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20 条记录 (耗时 0.013 秒)

    Pharmacologically active CNS compound
    5.
    发明公开
    Pharmacologically active CNS compound 失效
    药物活性CNS化合物

    公开(公告)号：EP0459819A3

    公开(公告)日：1992-03-11

    申请号：EP91304935.9

    申请日：1991-05-31

    申请人： THE WELLCOME FOUNDATION LIMITED

    发明人： Leach, Michael John ,  Nobbs, Malcolm Stuart ,  Iyer, Ramachandran ,  Yeates, Clive Leonard ,  Skone, Philip Alan

    IPC分类号： C07D239/48 ,  A61K31/505

    CPC分类号： C07D239/48

    摘要： The invention provides a series of compounds of formula (I)

    and salts thereof, wherein for example,
    R¹ and R², which may be the same or different each represent -NR¹³R¹⁴ where R¹³ and R¹⁴ may each independently represent hydrogen or alkyl or, taken together with the nitrogen atom to which they are attached form a heterocyclic ring, optionally substituted by one or more alkyl or arylalkyl groups and optionally containing a further heteroatom;
    R³ is hydrogen, haloalkyl, alkoxymethyl or alkyl;
    R⁴ is hydrogen, nitro or halo;
    R⁵ is hydrogen or halo;
    R⁶ is hydrogen, halo, nitro, amino, alkylamino or dialkylamino;
    R⁷ is hydrogen or halo;
    R⁸ is hydrogen or halo; The compounds may be used for the treatment or prophylaxis of a neurodegenerative or other neurological disorder of the CNS, the aetiology or which includes excessive release of the neurotransmitter glutamate.

    Aryl derivatives of heterobicyclic compounds
    10.
    发明公开
    Aryl derivatives of heterobicyclic compounds 失效
    芳族化合物的芳基衍生物

    公开(公告)号：EP0166609A3

    公开(公告)日：1987-06-10

    申请号：EP85304548

    申请日：1985-06-26

    申请人： THE WELLCOME FOUNDATION LIMITED

    发明人： Barraclough, Paul ,  Smith, Steven ,  Iyer, Ramachandran ,  Nobbs, Malcolm Stuart

    IPC分类号： C07D487/04 ,  A61K31/495 ,  A61K31/505 ,  C07D241/00 ,  C07D235/00 ,  C07D239/00

    CPC分类号： C07D487/04

    摘要： The invention relates to use of compounds of formula (I)
    wherein
    n is 1, 2 or 3; m is 0, 1, 2 or 3; any one of A', A 2 and A 3 is nitrogen and the other two are CH; R' groups are independently selected from those specified in (a) and (b) below, namely: (a) cyano, hydroxy, groups of formula -S(O) x R a in which x is 0, 1 or 2 and R a is a C 1-4 alkyl group and groups of formula -OR b in which R b is allyl or a C 1-4 alkyl group, which alkyl group is optionally substituted by one or more radicals selected from halo, C 1-4 alkoxy and groups of formula -S(O) x R a in which x and R a are as defined above; (b) C 1-4 alkanoyl, C 1-4 alkanoylamino, 2-methyl-1,3-dioxalan-2-yl, sulphamoyl, N-C 1-4 alkylsulphamoyl, N, N-di-C 1-4 alkylsulphamoyl, C 1-4 alkylsulphonyloxy, C 1-4 alkylsulphonylamino, aminosulphonyloxy, N-C 1-4 alkylaminosulphonyloxy, N,N-di-C 1-4 alkylaminosulphonyloxy, ureido, 3-C 1-4 alkylureido, 3,3-di-C 1-4 alkylureido, aminosulphonylamino, (C 1-4 alkylaminosulphonyl)amino, (di-C 1-4 alkylaminosulphonyl)-animo, carboxy, carboxylic derivatives (selected from carbamoyl, N-C 1-4 alkylcarbamoyl, N, N-di-C 1-4 alkylcarbamoyl, carboxylic acid halides, C 1-4 alkoxycarbonyl, hydroxy-C 1-4 alkoxycarbonyl and hydroxymethylene) and groups of formula -OR c in which R e is a straight or branched aliphatic moiety having 1 to 4 carbon atoms, optionally substituted by one or more radicals independently selected from halo, C 1-4 alkoxy and groups of formula -S(O) x R a in which x and R a are as defined above, provided that R° is not a group as defined for R b above; R 2 is selected from hydrogen, halo, amino, hydroxy, C 1-4 alkyl and C 1-4 alkoxy; R 3 groups are independently selected from halo, carboxy, amino, C 1-4 alkylamino hydroxy, C 1-4 alkoxy, hydroxy-C 1-4 alkoxy, C 1-4 alkylthio and C 1-4 alkylsulphonyloxy; provided that when R 2 is hydrogen and either m is 0 or m is 1 and R 3 represents halo, then at least one R' group must be selected from (b) above; and physiologically acceptable salts and/or N-oxides thereof, as inotropic agents, and to pharmaceutical formulations containing them. The invention also includes compounds of formula (I) (including physiologically acceptable salts and/or their N-oxides) perse, with the proviso that when n and m are both 1, and R 2 is H, then when A' is nitrogen, A 2 and A 3 are both CH and R' is a 4-methoxy group, R 3 is nota 7-methoxy group, and when A 3 is nitrogen and A' and A 2 are both CH and R' is a 4-methylsulphonyl group, R 3 is not a 6-methoxy group, and processes for their preparation.

