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    C6- AND C9-SUBSTITUTED CHROMENO[4,3-C]ISOXAZOLINE DERIVATIVES AND THEIR USE AS ANTI-DEPRESSANTS
    6.
    发明公开
    C6- AND C9-SUBSTITUTED CHROMENO[4,3-C]ISOXAZOLINE DERIVATIVES AND THEIR USE AS ANTI-DEPRESSANTS 有权
    C6和C9取代-chromeno并[4,3-C]异恶唑啉和它们作为抗抑郁使用

    公开(公告)号：EP1532155A2

    公开(公告)日：2005-05-25

    申请号：EP03753363.5

    申请日：2003-08-19

    申请人： JANSSEN PHARMACEUTICA N.V.

    发明人： ANDRES-GIL, José I.Johnson & Johnson PharmA R+D ,  ALCAZAR-VACA,Manuel.Johnson & Johnson PharmA R+D ,  MATESANZ-BALLESTEROS M.Johnson & Johnson PharmA ,  BAKKER, Margaretha, Henrica, Maria ,  MEGENS, Antonius, Adrianus, Hendrikus, Petrus

    IPC分类号： C07D498/04 ,  A61K31/424 ,  A61P25/00

    CPC分类号： C07D498/04

    摘要： 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-R7, S or O, R1, R2, R14 and R15 are certain specific substituents, with the proviso that at least one of R14 and R15 is not hydrogen, Pir is preferably an optionally substituted piperidinyl or piperazinyl radical and R3 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 α2-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.

    COMBINATIONS COMPRISING PDE 2 INHIBITORS SUCH AS 1-ARYL-4-METHYL- [1,2,4]TRIAZOLO [4,3-A]QUINOXALINE COMPOUNDS AND PDE 10 INHIBITORS FOR USE IN THE TREATMENT OF NEUROLOGICAL OR METABOLIC DISORDERS
    9.
    发明公开
    COMBINATIONS COMPRISING PDE 2 INHIBITORS SUCH AS 1-ARYL-4-METHYL- [1,2,4]TRIAZOLO [4,3-A]QUINOXALINE COMPOUNDS AND PDE 10 INHIBITORS FOR USE IN THE TREATMENT OF NEUROLOGICAL OR METABOLIC DISORDERS 审中-公开
    WITH PDE-2抑制剂如1-芳基-4-甲基组合[1,2,4]三唑并[4,3-A]喹喔啉和PDE-10抑制剂用于在神经系统和代谢性疾病的治疗中使用

    公开(公告)号：EP2863909A1

    公开(公告)日：2015-04-29

    申请号：EP13731752.5

    申请日：2013-06-25

    申请人： Janssen Pharmaceutica N.V.

    发明人： MEGENS, Antonius, Adrianus, Hendrikus, Petrus ,  LANGLOIS, Xavier, Jean, Michel ,  VANHOOF, Greta, Constantia, Peter ,  ANDRÉS-GIL, José, Ignacio ,  DE ANGELIS, Meri ,  BUIJNSTERS, Peter, Jacobus, Johannes, Antonius ,  TRABANCO-SUÁREZ, Andrés, Avelino ,  ROMBOUTS, Frederik, Jan, Rita

    IPC分类号： A61K31/4709 ,  A61K31/517 ,  A61K31/5377 ,  A61P21/00 ,  A61K45/06 ,  A61K31/4725 ,  A61K31/472

    摘要： The present invention relates to combinations of phosphodiesterase 2 (PDE2) inhibitors with inhibitors of phosphodiesterase 10 (PDE10). In particular, the invention relates to combinations of 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives which have been found to inhibit phosphodiesterase 2 (PDE2), with inhibitors of phosphodiesterase 10 (PDE10). Particular PDE10 inhibitors are selected from the group of MP-10, PQ-10, TP-10, papaverine, and the compounds disclosed in WO 2011/051324 and in WO 2011/110545. The invention is also directed to pharmaceutical compositions comprising such combinations, to processes for preparing such compositions, to the use of PDE2 inhibitors, in particular of 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives for the potentiation of said PDE10 inhibitors, and to the use of said PDE10 inhibitors for the potentiation of the effect of said PDE2 inhibitors, in particular, 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives, and to the use of such combinations and compositions for the prevention and treatment of disorders in which PDE2 and PDE10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases.

    摘要翻译： 本发明涉及一种具有磷酸二酯酶10（PDE10）的磷酸二酯酶抑制剂2（PDE2）抑制剂的组合。 特别地，本发明涉及的组合1-芳基-4-甲基 - [1,2,4]三唑并[4,3-A]已发现，以抑制磷酸二酯酶2（PDE2） - 喹喔啉衍生物，其中的抑制剂 磷酸二酯酶10（PDE10）。 特别PDE10抑制剂选自MP-10的选择，PQ-10，TP-10，罂粟碱，和所述化合物在盘WO 2011/051324和游离缺失WO十一万零五百四十五分之二千零一十一英寸 因此，本发明涉及药物组合物，包含寻求组合，以用于制备寻求组合物，于使用PDE 2抑制剂的，在1-芳基-4-甲基的具体[1,2,4]三唑并[4,3 一个]用于所述PDE10抑制剂的增强，以及使用PDE10抑制剂的喹喔啉衍生物对所述的说PDE2抑制剂的效果的增强作用，特别是，1-芳基-4-甲基 - [1,2,4] 三唑并[4,3-A]喹喔啉衍生物，并于使用搜索组合和组合物的对疾病，其中PDE2的预防和治疗和PDE10涉及,:如神经和精神障碍，和内分泌或代谢性疾病。