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    Substituted naphthyridines and their use as medicaments
    2.
    发明授权
    Substituted naphthyridines and their use as medicaments 有权
    取代的萘啶并用作药物

    公开(公告)号：US08969568B2

    公开(公告)日：2015-03-03

    申请号：US13013973

    申请日：2011-01-26

    申请人： Matthias Hoffmann ,  Georg Dahmann ,  Dennis Fiegen ,  Sandra Handschuh ,  Jasna Klicic ,  Guenter Linz ,  Gerhard Schaenzle ,  Andreas Schnapp ,  Stephen Peter East ,  Michael Philip Mazanetz ,  Robert John Scott ,  Edward Walker

    发明人： Matthias Hoffmann ,  Georg Dahmann ,  Dennis Fiegen ,  Sandra Handschuh ,  Jasna Klicic ,  Guenter Linz ,  Gerhard Schaenzle ,  Andreas Schnapp ,  Stephen Peter East ,  Michael Philip Mazanetz ,  Robert John Scott ,  Edward Walker

    IPC分类号： C07D471/02 ,  C07D471/04 ,  C07D519/00

    CPC分类号： C07D471/04 ,  C07D498/04 ,  C07D519/00

    摘要： The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 is selected from among —O—R3 or —NR3R4, R3 is C1-6-alkyl which is substituted by R5 and R6, R5 is selected from hydrogen, branched or linear C1-6-alkyl, C2-6-alkenyl, —C1-6-alkylen-O—C1-3-alkyl, C1-3-haloalkyl, R6 is ring X wherein n is either 0 or 1, and is a either a single or a double bond and wherein A, B, D and E are each independently from one another selected from CH2, CH, C, N, NH, O or S and wherein ring X is attached to the molecule either via position A, B, D or E, wherein said ring X may optionally be further substituted by one, two or three residues each selected individually from the group consisting of -oxo, hydroxy, —C1-3-alkyl, —C1-3-haloalkyl, —O—C1-3-alkyl, —C1-3-alkanol and halogen, and wherein R4, R2, R7, R8, R9, R10, R11 and Q may have the meanings as given in claim 1, as well as pharmaceutical compositions containing these compounds.

    摘要翻译： 本发明涉及式1的新取代的萘啶，以及其药学上可接受的盐，非对映异构体，对映异构体，外消旋体，水合物或溶剂合物，其中R 1选自-O-R 3或-NR 3 R 4，R 3是C 1-6 - 烷基 其被R5和R6取代，R5选自氢，支链或直链C 1-6 - 烷基，C 2-6 - 烯基，-C 1-6 - 亚烷基-O-C 1-3 - 烷基，C 1-3 - 卤代烷基， R6是环X，其中n是0或1，并且是单键或双键，并且其中A，B，D和E各自独立地选自CH 2，CH，C，N，NH，O 或S，并且其中环X通过位置A，B，D或E连接到分子，其中所述环X可任选地被一个，两个或三个残基进一步取代，每个残基各自独立地选自氧基，羟基 ，-C 1-3 - 烷基，-C 1-3 - 卤代烷基，-O-C 1-3 - 烷基，-C 1-3 - 链烷醇和卤素，其中R4，R2，R7，R8，R9，R10，R11和Q 可能具有的含义 权利要求1中给出，以及含有这些化合物的药物组合物。

    4-DIMETHYLAMINO-PHENYL-SUBSTITUTED NAPHTHYRIDINES, AND USE THEREOF AS MEDICAMENTS
    6.
    发明申请
    4-DIMETHYLAMINO-PHENYL-SUBSTITUTED NAPHTHYRIDINES, AND USE THEREOF AS MEDICAMENTS 有权
    4-二甲基苯胺基 - 取代的萘啶，并作为药物使用

    公开(公告)号：US20110263549A1

    公开(公告)日：2011-10-27

    申请号：US13057330

    申请日：2009-07-23

    申请人： Dennis Fiegen ,  Sandra Handschuh ,  Silke Hobbie ,  Matthias Hoffmann ,  Takeshi Kono ,  Yayoi Sato ,  Andreas Schnapp ,  Annette Schuler-Metz

