药物的用途。 根据本发明的化合物可用于预防和/或治疗精神病学障碍，包括但不限于焦虑，进食障碍，情绪障碍，例如双相性精神障碍和抑郁症，精神病如精神分裂症和睡眠障碍; 肥胖; 糖尿病; 性障碍和神经障碍。

    C6- AND C9-SUBSTITUTED '4, 3-C! ISOXAZOLINE DERIVATIVES AND THEIR USE AS ANTI-DEPRESSANTS
    2.
    发明申请
    C6- AND C9-SUBSTITUTED '4, 3-C! ISOXAZOLINE DERIVATIVES AND THEIR USE AS ANTI-DEPRESSANTS 审中-公开
    C6-和C9-取代的'4，3-C！ 异恶唑啉衍生物及其作为抗抑郁剂的用途

    公开(公告)号：WO2004018482A3

    公开(公告)日：2004-04-01

    申请号：PCT/EP0309532

    申请日：2003-08-19

    Applicant: JANSSEN PHARMACEUTICA NV ,  ANDRES-GIL JOSE IGNACIO ,  ALCAZAR-VACA MANUEL JESUS ,  MATESANZ-BALLESTEROS MARIA ENC ,  BAKKER MARGARETHA HENRICA MARI ,  MEGENS ANTONIUS ADRIANUS HENDR

    Inventor： ANDRES-GIL JOSE IGNACIO ,  ALCAZAR-VACA MANUEL JESUS ,  MATESANZ-BALLESTEROS MARIA ENC ,  BAKKER MARGARETHA HENRICA MARI ,  MEGENS ANTONIUS ADRIANUS HENDR

    IPC: A61K31/424 ,  A61K31/496 ,  A61P25/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  C07D498/04

    CPC classification number: C07D498/04

    Abstract: The invention concerns substituted tricyclic isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline , dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on at least one of the C6- and C9-positions of the phenylpart of the tricyclic moiety with a selected radical, according to Formula (I) wherein X = CH

    Abstract translation: 本发明涉及取代的三环异恶唑啉衍生物，更特别是三环二氢苯并吡喃异恶唑啉，二氢喹啉恶唑啉，二氢萘并异恶唑啉和二氢苯并噻喃恶唑啉衍生物，所述衍生物在三环部分的苯基部分的至少一个C6-和C9-位上被选定的基团取代， ）其中X = CH 2＃191，NR 7，S或O，R 1，R 2，R 14， R1和R5是某些特定的取代基，条件是至少一个R14- 和R15？ 不是氢，Pir优选是任选取代的哌啶基或哌嗪基，R 3' 表示任选取代的芳族碳环或杂环体系，其包含部分或完全氢化的最多6个原子长度的烃链，与该环体系连接的Pir基团可以含有一个或多个选自O，N 和S; 它们的制备方法，包含它们的药物组合物以及它们作为药物的用途，特别是用于治疗抑郁症，焦虑症，运动障碍，精神病，帕金森病和体重障碍的药物。令人惊讶地显示了根据本发明的化合物 与另外的α2-肾上腺素受体拮抗剂活性组合具有血清素（5-HT）再摄取抑制剂活性，并且在没有镇静作用的情况下显示出强烈的抗抑郁活性。 本发明还涉及根据本发明的异恶唑啉衍生物与一种或多种选自抗抑郁药，抗焦虑药，抗精神病药和抗帕金森病药物的其他化合物的新组合，以改善作用的效力和/或起效。

    C6- AND C9-SUBSTITUTED CHROMENO[4, 3-C]ISOXAZOLINE DERIVATIVES AND THEIR USE AS ANTI-DEPRESSANTS
    5.
    发明申请
    C6- AND C9-SUBSTITUTED CHROMENO[4, 3-C]ISOXAZOLINE DERIVATIVES AND THEIR USE AS ANTI-DEPRESSANTS 审中-公开
    C6-和C9-取代的CHROMENO [4,3-C]异辛唑衍生物及其作为抗病毒剂的用途

    公开(公告)号：WO2004018482A8

    公开(公告)日：2005-03-24

    申请号：PCT/EP0309532

    申请日：2003-08-19

    Applicant: JANSSEN PHARMACEUTICA NV ,  ANDRES-GIL JOSE IGNACIO ,  ALCAZAR-VACA MANUEL JESUS ,  MATESANZ-BALLESTEROS MARIA ENC ,  BAKKER MARGARETHA HENRICA MARI ,  MEGENS ANTONIUS ADRIANUS HENDR

