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    OXY-CYCLOHEXYL-4H,6H-5-OXA-2,3,10B-TRIAZA-BENZO[E]AZULENES AS V1A ANTAGONISTS
    4.
    发明公开
    OXY-CYCLOHEXYL-4H,6H-5-OXA-2,3,10B-TRIAZA-BENZO[E]AZULENES AS V1A ANTAGONISTS 有权
    OXY-CYCLOHEXYL-4H，6H-5-OXA-2,3,10B-三唑 - 苯并[E]亚油酸乙酯V1A-ANTAGONISTEN

    公开(公告)号：EP2760871A1

    公开(公告)日：2014-08-06

    申请号：EP12761740.5

    申请日：2012-09-24

    申请人： F.Hoffmann-La Roche AG

    发明人： DOLENTE, Cosimo ,  SCHNIDER, Patrick

    IPC分类号： C07D498/04 ,  A61K31/553 ,  A61P9/12

    CPC分类号： C07D498/04 ,  A61K31/553

    摘要： The present invention provides 4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes of the formula wherein R1 and R2 are as defined herein and which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments.

    摘要翻译： 本发明提供具有下式的4H，6H-5-氧杂-2,3,10b-三氮杂 - 苯并[e]薁其中R 1和R 2如本文所定义并且作为V1a受体调节剂，特别是作为V1a受体 拮抗剂，它们的制造，含有它们的药物组合物及其作为药物的用途。

    DUAL NK1/NK3 ANTAGONISTS AGAINST SCHIZOPHRENIA
    9.
    发明公开
    DUAL NK1/NK3 ANTAGONISTS AGAINST SCHIZOPHRENIA 审中-公开
    DUAL NK 1 / NK-3拮抗剂反对精神分裂症

    公开(公告)号：EP1776117A1

    公开(公告)日：2007-04-25

    申请号：EP05769687.4

    申请日：2005-07-27

    申请人： F.HOFFMANN-LA ROCHE AG

    发明人： SCHNIDER, Patrick

    IPC分类号： A61K31/44 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  C07D213/82 ,  A61P25/18

    CPC分类号： C07D213/75 ,  A61K31/44 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  C07D213/89 ,  C07D401/04 ,  C07D409/04

    摘要： The present invention relates to the use of compounds of the general formula (I) wherein R1 is lower alkyl or halogen; R2 is hydrogen or halogen; R3 -(CHR')nOH, phenyl, optionally substituted by -(CHR')nOH, or is a saturated, partial saturated or aromatic 5-or 6-membered heterocyclic ring with one heteroatom, selected from the group consisting of-N(R4)-, -N=, formula (II), -S- or -S(O)2, and which rings are optionally substituted by - (CHR’)nOH ; R’ is independently from “n” hydrogen or - (CH2)nOH; R4 is hydrogen, -S(O2)-lower alkyl or -C(O)-lower alkyl; X is -O-, -CH2O-, -S- or a bond; n is 1 or 2; or to pharmaceutically active acid-addition salts thereof, for the preparation of medicaments for the treatment of schizophrenia.

    SPIRO-OXAZOLONES
    10.
    发明公开
    SPIRO-OXAZOLONES 有权
    螺恶唑酮

    公开(公告)号：EP3083633A1

    公开(公告)日：2016-10-26

    申请号：EP14815318.2

    申请日：2014-12-16

    申请人： F.Hoffmann-La Roche AG

    发明人： RUNTZ-SCHMITT, Valerie ,  SCHNIDER, Patrick ,  DOLENTE, Cosimo ,  FASCHING, Bernhard

    IPC分类号： C07D491/10 ,  C07D491/12 ,  C07D498/10 ,  A61K31/438 ,  A61P25/00

    CPC分类号： C07D491/107 ,  C07D491/10 ,  C07D491/12 ,  C07D491/20 ,  C07D498/10 ,  C07D519/00

    摘要： The present invention provides spiro-oxazolones, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The present compounds are useful as therapeutics acting peripherally and centrally in the conditions of inappropriate secretion of vasopressin, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, aggressive behavior and phase shift sleep disorders, in particular jetlag.

    摘要翻译： 本发明提供作为V1a受体调节剂的螺恶唑酮，特别是作为V1a受体拮抗剂，其制造方法，含有它们的药物组合物及其作为药物的用途。 本发明化合物可用作在血管加压素分泌不适，焦虑症，抑郁障碍，强迫症，自闭症谱系，精神分裂症，侵袭行为和相移睡眠障碍，特别是jetlag中的外周作用和中枢作用的治疗剂。