2-amino-thiazole derivatives, process for their preparation, and their use as antitumor agents
申请人:Pharmacia & Upjohn S.p.A.
公开号:US07037929B1
公开(公告)日:2006-05-02
Compounds which are 2-amino-1,3-thiazole derivatives of formula (I)
wherein R is a halogen atom, a nitro group, an optionally substituted amino group or it is a group, optionally further substituted, selected from i) straight or branched C1–C8 alkyl, C2–C6 alkenyl or C2–C6 alkynyl; ii) C3–C6 cycloalkyl; iii) aryl or arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; R1 is an optionally further substituted group selected from: i) straight or branched C1–C8 alkyl or C2–C6 alkenyl; ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring; iii) aryl or arylcarbonyl; iv) arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; v) arylalkenyl with from 2 to 6 carbon atoms within the straight or branched alkenyl chain; vi) an optionally protected amino acid residue; or a pharmaceutically acceptable salt thereof; are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.
公式(I)的2-氨基-1,3-噻唑衍生物化合物,其中R是卤素原子、硝基、可选择取代的氨基基团或是选择自i)直链或支链C1-C8烷基、C2-C6烯基或C2-C6炔基的基团,可选地进一步取代;ii)C3-C6环烷基;iii)芳基或芳基烷基,其在直链或支链烷基链内有1至8个碳原子;R1是可选择进一步取代的基团,包括i)直链或支链C1-C8烷基或C2-C6烯基;ii)3至6成员的碳环或5至7成员的杂环;iii)芳基或芳基羰基;iv)芳基烷基,其在直链或支链烷基链内有1至8个碳原子;v)芳基烯基,其在直链或支链烯基链内有2至6个碳原子;vi)可选择保护的氨基酸残基;或其药学上可接受的盐;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。