3-AMINO-TRIAZOLE DERIVATIVES WITH MEDICINAL APPLICABILITY, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE

• Main Authors: MORVAI MIKLOS, PODANYI BENJAMIN DR, GOENCZI CSABA DR, HEJA GERGELY DR, VARKONYINE SCHLOVICSKO ERIKA, CSIKOS EVA
• Format: Patent
• Language: English; Hungarian
• Published: 28.03.2003
• Edition: 7

3-[2-[[[1-(2-Cyclohexylethyl)-5-(2,5-dimethoxy-4-methylphenyl)-1H-1,2,4-triazol-3-yl]amino]carbonyl]-6-methoxy-4,5-1H-indol-1-yl]propionic acid (I) and its solvates, hydrates, polymorphs or salts are new. Independent claims are included for included for the following: (1) salts of (I) obtained with ethanolamine (a), diethanolamine (b), diethylamine (c) or adamantanamine (d); (2) preparation of (I) by hydrolyzing a compound of formula (II); and if desired further converting into its solvates, hydrates, polymorphs and salts; and (3) use of (I) in the preparation of a medicament. ACTIVITY : Anorectic; Antiinflammatory; Neuroleptic; Antiparkinsonian; Nootropic; Anti-HIV; Tranquilizer; Neuroprotective; and Gastrointestinal-Gen. MECHANISM OF ACTION : Cholecystokin in (cck 1) receptor agonist. The agonist activity of 3-[2-[[[1-(2-cyclohexylethyl)-5-(2,5-dimethoxy-4-methylphenyl)-1H-1,2,4-triazol-3-yl]amino]carbonyl]-6-methoxy-4,5-1H-indol-1-yl]propionic acid) (I) towards cck 1 receptors was evaluated in vitro in 3T3 cells expressing the human cck 1 receptor, by measuring the mobilization of intracellular calcium (Ca 2> +>), according to technique derived from Lignon MF et al.,Ear.J.pharmacolo., 1993, 245, 241 - 245.. The calcium concentration was evaluated by Fura-2 by the double excitation wavelength method. (I) had an EC 50 of 1nM. A találmány az (I) képletű sav polimorf és pszeudopolimorfmódosulataira és az (I) képletű sav, polimorf és pszeudopolimorfmódosulatainak etanolaminnal, vagy dietanolaminnal, vagydietilaminnal, vagy Adamantán-aminnal képezett új sóira, a vegyületekelőállítási eljárására és azokat tartalmazó gyógyászati készítményekreés ezek alkalmazására vonatkozik gasztrotesztinális rendszer, illetvea központi idegrendszer rendellenességeinek kezelésével. Ó