NOVEL THEOPHYLLINE DERIVATIVES, SUBSTITUTED IN POSITION -7 AND PROCESS FOR PREPARING AND USE THEREOF

7-(1,2,4-Oxadiazol-3-yl alkyl)-theophylline derivs. of formula (I) and their physiologically tolerable acid addn. salts are new. In (I), A is opt. branched 1-5C alkylene or -CH2-CHOH-CH2-; and R1 is 1-10C alkyl, haloalkyl or hydroxyalkyl, 5-6C cycloalkyl, vinyl, 2-ethoxyethyl, carboxylalkyl, or a gp...

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Hauptverfasser: GONCZI CSABA, PALOSI ENDRE, MINKER EMIL DR, KISS PAL, SZUTS TAMAS, SZOMOR MARIA, KUN JUDIT, SEBESTYEN GYULA DR, KOVACS GABOR, KORBONITS DESZO, HEJA GERGELY, VIRAG SANDOR DR, SZVOBODA IDA
Format: Patent
Sprache:eng
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Zusammenfassung:7-(1,2,4-Oxadiazol-3-yl alkyl)-theophylline derivs. of formula (I) and their physiologically tolerable acid addn. salts are new. In (I), A is opt. branched 1-5C alkylene or -CH2-CHOH-CH2-; and R1 is 1-10C alkyl, haloalkyl or hydroxyalkyl, 5-6C cycloalkyl, vinyl, 2-ethoxyethyl, carboxylalkyl, or a gp. -(CH2)n-CHR-N(R2)(R3) in which R is H or CH3, n is 0, 1, 2 or 3, and R2 and R3 are H or 1-4C alkyl or N(R2)(R3) is a 5- or 6-membered heterocyclic ring opt. additionally contg. an O-atom or an NH- or NCH3 gp.; or R1 is an opt. substd. phenyl gp. C6H3(R4)(R5) in which R4 and R5 are H, Cl, OH, OCH3, OC2H5, CH3 or amino; or R1 is OH, benzyl, 2,2-diphenylethyl or theophyllin-4-ylmethyl. The new cpds. have antitussive, bronchodilating and antiinflammatory activity, with adiantaysom toxicological, absorption and solubility properties. Specific (I) include 7-((5-methyl-1,2,4- oxodiazol-3-yl)-methyl) theophylline.