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    PIPERAZINE OXIME DERIVATIVES HAVING NK-1 RECEPTOR ANTAGONISTIC ACTIVITY
    4.
    发明申请
    PIPERAZINE OXIME DERIVATIVES HAVING NK-1 RECEPTOR ANTAGONISTIC ACTIVITY 审中-公开
    具有NK-1受体拮抗活性的哌嗪衍生物

    公开(公告)号：WO2003006459A1

    公开(公告)日：2003-01-23

    申请号：PCT/EP2002/007472

    申请日：2002-07-03

    Applicant: SOLVAY PHARMACEUTICALS B.V. ,  VAN MAARSEVEEN, Jan, H. ,  VAN SCHARRENBURG, Gustaaf, J., M. ,  TULP, Martinus, Th., M. ,  MCCREARY, Andrew, C. ,  IWEMA BAKKER, Wouter, I. ,  COOLEN, Hein, K., A., C. ,  HERREMANS, Arnoldus, H., J. ,  VAN DEN HOOGENBAND, Adrianus

    Inventor： VAN MAARSEVEEN, Jan, H. ,  VAN SCHARRENBURG, Gustaaf, J., M. ,  TULP, Martinus, Th., M. ,  MCCREARY, Andrew, C. ,  IWEMA BAKKER, Wouter, I. ,  COOLEN, Hein, K., A., C. ,  HERREMANS, Arnoldus, H., J. ,  VAN DEN HOOGENBAND, Adrianus

    IPC: C07D403/06

    CPC classification number: C07D401/14 ,  C07D241/04 ,  C07D403/06 ,  C07D403/14 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D471/04

    Abstract: The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity. The invention relates to compounds of the general formula (1) wherein:X represents phenyl or pyridyl substituted with 1 or 2 substituents from the group CH 3 , CF 3 , OCH 3 , halogen, cyano and 5-CF 3 -tetrazol-1-yl; Y represents 2- or 3-indolyl, phenyl, 7-aza-indol-3-yl or 3-indazolyl, 2-naphthyl, 3-benzo[b]thiophenyl, 2-benzofuranyl, which groups may be substituted with one or more halogen or alkyl (1-3C); n has the value 0-3; m has the value 0-2; R 1 represents NH 2 , NH-alkyl (1-3C), dialkyl (1-3C)N, morpholino or morpholino substituted with one or two methyl and/or methoxymethyl groups, thiomorpholino, 1,1-dioxothiomorpholino, 2-, 3- or 4-pyridyl or 4-CH 3 -piperazinyl; R 2 is hydrogen, alkyl (1-4C) or phenyl, or R 2 together with (CH 2 ) m wherein m is 1, and the intermediate carbon, nitrogen and oxygen atoms forms an isoxazolyl or a 4,5-dihydroisoxazolyl group; R 3 and R 4 independently represent hydrogen or methyl, or R 3 and R 4 together are oxygen. The invention also relates to a method for the preparation of the novel compounds, and to pharmaceutical compositions comprising compounds with formula (1) as an active ingredient and the use of these compounds for the treatment of disorders in which neurokinin-1 receptors are involved.

    Abstract translation: 本发明涉及一组具有有趣的NK-1拮抗活性的新型哌嗪肟衍生物。 本发明涉及通式（1）的化合物，其中：X表示苯基或被1或2个取代基取代的吡啶基，所述取代基为CH 3，CF 3，OCH 3，卤素，氰基和5-CF > 3 < - 四唑-1-基; Y代表2-或3-吲哚基，苯基，7-氮杂 - 吲哚-3-基或3-吲唑基，2-萘基，3-苯并[b]噻吩基，2-苯并呋喃基，它们可以被一个或多个 卤素或烷基（1-3C）; n的值为0-3; m的值为0-2; R 1表示被一个或两个甲基和/或甲氧基甲基取代的二烷基（1-3C）N，吗啉代或吗啉代，硫代吗啉代，1,1-二氧代硫代吗啉代， 2-，3-或4-吡啶基或4- CH 3'-哌嗪基; R 2是氢，烷基（1-4C）或苯基，或R 2与（CH 2）m（其中m是1）一起，中间体碳，氮和氧原子形成异恶唑基或 4,5-二氢异恶唑基; R 3和R 4独立地代表氢或甲基，或R 3和R 4一起是氧。 本发明还涉及一种制备新化合物的方法，以及包含式（1）化合物作为活性成分的药物组合物，以及这些化合物用于治疗涉及神经激肽-1受体的疾病的用途。

