公开(公告)号：EP1387829A1

公开(公告)日：2004-02-11

申请号：EP02728285.4

申请日：2002-04-29

申请人： AstraZeneca AB

发明人： JOHANSSON, Magnus ,  ROSENQUIST, sa ,  SEMPLE, Graeme

IPC分类号： C07D213/64 ,  C07D239/34 ,  C07D237/14 ,  C07D401/08 ,  C07D403/08 ,  C07D413/08 ,  A61K31/4412 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/506 ,  A61K31/513 ,  A61P25/04 ,  A61P11/14 ,  A61P23/02 ,  A61P29/00

CPC分类号： C07D213/64 ,  A61K31/4412 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/506 ,  A61K31/513 ,  C07D213/74 ,  C07D237/14 ,  C07D239/22

摘要： The present invention relates to a compound of formula (1), (2) or (3) having the following structures: Formula 1, 2, 3 wherein X, Y, and Z are independently C or N; A is a direct bond, CH2 or NH;B is a direct bond or NH; n= 0-2; R1 is H, optionally substituted C1-4191 alkyl, C3-7191 cycloalkyl, halogen, cyano, nitro, aryl, or alkylaryl; R2 is H, C1-4191 alkyl, or alkoxy C1-4191 alkyl;or R1 and R2 are taken together to form an unsaturated 6-membered aromatic or heterocyclic ring containing one or two heteroatoms fused to the pyridone; R3 is a direct bond, H, C1-4191 alkyl, substituted C1-4191 alkyl, C3-7191 cycloalkyl, aryl or alkylaryl; R4 is a direct bond or H; R5 is C1-4191 alkyl or aryl; R6 and R7 are independently H or C1-4191 alkyl; R8 and R9 are independently H, C1-4191 alkyl, or tert-butoxycarbonyl or R8 and R9 are taken together with the nitrogen to which they are attached and form optionally, unsubstituted, substituted, fused or unsaturated 5-,6-,7-membered heterocycles containing one or two heteroatoms wherein said substituents are selected from the group consisting of hydroxyl, hydroxymethyl, carboxymethyl, carboxy, methoxy, and tert-butoxy;as (R)-enantiomers, (S)-enantiomers or a racemate in the form of a free base or a pharmaceutically acceptable salt or solvate thereof.