摘要:
Disclosed are quinoxalinone compounds of the formula I or Ia ##STR1## and physiologically tolerated salts and prodrugs thereof, in which n=zero, one or two; R.sup.1 =fluorine, chlorine, hydroxyl or C.sub.1 -C.sub.3 -alkoxy; R.sup.2 =C.sub.1 -C.sub.4 -alkyl which is unsubstituted or is substituted by hydroxyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -alkylthio; R.sup.3 =C.sub.1 -C.sub.6 -alkyloxycarbonyl or C.sub.2 -C.sub.6 -alkenyloxycarbonyl, and X=oxygen, sulfur or selenium, a process for their preparation and pharmaceutical compositions containing the compounds.
摘要:
The use of a compound of the formula I ##STR1## in which V is an alkyl group, fluorine, chlorine, bromine, or iodine, n is an integer from 1 to 5, W is an alkyl, alkenyl, alkynyl or alkoxy group, cyanide, nitro, carboxyl, hydrogen or a cycloalkyl, aryl, aralkyl or carboalkoxy group, R.sup.1 and R.sup.2 are an alkyl, alkenyl, alkynyl, cycloalkyl or halogenoalkyl group, sodium, potassium, calcium, magnesium, aluminum, lithium, ammonium, triethylammonium or hydrogen, R.sup.1 and R.sup.2 together form a cyclic diester, R.sup.3 and R.sup.4 are an alkyl, alkenyl, alkynyl, carboalkoxy, cycloalkyl or alkoxy group, hydrogen, fluorine, chlorine, bromine or iodine and X, Y and Z are oxygen or sulfur, for the treatment of diseases caused by DNA viruses or RNA viruses is described.
摘要:
The invention relates to compounds of the formula I ##STR1## where R.sup.1 is H, alkyl, acyl, aryl, or a phosphate residue; R.sup.2 is H, OH, alkoxy, NH.sub.2, or halogen; B is a base customary in nucleotide chemistry; a is O or CH.sub.2 ; n is an integer from 1 to 100; W=O, S or Se; V=O, S, or NH; Y=O, S, NH, or CH.sub.2 ; Y'=O, S, NH, or alkylene; X=OH or SH; U=OH, SH, SeH, alkyl, alkoxy, aryl, aryloxy, or amine, and Z=OH, SH, SeH, an optionally substituted radical from the group comprising alkyl, aryl, heteroaryl, alkoxy, or amino, or a group which favors intracellular uptake or serves as the label of a DNA probe or attacks the target nucleic acid during hybridization, where if Z=OH, SH, CH.sub.3, or OC.sub.2 H.sub.5, at least one of the groups X, Y, Y', V, or W is not OH or O or R.sup.1 is not H; a process for their preparation and their use as inhibitors of gene expression, as probes for detecting nucleic acids and as aids in molecular biology.
摘要翻译:本发明涉及式Ⅰ化合物,其中R1是H,烷基,酰基,芳基或磷酸酯残基; R2是H,OH,烷氧基,NH2或卤素; B是核苷酸化学中常规的基础; a是O或CH2; n为1〜100的整数, W = O,S或Se; V = O,S或NH; Y = O,S,NH或CH 2; Y'= O,S,NH或亚烷基; X = OH或SH; U = OH,SH,SeH,烷基,烷氧基,芳基,芳氧基或胺,Z = OH,SH,SeH,任选取代的基团,其包含烷基,芳基,杂芳基,烷氧基或氨基, 其有利于细胞内吸收或用作DNA探针的标记或在杂交期间攻击靶核酸,其中如果Z = OH,SH,CH 3或OC 2 H 5,X,Y,Y',V, 或W不是OH或O或R 1不是H; 其制备方法及其作为基因表达抑制剂的用途,作为检测核酸的探针和分子生物学的辅助工具。
摘要:
Compounds of the formula I, ##STR1## and also their tautomeric forms of the formula Ia, ##STR2## in which the substituents R.sup.1 to R.sup.6 and X have said meanings, exhibit antiviral activity.
摘要:
The invention relates to compounds of formula (I) wherein the groups R and R′, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.
摘要:
Substituted quinoline derivatives, processes for their preparation, and their use.Compounds of the formula I ##STR1## and their tautomeric forms, of the formula Ia ##STR2## in which m, n and the substituents X and R.sup.1 to R.sup.5 have the meanings mentioned, have an action against viruses.
摘要:
The invention concerns prodrugs of enzyme inhibitors in which at least one OH-- group in the enzyme inhibitor has been converted into a derivative grouping of the formula III, IV or V: ##STR1## in which the groups R.sup.11 to R.sup.25 and s,l, m, o, q, and r are as defined in the description. Such prodrugs exhibit an improved solubility in water and improved pharmaco-kinetic characteristics.
摘要:
The disclosure relates to a compound of the formula (I) wherein R1 is H, C(O)—(C1-C6)alkyl or C(O)—O—(C1-C6)alkyl; R2 is OH, NH2, NH—(C1-C6)alkyl, NH—(C1-C4)alkylene-phenyl or NH—(C1-C4)alkylene-pyridyl; R3 and R4 are independently of each other H or OH, or R3 and R4 together are ═O; and m and n are independently of one another 0, 1 or 2; in any stereochemical form, or a mixture of any stereochemical forms in any ratio, or a physiologically acceptable salt thereof, obtainable from Actinomadura namibiensis (DSM 6313), and its use for the treatment of bacterial infections, viral infections and/or pain, and pharmaceutical composition comprising it.