    N-OXIDES AS PRODRUGS OF PIPERAZINE & PIPERIDINE DERIVATIVES
    5.
    发明申请
    N-OXIDES AS PRODRUGS OF PIPERAZINE & PIPERIDINE DERIVATIVES 审中-公开
    N-氧化物作为哌嗪和哌啶衍生物的制剂

    公开(公告)号：WO2007023141A1

    公开(公告)日：2007-03-01

    申请号：PCT/EP2006/065477

    申请日：2006-08-21

    Applicant: SOLVAY PHARMACEUTICALS B.V. ,  KOOPMAN, Theodorus, S., M. ,  KOSTER, Hendrik, J. ,  VAN AMSTERDAM, Peter, H. ,  FEENSTRA, Roelof, W. ,  VERHAGE, Marinus ,  MCCREARY, Andrew, C. ,  HESSELINK, Mayke, B. ,  VAN SCHARRENBURG, Gustaaf, J., M.

    Inventor： KOOPMAN, Theodorus, S., M. ,  KOSTER, Hendrik, J. ,  VAN AMSTERDAM, Peter, H. ,  FEENSTRA, Roelof, W. ,  VERHAGE, Marinus ,  MCCREARY, Andrew, C. ,  HESSELINK, Mayke, B. ,  VAN SCHARRENBURG, Gustaaf, J., M.

    IPC: C07D263/58 ,  A61K31/423 ,  A61P25/00 ,  C07D295/24

    CPC classification number: C07D263/58

    Abstract: The present invention relates to N-oxides of certain piperazine and piperidine derivatives and to methods for the preparation of these compounds. The invention also relates to the use of compounds disclosed herein for the manufacture of a medicament giving a beneficial effect. A beneficial effect is disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art. The invention also relates to the use of a compound of the invention for the manufacture of a medicament for treating or preventing a disease or condition. More particularly, the invention relates to a new use for the treatment of a disease or condition disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art. In embodiments of the invention specific compounds disclosed herein are used for the manufacture of a medicament useful in the treatment of CNS-disorders, in particular the treatment of anxiety disorders, including generalized anxiety disorder and panic disorder, obsessive compulsive disorder, aggression, addiction (including craving), depression, autism, vertigo, schizophrenia and other psychotic disorders, Parkinson's disease and disturbances of cognition and memory. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.

    Abstract translation: 本发明涉及某些哌嗪和哌啶衍生物的N-氧化物及其制备方法。 本发明还涉及本文公开的化合物用于制备产生有益效果的药物的用途。 本领域技术人员根据本领域的技术人员和一般知识，在此公开有益效果或显而易见的。 本发明还涉及本发明化合物在制备用于治疗或预防疾病或病症的药物中的用途。 更具体地说，本发明涉及本领域技术人员从本领域技术人员的说明书和一般知识中治疗本文所揭示的疾病或病症的新用途。 在本发明的实施方案中，本文公开的具体化合物用于制备可用于治疗CNS病症的药物，特别是治疗焦虑症，包括广泛性焦虑症和惊恐障碍，强迫症，侵略，成瘾（ 包括渴望），抑郁症，自闭症，眩晕，精神分裂症等精神障碍，帕金森氏病和认知和记忆障碍。 化合物具有通式（1），其中符号具有说明书中给出的含义。

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