首页> 外国专利> SUBSTITUTED 2-METHYLIDEN-5-(PHENYLAMINO)-2,3-DIHYDROTIOPHEN-3-ONE FOR TREATMENT OF LEUKEMIAS WITH TRANSLOCATIONS OF MLL-GENE AND OTHER ONCOLOGICAL DISEASES

SUBSTITUTED 2-METHYLIDEN-5-(PHENYLAMINO)-2,3-DIHYDROTIOPHEN-3-ONE FOR TREATMENT OF LEUKEMIAS WITH TRANSLOCATIONS OF MLL-GENE AND OTHER ONCOLOGICAL DISEASES

机译:替代2-Methylyliden-5-(Phenylamino)-2,3-DiHydrotiophoen-3-one用于白血病的转移并传给MLL基因和其他肿瘤疾病

摘要

FIELD: chemistry.;SUBSTANCE: invention relates to compounds of general formula (I), general formula (II) or general formula (III): formula (I); formula (II); formula (III), where R1, R2 are independently selected and represent -H, substituted or unsubstituted -C1-C6-alkyl, the substituents R1 and R2 together with the carbon atom to which they are attached, can form a substituted or unsubstituted -C3-C12-cycloalkyl; A is independently selected and is: or ;the asterisk indicates the attaching place of substituents; B is selected independently and is: the asterisk indicates the attaching place of substituents; each substituent Rk is independently selected and represents -H, halogen; Q is independently selected and represents -H, -C(=O)-RL; RL is independently selected and represents a substituted or unsubstituted -C1-C6-alkyl (the values of the remaining radicals are presented in paragraph 1 of the claims).;EFFECT: formula is proposed for the treatment of hyperproliferative diseases associated with malignant transformation of cells expressing the carboxyl esterase hCE1 enzyme, in particular acute leukemias with MLL gene translocations, hepatocellular carcinomas and lung adenocarcinomas.;11 cl, 7 dwg, 12 tbl, 96 ex
机译:技术领域本发明涉及通式(I),通式(II)或通式(III)的化合物:<图像文件=“ 00000150.JPG” he =“ 34” imgContent =“ undefined” imgFormat =“ JPEG” wi =“ 40” />公式(I); 公式(II); 公式(III),其中R 1 ,R 2 是独立选择的,代表-H,取代或未取代的-C 1 -C 6 -烷基,取代基R 1 和R 2 与它们所连接的碳原子一起可以形成取代或未取代的-C 3 -C 12 -环烷基; A是独立选择的,并且是: 或<图像文件=” 00000155.JPG“ he =” 24“ imgContent =” undefined“ imgFormat =” JPEG“ wi =” 37“ / >;星号表示取代基的连接位置; B独立选择,并且是:星号表示取代基的连接位置;每个取代基R k 是独立选择的,代表-H,卤素; Q是独立选择的,代表-H,-C(= O)-R L ; R L 是独立选择的,代表取代或未取代的-C 1 -C 6 -烷基(其余基团的值在效果:提出了用于治疗与表达羧基酯酶hCE1酶的细胞恶变有关的过度增殖性疾病的配方,特别是具有MLL基因易位的急性白血病,肝细胞癌和肺腺癌。11cl ,7 dwg,12 tbl,96 ex

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