首页> 外国专利> (3,4-A:3,4-C)CARBAZOLE COMPOUNDS USED FOR TREATMENT OF CANCER SUCH AS ADENOCARCINOMAS AND CARCINOMAS, SARCOMAS, GLIOMAS AND LEUKEMIAS, PROCESS FOR PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

(3,4-A:3,4-C)CARBAZOLE COMPOUNDS USED FOR TREATMENT OF CANCER SUCH AS ADENOCARCINOMAS AND CARCINOMAS, SARCOMAS, GLIOMAS AND LEUKEMIAS, PROCESS FOR PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

机译:(3,4-A:3,4-C)卡巴唑化合物,用于治疗腺癌和癌瘤,肉瘤,胶质瘤和白血病,其制备方法和含有该化合物的药物组合物

摘要

PURPOSE: (3,4-a:3,4-c)Carbazole compounds, a process for preparation thereof and pharmaceutical compositions containing the same compounds are provided. The compounds are useful especially in the treatment of cancer such as adenocarcinomas and carcinomas, sarcomas, gliomas and leukaemias, so that they can advantageously be associated with all cytotoxic treatments currently in use, as well as with radiotherapies, whose toxicity is not increased thereby, and with the various hormone therapies directed against cancers (blood and prostate). CONSTITUTION: The (3,4-a:3,4-c)carbazole compound selected from those of the formula(I), its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base are provided, wherein A is a saturated or partially or fully unsaturated ring, wherein the unsaturation optionally confers an aromatic nature on the ring; W1 is, together with carbon to which it is bonded, phenyl or pyridyl; Z is a group of the formula(U-V); Q1 is oxygen or NR2; Q2 is oxygen or NR'2; X1, X2, X'1 and X'2 are independently hydrogen, hydroxy, alkoxy, mercapto or alkylthio; Y1, Y2, Y'1 and Y'2 are independently hydrogen, or X1 and Y1, X2 and Y2, X'1 and Y'1, X'2 and Y'2 with carbon carrying them, together form carbonyl or thiocarbonyl; and R1 is a group selected from hydrogen, linear or branched (C1-C6)alkyl that is optionally substituted by one or more groups selected from hydroxy, linear or branched (C1-C6)alkoxy, linear or branched (C1-C6)hydroxyalkoxy or NR3R4.
机译:目的:提供(3,4-a:3,4-c)咔唑化合物,其制备方法和包含相同化合物的药物组合物。所述化合物尤其可用于治疗癌症,例如腺癌和癌,肉瘤,神经胶质瘤和白血病,因此它们可有利地与目前使用的所有细胞毒性治疗以及放射治疗结合,其毒性不会因此而增加,以及针对癌症(血液和前列腺癌)的各种激素疗法。组成:提供选自式(I)化合物的(3,4-a:3,4-c)咔唑化合物,其异构体及其与可药用酸或碱的加成盐,其中A为饱和或部分或完全不饱和的环,其中所述不饱和基团任选地赋予所述环芳香性; W1及其键合的碳是苯基或吡啶基; Z是式(U-V)的基团; Q1是氧或NR2; Q2是氧或NR'2; X 1,X 2,X′1和X′2独立地是氢,羟基,烷氧基,巯基或烷硫基; Y 1,Y 2,Y′1和Y′2独立地是氢,或X 1和Y 1,X 2和Y 2,X′1和Y′1,X′2和Y′2带有碳,它们一起形成羰基或硫代羰基。 R1是选自氢,直链或支链(C1-C6)烷基的基团,其任选地被一个或多个选自羟基,直链或支链(C1-C6)烷氧基,直链或支链(C1-C6)羟基烷氧基的基团取代或NR3R4。

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