公开(公告)号：WO2008003736A1

公开(公告)日：2008-01-10

申请号：PCT/EP2007/056792

申请日：2007-07-05

Applicant: SOLVAY PHARMACEUTICALS B.V. ,  STOIT, Axel ,  COOLEN, Hein K.A.C. ,  VAN DER NEUT, Martina A.W. ,  KRUSE, Cornelis G.

Inventor： STOIT, Axel ,  COOLEN, Hein K.A.C. ,  VAN DER NEUT, Martina A.W. ,  KRUSE, Cornelis G.

IPC: C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  A61P25/16 ,  A61P25/28 ,  A61P25/30 ,  A61K31/445 ,  A61K31/40

CPC classification number: C07D471/04 ,  C07D487/04 ,  C07D519/00

Abstract: The invention concerns azaindole derivatives having the general formula (I) wherein the symbols have the meanings given in the specification. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition. The invention also relates to pharmaceutical compositions containing these compounds, to methods for preparing them, methods for preparing novel intermediates useful for their synthesis, methods for preparing compositions, and uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in disorders in which nicotinic receptors and/or dopamine transporters are involved, or that can be treated via manipulation of those receptors.

Abstract translation: 本发明涉及具有通式（I）的氮杂吲哚衍生物，其中符号具有说明书中给出的含义。 这些化合物具有部分烟碱乙酰胆碱受体激动和多巴胺再摄取抑制的组合。 本发明还涉及含有这些化合物的药物组合物，其制备方法，制备用于其合成的新中间体的方法，制备组合物的方法，以及这些化合物和组合物的用途，特别是其用于给患者施用 在其中涉及烟碱受体和/或多巴胺转运蛋白的病症中的治疗效果，或者可以通过这些受体的操纵来治疗。

公开(公告)号：WO2006061376A1

公开(公告)日：2006-06-15

申请号：PCT/EP2005/056505

申请日：2005-12-06

Applicant: SOLVAY PHARMACEUTICALS B.V. ,  FEENSTRA, Roelof W. ,  STOIT, Axel ,  TERPSTRA, Jan-willem ,  PRAS-RAVES, Maria L. ,  MCCREARY, Andrew C. ,  VAN VLIET, Bernard J. ,  HESSELINK, Mayke B. ,  KRUSE, Cornelis G. ,  VAN SCHARRENBURG, Gustaaf J.m.

Inventor： FEENSTRA, Roelof W. ,  STOIT, Axel ,  TERPSTRA, Jan-willem ,  PRAS-RAVES, Maria L. ,  MCCREARY, Andrew C. ,  VAN VLIET, Bernard J. ,  HESSELINK, Mayke B. ,  KRUSE, Cornelis G. ,  VAN SCHARRENBURG, Gustaaf J.m.

IPC: A61K31/423 ,  C07D263/58 ,  C07D413/12 ,  A61P25/00

CPC classification number: C07D263/58 ,  C07D413/12

Abstract: The invention relates to a group of novel aryloxyethylamine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine -D 2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): Z-T-Ar wherein: Z is a fragment of the general formula (2): and wherein the other symbols have the meanings given in the specification, and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.

Abstract translation: 本发明涉及一组具有双重作用模式的新型芳氧基乙胺衍生物：5-羟色胺再摄取抑制和对多巴胺-D2受体的部分激动作用。 本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。 所述化合物具有通式（1）：ZT-Ar其中：Z是通式（2）的片段：其中，其它符号具有本说明书中给出的含义及其互变异构体，立体异构体和N-氧化物， 以及所述式（1）化合物及其互变异构体，立体异构体和N-氧化物的药理学上可接受的盐，水合物和溶剂化物。