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    NEUE UNSYMMETRISCH SUBSTITUIERTE XANTHIN-DERIVATE, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG ALS ARZNEIMITTEL MIT ADENOSINANTAGONISTISCHER WIRKUNG
    2.
    发明公开
    NEUE UNSYMMETRISCH SUBSTITUIERTE XANTHIN-DERIVATE, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG ALS ARZNEIMITTEL MIT ADENOSINANTAGONISTISCHER WIRKUNG 审中-公开
    新的取代不平衡黄嘌呤衍生物，其制造方法相同，并且它们作为WITH EFFECT ADENOSINANTAGONISTISCHER DRUGS

    公开(公告)号：EP1084123A1

    公开(公告)日：2001-03-21

    申请号：EP99916914.7

    申请日：1999-04-13

    申请人： Boehringer Ingelheim Pharma KG

    发明人： BLECH, Stefan ,  CARTER, Adrian ,  GAIDA, Wolfram ,  GATH, Ursula ,  HOFFMANN, Matthias ,  KUEFNER-MUEHL, Ulrike ,  LEHR, Erich ,  MIERAU, Joachim ,  POHL, Gerald ,  WEISER, Thomas

    IPC分类号： C07D473/06 ,  A61K31/52

    CPC分类号： C07D473/06 ,  C07D473/04

    摘要： The invention relates to novel asymmetrically substituted xanthine derivatives of general formula (I), to methods for producing them and to their use as medicaments with an adenosine-antagonistic effect. The broken line between the nitrogen atoms of the general formula (I) indicates the existence of a double bond in one of two possible positions so that the radicals R?4 and R5¿ cannot be present at the same time. R1 cannot have the meaning of R2 at the same time. The radicals R?1, R2, R3, R4 and R5¿ are defined as follows: R1 is hydrogen, C¿1?-C6 alkyl, C3-C6 alkenyl or C3-C6 alkinyl; R?2¿ is a C¿1?-C6 alkyl, C3-C6 alkenyl or C3-C6 alkinyl radical which is substituted by -OR?6, -SO¿2R?6, -OCOR9, -COOR9, -NR7R8¿, -OCH¿2?CH2-NR?7R8, -CONR7R8¿, -OCH¿2?-CONR?7R8¿ or OCH¿2?CH2-CONR?7R8; R2¿ is a C¿1?-C6 alkyl, C3-C6 alkenyl or C3-C6 alkinyl radical which is substituted by a C-bonded 5 or 6-membered heterocyclic ring which may contain 1, 2, 3 or 4 heteroatoms selected from the following group: oxygen, nitrogen or sulphur; and may optionally be substituted by C1-C4 alkyl or benzyl; R?3 is C¿1-C6 alkyl which can be substituted by OH or optionally, norbornanyl, norbornenyl, adamantyl or noradamantyl substituted by methyl or OH and R4 or R5 is hydrogen, benzyl or benzyl substituted once, twice or three times by methoxy. R6 can mean hydrogen, C¿3?-C6 cycloalkyl or C1-C4 alkyl which may be substituted by -OR?9¿ or -OCOR9, R7 can mean hydrogen, -SO¿2R?6, C1-C4 alkyl, -COR9 or -COOR9; R8 can mean hydrogen, -SO¿2R?6, C1-C4 alkyl, -COR9 or -COOR?9 or R7 and R8¿ can form a 5 or 6-membered ring together with the nitrogen, whereby said ring may contain oxygen or nitrogen as a further heteroatom and may optionally be substituted by C¿1?-C4 alkyl or benzyl; and R?9¿ can mean hydrogen or C¿1?-C4 alkyl, optionally in the form of their racemates, their enantiomers, their diastereomers and their mixtures, and optionally in the form of their pharmacologically safe acid addition salts.