    Inventor： ANDRES-GIL JOSE IGNACIO ,  ALCAZAR-VACA MANUEL JESUS ,  MATESANZ-BALLESTEROS MARIA ENC ,  BAKKER MARGARETHA HENRICA MARI ,  MEGENS ANTONIUS ADRIANUS HENDR

    IPC: A61K31/424 ,  A61K31/496 ,  A61P25/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  C07D498/04

    CPC classification number: C07D498/04

    Abstract: The invention concerns substituted tricyclic isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline , dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on at least one of the C6- and C9-positions of the phenylpart of the tricyclic moiety with a selected radical, according to Formula (I) wherein X = CH2, N-R , S or O, R , R , R and R are certain specific substituents, with the proviso that at least one of R and R is not hydrogen, Pir is preferably an optionally substituted piperidinyl or piperazinyl radical and R represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S ; a process for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for the treatment of depression, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders.. The compounds according to the invention have surprisingly been shown to have a serotonine (5-HT) reuptake inhibitor activity in combination with additional alpha2-adrenoceptor antagonist activity and show a strong anti-depressant activity without being sedative. The invention also relates to novel combination of isoxazoline derivatives according to the invention with one or more other compounds selected from the group of antidepressants, anxiolytics, anti-psychotics and anti-Parkinson's disease drugs to improve efficacy and/or onset of action.

    Abstract translation: 本发明涉及取代的三环异恶唑啉衍生物，更具体地是三环二氢苯并吡喃恶唑啉，二氢喹啉基异恶唑啉，二氢萘硫基异恶唑啉和二氢苯并噻唑并恶唑啉衍生物，其被三选择基团的苯基部分的C 6 - 和C 9位中的至少一个与选定的基团取代， ）其中X = CH 2，NR 7，S或O，R 1，R 2，R 14和R 15是某些具体的取代基，条件是R 14中的至少一个 并且R 15不是氢，Pir优选为任选取代的哌啶基或哌嗪基，R 3表示任选取代的芳族碳环或杂环系统，其包含最多6个原子长的部分或完全氢化的烃链，其中 环体系连接到Pir基团上并且可以含有一个或多个选自O，N和S的杂原子; 其制备方法，包含它们的药物组合物及其作为药物的用途，特别是用于治疗抑郁症，焦虑症，运动障碍，精神病，帕金森病和体重障碍。根据本发明的化合物已被惊奇地显示 具有5-羟色胺（5-HT）再摄取抑制剂活性与额外的α2-肾上腺素受体拮抗剂活性的组合，并且在没有镇静作用的情况下显示出强烈的抗抑郁活性。 本发明还涉及根据本发明的异恶唑啉衍生物与一种或多种选自抗抑郁药，抗焦虑药，抗精神病药和抗帕金森病药物的其它化合物的新组合，以改善疗效和/或起效。

    ЛИГАНДЫ mGluR2/3 ДЛЯ PET, МЕЧЕННЫЕ РАДИОАКТИВНЫМИ ИЗОТОПАМИ
    9.
    发明专利
    ЛИГАНДЫ mGluR2/3 ДЛЯ PET, МЕЧЕННЫЕ РАДИОАКТИВНЫМИ ИЗОТОПАМИ 未知

    公开(公告)号：EA037941B1

    公开(公告)日：2021-06-09

    申请号：EA201891444

    申请日：2016-12-16

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： ANDRES-GIL JOSE IGNACIO ,  VAN GOOL MICHIEL LUC MARIA ,  BORMANS GUY MAURITS R ,  VERBEEK JOOST

    IPC: A61K51/04 ,  A61K101/02 ,  C07B59/00 ,  C07D487/04

    Abstract: Настоящееизобретениеотноситсяк новыммеченнымрадиоактивнымиизотопамилигандам mGluR2/3, избирательнымпосравнениюс другими mGlu-рецепторами, которыеявляютсяприменимымидлявизуализациии количественногоопределенияметаботропныхглутаматныхрецепторов mGlu2 и mGlu3 втканяхс помощьюпозитронно-эмиссионнойтомографии (PET). Настоящееизобретениетакженаправленонакомпозиции, содержащиетакиесоединения, наспособыполучениятакихсоединенийи композиций, наприменениетакихсоединенийи композицийдлявизуализацииткани, клетокилимлекопитающего in vitro или in vivo инапредшественниковуказанныхсоединений.

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