本发明属于药物化学领域,具体涉及一类以FGFR1为靶点的多取代嘧啶类化合物及其制备方法和用途,该化合物可以选择性地抑制FGFR1激酶的磷酸化从而用于治疗与此激酶密切联系的恶性肿瘤,同时能减少不良反应;能够用于治疗FGFR1激酶相关的肿瘤或相关的疾病。多取代嘧啶类化合物的通式为A~D,其中:以上R1、R2、R3、R4、R5、R6可以多种取代基选择,R1、R2、R3、R4、R5、R6取代基可以任意组合。本发明所述的以FGFR1为靶点的多取代嘧啶类化合物对FGFR1激酶具有良好的抑制作用;可用于制备抗肿瘤药物,且抗肿瘤效果较好。A B C D
SUBSTITUTED ARYLSULPHONYLGLYCINES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS
申请人:Wagner Holger
公开号:US20100093703A1
公开(公告)日:2010-04-15
The present invention relates to substituted arylsulphonylglycines of general formula wherein R, R
4
, X, Y, Z and m are defined as in claim
1
, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the G
L
subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
The invention concerns quinazoline derivatives of Formula (I); wherein each of Q
1
, Q
2
, Z, R
1
, R
2
, R
3
, and m have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosin kinases.