| 主权项 |
1. A compound of formula I′:whereinW and X are the same or different and each is independently selected from the group consisting of
H, hydroxyl-C1-6-alkyl, and C1-6-alkyl that optionally includes 1-3 deuterium atoms,or alternatively, W together with the nitrogen to which it is bound and Y together with the carbon to which it is bound can form a C3-9-heterocycle;Y is C1-6-alkylZ is selected from the group consisting of
C1-6-alkyl that optionally may be substituted with aryl, aryl that optionally may be substituted with cyano, C1-6-alkyl, C1-6-alkoxy, C3-7-cycloalkyl, OCD3, halo-C16-alkoxy, halo, COO—C1-6-alkyl, COOH or CON(H, C1-6-alkyl), and heteroaryl that optionally may be substituted with C1-6-alkyl, C1-6-alkoxy, C3-7-cycloalkyl, halo-C1-6-alkoxy, halo, COOR9, CONR6R7, oxo or phenyl that optionally may be substituted with cyano, CONR10R11; R1, R2 and R3 are selected from the group consisting of H, CN, halo, and halo-C1-6-alkyl;R4 is selected from the group consisting of
H, C1-6-alkyl, and aryl;R5 is selected from the group consisting of
H, benzyl, that optionally may be substituted with acetyl, amido, amino, cyano, C1-6-alkyl, C1-6-alkoxy, hydroxy-C1-6-alkyl, halo and nitro, aryl that optionally may be substituted with acetyl, amido, amino, cyano, C1-6-alkyl, C1-6-alkoxy, hydroxy-C1-6-alkyl, halo and nitro, heteroaryl, C1-6-alkyl that optionally may be substituted with aryl that optionally may be substituted with cyano or C1-6-alkoxy, C(O)R6, SO2—CH2—SO2—C1-6-alkyl, SO2—N(C1-6-alkyl)2, SO2—NH2, SO2—N(H,C1-6-alkyl), SO2-aryl that optionally may be substituted with C1-6-alkoxy, nitro, amino, N(H, C(O)—C1-6-alkyl) or C(O)—C1-6-alkyl, SO2—C1-6-alkyl, and COO—C1-6-alkyl, and R5 optionally may be linked with Z to form —C(═O)—(CH2)a—NR12—C(═O)-aryl-CH2—, whereby a is 1, 2, 3 or 4, and the aryl moiety can optionally be substituted by C1-6-alkoxy;R6 is selected from the group consisting of
C1-6-alkyl that optionally may be substituted with amino, N(H, C1-6-alkyl), COOH, nitro or C1-6-alkoxy, (CH2)i-aryl that optionally may be substituted with amino, cyano, nitro, halo, SO2—C1-6-alkyl, C(O)—C1-6-alkyl, C(O)—O—C1-6-alkyl, C(O)—OH, C1-6-alkoxy, C(O)—NH2, C(O)—NH—(CH2)j—C3-7-cycloalkyl, N(H, C(O)—C1-6-alkyl), N(H, C(O)—O—C1-6-alkyl-aryl) or C1-6-alkyl that optionally may be substituted with halo and hydroxy, i=0 or 1 and j=0 or 1, (CH2)k-heterocycle that optionally may be substituted with C1-6-alkyl, k=0, 1 or 2, (CH2)l-heteroaryl that optionally may be substituted with C1-6-alkyl, C3-7-cycloalkyl, phenyl or halo, l=0, 1 or 2 and the aryl moiety may optionally be substituted by CN, (CH2)m—O—(CH2)n—O—C1-6-alkyl, m=1 or 2, n=1, 2 or 3, (CH2)o—(C═O)—NR7R8, o=0, 1 or 2, (CH2)p—O—(CH2)q—O—(CH2)r—O—C1-6-alkyl, p=l or 2, q=1, 2 or 3, r=1, 2 or 3, (CH2)s—(C═O)—C1-6-alkyl, s=1, 2 or 3, (CH2)t—(C═O)—O—C1-6-alkyl, t=1, 2, 3 or 4, (CH2)u—C3-7-cycloalkyl, u=1 or 2, (CH2)v—NH—(C═O)—O—(CH2)w-aryl, v=1, 2 or 3, w=1 or 2, and (CH2)x-SO2—C1-6-alkyl, x=1 or 2, N(H, C1-6-alkyl);R7 or R8 each individually selected from the group consisting of
H, and C1-6-alkyl;R9 is selected from the group consisting of
H,R10 is selected from the group consisting of
H,R11 is selected from the group consisting of
aryl, and heteroaryl;R12 is selected from the group consisting of
H, and C1-6-alkyl;or a pharmaceutically acceptable salt thereof. |
