首页> 外国专利> COMPOUND HAVING INHIBITORY ACTIVITY ON A RHO-GTPASE CELL PROTEIN, A PROCESS FOR OBTAINING THE SAME, PHARMACEUTICAL COMPOSITIONS COMPRISING THEREOF AND A METHOD FOR THE TREATMENT OF RHO-GTPASE CELL PROTEIN-MEDIATED CONDITION

COMPOUND HAVING INHIBITORY ACTIVITY ON A RHO-GTPASE CELL PROTEIN, A PROCESS FOR OBTAINING THE SAME, PHARMACEUTICAL COMPOSITIONS COMPRISING THEREOF AND A METHOD FOR THE TREATMENT OF RHO-GTPASE CELL PROTEIN-MEDIATED CONDITION

机译:在Rho-GTPase细胞蛋白上具有抑制活性的化合物,获得相同蛋白的方法,包含其的药物组合物以及Rho-GTPase细胞蛋白介导的条件的治疗方法

摘要

The present invention relates to a compound having inhibitory activity on a Rho-GTPase cell protein, the compound having the formula I (Formula I) wherein A is selected from N and N—H, R1 is selected from H and NHR3, R2 is selected from NHR4, OR4, O and halogen, R3 is selected from H and —COR5, R4 is selected from H, a C1-C6 alkyl and a substituted or unsubstituted phenyl, R5 is selected from a C1-C12 alkyl and a substituted or unsubstituted phenyl, R6 is selected from H, —COR5, —CO2R5, —PR7R8 and —PR7R8OPR7R8R8R7, R7 is selected from O and S, R8 is selected from H, OR4 and OSATE (—OCH2CH2SCOR5), and wherein each represents a single bond or a double bond, provided that when one of them is a double bond the other one is a single bond, and pharmaceutically acceptable salts and derivatives thereof. In particular, the compounds of the invention may be used as antitumor agents the action of which interfere with the signaling pathways normally involved in tumor development processes. The invention also relates to processes for obtaining of compounds having inhibitory activity of a Rho-GTPase cell protein, to the pharmaceutical compositions thereof and to the therapeutic methods comprising the use of said compounds and compositions.;
机译:本发明涉及对Rho-GTPase细胞蛋白具有抑制活性的化合物,该化合物具有式I(式I),其中A选自N和NH,R 1 选自H和NHR 3 ,R 2 选自NHR 4 ,OR 4 ,O和卤素,R从H中选择 3 ,从H中选择-COR 5 ,从H中选择R 4 ,C 1 -C 6 烷基和一个取代或未取代的苯基R 5 选自C 1 -C 12 烷基和取代或未取代的苯基,R 6 选自H,-COR 5 ,-CO 2 R 5 ,-PR 7 R 8 和-PR 7 R 8 OPR 7 R 8 R 8 R 7 ,R 7 选自O和S,R 8 选自H,OR 4 和OSATE(-OCH 2 CH 2 SCOR 5 ),以及其中每个代表一个单键或一个双b前提是,当其中一个是双键时,另一个是单键,及其药学上可接受的盐和衍生物。特别地,本发明的化合物可以用作抗肿瘤剂,其作用干扰通常参与肿瘤发展过程的信号传导途径。本发明还涉及获得具有Rho-GTPase细胞蛋白抑制活性的化合物的方法,其药物组合物以及涉及使用所述化合物和组合物的治疗方法。

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