首页> 外国专利> DERIVATIVES OF TRIAZOLYL-IMIDAZOPYRIDINE AND OF THE TRIAZOLYLPURINES USEFUL AS LIGANDS OF THE ADENOSINE A2a? RECEPTOR AND THEIR USE AS MEDICAMENTS

DERIVATIVES OF TRIAZOLYL-IMIDAZOPYRIDINE AND OF THE TRIAZOLYLPURINES USEFUL AS LIGANDS OF THE ADENOSINE A2a? RECEPTOR AND THEIR USE AS MEDICAMENTS

机译:作为腺嘌呤A2a配体的三唑基-咪唑并吡啶衍生物和三唑类的衍生物?受体及其作为药物的用途

摘要

Compounds of formula (I) wherein: X is N; RSUB1 /SUBis CSUB1/SUB-CSUB6 /SUBlinear or branched alkyl or CSUB1/SUB-CSUB6 /SUBlinear or branched alkenyl; RSUB2 /SUBis hydrogen, CSUB1/SUB-CSUB6 /SUBlinear or branched alkyl or CSUB1/SUB-CSUB6 /SUBlinear or branched alkenyl, CSUB6/SUB-CSUB14 /SUBaryl or CSUB6/SUB-CSUB14 /SUBaryl(CSUB1/SUB-CSUB6/SUB) linear or branched alkyl or CSUB6/SUB-CSUB14 /SUBaryl(CSUB1/SUB-CSUB6/SUB) linear or branched alkenyl, with the aryl group optionally substituted by one or more substituents, either the same or different, selected from the group consisting of halogen, hydroxy, CSUB1/SUB-CSUB6 /SUBalkoxy linear or branched or CSUB1/SUB14 CSUB6 /SUBalkenyloxy linear or branched, amino, optionally mono- or disubstituted with CSUB1/SUB-CSUB6 /SUBlinear or branched alkyl; RSUB3 /SUBis NHSUB2/SUB, NHRSUB4/SUB; RSUB4 /SUBis CSUB1/SUB-CSUB6 /SUBalkyl or CSUB1/SUB-CSUB6 /SUBhydroxyalkyl, CSUB1/SUB-CSUB3 /SUBalkoxyalkyl, amino(CSUB1/SUB-CSUB6/SUB)alkyl, where the amino group is optionally substituted with one or two CSUB1/SUB-CSUB3 /SUBlinear or branched alkyl groups, or with one or two CSUB2/SUB-CSUB3 /SUBalkenyl groups CSUB6/SUB-CSUB14 /SUBaryl or CSUB6/SUB-CSUB14 /SUBaryl(CSUB1/SUB-CSUB6/SUB)alkyl, with the aryl group optionally substituted by one or more substituents, either the same or different, selected from the group consisting by halogen, hydroxy, CSUB1/SUB-CSUB6 /SUBalkoxy linear or branched or CSUB1/SUB-CSUB6 /SUBalkenyloxy linear or branched, amino, mono- or di-substituted with CSUB1/SUB-CSUB6 /SUBalkyl linear or branched or CSUB1/SUB-CSUB6 /SUBalkenyl linear or branched; and their pharmaceutically acceptable salts. These compounds are antagonists of the adenosine ASUB2a /SUBreceptor and useful as medicaments, in particular for the treatment of Parkinson's disease.
机译:式(I)的化合物,其中:X为N; R 1 是C 1 -C 6 直链或支链烷基或C 1 -C 6 < / SUB>直链或支链烯基; R 2 是氢,C 1 -C 6 直链或支链烷基或C 1 -C 6 直链或支链烯基,C 6 -C 14 芳基或C 6 -C 14 芳基(C 1 -C 6 )直链或支链烷基或C 6 -C 14 芳基(C < SUB> 1 -C 6 )直链或支链烯基,其中的芳基可选地被一个或多个选自卤素,羟基的相同或不同取代基取代,C 1 -C 6 烷氧基直链或支链或C 1 14 C 6 烯氧基直链或支链的氨基,任选被C 1 -C 6 直链或支链烷基单取代或二取代; R 3 是NH 2 ,NHR 4 ; R 4 是C 1 -C 6 烷基或C 1 -C 6 羟烷基,C 1 -C 3 烷氧基烷基,氨基(C 1 -C 6 )烷基,其中氨基该基团任选被一个或两个C 1 -C 3 直链或支链烷基,或一个或两个C 2 -C < SUB> 3 烯基C 6 -C 14 芳基或C 6 -C 14 芳基(C 1 -C 6 )烷基,其中芳基任选地被一个或多个选自卤素,羟基的相同或不同取代基取代,C 1 -C 6 烷氧基直链或支链或C 1 -C 6 烯氧基直链或支链的氨基,被直链或支链的C 1 -C 6 烷基或C 1 -C 6 单或二取代>烯基直链或支链;及其药学上可接受的盐。这些化合物是腺苷A 2a 受体的拮抗剂,可用作药物,特别是用于治疗帕金森氏病。

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