20-07-2017 дата публикации
Номер: US20170204101A1
The present disclosure provides compounds useful in the amelioration, prevention or treatment of A3 adenosine receptor mediated diseases, such as glaucoma and glaucoma-related ocular disorders, having the structure of Formula I as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for ameliorating, preventing or treating A3 adenosine receptor mediated diseases using the compound. 2. The compound of claim 1 , wherein Ris NRRor CRRR claim 1 , wherein said R claim 1 , R claim 1 , and Rare each independently H claim 1 , C1-6 alkyl claim 1 , substituted C1-6 alkyl claim 1 , C3-7 cycloalkyl claim 1 , substituted C3-7 cycloalkyl claim 1 , aryl claim 1 , substituted aryl claim 1 , heteroaryl claim 1 , substituted heteroaryl claim 1 , heterocycle claim 1 , substituted heterocycle claim 1 , heterocycloalkyl claim 1 , substituted heterocycloalkyl claim 1 , or C2-6 alkynyl optionally substituted with aryl or heteroaryl.3. The compound of claim 1 , wherein the compound is any one selected from the group consisting of(2S,3R,4S)-2-(8-((3-chlorobenzyl)amino)-[1,2,4]triazolo[4,3-a]pyrazine-3-yl)tetrahydrothiophene-3,4-diol (Compound 1),(2S,3R,4S)-2-(8-(methylamino)-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)tetrahydrothiophene-3,4-diol (Compound 2),(2S,3R,4S)-2-(8-(benzylamino)-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)tetrahydrothiophene-3,4-diol (Compound 5),(2S,3R,4S)-2-(8-((3-iodobenzyl)amino)-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)tetrahydrothiophene-3,4-diol (Compound 6),(2S,3R,4S)-2-(8-((cyclopropylmethyl)amino)-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)tetrahydrothiophene-3,4-diol (Compound 7),(2S,3R,4S)-2-(8-(cyclobutylamino)-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)tetrahydrothiophene-3,4-diol (Compound 8),(2S,3R,4S)-2-(8-((3-(trifluoromethyl)benzyl)amino)-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)tetrahydrothiophene-3,4-diol (Compound 9),(2S,3R,4S)-2-(8-((thiophen-3-ylmethyl)amino)-[1,2,4]triazolo[4,3-a]pyrazin-3-yl)tetrahydrothiophene-3,4- ...
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