    发明人： Dennis Fiegen ,  Sandra Handschuh ,  Silke Hobbie ,  Matthias Hoffmann ,  Takeshi Kono ,  Yayoi Sato ,  Andreas Schnapp ,  Annette Schuler-Metz

    IPC分类号： A61K31/573 ,  A61K31/4375 ,  A61P11/00 ,  A61P19/10 ,  A61P1/04 ,  A61P31/14 ,  A61P7/06 ,  A61P25/00 ,  C07D471/04 ,  A61P19/02

    CPC分类号： C07D471/04 ,  C07D519/00

    摘要： 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, —CR3R4R5, -(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 claims 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.

    摘要翻译： 本发明涉及式1的新型取代萘啶以及其药理学上可接受的盐，非对映异构体，对映异构体，外消旋物，水合物或溶剂合物。 在式1中，R 1可以表示选自-O-R 3，-NR 3 R 4，-CR 3 R 4 R 5， - （乙炔）-R 3，-S-R 3，-SO-R 3和SO 2 -R 3的基团A， 或R 1表示选自包括以下基团的基团：-C 6-10 - 芳基; - 含有1至3个独立地选自以下的杂原子的五元至十元单环或双环杂芳基：N，O， 和S，其中所述杂芳基通过C原子或N原子连接到根据式1的结构; - 含有1至3个独立选择的杂原子的三元至十元单环或双环饱和或部分饱和的杂环 包括N，O和S的基团，其中所述杂环通过C原子或N原子连接到根据式1的结构; 和可以任选地含有1,2或3个独立地选自包括N，O和S的基团的杂原子的5元至11元螺环，其中所述螺环与根据式1的结构连接 通过C原子或N原子，其中所述基团B可以如权利要求1所述任选被取代，并且R 3，R 4，R 5，R 6和m可以具有权利要求1中所示的含义。本发明还涉及药物组合物 含有所述化合物。

    4-dimethylamino-phenyl-substituted naphthyridines, and use thereof as medicaments
    8.
    发明授权
    4-dimethylamino-phenyl-substituted naphthyridines, and use thereof as medicaments 有权
    4-二甲基氨基 - 苯基取代的萘啶，及其用作药物

    公开(公告)号：US08604049B2

    公开(公告)日：2013-12-10

    申请号：US13057330

    申请日：2009-07-23

    申请人： Dennis Fiegen ,  Sandra Handschuh ,  Silke Hobbie ,  Matthias Hoffmann ,  Takeshi Kono ,  Yayoi Sato ,  Andreas Schnapp ,  Annette Schuler-Metz

    发明人： Dennis Fiegen ,  Sandra Handschuh ,  Silke Hobbie ,  Matthias Hoffmann ,  Takeshi Kono ,  Yayoi Sato ,  Andreas Schnapp ,  Annette Schuler-Metz

    IPC分类号： A61K31/573 ,  A61K31/4375 ,  A61P11/00 ,  A61P19/10 ,  A61P1/04 ,  A61P31/14 ,  A61P7/06 ,  A61P25/00 ,  A61P19/02 ,  C07D471/04

    CPC分类号： C07D471/04 ,  C07D519/00

    摘要： 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, —NR3R4, —CR3R4R5, -(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 claims 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.

    摘要翻译： 本发明涉及式1的新型取代萘啶以及其药理学上可接受的盐，非对映异构体，对映异构体，外消旋物，水合物或溶剂合物。 在式1中，R 1可以表示选自-O-R 3，-NR 3 R 4，-CR 3 R 4 R 5， - （乙炔）-R 3，-S-R 3，-SO-R 3和SO 2 -R 3的基团A，或 R 1表示选自以下的基团B：-C 6-10 - 芳基; 包含1至3个独立地选自N，O和S的杂原子的五元至十元单环或二环杂芳基，其中所述杂芳基通过C原子连接至根据式1的结构，或 一个N原子; 包含1-3个独立地选自包括N，O和S的杂原子的3至10元，单环或双环饱和或部分饱和的杂环，其中所述杂环与根据式1的结构连接 通过C原子或N原子; 和可以任选地含有1,2或3个独立地选自N，O和S的组的杂原子的5元至11元螺环，其中所述螺环与根据式1的结构连接 通过C原子或N原子，其中所述基团B可以如权利要求1所述任选被取代，并且R 3，R 4，R 5，R 6和m可以具有权利要求1中所示的含义。本发明还涉及药物组合物 含有所述化合物。

