New xanthine derivs. are selective A1 adenosine antagonists - useful for treating CNS disorders (e.g. senile dementia) and heart and circulation disorders

Xanthine derivs. of formula (I), as racemates, optically active cpds., pure diastereomers or mixts., and their pharmaceutically acceptable acid addn. salts are new. R1 and R2 = 1-6C alkyl or 3-4C alkenyl or alkynyl; R3 = (a) N-linked, opt. substs. satd. or unsatd. 5-7 membered N-cont. heterocycle, o...

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Hauptverfasser:	SCHINGNITZ, GUENTER., 6550 BAD KREUZNACH, DE, ENSINGER, HELMUT. DR., 6507 INGELHEIM, DE, KUHN, FRANZ JOSEF., 6535 GAU-ALGESHEIM, DE, LEHR, ERICH., 6531 WALDALGESHEIM, DE, STRANSKY, WERNER. DR., 6535 GAU-ALGESHEIM, DE, KUEFNER-MUEHL, ULRIKE. DR., 6500 MAINZ, DE, WEBER, KARL-HEINZ. DR., 6535 GAU-ALGESHEIM, DE, WALTHER, GERHARD. DR., 6530 BINGEN, DE
Format:	Patent
Sprache:	eng ; ger
Schlagworte:	BLASTING CHEMISTRY DERIVATIVES THEREOF HEATING HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE INDEXING SCHEME RELATING TO MATERIALS, MATERIAL PROPERTIES ORMATERIAL CHARACTERISTICS FOR MACHINES, ENGINES OR PUMPS OTHERTHAN NON-POSITIVE-DISPLACEMENT MACHINES OR ENGINES INDEXING SCHEMES RELATING TO ENGINES OR PUMPS IN VARIOUSSUBCLASSES OF CLASSES F01-F04 LIGHTING MECHANICAL ENGINEERING MEDICAL OR VETERINARY SCIENCE METALLURGY NUCLEIC ACIDS NUCLEOSIDES NUCLEOTIDES ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS SUGARS WEAPONS
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Beschreibung
Zusammenfassung:	Xanthine derivs. of formula (I), as racemates, optically active cpds., pure diastereomers or mixts., and their pharmaceutically acceptable acid addn. salts are new. R1 and R2 = 1-6C alkyl or 3-4C alkenyl or alkynyl; R3 = (a) N-linked, opt. substs. satd. or unsatd. 5-7 membered N-cont. heterocycle, opt. contg. as further heteroatom O, S and/or substd. N, and opt. substd. by 1-6C alkyl, OR4, OR7, Oxo, (CH2)1-4(OR4 or OR7); (b) monosaccharide residue; (c) opt. substd. 4-8C cycloalkane, cycloalkanone or cycloalkanol; opt. substd. by 1 or more 1-6C alkyl; 3-6C alkenyl or alkynyl; 1-4C alkylidene; opt. substd. phenyl; opt. substd. aralkyl; NR5R6; COOR4; CONR5R6; OR4; SR4; OR7; (CH2)1-4(CONR5R6, NR5R6 or NHR7); 1-4C alkyl substd. by SR4, OR4, OR7 or COOR4; NHR7; NHCO(1-6C alkyl) or opt. substd. 3-6C cycloalkyl; (i) where A = O or Si m and n = 0-6, totalling 2-6; Ra and Rb = 1-4C alkyl or together form a 203C alkylene bridge (opt. substd. by 1 or 2 1-5C alkyl, 1-5C alkoxycarbonyl or 1-5C hydroxyalkyl) and the carbocyclic ring of the ketal can be substd. by 1 or more of the opt. substits. listed in (b); (ii) where A1 = CH2, O or S; n' and m' = 0-4, totalling 2-4; one or both rings can be substd. by 1 or more of the substits. listed in (b) (but excluding (CH2)1-4-NHR7) or oxo; (iii)-(ix) where A'' = O, CH2 or CH2CH2, and A'' - contg. ring systems can be substd. by 1 or more of 1-6C alkyl, 2-6C alkenyl or alkynyl, NR5R6, COOR4, CONR5R6, OR4, OR7, SR4, oxo, CH2OR4, CH2OR7, CH2COOR4 or CH2CONR5R6; R4 = H, 1-8C alkyl, opt. substd. 3-6C cycloalkyl, opt. substd. 1-4C alkylphenyl, 3-6C alkenyl or opt. substd. aralkyl, R5 = H, 1-6C alkyl, opt. substd. 3-6C cycloalkyl or opt. substd. aralkyl; R6 = H, 1-6C alkyl, opt. substd. aralkyl, (CH2)n''-(NR5R5, CN, OR4, OR7 or NHR7); n'' = 2-8; R5 + R6 can (substd.) 5-7 membered ring, opt. contg. O, S or N (opt. substd. by R4); R7 = CO-bond residue of a natural aminoacid, 1-13C alkylocarbonyl or opt. substd. 1-13C alkylbenzoyl; R8 and R9 The invention concerns new xanthine derivatives of formula (I), a method for preparing them, and their use as drugs.