FUSED AMINODIHYDROPYRIMIDONE DERIVATIVES
    1.
    发明申请
    FUSED AMINODIHYDROPYRIMIDONE DERIVATIVES 有权
    熔融的氨基二氢咪唑啉酮衍生物

    公开(公告)号:US20120202828A1

    公开(公告)日:2012-08-09

    申请号:US13386199

    申请日:2010-07-21

    CPC分类号: C07D491/048

    摘要: A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1, R2 and Rx are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.

    摘要翻译: 由通式(I)表示的化合物或其药学上可接受的盐或其溶剂合物,其中环A为C 6-14芳基等,L为-NReCO-等(其中Re为氢原子 等),环B为C 6-14芳基等,X为C 1-3亚烷基等,Y为单键等,Z为C1-3亚烷基等 R 1,R 2和R 3各自独立地为氢原子等,R 3,R 4,R 5和R 6独立地为氢原子,卤素原子等,具有A&bgr; 产生抑制作用或BACE1抑制作用,可用作由A&Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。

    Fused aminodihydropyrimidone derivatives
    2.
    发明授权
    Fused aminodihydropyrimidone derivatives 有权
    熔融氨基二氢嘧啶酮衍生物

    公开(公告)号:US09139594B2

    公开(公告)日:2015-09-22

    申请号:US13386199

    申请日:2010-07-21

    CPC分类号: C07D491/048

    摘要: A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1, R2 and Rx are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.

    摘要翻译: 由通式(I)表示的化合物或其药学上可接受的盐或其溶剂合物,其中环A为C 6-14芳基等,L为-NReCO-等(其中Re为氢原子 等),环B为C 6-14芳基等,X为C 1-3亚烷基等,Y为单键等,Z为C1-3亚烷基等 R 1,R 2和R 3各自独立地为氢原子等,R 3,R 4,R 5和R 6独立地为氢原子,卤素原子等,具有A&bgr; 产生抑制作用或BACE1抑制作用,可用作由A&Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。

    Azetidine, pyrrolidine and piperidine derivatives as 5-HT receptor
agonists
    8.
    发明授权
    Azetidine, pyrrolidine and piperidine derivatives as 5-HT receptor agonists 失效
    氮杂环丁烷,吡咯烷和哌啶衍生物作为5-HT受体激动剂

    公开(公告)号:US6140347A

    公开(公告)日:2000-10-31

    申请号:US171208

    申请日:1998-10-14

    摘要: A class of compounds of formula (I) wherein Z, E, Q, T, U, V, W, M, R.sup.1, R.sup.7 and R.sup.8 are as defined herein; 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 receptor agonists. ##STR1##

    摘要翻译: PCT No.PCT / GB97 / 01137 Sec。 371日期:1998年10月14日 102(e)日期1998年10月14日PCT 1997年4月24日PCT公布。 出版物WO97 / 42189 日期:1997年11月13日一类其中Z,E,Q,T,U,V,W,M,R 1,R 7和R 8如本文所定义的式(I)化合物; 是5-HT1样受体的选择性激动剂,其是人类5-HT1Dα受体亚型的有效激动剂,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。