    SUBSTITUTED NAPHTHYRIDINES AND USE THEREOF AS MEDICINES
    9.
    发明申请
    SUBSTITUTED NAPHTHYRIDINES AND USE THEREOF AS MEDICINES 审中-公开
    取代的萘啶酮及其作为药物的用途

    公开(公告)号：US20110201608A1

    公开(公告)日：2011-08-18

    申请号：US13057288

    申请日：2009-07-23

    申请人： Matthias Hoffmann ,  Thierry Bouyssou ,  Georg Dahamnn ,  Harald Engelhardt ,  Dennis Fiegen ,  Sandra Handschum ,  Silke Hobbie ,  Takeshi Kono ,  Ulrich Reiser ,  Yayoi Sato ,  Andreas Schnapp ,  Annette Schuler-Metz

    发明人： Matthias Hoffmann ,  Thierry Bouyssou ,  Georg Dahamnn ,  Harald Engelhardt ,  Dennis Fiegen ,  Sandra Handschum ,  Silke Hobbie ,  Takeshi Kono ,  Ulrich Reiser ,  Yayoi Sato ,  Andreas Schnapp ,  Annette Schuler-Metz

    IPC分类号： A61K31/5377 ,  C07D471/04 ,  A61K31/496 ,  A61P11/06 ,  A61P19/02 ,  A61P1/04 ,  A61P17/06 ,  A61P35/00 ,  A61P17/00 ,  A61P11/00

    CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D513/04

    摘要： The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 denotes a group A selected from among —O—R3, —NR3R4, —CR3R4R5, -(ethyne)-R3, —S—R3, —SO—R3 and SO2—R3 or R1 denotes a group B selected from among C6-10-aryl, five- to ten-membered, mono- or bicyclic heteroaryl with 1-3 heteroatoms selected independently of one another from among N, O and S; while this heteroaryl is linked to the structure according to formula 1 via either a C atom or an N atom, three- to ten-membered, mono- or bicyclic, saturated or partially saturated heterocyclic group with 1-3 heteroatoms selected independently of one another from among N, O and S, while this heterocyclic group is linked to the structure according to formula 1 via either a C atom or an N atom, and 5- to 11-membered spiro group which may optionally contain 1, 2 or 3 heteroatoms selected independently of one another from among N, O and S, while this spiro group is linked to the structure according to formula 1 via either a C atom or an N atom, while this group B may optionally be substituted as described in claim 1 and wherein R2 is and R3, R4, R5, R6, R6′, R7, R8, R9, R10, V, n and m may have the meanings given in claim 1, as well as pharmaceutical compositions containing these compounds.

    摘要翻译： 本发明涉及式1的新取代的萘啶，以及其药学上可接受的盐，非对映异构体，对映异构体，外消旋体，水合物或溶剂化物，其中R1表示选自-O-R3，-NR3R4，-CR3R4R5， （乙炔）-R 3，-S-R 3，-SO-R 3和SO 2 -R 3或R 1表示选自C 6-10 - 芳基，5至10元，单 - 或双环杂芳基和1-3 从N，O和S中彼此独立地选择的杂原子; 而该杂芳基通过C原子或N原子连接到根据式1的结构，具有1-3个互相独立选择的杂原子的三至十元，单环或二环，饱和或部分饱和的杂环基 N，O和S中的至少一个，而该杂环基通过C原子或N原子与根据式1的结构连接，并且可以任选地含有1,2或3个杂原子的5至11元螺环 N，O和S彼此独立地选择，而该螺环通过C原子或N原子连接到根据式1的结构，而该基团B可以任选地被如权利要求1和 其中R2是和R3，R4，R5，R6，R6'，R7，R8，R9，R10，V，n和m可以具有权利要求1中给出的含义，以及含有这些化合物的药物组合物。