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    • 3. 发明授权
    • 2-amino-nicotinamide derivatives and their use as VEGF-receptor tyrosine kinase inhibitors
    • 2-氨基 - 烟酰胺衍生物及其作为VEGF-受体酪氨酸激酶抑制剂的用途
    • US06624174B2
    • 2003-09-23
    • US10181005
    • 2002-07-11
    • Paul William ManleyGuido Bold
    • Paul William ManleyGuido Bold
    • C07D21382
    • C07D213/82A61K31/445C07D213/89C07D401/14C07D417/14
    • 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; R1 and R3 represent independently of each other hydrogen, lower alkyl or lower acyl; R2 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 acceptable 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.
    • 本发明涉及式I的2种氨基 - 烟酰胺衍生物的用途,其中n为1至6,W为O或S; R 1和R 3彼此独立地为氢,低级烷基或低级酰基; R 2表示 环烷基,芳基或包含一个或多个环氮原子和0,1或2个彼此独立地选自氧和硫的杂原子的单环或双环杂芳基,这些基团在每种情况下是未取代的 或单取代或多取代; R和R'彼此独立地为氢或低级烷基; X表示芳基,或单环或双环杂芳基,其包含一个或多个环氮原子和0,1或2个独立地为 彼此选自氧和硫,这些基团在每种情况下都是未取代的或单取代或多取代的;或N-氧化物,其可能的互变异构体或这种化合物的药学上可接受的盐,alo ne或与一种或多种其它药学活性化合物组合用于制备用于治疗对VEGF-受体酪氨酸激酶活性的抑制作出反应的疾病的药物组合物;以及新的2-氨基 - 烟酰胺衍生物 式I及其制备方法。