PYRIDOPYRIMIDONE DERIVATIVES, PREPARATION THEREOF, THERAPEUTIC USE THEREOF
    54.
    发明申请
    PYRIDOPYRIMIDONE DERIVATIVES, PREPARATION THEREOF, THERAPEUTIC USE THEREOF 失效
    吡咯烷酮衍生物,其制备方法,其治疗方法

    公开(公告)号:US20090048277A1

    公开(公告)日:2009-02-19

    申请号:US12166431

    申请日:2008-07-02

    IPC分类号: A61K31/519 C07D471/04

    CPC分类号: C07D471/04

    摘要: The disclosure relates to pyrido[2,3-d]pyrimidone compounds, to the preparation thereof and to the therapeutic use thereof, wherein said compounds are of general formula (I): in the form of a base or of an addition salt with an acid which is pharmaceutically acceptable, in the form of hydrates or of solvates, and also in the form of enantiomers, diastereoisomers and a mixture thereof. The disclosure also relates to processes for preparing said compounds, to pharmaceutical compositions containing a compound of general formula (I), and to the therapeutic use of said compounds and compositions.

    摘要翻译: 本公开涉及吡啶并[2,3-d]嘧啶酮化合物,其制备方法及其治疗用途,其中所述化合物为通式(I):以碱的形式或加成盐与 其为药学上可接受的,为水合物或溶剂化物形式,也为对映异构体,非对映异构体及其混合物的形式。 本公开还涉及制备所述化合物的方法,含有通式(I)化合物的药物组合物以及所述化合物和组合物的治疗用途。

    Aralkyltetrahydropyridines, Their Preparation and Pharmaceutical Compositions Containing Them
    57.
    发明申请
    Aralkyltetrahydropyridines, Their Preparation and Pharmaceutical Compositions Containing Them 失效
    芳烷基四氢吡啶,它们的制备和含有它们的药物组合物

    公开(公告)号:US20080097117A1

    公开(公告)日:2008-04-24

    申请号:US11958476

    申请日:2007-12-18

    IPC分类号: C07C61/29

    CPC分类号: C07D401/04 C07D211/70

    摘要: The present invention relates to compounds of formula (I): in which X represents N or CH; R1 represents a hydrogen or halogen atom or a CF3 group; n is an integer from 1 to 5; A represents a partially saturated carbonaceous bi- or tricycle; it also relates to their salts, solvates, N-oxides, the pharmaceutical compositions containing them, a method for their preparation and synthesis intermediates in this method.

    摘要翻译: 本发明涉及式(I)化合物:其中X表示N或CH; R 1表示氢或卤素原子或CF 3 N 3基团; n为1〜5的整数; A表示部分饱和的碳质二元或三轮车; 它还涉及它们的盐,溶剂合物,N-氧化物,含有它们的药物组合物,其制备方法和该方法中的合成中间体。

    Use of tetrahydropyridine derivatives to prepare medicines for treating diseases causing demyelination

    公开(公告)号:US06344464B1

    公开(公告)日:2002-02-05

    申请号:US09403507

    申请日:2000-04-18

    IPC分类号: A61K31445

    CPC分类号: A61K31/444 A61K31/4418

    摘要: The invention relates to the use of tetrahydropyridine derivatives of the formula in which: R1 is a halogen or a CF3, (C1-C4)alkyl or (C1-C4)alkoxy group; Y is a nitrogen atom or a CH group; Z′ and Z″ are each hydrogen or a (C1-C3)alkyl group, or one is hydrogen and the other is a hydroxyl group, or the two together are an oxo group; and Z is: a phenyl radical; a phenyl radical monosubstituted by a substituent X, X being: (a) a (C1-C6)alkyl, (C1-C6)alkoxy, (C3-C7)carboxyalkyl, (C1-C4)alkoxycarbonyl(C1-C6)alkyl, (C3-C7)carboxyalkoxy or (C1-C4)alkoxycarbonyl(C1-C6)alkoxy group; (b) a group selected from (C3-C7)cycloalkyl, (C3-C7)cycloalkoxy, (C3-C7)cycloalkylmethyl, (C3-C7)cycloalkylamino and cyclohexenyl, it being possible for said group to be substituted by a halogen, hydroxy, (C1-C4)alkoxy, carboxy, (C1-C4)alkoxycarbonyl, amino or mono- or di-(C1-C4)alkylamino group; or (c) a group selected from phenyl, phenoxy, phenylamino, N—(C1-C3)alkyl-phenylamino, phenylmethyl, phenylethyl, phenylcarbonyl, phenylthio, phenylsulfonyl, phenylsulfinyl and styryl, it being possible for said group to be monosubstituted or polysubstituted on the phenyl group by a halogen, CF3, (C1-C4)alkyl, (C1-C4)alkoxy, cyano, amino, mono- or di-(C1-C4)alkylamino, (C1-C4)acylamino, carboxy, (C1-C4)alkoxycarbonyl, aminocarbonyl, mono- or di-(C1-C4)alkylaminocarbonyl, amino(C1-C4)alkyl, hydroxy(C1-C4)alkyl or halogeno(C1-C4)alkyl group; a phenyl radical disubstituted by a substituent R2, R2 being a halogen or a hydroxy, methyl, ethyl, (C3-C6)alkyl, (C1-C4)alkoxy or trifluoromethyl group, and by a substituent X, X being as defined above; a 1-naphthyl or 2-naphthyl radical; or a 1-naphthyl or 2-naphthyl radical substituted in the 5-, 6-, 7- and/or 8-positions by one or two hydroxy groups, one or two (C1-C4)alkoxy groups or a 6,7-methylenedioxy group; or Z″ is hydrogen and Z and Z′ are each independently an unsubstituted or mono-, di- or tri-substituted phenyl group, or a pharmaceutically acceptable salt and solvate thereof, for the preparation of pharmaceutical compositions intended for treating diseases which cause demyelination.