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    • 1. 发明授权
    • Piperazine, piperidine and tetrahydropyridine derivatives
    • 哌嗪,哌啶和四氢吡啶衍生物
    • US5977116A
    • 1999-11-02
    • US68680
    • 1998-05-12
    • Jose Luis Castro PineiroAngus Murray MacLeodMichael RowleyMonique Bodil Van Niel
    • Jose Luis Castro PineiroAngus Murray MacLeodMichael RowleyMonique Bodil Van Niel
    • C07D521/00A01N43/60C07D401/00C07D403/00C07D413/00
    • C07D231/12C07D233/56C07D249/08
    • A class of N-substituted piperazine, piperidine and tetrahydropyridine derivatives, linked by a fluoro-substituted alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and further substituted at the 4-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D recptor agonists.
    • PCT No.PCT / GB96 / 02762 Sec。 371日期:1998年5月12日 102(e)日期1998年5月12日PCT提交1996年11月13日PCT公布。 公开号WO97 / 18203 日期1997年5月22日一类N-取代的哌嗪,哌啶和四氢吡啶衍生物通过氟取代的亚烷基链连接到稠合双环杂芳族部分如吲哚基,并且在4-位被进一步被任选取代的烯基,炔基 ,芳基 - 烷基或杂芳基 - 烷基部分是5-HT1样受体的选择性激动剂,是人类5-HT1Dα受体亚型的有效激动剂,同时对5-HT1Dα受体具有至少10倍的选择性亲和力 亚型相对于5-HT1D beta亚型; 因此,它们可用于治疗和/或预防临床状况,特别是偏头痛和相关疾病,其中指出5-HT1D受体的亚型选择性激动剂,同时引起较少的副作用,特别是不利的心血管事件,比 与非亚型选择性5-HT1D受体激动剂相关的那些。
    • 5. 发明授权
    • Azetidine, pyrrolidine and piperidine derivatives
    • 氮杂环丁烷,吡咯烷和哌啶衍生物
    • US5998440A
    • 1999-12-07
    • US68620
    • 1998-05-08
    • Jose Luis Castro PineiroAngus Murray MacLeodMonique Bodil Van Niel
    • Jose Luis Castro PineiroAngus Murray MacLeodMonique Bodil Van Niel
    • C07D521/00A61K31/445C07D401/06
    • C07D231/12C07D233/56C07D249/08
    • A class of substituted azetidine, pyrrolidine and piperidine derivatives, linked by a fluoro-substituted alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
    • PCT No.PCT / GB96 / 02764 Sec。 371日期1998年5月8日 102(e)日期1998年5月8日PCT 1996年11月13日PCT PCT。 第WO97 / 18201号公报 日期1997年5月22日一类通过氟取代的亚烷基链连接到稠合双环杂芳族部分如吲哚基的氮杂环丁烷,吡咯烷和哌啶衍生物是5-HT1样受体的选择性激动剂,是人的有效激动剂 5-HT1Dα受体亚型,同时相对于5-HT1Dβ亚型对5-HT1Dα受体亚型具有至少10倍的选择性亲和力; 因此,它们可用于治疗和/或预防临床症状,特别是偏头痛和相关疾病,其中指出5-HT1D受体的亚型选择性激动剂,同时引起更少的副作用,特别是不利的心血管事件,比 与非亚型选择性5-HT1D受体激动剂相关的那些。