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    • 3. 发明申请
    • NEW PYRIDOTHIENOPYRIMIDINE DERIVATIVES
    • 新的吡啶并吡啶衍生物
    • WO2006058724A1
    • 2006-06-08
    • PCT/EP2005/012774
    • 2005-11-30
    • ALMIRALL PRODESFARMA, S.A.PAGES SANTACANA, Lluis, MiquelTALTAVULL MOLL, Joan
    • PAGES SANTACANA, Lluis, MiquelTALTAVULL MOLL, Joan
    • C07D495/14C07D495/22A61K31/519A61P11/06
    • C07D495/14A61K31/519
    • Use of a pyridothienopyrimidine derivative of formula (I), and the pharmaceutically acceptable salts and N-oxides thereof, wherein G 1 represents a group selected from -CR 6 R 7 - or -NR 6 being R 6 and R 7 independently selected from hydrogen atoms and C 1-4 alkyl groups m and n are integers selected from 0 or 1 R 1 and R 2 are independently selected from hydrogen atoms and C 1-4 alkyl groups R 3 represents a group selected from alkyl, amino, monoalkylamino, dialkylamino, aryl, heteroaryl and saturated N-containing heterocyclyl groups bound through the nitrogen atom to the piridine ring, all of them being optionally substituted by one or more substituents selected from the group consisting of halogen atoms and alkyl, alkoxyalkyl, arylalkyl, R 8 OCO-, alkoxy, R 8 R 9 N-CO-, -CN, -CF 3 , -NR 8 R 9 , -SR 8 and - SO 2 NH 2 groups wherein R 8 and R 9 are independently selected from hydrogen atoms and C 1-4 alkyl groups R 4 and R 5 are independently selected from the group consisting of hydrogen atoms alkyl groups and groups of formula (II), wherein p and q are integers selected from 1, 2 and 3; A is either a direct bond or a group selected from -CONR 14 -, -NR 14 CO-, -O-, -COO-, -OCO-, -NR 14 OCO-, - OCONR 14 -, -NR 14 CONR 15 -, -S-, -SO-, -SO 2 -, -COS- and -SCO-; and G 2 is a group selected from aryl, heteroaryl or heterocyclyl; wherein the alkyl groups and the group G 2 are optionally substituted by one or more substituents selected from group consisting of halogen atoms and alkyl, alkoxyalkyl, arylalkyl, R 16 OCO-, hydroxy, alkoxy, oxo, R 16 R 17 NCO-, -CN, -CF 3 , -NR 16 R 17 , -SR 16 and -SO 2 NH 2 groups; wherein R 10 to R 17 are independently selected from hydrogen atoms and C 1-4 alkyl groups; in the manufacture of a medicament for the treatment or prevention of a pathological condition or disease susceptible to amelioration by inhibition of phosphodiesterase 4.
    • 式(I)的吡啶并噻吩并嘧啶衍生物及其药学上可接受的盐和N-氧化物的用途,其中G 1表示选自-CR 6, > 7 - 或-NR 6 - ,其中R 6和R 7独立地选自氢原子和C 1〜 4个烷基m和n是选自0或1的整数,R 1和R 2独立地选自氢原子和C 1-4 烷基R 3表示选自通过氮原子与吡啶环结合的烷基,氨基,单烷基氨基,二烷基氨基,芳基,杂芳基和饱和的含N的杂环基的基团,全部是 它们任选地被一个或多个选自卤素原子和烷基,烷氧基烷基,芳基烷基,R 8 OCO-,烷氧基,R 8 O, > 9个N-CO-,-CN,-CF 3,-NR 8 R 9,-SR 8和 - SO