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Use of 17-ketosteroid compounds and derivatives, metabolites and precursors thereof in the treatment of hepatitis C virus and other togaviruses

机译:17-酮类固醇化合物及其衍生物,代谢产物和前体在治疗丙型肝炎病毒和其他披膜病毒中的用途

摘要

A 17-ketosteroid derivative of formula (I) or the salts, stereoisomers, positional isomers, metabolites, analogs, precursors, hydrates, tautomers, ionized forms and solvates thereof is used in the manufacture of a medicament to treat or prevent togaviral infection, or to ameliorate or reduce one or more symptoms of a togaviral infection, in a subject suffering from or susceptible to the togaviral infection, In formula (I): Q1 is -C(R1)2- or -C(O)-; Q2 is -C(R1)2, -C(R1)(Y)-, -C(Y)- or CH2-CH2-; Q3 is -H or -C(R1)3-; Q4 is -C(R1)2-, -C(O)-, hydroxyvinylidine or methyl methylene; Q5 is -C(R1)2- or -C(O)-; Q6 is H, CH2OH or -C(R1)3- X and Y independently are -OH, -H, alkyl, -O-C(O)-R5, -C(O)-OR5, halogen or when a double bond exits between position 11 and -X, X is =O; each R1 independently is -H, halogen, -OH, alkoxy, or alkyl or at position 3 R1 is additionally OR53; R2 is-H, -OH, halogen, alkyl, alkoxy, -OR3, a fatty acid, alkynyl, (J)n-phenyl=alkyl, (J)n-phenyl-alkenyl, an ester, or -S- C(O)-(CH2)m-R4, -C(O)-S-(CH2)m-R4, -O-S(O)(O)-(CH2)m-R4, -O-S(O)(O)-O-(CH2)m-R4, -O-C(O)-NH-(CH2)m-R4, -NH-C(O)-O-(CH2)m-R4, -O-C(S)-(CH2)m-R4, -C(S)-O-(CH2)m-R4 or R2, together with the R1 that is bonded to the same carbon atom is =O; m is 0 to 3; R53, R3, R4, R5 are as defined in the specification and the dotted lines represent an optional double bond, provided that there are not double bonds at both the 4-5 and 5-6 positions and provided that when a double bond is present optionally an R1 group is bonded to carbon atoms at the 1-, 2-, 4-, 5- or -6 positions to satisfy the tetravalency of these carbon atoms provided that the compound is not dehydroepiandrosterone, dehydroepiandrosterone-3b-sulphate, 3b, 7b-dihydroandrost- 5-one or an ester or ether of any of these compounds..
机译:式(I)的17-酮类固醇衍生物或其盐,立体异构体,位置异构体,代谢产物,类似物,前体,水合物,互变异构体,离子化形式和溶剂化物被用于制备药物以治疗或预防披膜病毒感染,或在式(I)中,Q 1为-C(R 1)2-或-C(O)-;或改善或减轻所述病毒的一种或多种症状。 Q2是-C(R1)2,-C(R1)(Y)-,-C(Y)-或CH2-CH2-; Q3是-H或-C(R1)3-; Q4是-C(R1)2-,-C(O)-,羟乙烯基或甲基亚甲基; Q5是-C(R1)2-或-C(O)-; Q6是H,CH2OH或-C(R1)3--X和Y独立地是-OH,-H,烷基,-OC(O)-R5,-C(O)-OR5,卤素或当双键之间存在时位置11和-X,X == O每个R 1独立地为-H,卤素,-OH,烷氧基或烷基,或在3位R 1另外为OR53; R 2是-H,-OH,卤素,烷基,烷氧基,-OR 3,脂肪酸,炔基,(J)n-苯基=烷基,(J)n-苯基-烯基,酯或-S-C( O)-(CH2)m-R4,-C(O)-S-(CH2)m-R4,-OS(O)(O)-(CH2)m-R4,-OS(O)(O)- O-(CH2)m-R4,-OC(O)-NH-(CH2)m-R4,-NH-C(O)-O-(CH2)m-R4,-OC(S)-(CH2) m-R4,-C(S)-O-(CH2)m-R4或R2以及与相同碳原子键合的R1一起为= O; m为0至3; R53,R3,R4,R5如说明书中所定义,虚线表示可选的双键,条件是在4-5和5-6位置均不存在双键,并且当存在双键时任选地,R1基团在1,,2-,4-,5-或-6位置上的碳原子上键合以满足这些碳原子的四价,条件是该化合物不是脱氢表雄甾酮,脱氢表雄酮-3b-硫酸盐,3b, 7b-二氢雄酮-5-或这些化合物中任何一种的酯或醚。

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