Phenyl- and pyridylpiperidines with TNF activity
    23.
    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。

    Pyrido-pyrimidine derivatives, preparation thereof, and therapeutic use thereof
    24.
    发明申请
    Pyrido-pyrimidine derivatives, preparation thereof, and therapeutic use thereof 有权
    吡啶并嘧啶衍生物及其制备方法及其治疗用途

    公开(公告)号:US20070167469A1

    公开(公告)日:2007-07-19

    申请号:US11651376

    申请日:2007-01-08

    IPC分类号: A61K31/519 C07D487/02

    CPC分类号: C07D471/04

    摘要: The disclosure concerns pyrido[2,3-d]pyrimidine derivatives, their preparation and their therapeutic application, of general formula (I) and acid addition salts, hydrates and solvates thereof, as well as in the form of enantiomers, diastereoisomers and mixtures thereof. The disclosure also concerns methods for preparing said derivatives, pharmaceutical compositions containing a compound of general formula (I), and their therapeutic use.

    摘要翻译: 本公开涉及通式(I)的吡啶并[2,3-d]嘧啶衍生物及其制备方法及其治疗应用,以及其对映异构体,非对映异构体及其混合物的酸加成盐,水合物和溶剂化物 。 本公开还涉及制备所述衍生物的方法,含有通式(I)的化合物的药物组合物及其治疗用途。

    Pyridoindolone derivatives substituted in the 3-position by a heterocyclic group, their preparation and their application in therapeutics
    28.
    发明申请
    Pyridoindolone derivatives substituted in the 3-position by a heterocyclic group, their preparation and their application in therapeutics 失效
    吡啶并吲哚酮衍生物在3位被杂环基取代,其制备及其在治疗中的应用

    公开(公告)号:US20050222192A1

    公开(公告)日:2005-10-06

    申请号:US11109121

    申请日:2005-04-19

    CPC分类号: C07D471/04

    摘要: The present invention relates to pyridoindolone derivatives substituted in the 3-position by a heterocyclic group of general formula (I): in which: R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 represents a hydrogen atom or a (C1-C4)alkyl group; R3 represents a thienyl mono- or polysubstituted by a methyl group; or a monocyclic or bicyclic heterocyclic radical chosen from: a pyridyl, an N-oxidopyridinio, a pyrazolyl, an (N-phenyl)pyrazolyl, an (N-halophenyl)pyrazolyl, a furyl, an indolyl, an (N-benzyl)indolyl, an (N-halobenzyl)indolyl, a benzothienyl or a benzofuryl, the said radicals being unsubstituted or substituted one or more times by a halogen atom or a methyl or methoxy group; R4 and R5 are identical or different and each independently represent a hydrogen or halogen atom or a hydroxyl, hydroxymethyl, (C1-C4)alkyl, trifluoromethyl, C1-C4)alkoxy, (C1-C4)alkoxycarbonyl or cyano group. Preparation process and application in therapeutics.

    摘要翻译: 本发明涉及通式(I)的杂环基在3-位上取代的吡啶并吲哚酮衍生物:其中:R 1表示氢原子或(C 1〜 (C 1 -C 4)烷基; R 2表示氢原子或(C 1 -C 4 -C 4)烷基; R 3表示被甲基单取代或多取代的噻吩基; 或选自以下的单环或双环杂环基:吡啶基,N-氧化吡啶基,吡唑基,(N-苯基)吡唑基,(N-卤代苯基)吡唑基,呋喃基,吲哚基,(N-苄基)吲哚基 ,(N-卤代苄基)吲哚基,苯并噻吩基或苯并呋喃基,所述基团是未取代的或被卤素原子或甲基或甲氧基取代一次或多次; R 4和R 5相同或不同,并且各自独立地表示氢或卤素原子或羟基,羟甲基,(C 1 -C 3 - (C 1 -C 4)烷基,三氟甲基,C 1 -C 4烷氧基,(C 1 -C 4 - 4)烷氧基羰基或氰基。 制剂工艺及其在治疗中的应用