摘要:
The invention pertains to triazolopurines of formula (I). The claimed compounds show an affinity to adenosine receptors and thus represent a new class of adenosine antagonists. Generally, adenosine antagonists can have a therapeutically useful effect in cases where diseases or pathological situations involve activation of adenosine receptors.
摘要:
The invention pertains to triazolopurines of formula (I). The claimed compounds show an affinity to adenosine receptors and thus represent a new class of adenosine antagonists. Generally, adenosine antagonists can have a therapeutically useful effect in cases where diseases or pathological situations involve activation of adenosine receptors.
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.
摘要:
New xanthine derivatives, a process for preparing the same and their use as medicaments are disclosed, as well as their use as intermediate compounds.