公开(公告)号：US06863647B2

公开(公告)日：2005-03-08

申请号：US09830668

申请日：1999-10-27

申请人： Paolo Pevarello ,  Raffaella Amici ,  Gabriella Traquandi ,  Manuela Villa ,  Anna Vulpetti ,  Antonella Isacchi

发明人： Paolo Pevarello ,  Raffaella Amici ,  Gabriella Traquandi ,  Manuela Villa ,  Anna Vulpetti ,  Antonella Isacchi

IPC分类号： C07D277/20 ,  A61K31/426 ,  A61K31/427 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  A61P9/10 ,  A61P11/00 ,  A61P13/08 ,  A61P13/12 ,  A61P17/06 ,  A61P19/02 ,  A61P25/28 ,  A61P31/12 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  A61P37/00 ,  A61P43/00 ,  C07D277/44 ,  C07D277/48 ,  C07D277/62 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D491/10 ,  C07D877/48

CPC分类号： C07D277/62 ,  C07D277/48 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D491/10

摘要： Compounds which are 2-ureido-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-C6 alkyl; ii) C3-C6 cycloalkyl; iii) aryl or arylalkyl with from 1 to 6 carbon atoms within the straight or branched alkyl chain; R1 is an optionally substituted group selected from: i) straight or branched C1-C6 alkyl; ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring; iii) aryl or arylcarbonyl; iv) arylalkyl with from 1 to 6 carbon atoms within the straight or branched alkyl chain; R2 is hydrogen, a straight or branched C1-C6 alkyl or C2-C4 alkenyl or alkynyl group; or, taken together with the nitrogen atom so which they are bonded, R1 and R2 form a substituted or unsubstituted group selected from: i) an optionally benzocondensed or bridged 5 to 7 membered heterocycle; or ii) a 9 to 11 membered spiro-heterocyclic compound; or a pharmaceutically acceptable salt thereof; are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.

摘要翻译： 作为式（I）的2-脲基-1,3-噻唑衍生物的化合物，其中R是卤素原子，硝基，任选取代的氨基，或者是任选进一步取代的基团，其选自：i）直链或 支链C 1 -C 6烷基; ii）C 3 -C 6环烷基; iii）在直链或支链烷基链中具有1至6个碳原子的芳基或芳基烷基; R1是任选取代的基团，其选自：i）直链或支链C 1 -C 6烷基; ii）3至6元碳环或5至7元杂环; iii）芳基或芳基羰基; iv）在直链或支链烷基链中具有1至6个碳原子的芳基烷基; R2是氢，直链或支链C1-C6烷基或C2-C4烯基或炔基; 或者与它们所键合的氮原子一起，R1和R2形成取代或未取代的基团，其选自：i）任选苯并稠合或桥连的5至7元杂环; 或ii）9至11元螺 - 杂环化合物; 或其药学上可接受的盐; 可用于治疗与改变的细胞依赖性激酶活性相关的细胞增殖性疾病。