| 摘要 |
Disclosed herein are small molecule heterocyclic inhibitors of sepiapterin reductase (SPR), and prodrugs and pharmaceutically acceptable salts thereof. The Also featured are pharmaceutical compositions of the compounds and uses of these compounds for the treatment or prevention of pain (e.g., inflammatory pain, nociceptive pain, functional pain, and neuropathic pain). |
| 主权项 |
1. A compound of Formula (1): wherein, X1 and X2 are independently selected from N, C—H, and C-halogen; R2 is CH2OR2A or C1-6 alkyl; R2A is H or C1-6 alkyl; R3A and R3B are both H; R4A and R4B are both H; and R5 and R6 are independently selected from the group consisting of H and C1-6 alkyl
wherein the alkyl may be unsubstituted or substituted one or more times with groups independently selected from the group consisting of: C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, heteroaryl, halogen; azido(—N3), nitro (—NO2), cyano (—CN), acyloxy(—OC(═O)R′), acyl (—C(═O)R′), alkoxy (—OR′), amido (—NR′C(═O)R″ or —C(═O)NRR′), amino (—NRR′), carboxylic acid (—CO2H), carboxylic ester (—CO2R′), carbamoyl (—OC(═O)NR′R″ or —NRC(═O)OR′), hydroxy (—OH), isocyano (—NC), sulfonate (—S(═O)2OR), sulfonamide (—S(═O)2NRR′ or —NRS(═O)2R′), or sulfonyl (—S(═O)2R), where each R or R′ is selected, independently, from H, C1-6 alkyl, C2-6 alkenyl, C2 -6 alkynyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl; or the compound is a pharmaceutically acceptable salt thereof. |
