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    N-OXIDES OF PYRIDYLMETHYL -PIPERAZINE AND -PIPERIDINE DERIVATIVES
    1.
    发明申请
    N-OXIDES OF PYRIDYLMETHYL -PIPERAZINE AND -PIPERIDINE DERIVATIVES 审中-公开
    吡咯并吡啶和哌啶衍生物的N-氧化物

    公开(公告)号：US20070275977A1

    公开(公告)日：2007-11-29

    申请号：US11743049

    申请日：2007-05-01

    申请人： Marcel Van Aar ,  Peter Van Amsterdam ,  Gerrit Barf ,  Johan Bakker ,  Cathaline Den Besten ,  Arnoldus Herremans ,  Jan Zorgdrager

    发明人： Marcel Van Aar ,  Peter Van Amsterdam ,  Gerrit Barf ,  Johan Bakker ,  Cathaline Den Besten ,  Arnoldus Herremans ,  Jan Zorgdrager

    IPC分类号： A61K31/496 ,  C07D405/14

    CPC分类号： C07D405/12

    摘要： N-oxides of certain pyridylmethylpiperazine and -piperidine derivatives are provided as alternatives to or as “prodrugs” of their respective parent compounds, as well as pharmaceutical compositions containing these N-oxides, methods for preparing them, and compositions comprising them. The N-oxides have the formula (a) wherein the substituents have the meanings given in the description, and wherein the oxidized nitrogen atom can be the nitrogen atom in the pyridyl ring of R5, or the nitrogen atom in the piperidine ring (when Z is carbon) or either one of the nitrogen atoms in the piperazine ring (when Z is nitrogen), or both the nitrogen atom connected to R5 via a methylene group, and the nitrogen atom in the pyridyl ring of R5, and tautomers, stereoisomers, pharmacologically acceptable salts, hydrates, and solvates thereof. In addition, the N-oxides and compositions can be used as medicaments useful in the treatment of affections or diseases of the central nervous system caused by disturbances in either the dopaminergic or serotinergic systems.

    摘要翻译： 提供某些吡啶基甲基哌嗪和哌啶衍生物的N-氧化物作为其各自母体化合物的“前体药物”的替代物或含有这些N-氧化物的药物组合物，其制备方法和包含它们的组合物。 N-氧化物具有式（a），其中取代基具有本说明书中给出的含义，其中氧化的氮原子可以是R 5的吡啶环中的氮原子，或氮 哌啶环中的一个原子（当Z为碳时）或哌嗪环中的氮原子之一（当Z为氮时），或通过亚甲基与R 5连接的氮原子， 和R 5的吡啶环中的氮原子，以及互变异构体，立体异构体，药理学上可接受的盐，水合物和溶剂化物。 此外，N-氧化物和组合物可以用作治疗由多巴胺能或血清素能系统中的紊乱引起的中枢神经系统的情感或疾病的药物。

    NOVEL MEDICAL USES OF 4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVES HAVING CB1- ANTAGONISTIC ACTIVITY
    3.
    发明申请
    NOVEL MEDICAL USES OF 4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVES HAVING CB1- ANTAGONISTIC ACTIVITY 审中-公开
    具有CB1-拮抗活性的4,5-二氢-1H-吡唑衍生物的新医学用途

    公开(公告)号：US20050239859A2

    公开(公告)日：2005-10-27

    申请号：US10929377

    申请日：2004-08-31

    申请人： Jochen Antel ,  Gunter Krause ,  Josephus Lange ,  Cornelis Kruse ,  Peter-Colin Gregory ,  Cathaline Den Besten

    发明人： Jochen Antel ,  Gunter Krause ,  Josephus Lange ,  Cornelis Kruse ,  Peter-Colin Gregory ,  Cathaline Den Besten

    IPC分类号： A61K31/415

    CPC分类号： A61K31/415

    摘要： Abstract of the DisclosureThe present invention relates to a novel medical use of 4,5-dihydro-1H-pyrazole compounds which are potent antagonists of the cannabis CB1-receptor. Said compounds are particularly suitable in the manufacture of medicaments for the treatment and/or prophylaxis of CB1 receptor related diseases in juvenile patients and/or for the treatment and/or prophylaxis of drug induced obesity in juvenile as well as in adolescent patients. The compounds have the general formula (I) wherein the group Bb represents sulfonyl or carbonyl, and the substituents R, R1, R2 and R3, and the group Aa are defined as shown in the description.

    摘要翻译： 本发明摘要本发明涉及作为大麻CB 1受体的有效拮抗剂的4,5-二氢-1H-吡唑化合物的新型医疗用途。 所述化合物特别适用于制备用于治疗和/或预防少年患者中CB 1受体相关疾病的药物和/或用于治疗和/或预防未成年人药物诱导的肥胖的药物 就像青少年患者一样。 化合物具有通式（I），其中基团Bb表示磺酰基或羰基，取代基R 1，R 1，R 2和R 3， SUB>，并且组Aa如说明书所示定义。