申请人:Boehringer Ingelheim International GmbH
公开号:US20150126503A1
公开(公告)日:2015-05-07
The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof,
wherein
R
1
is selected from among —O—R
3
or —NR
3
R
4
,
R
3
is C
1-6
-alkyl which is substituted by R
5
and R
6
,
R
5
is selected from hydrogen, branched or linear C
1-6
-alkyl, C
2-6
-alkenyl, —C
1-6
-alkylen-O—C
1-3
-alkyl, C
1-3
-haloalkyl,
R
6
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 CH
2
, 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, —C
1-3
-alkyl, —C
1-3
-haloalkyl, —O—C
1-3
-alkyl, —C
1-3
-alkanol and halogen,
and wherein R
4
, R
2
, R
7
, R
8
, R
9
, R
10
, R
11
and Q may have the meanings as given in claim
1
, as well as pharmaceutical compositions containing these compounds.
该发明涉及公式1的新取代萘啶,以及其药学上可接受的盐、对映异构体、对映体、外消旋体、水合物或溶剂化物,其中R1从—O—R3或—NR3R4中选择,R3是由R5和R6取代的C1-6烷基,R5选择氢、支链或直链C1-6烷基、C2-6烯基、—C1-6-烷基-O—C1-3-烷基、C1-3卤代烷基,R6是环X,其中n为0或1,且是单键或双键,A、B、D和E各自独立地从CH2、CH、C、N、NH、O或S中选择,环X通过位置A、B、D或E连接到分子上,其中环X可以选择进一步由选自-氧代、羟基、—C1-3-烷基、—C1-3卤代烷基、—O—C1-3-烷基、—C1-3-醇基和卤素的一、两或三个残基取代,R4、R2、R7、R8、R9、R10、R11和Q的含义如权利要求1所述,以及含有这些化合物的制药组合物。