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Tripeptide Ketone Epoxy Protease Inhibitors
专利权人:
Inc.;Onyx Therapeutics
发明人:
MCMINN, Dustin,JOHNSON, Henry,BOWERS, Simeon,MOEBIUS, David
申请号:
ES14722443
公开号:
ES2642765T3
申请日:
2014.03.14
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of Formula (X): ** (See formula) ** where: each of m and n is independently 0, 1 or 2, and m + n>; = 2, 3, or 4; p is 0 or 1; q is 0, 1, or 2; K is selected from the group consisting of CR5R6, NR7, N (C>; = O) OR7, -NH- (C>; = O) -, O, S, SO, and SO2; E is N or CR7; R1 is selected from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, and 3-6 membered heterocycloalkyl, wherein R1 is optionally substituted with one or more selected substituents from the group consisting of halo, OR7, SR7, N (R7) 2, CN, and (C>; = O) N (R7) 2; R2 is C1-2-G alkylene or (C>; = O) -G; wherein G is selected from the group consisting of aryl, heteroaryl, and pyridinone, with the proviso that when R2 is CH2phenyl, the phenyl is substituted with one or more substituents selected from the group consisting of OR7, halo, C1-3 alkyl , OCF3, SO2R7, (C>; = O) N (R7) 2, CN, and SO2N (R7) 2; R3 is selected from the group consisting of C3-7 cycloalkyl, C3-7 cycloalkenyl, a 3-7 membered heterocycloalkyl, and a 3-7 membered heterocycloalkenyl, wherein R3 is optionally substituted with one or more substituents selected from the group that consists of halo,>; = O, OR7, SR7, N (R7) 2, O (C>; = O) N (R7) 2, and C1-6 alkyl; R4 is H or C1-3 alkyl; each of R5 and R6 is independently selected from the group consisting of H, OH, halo, C1-3alkyl, and CF3, or R5 and R6 together with the carbon to which they are attached form C>; = O or ** (See formula) ** where W is O or NR7, and r is 1, 2 or 3; and each of R7 is independently H or C1-6 alkyl, or a pharmaceutically acceptable salt thereof.Un compuesto de Fórmula (X): **(Ver fórmula)** en donde: cada uno de m y n es independientemente 0, 1 o 2, y m + n >;= 2, 3, o 4; p es 0 o 1; q es 0, 1, o 2; K se selecciona del grupo que consiste en CR5R6, NR7, N(C>;=O)OR7, -NH-(C>;=O)-, O, S, SO, y SO2; E es N o CR7; R1 se selecciona del grupo que consiste en H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, c
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