| 摘要 |
Disclosed are chemical entities that inhibit Uba6, each of which is a compound of Formula /: Formula (I) or a pharmaceutically acceptable salt thereof, wherein R*1 is —H or —CH3; and Y is Formula (II) or Formula (III), wherein R2 is —H, —CH3 or C1-4 alkyloxycarbonyl; and RS7.1, RS7.2 and RS8.1 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers. |
| 主权项 |
1. A chemical entity comprising a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein: R*1 is —H or —CH3; Y is R2 is —H, —CH3 or —C(═O)—OR†4; each of RS7.1 and RS7.2 is independently —H, (a) halo, (b1) C1-3 aliphatic, (b2) R#2-1, (c) —OR*3, (d) —N(R*3)2 or (e) —SR†3; RS8.1 is —H, (a) halo, (b1) C1-4 aliphatic, (b2) R̂4-2, (c) —OR*4, (d) —N(R*4)2, (e) —SR†4 (f) C1-3 fluoroalkyl, (g1) C1-2 fluoroalkoxy, (g2) C1-2 fluoroalkylthio, (h) —NO2, (i) —CN, (j) —C(O)—R†4, (k) —C(O)—OR*4, (I) —C(O)—N(R*4)2, (n) —N(R*4)—C(O)—R†, (q) —N(R*4)—C(O)—OR*4 or (r) —N(R*4)—C(O)—N(R*4)2;
provided that at least one of RS7.1, RS7.2 and RS8.1 is —H; each instance of R*4 is independently —H or C1-4 alkyl; each instance of R*3 is independently —H or C1-3 alkyl; each instance of R†4 is independently C1-4 alkyl; each instance of R†3 is independently C1-3 alkyl; each instance of R̂4-2 is independently wherein represents C1-4 alkyl; and each of m1 and m2 is independently 0 or 1; each instance of R#2-1 is independently wherein represents C1-2 alkyl; and m1 is 0 or 1. each instance of RS1 is independently —H, (a) halo, (c) —OR*2, (d) —N(R*2)2 or (e) —SR†2; and each instance of RS2 is independently —H, (a) halo, (c) —OR*2, (d) —N(R*2)2, (e) —SR†2, (h) —NO2, (i) —CN, (j) —C(O)—R†2, (k) —C(O)—OR*2, (I) —C(O)—N(R*2)2, (m) —O—C(O)—R†2 (n) —N(R*2)—C(O)—R†2, (o) —O—C(O)—OR*2, (p) —O—C(O)—N(R*2)2, (q) —N(R*2)—C(O)—OR*2 or (r) —N(R*2)—C(O)—N(R*2)2; each instance of R*2 is independently —H or C1-2 alkyl; and each instance of R†2 is independently C1-2 alkyl. |