    摘要翻译： 本发明涉及式（I）化合物的用途，其中n为1,2或3; m为0,1,2或3; A 1，A 2和A 3中的任一个是氮，另外两个是CH; R 1独立地选自下面的（a）和（b）中指定的那些，即：（a）氰基，羟基，式-S（O）x R 8的基团，其中x是0,1或 2和R a是C 1-4烷基和式-OR b的基团，其中R b是烯丙基或C 1-4烷基，该烷基任选被一个或多个选自下列的基团取代： 卤素，C 1-4烷氧基和式-S（O）x R a基团，其中x和R a如上定义（b）C 1-4烷酰基，C 1-4烷酰基氨基，2-甲基-1 ，3-二氧杂环戊烷-2-基，氨磺酰基，N-C 1-4烷基氨磺酰基，N，N-二-C 1-4烷基氨磺酰基，C 1-4烷基磺酰氧基，C 1-4烷基磺酰基氨基，氨基磺酰氧基，N-C 1-4烷基氨基磺酰氧基，N， 二-C 1-4烷基氨基磺酰氧基，脲基，3-C 1-4烷基脲基，3,3-二-C 1-4烷基脲基，氨基磺酰基氨基，（C 1-4烷基氨基磺酰基）氨基，（二-C 1-4烷基氨基磺酰基） 衍生物（选自氨基甲酰基，N-C 1-4烷基氨基甲酰基，N，N-二-C 1-4烷基氨基甲酰基，羧酸卤化物，C 1-4烷氧基 羰基，羟基-C 1-4烷氧基羰基和羟基亚甲基）和式-COR的基团，其中R c是具有1至4个碳原子的直链或支链脂族部分，任选地被一个或多个独立地选自 卤素，C 1-4烷氧基和式-S（O）x R a基团，其中x和R a如上所定义，条件是R c不是如上定义的基团 ; R 2选自氢，卤素，氨基，羟基，C 1-4烷基和C 1-4烷氧基; R 3基团独立地选自卤素，羧基。 氨基C 1-4烷基氨基羟基，C 1-4烷氧基，羟基-C 1-4烷氧基，C 1-4烷硫基和C 1-4烷基磺酰氧基; 条件是当R 2为氢且m为0或m为1且R 3为卤素时，则至少一个R 1基团必须选自上述（b）; 和其生理上可接受的盐和/或N-氧化物，作为变力剂，以及含有它们的药物制剂。