摘要:
The present invention relates to novel compounds of formula I
wherein: q is 0 or 1; • A is -S- and B is =N-; or • A is =N- and B is -S-; one of -A≃C(R 6 )- or -B≃C(R 6 )- is a double bond and the other is a single bond; R 1 is selected from the group consisting of hydroxyl, alkoxy, substituted alkoxy, acyloxy, cycloalkoxy, substituted cycloalkoxy, aryloxy, substituted aryloxy, heteroaryloxy, substituted heteroaryloxy, heterocyclyloxy, substituted heterocyclyloxy, mercapto, thioether, sustituted alkylthio, arylsulfanyl, heteroarylsulfanyl, amino, substituted amino, acylamino, and aminoacyl; R 2 is selected from the group consisting of hydrogen, deuterium, and methyl; R 3 is selected from the group consisting of hydrogen, deuterium, alkyl, and substituted alkyl; R 4 is selected from the group consisting of hydrogen, alkyl, and substituted alkyl; and R 5 and R 6 are as defined in claim 1; capable of modulating the stability and/or activity of hypoxia inducible factor (HIF).
摘要翻译:本发明涉及新的式I化合物,其中:q为0或1; ¢A是-S-,B是= N-; 或¢A为= N-和B为-S-; -A‰ƒC(R 6) - 或-B‰ƒC(R 6) - 是双键,另一个是单键; R 1选自羟基,烷氧基,取代的烷氧基,酰氧基,环烷氧基,取代的环烷氧基,芳氧基,取代的芳氧基,杂芳氧基,取代的杂芳氧基,杂环氧基,取代的杂环氧基,巯基,硫醚,取代的烷硫基,芳基硫烷基,杂芳基硫烷基,氨基 取代氨基,酰氨基和氨酰基; R 2选自氢,氘和甲基; R 3选自氢,氘,烷基和取代的烷基; R 4选自氢,烷基和取代的烷基; R 5和R 6如权利要求1所定义; 能够调节缺氧诱导因子(HIF)的稳定性和/或活性。
摘要:
The present invention relates to novel compounds of formula (I) capable of modulating the stability and/or activity of hypoxia inducible factor (HIF) by inhibiting the activity of at least one HIF hydroxylase enzyme.
摘要:
The present invention relates to methods for treating anemia by increasing endogenous erythropoietin via inhibition of HIF prolyl hydroxylase enzyme activity.
摘要:
The present invention relates to novel compounds of formula (I), and compositions capable of inhibiting PHD1 enzyme activity selectively over other isoforms, for example, PHD2 and/or PHD3 enzymes. The invention also relates to compounds of formula (I) for use in disorders such as muscle degeneration, colitis, IBD, and certain ischemias.
摘要:
The present invention relates to novel compounds, methods, and compositions capable of decreasing HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).
摘要:
The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF) by inhibiting the activity of at least one HIF hydroxylase enzyme.
摘要:
The present invention relates to compounds for use in methods for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo . Compounds for use in methods for treating, pretreating or preconditioning, or preventing erythropoietin-associated conditions are also included.