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    Compounds active at the histamine H3 receptor
    1.
    发明公开
    Compounds active at the histamine H3 receptor 审中-公开
    组胺H3 Rezeptor aktive Verbindungen

    公开(公告)号：EP2386554A1

    公开(公告)日：2011-11-16

    申请号：EP11176842.0

    申请日：2006-06-30

    申请人： High Point Pharmaceuticals, LLC

    发明人： Hohlweg, Rolf ,  Andersen, Knud Erik ,  Sörensen, Jan, Lindy ,  Lundbeck, Jane Marie

    IPC分类号： C07D405/04 ,  A61K31/501 ,  C07D237/20 ,  C07D417/10 ,  C07D213/74

    CPC分类号： C07D213/74 ,  C07D213/84 ,  C07D213/87 ,  C07D237/20 ,  C07D403/04 ,  C07D403/12 ,  C07D417/10

    摘要： Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.

    摘要翻译： 定义与组胺H3受体相互作用的新型化合物。 这些化合物特别可用于治疗组胺H3相互作用有益的各种疾病或病症。 因此，该化合物可用于例如治疗中枢神经系统，周围神经系统，心血管系统，肺系统，胃肠系统和内分泌系统的疾病。 新化合物具有由在环中含有至少一个氮原子和两个碳原子的6元芳香环组成的核心，并且在环的其余位置上有碳原子或氮原子。

    Benzodioxolylcyclopropylpiperazinylpyridazines
    2.
    发明公开
    Benzodioxolylcyclopropylpiperazinylpyridazines 审中-公开

    公开(公告)号：EP2402324A1

    公开(公告)日：2012-01-04

    申请号：EP11182795.2

    申请日：2007-05-22

    申请人： High Point Pharmaceuticals, LLC

    发明人： Hohlweg, Rolf

    IPC分类号： C07D237/20 ,  C07D405/04

    CPC分类号： C07D405/04

    摘要： A process for synthesizing 3-(1,3-benzodioxol-5-yl)-6-(4-cyclopropylpiperazin-1-yl)pyridazine, where the process comprises reacting 3-chloro-6-(4-cyclopropyl-piperazin-1-yl)pyridazine with 3,4-methylene-dioxybenzene boronic acid.

    摘要翻译： 合成3-（1,3-苯并间二氧杂环戊烯-5-基）-6-（4-环丙基哌嗪-1-基）哒嗪的方法，其中该方法包括使3-氯-6-（4-环丙基 - 哌嗪-1 - 基）哒嗪与3,4-亚甲基 - 二氧苯硼酸反应。

    New heteocyclic h3 antagonists
    5.
    发明公开
    New heteocyclic h3 antagonists 审中-公开
    新的杂环H3拮抗剂

    公开(公告)号：EP2014656A3

    公开(公告)日：2011-08-24

    申请号：EP07109949.3

    申请日：2007-06-11

    申请人： High Point Pharmaceuticals, LLC

    发明人： Hohlweg, Rolf ,  Lundbeck, Jane Marie ,  De jong, Johannes Cornelis

    IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14

    CPC分类号： C07D405/14 ,  C07D401/04 ,  C07D401/14 ,  C07D413/10 ,  C07D413/14

    摘要： Compound of formula I

    wherein W, X, Y, Z is -C(R 1 )= or N; R 1 is hydrogen or alkyl, V is N or C (i.e. carbon),
    A is a bond or an alkylene linker with 1 to 3 carbon atoms, with the proviso that when A is a bond, V must be CH, R is ethyl, propyl, a branched C 3-6 alkyl or a cyclic C 3-8 alkyl, m and n is 1-3, D is heteroaryl optionally substituted with halogen, hydroxy, cyano, alkyl, cycloalkyl, alkoxy, -(CH 2 ) o -(C=O) p -NR 2 R 3 , or D is aryl optionally substituted with one or more of the groups independently selected from hydrogen, halogen, hydroxy, cyano, alkyl, cycloalkyl, haloalkyl, alkoxy, haloalkoxy, alkylsulfonyl, alkylsulfinyl, heterocyclyl, heterocyclylalkyl, heterocyclylalkoxy, heterocyclylcarbonyl, alkylcarbonyl, alkoxycarbonyl, alkylcarboxy, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, alkylcarbonylamino, alkylcarbonylaminoalkyl, arylcarbonylamino, arylcarbonylaminoalkyl, heteroarylcarbonylamino or heteroarylcarbonylaminoalkyl, -(CH 2 ) o -(C=O) p -NR 2 R 3 , wherein o is 0-3, p is 0 or 1, and R 2 and R 3 independently are hydrogen, alkyl or cycloalkyl; or R 2 and R 3 can together with the attached nitrogen form a heterocyclyl group, and salts and solvates thereof have binding affinity for the histamine H3 receptor.