| 摘要 |
Disclosed are the use of compounds that selectively inhibit the activity of Bcl-2 proteins for the treatment of systemic lupus erythematosus, lupus nephritis or Sjogren’s Syndrome. These inhibitors may have a structure of formula (I), wherein, A1, B1, Y1, R3, R5, R6, m and p are disclosed in the specification. These compounds may also have a binding affinity for Bcl- 2 that is less than the binding affinity for Bcl-xL. Example compounds include: 2-[(6-amino-5-chloropyridin-3-yl)oxy]-4-(4-{ [2-(4-chlorophenyl)-4,4-dimethylcyclohexl-1-en-1-yl]methyl} piperazin-1-yl)-N-({ 3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl} sulfonyl)benzamide; trans-4-(4-{ [2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl} piperazin-1-yl)-N-[(4-{ [(4-methoxycyclohexyl)methyl]amino} -3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide. |
