Compounds having the formula (I):
wherein A represents a group such as a cyclic group, R
1
and R
2
represent groups such as alkyl groups or hydroxymethyl groups, and n represents 1 or 2, or pharmacologically acceptable salts thereof or pharmacologically acceptable esters thereof have superior activity and stability, and are useful for the treatment and/or prevention of diabetes mellitus, or the like.
A pharmaceutical composition effective for the prophylaxis and treatment of diabetes is provided. This pharmaceutical composition comprises the combination of an α-amylase inhibitor selected from a compound represented by the following general formula (I):
[wherein A represents, for example, a cyclic group, etc.
R
1
and R
2
represent an alkyl group, hydroxymethyl group, etc., and n represents 1 or 2], or a pharmacologically acceptable salt or ester thereof, and at least one type of drug selected from an insulin sensitizer, an insulin secretagogue, a biguanide drug, an insulin preparation and a DPP-IV inhibitor.
Compounds having the formula (I):
wherein A represents a group such as a cyclic group, R
1
and R
2
represent groups such as alkyl groups or hydroxymethyl groups, and n represents 1 or 2, or pharmacologically acceptable salts thereof or pharmacologically acceptable esters thereof have superior activity and stability, and are useful for the treatment and/or prevention of diabetes mellitus, or the like.
A pharmaceutical composition effective for the prophylaxis and treatment of, diabetes is provided. This pharmaceutical composition comprises the combination of an α-amylase inhibitor selected from a compound represented by the following general formula (I):
[wherein A represents, for example, a cyclic group, etc.
R1 and R2 represent an alkyl group, hydroxymethyl group, etc., and n represents 1 or 2], or a pharmacologically acceptable salt or ester thereof, and at least one type of drug selected from an insulin sensitizer, an insulin secretagogue, a biguanide drug, an insulin preparation and a DPP-IV inhibitor.
本发明提供了一种有效预防和治疗糖尿病的药物组合物。这种药物组合物包括一种α-淀粉酶抑制剂,该抑制剂选自以下通式(I)所代表的化合物:
[其中 A 代表环状基团等。
R1和R2代表烷基、羟甲基等,n代表1或2],或其药理上可接受的盐或酯,以及至少一种选自胰岛素增敏剂、胰岛素促泌剂、双胍类药物、胰岛素制剂和DPP-IV抑制剂的药物。
[EN] TUMOR-INHIBITING SACCHARIDE CONJUGATES
申请人:DEUTSCHES KREBSFORSCHUNGSZENTRUM STIFTUNG DES ÖFFENTLICHEN RECHTS
公开号:WO1990004597A1
公开(公告)日:1990-05-03
(DE) Die Erfindung betrifft ein Verfahren zur Herstellung von Glycokonjugaten von Phosphoramiden der allgemeinen Formel (1) und (1a), wobei die Verknüpfung des Zuckers mit der Phosphoramid-Lost-Funktion bzw. der Ifosfamid-Lost-Funktion, vorzugsweise in der 1-Stellung erfolgt und R1 und R2 gleich oder verschieden sein und Wasserstoff, niederes C1-C4-Alkyl oder C1-C6-Halogenalkyl bedeuten können und als Zucker Mono-, Di- oder Polysaccharide in allen existierenden isomeren und enantiomeren Formen vorliegen können, indem man in an sich bekannter Weise geschützte Bromzucker mit den entsprechenden Phosphorverbindungen konjugiert und von den Schutzgruppen befreit sowie D-Glucopyranosyl-N,N'-Di(2-chlorethyl)-phosphorsäurediamide und die Verwendung der Verbindungen als Antitumormittel.(EN) The invention concerns a process for preparing glycoconjugates of phosphoramides of general formula (1) and (1a) in which the sugar is linked to the phosphoramide mustard function or the ifosfamide mustard function preferably in the 1 position and R1 and R2 are identical or different and may denote hydrogen, lower C1-C4 alkyl or C1-C6 alkyl halide and the sugar may be present as mono-, di- or polysaccharides in all existing isomeric and enantiomeric forms by conjugating protected bromine sugar in a manner known per se with the corresponding phosphorus compounds and releasing it from the protective groups. Also described are D-glycopyranosyl-N,N'-di(2-chloroethyl)-phosphoric acid diamides and the use of the compounds as antitumoral agents.(FR) Est décrit un procédé pour préparer des glycoconjugués de phosphoramides de formule générale (1) et (1a), où le sucre est lié à la fonction phosphoramide-ypérite ou la fonction ifosfamide-ypérite de préférence en position 1, et R1 et R2 sont identiques ou différents et peuvent représenter hydrogène, alkyle inférieur, C1-C4 ou halogénure d'alkyle C1-C6 et le sucre peut être présent à titre de mono, di- ou polysaccharides sous toutes les formes isomères et énantiomères existantes, en conjuguant du sucre de bromure protégé d'une manière connue en soi avec les composés de phosphores correspondants et en le libérant des groupes protecteurs. Sont également décrits des D-glucopyranosyl-N,N'-di(2-chloréthyl)-diamides d'acide phosphorique, ainsi que l'emploi de ces composés comme agents antitumoraux.