Alpha acid Derivatives hidrocarboxilico heterociclicamente replaced, their use for the preparation of a Pharmaceutical composition, combinations of these derivatives and one or more active substancesPharmaceutical preparations for peroral Administration and Structural fragment from parental and

摘要

Derivatives of the heterocyclicly substituted alpha-hydrocarboxylic acid according to formula (I) wherein R1 means tetrazole or a group of formula II where R has the following meaning: a) an OR5 moiety, wherein R5 means: hydrogen, the cation of an alkali metal , the cation of a physiologically tolerable alkaline earth metal or organic ammonium bond; C3-8 cycloalkyl C1-8 alkyl, CH2-phenyl, C3-8 alkenyl, C3-8 alkylinyl or phenyl optionally substituted. b) a 5-membered heteroaromatic compound, bound through a nitrogen atom, chosen from: pyrrolyl, pyrazolyl, imidazolyl and triazolyl, which can carry one or two halogen atoms,Or 1 to 2 groups of C1-4 tar, or 1 to 2 groups of C1-4 (III) formula.in which k can take the values 0, 1 and 2, p the values 1, 2, 3 and 4 and R6 represents: C1-4 alkyl, C3-8 cycloalkyl, C3-8 alkenyl, C3-8 alkynyl or possibly substituted phenyl ) a residue of formula (IV) wherein R7 means: C1-4 alkyl, C3-8 alkenyl, C3-8 alkynyl, C3-8 cycloalkyl, these being able to carry a C1-4 alkoxy moiety, C1-4 alkylthio and / or a phenyl moiety; C1-4 hologenoalkyl or phenyl, optionally substituted. A means NR8R9, azido, OR10, SR10, or C1-4 alkyl; X means oxygen, sulfur, CR11 or NR12; with the proviso that if X = CR11 then Y = oxygen or sulfur or NR14. Y means oxygen, sulfur, CR13 or NR14;The condition is y = oxygen or sulfur or nr14, eentonces x = cr11. R2 and R3 (may be the same or different) mean: phenyl or naftyl, which will eventually be replaced; ofenero or naftyl; they can be connected in orthogonal form through direct ligation, a methylene, ethylene or etenil group, an oazufe or a SO2, NH or N group (C1-4 tar);Cycloquilo C5-6, which will eventually be replaced; R4 and R11 (which may be the same or different) mean: hydrogen, halogenation, alcox C1-4, halogenated propoxyc1-4, alqueniloxi C3-6, asphalt C3-6, C1-4, C1-4, alcoxilo carbon-4,