AZAINDOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION, AND THEIR USE AS ANTITUMOR AGENTS
申请人:PHARMACIA & UPJOHN
公开号:US20030004350A1
公开(公告)日:2003-01-02
Novel 1H-pyrrolo[2,3-b]pyridines which are represented by formula (I):
1
wherein R is a hydrogen or halogen atom or a group selected from —CN, —OH, —OCOR
4
, —(CH
2
)
n
NH
2
, —(CH
2
)
n
NHR
4
, —(CH
2
)
n
NHCOR
4
, —(CH
2
)
n
NHCONR
4
R
5
, —(CH
2
)
n
NHCOOR
4
, or —(CH
2
)
n
NHSO
2
R
4
, wherein n is either 0 or 1, R
4
and R
5
are as described in the specification; R
1
is hydrogen or an optionally substituted alkyl group; R
2
is an optionally substituted group selected from alkyl or aryl; R
3
is hydrogen or a group selected from —CONR
4
R
5
, —COOR
4
, —CONHOR
4
, —SO
2
NHR
4
, alkylsulphonylaminocarbonyl or perfluorinated alkylsulphonylaminocarbonyl; or a pharmaceutically acceptable salt thereof, are disclosed.
These compounds are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.
化合物1H-pyrrolo[2,3-b]pyridines,其由式(I)表示:其中R是氢原子或卤素原子或从-CN,-OH,-OCOR4,-(CH2)nNH2,-(CH2)nNHR4,-(CH2)nNHCOR4,-(CH2)nNHCONR4R5,-(CH2)nNHCOOR4或-(CH2)nNHSO2R4中选择的基团,其中n为0或1,R4和R5如规范中所述;R1是氢原子或可选择地取代的烷基基团;R2是可选择地取代的烷基或芳基基团;R3是氢原子或从CONR4R5,-COOR4,-CONHOR4,-SO2NHR4,烷基磺酰胺基羰基或全氟烷基磺酰胺基羰基中选择的基团;或其药学上可接受的盐。这些化合物可用于治疗与细胞依赖性激酶活性改变相关的细胞增殖性疾病。