Phenyl- and pyridylpiperidines with TNF activity
    34.
    发明授权
    Phenyl- and pyridylpiperidines with TNF activity 失效
    具有TNF活性的苯基和吡啶基哌啶

    公开(公告)号:US07326720B2

    公开(公告)日:2008-02-05

    申请号:US10475272

    申请日:2002-04-19

    CPC分类号: C07D401/06

    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; R2 and R3 independently represent a hydrogen atom or a methyl group; n is 0 or 1; A represents a condensed heterocyclic group of formula (w) where W completes an aromatic or saturated 6-membered ring system comprising one or two nitrogen atoms or else an aromatic or saturated 5-membered ring system comprising a nitrogen, oxygen or sulfur atom which are optionally substituted, and to their N-oxides and to their salts or solvates, to the pharmaceutical compositions and the medicaments comprising them and to a process for their preparation.

    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; R 2和R 3独立地表示氢原子或甲基; n为0或1; A表示式(w)的稠合杂环基,其中W完成包含一个或两个氮原子的芳族或饱和的6-元环系统,或包含氮,氧或硫原子的芳族或饱和五元环系统, 任选取代,并且与它们的N-氧化物及其盐或溶剂合物相关的药物组合物和包含它们的药物及其制备方法。

    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.

    Therapeutic use for treating of leukemia
    40.
    发明授权
    Therapeutic use for treating of leukemia 失效
    治疗白血病的治疗用途

    公开(公告)号:US08236811B2

    公开(公告)日:2012-08-07

    申请号:US12485401

    申请日:2009-06-16

    IPC分类号: A61K31/519

    摘要: The disclosure relates to methods of treating leukaemia, in particular myeloid leukaemia, comprising administering the compound N-[2-(2,1,3-benzothiadiazol-5-ylamino)-6-(2,6-dichlorophenyl)pyrido[2,3-d]pyrimidin-7-yl]-N′-(1,1-dimethylethyl)-urea or a hydrate, a pharmaceutically acceptable salt or a solvate thereof.

    摘要翻译: 本公开涉及治疗白血病,特别是骨髓性白血病的方法,包括给予化合物N- [2-(2,1,3-苯并噻二唑-5-基氨基)-6-(2,6-二氯苯基)吡啶并[ 3-d]嘧啶-7-基] -N' - (1,1-二甲基乙基) - 脲或其水合物,其药学上可接受的盐或溶剂化物。