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    • 10. 发明申请
    • 4-DIMETHYLAMINO-PHENYL-SUBSTITUTED NAPHTHYRIDINES, AND USE THEREOF AS MEDICAMENTS
    • 4二甲氨基 - 取代萘啶及其作为药物
    • WO2010015518A2
    • 2010-02-11
    • PCT/EP2009059493
    • 2009-07-23
    • BOEHRINGER INGELHEIM INTFIEGEN DENNISHANDSCHUH SANDRAHOBBIE SILKEHOFFMANN MATTHIASKONO TAKESHISATO YAYOISCHNAPP ANDREASSCHULER-METZ ANNETTE
    • FIEGEN DENNISHANDSCHUH SANDRAHOBBIE SILKEHOFFMANN MATTHIASKONO TAKESHISATO YAYOISCHNAPP ANDREASSCHULER-METZ ANNETTE
    • C07D471/04A61K31/4375A61P11/06C07D519/00
    • C07D471/04C07D519/00
    • The invention relates to novel substituted naphthyridines of formula 1 as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates, or solvates thereof. In formula 1, R1 can represent a group A selected from among the group comprising -O-R3, -NR3 R4, -CR3 R4 R5,-(ethyne)-R3, -S-R3, -SO-R3, and SO2 -R3, or R1 represents a group B selected from among the group comprising: - C6-10-aryl; - a five-membered to ten-membered, monocyclic or bicyclic heteroaryl containing 1 to 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said heteroaryl is linked to the structure according to formula 1 via a C atom or an N atom; - a three-membered to ten-membered, monocyclic or bicyclic, saturated or partially saturated heterocycle containing 1 to 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said heterocycle is linked to the structure according to formula 1 via a C atom or an N atom; and - a 5-membered to 11-membered spiro group which can optionally contain 1, 2, or 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said spiro group is linked to the structure according to formula 1 via a C atom or an N atom, wherein said group B can be optionally substituted as described in claim 1, and R3,R4,R5, R6, and m can have the meanings indicated in claim 1. The invention also relates to pharmaceutical compositions containing said compounds.
    • 本发明涉及式1的新的取代的萘啶,以及其药理学上可接受的盐,非对映体,对映体,外消旋体,水合物或溶剂合物,其中R 1是选自-O-R 3,-NR 3 R 4,-CR 3 R 4 R组成的组中选择的基团A 5 , - (乙炔)-R 3,-S-R 3,-SO-R 3,和SO 2 -R 3或R 1是基团B选自的组中选择 - C6-10芳基, - 五到十元单环或双环杂芳基 具有选自N,O和S的组中独立选择的1-3个杂原子; 其中所述杂芳基或者通过一个C原子或通过N原子连接的,具有以下结构的根据式1, - 三至具有从所述组独立地选自1-3个杂原子至十元单环或双环,饱和或部分饱和的杂环 选自N,O和S,其中所述杂环或者通过一个C原子或通过N原子连接的,具有以下结构的根据式1,以及 - 5-至11-元螺环基团,任选地含有1,2或 3可以是选自N,O和S的组中独立选择的杂原子,所述螺环基团则通过一个C原子或通过N原子连接的,具有以下结构的根据式1,其中所述残基B是任选地作为 可以如权利要求1,其中R3,R4,R5,R6和m可以具有权利要求1中所述的含义,以及含有这些化合物的药物组合物中所述被取代。