2-Amino-nicotinamide derivatives and their use as vegf-receptor tyrosine kinase inhibitors
申请人:——
公开号:US20030032656A1
公开(公告)日:2003-02-13
The invention relates to the use of 2-amino-nicotinamide derivatives of formula (I) wherein n is from 1 up to and including 6; W is O or S; R
1
and R
3
represent independently of each other hydrogen, lower alkyl or lower acyl; R
2
represents a cycloalkyl group, an aryl group, or a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms and 0, 1 or 2 heteroatoms independently from each other selected from the group consisting of oxygen and sulfur, which groups in each case are unsubstituted or mono- or polysubstituted; R and R′ are independently of each other hydrogen or lower alkyl; X represents an aryl group, or a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms and 0, 1 or 2 heteroatoms independently from each other selected from the group consisting of oxygen and sulfur, which groups in each case are unsubstituted or mono- or polysubstituted; or a N-oxide, a possible tautomer thereof or a pharmaceutically acceptale salt of such a compound, alone or in combination with one or more other pharmaceutically active compounds for the preparation of a pharmaceutical composition for use for therapy of a disease which responds to an inhibition of the VEGF-receptor tyrosine kinase activity; and to new 2-amino-nicotinamide derivatives of formula (I) and processes for the preparation thereof.
1
本发明涉及使用公式(I)中的2-氨基烟酰胺衍生物,其中n为1至6,包括1和6;W为O或S;R1和R3分别表示氢、低烷基或低酰基;R2表示环烷基、芳基或含有一个或多个环氮原子和0、1或2个异原子的单环或双环杂芳基,这些基团在每种情况下都未取代或单取代或多取代;R和R'独立地表示氢或低烷基;X表示芳基或含有一个或多个环氮原子和0、1或2个异原子的单环或双环杂芳基,这些基团在每种情况下都未取代或单取代或多取代;或其N-氧化物、可能的互变异构体或其药学上可接受的盐,单独或与一个或多个其他药物活性化合物结合,用于制备用于治疗对抗VEGF受体酪氨酸激酶活性的抑制有反应的疾病的制剂;以及公式(I)的新型2-氨基烟酰胺衍生物及其制备方法。