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Fluorinated derivatives of 3-hydroxypyridin-4-ones
专利权人:
APOTEX TECHNOLOGIES INC.
发明人:
TAM, TIM FAT,LEUNG-TOUNG, REGIS,WANG, YINGSHENG,ZHAO, YANQING,XIN, TAO,SHAH, BIRENKUMAR,N'ZEMBA, BLAISE,WODZINSKA, JOLANTA MARIA,PREMYSLOVA, MARYNA,NZEMBA, BLAISE
申请号:
ES10793481
公开号:
ES2524342T3
申请日:
2010.07.05
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
A compound of Formula I: ** Formula ** where G1 is H, C1-C4 alkyl, CH2OH, CH 2NR1R2, CH (R4) CF3, CH (R7) CF2H, NR1R2 or ** Formula ** G2 is H, C1 -C4 alkyl, cyclopropyl or (CH2) nCF2R3; G3 is H, C1-C4 alkyl, CH2OH, CH2NR1R2, CH (R6) CF3, CH2-A-OH, CH2-A-NHR9 or CH2CF3 or ** Formula ** and G4 is H, C1-C4 alkyl, halo or CH (R8) CF3; n is 1, 2 or 3; R1 and R2 are (a) two independent groups or (b) together they form a single ring group; R1 and R2, when independent groups, are independently selected from the group consisting of: H, C1-C4 alkyl, C3-C6 cycloalkyl, allyl and propargyl; R1 and R2, when together they form a single ring group, are selected from the group consisting of: piperazinyl, piperacinyl substituted by N- (C1-C4 alkyl), morpholinyl and piperidinyl; R3 is H or F; R4 and R7 are independently selected from the group consisting of: H, OH, NR1R2, imidazolyl, 1-2-4-triazolyl, piperazinyl, N-C1-C4 alkylpiperazinyl, N-benzylpiperacinyl, N-phenylpiperacinyl, 2-pyridylpiperacinyl and A- NH-R10; and when R4 or R7 is imidazolyl, 1-2-4-triazolyl, piperazinyl, N-C1-C4 alkylpiperazinyl, N-benzylpiperacinyl, N phenylpiperacinyl, 2-pyridylpiperazinyl or -A-NH-R10; a point of attachment of R4 or R7 with the radical CH of G1 is an atom n of R4 or R7; R5 is C1-C4 alkyl; R6 is H or OH; R8 is selected from the group consisting of: NR1R2, imidazolyl, 1-2-4-triazolyl, piperazinyl, N-C1-C4 alkylpiperazinyl, N-benzylpiperacinyl, N-phenylpiperacinyl, 2-pyridylpiperacinyl and A-NH-R10; and when R8 is imidazolyl, 1-2-4-triazolyl, piperazinyl, N-C1-C4 alkylpiperazinyl, N-benzylpiperacinyl, N-phenylpiperacinyl, 2-pyridylpiperacinyl or A-NH-R10 a point of R8 with the radical CH of G4 is an N atom of R8; R9 and R10 are independently H or C1-C4 alkyl; A is -NH- (CH2) m-CO or an alpha amino acid residue.Un compuesto de Fórmula I:**Fórmula** donde G1 es H, C1-C4 alquilo, CH2OH, CH 2NR1R2, CH(R4)CF3, CH(R7)CF2H, NR1R2 o**Fórmula** G2 es H, C1-C4 alquilo, ciclopropilo o (CH2)nCF2R3; G3 es H
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