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Heterocyclic ether substituted imidazoquinolines and pharmaceutical compositions for cytokine induction, anti-tumor activty and antiviral activity

机译:杂环醚取代的咪唑并喹啉和用于细胞因子诱导,抗肿瘤活性和抗病毒活性的药物组合物

摘要

The compounds of formula (I)-(IX) and (XLIV) or pharmaceutically acceptable salts are described wherein: X is -CHR3-, -CHR3-alkyl- or-CHR3-alkenyl-; R1 is -heteroaryl, -heterocyclyl, -R4-heteroaryl or -R4-heterocyclyl, and in formulas (V) and (VI) R1 can also be -(CH2)1-10-CºC-R10; R2 is -hydrogen, -alkyl, -alkenyl, -aryl, -heteroaryl, -heterocyclyl, -alkyl-Y-alkyl, -alkyl-Y-alkenyl, -alkyl-Y-aryl, or -alkyl or alkenyl substituted by one or more substituents selected from the group consisting of -OH, -halogen, -N(R3)2, -CO-N(R3)2, -CO-C1-10alkyl, -CO-O-C1-10alkyl, - N3, -aryl, -heteroaryl, -heterocyclyl, -CO-aryl, and -CO-heteroaryl; R4 is alkyl or alkenyl, which may be interrupted by one or more -O- groups; Each R3 is independently H or C1-10alkyl; Each Y is independently -O-or-S(O)0-2-; n is 0 to 4; and each R present is independently selected from the group consisting of C1-10alkyl, C1-10 alkoxy, hydroxy, halogen and trifluoromethyl; and R10 is heteroaryl and heterocyclyl; R7 is tert-butyl or benzyl; and Z is NH2 or NO2. The compounds can be used in the manufacture of a pharmaceutical composition for inducing cytokine biosynthesis, preferably the cytokine IFN-a, for treating viral disease and for treating neoplastic disease.
机译:描述了式(I)-(IX)和(XLIV)的化合物或药学上可接受的盐,其中:X为-CHR 3-,-CHR 3-烷基-或-CHR 3-烯基-; R 1是-杂芳基,-杂环基,-R 4-杂芳基或-R 4-杂环基,并且在式(V)和(VI)中,R 1也可以是-(CH 2)1-10-C℃-R 10; R 2是-氢,-烷基,-烯基,-芳基,-杂芳基,-杂环基,-烷基-Y-烷基,-烷基-Y-烯基,-烷基-Y-芳基或-烷基或被一个或多个取代的烯基。选自-OH,-卤素,-N(R 3)2,-CO-N(R 3)2,-CO-C 1-10烷基,-CO-O-C 1-10烷基,-N 3,-芳基,-杂芳基,-杂环基,-CO-芳基和-CO-杂芳基; R4是可以被一个或多个-O-基团间断的烷基或烯基;每个R 3独立地为H或C 1-10烷基;每个Y独立地是-O-或-S(O)0-2-; n为0至4;每个存在的R独立地选自C1-10烷基,C1-10烷氧基,羟基,卤素和三氟甲基; R 10为杂芳基和杂环基; R7是叔丁基或苄基; Z为NH2或NO2。该化合物可用于制备药物组合物,以诱导细胞因子的生物合成,优选细胞因子IFN-α,用于治疗病毒性疾病和用于治疗肿瘤性疾病。

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