| 主权项 |
1. A method of treating a fungal infection, in a subject in need thereof, comprising administration of an effective amount of a compound of general formula (I) or a pharmaceutically acceptable salt or derivative thereof, wherein A represents:
—(CH2)m—X1,—(CH2)m—C3-C8cycloalkyl,—(CH2)m—W—X2,—(CH2)m—W—CH2—X1, or—(CH2)m—CHR9—(CH2)m—X1; X1 represents:
-aryl, optionally substituted by one, two or three R4,-heterocycle, optionally substituted by one or two R5,—C1-C8alkyl,—CH(OH)-phenyl,—S-phenyl,—NHSO2-phenyl,—CN,—OH,—C3-C8cycloalkyl, or-4-cyano-2,3,4,5-tetrafluoro-phenyl; X2 represents:
-aryl,-heterocycle,—C1-C8alkyl,—CH(OH)-phenyl, or—C3-C8cycloalkyl; W represents:
—NH—,—O—, or—S—; R4 represents:
—F,—Cl,—Br,—I,—NO2,—CF3,—CN,—CH2OH—C1-C6alkyl,—W—R10 —(CH2)m-aryl,—(CH2)m-heterocycle,—(CH2)m—C3-C8cycloalkyl—SO2—NH-heterocycle,—(CH2)m—NR14R15,—(SO2)—NR14R15;—(C═O)—NR14R15, or—(N—C═O)—NR14R15; R5 represents:
—H,—F,—Cl,—Br,—CF3,—W—R10,—C1-C6alkyl,—(CH2)m-aryl,—(CH2)m-heterocycle, or—(CH2)m—C3-C8cycloalkyl; R9 represents:
—C1-C7alkyl,—C3-C8cycloalkyl,—C(O)R11,—C(O)NHR11,—C(OH)R11,—CH2OH,—CO2R11, or-aryl; R10 represents:
—H,—C1-C6alkyl,—(CH2)m-aryl,—(CH2)m-heterocycle,—(CH2)m—C3-C8cycloalkyl, or—CH(R12)R13; R11 represents:
—H,—C1-C7alkyl,—(CH2)mX1, or—(CH2)m—C3-C8cycloalkyl; R12 represents:
—H,—(CH2)mCO2—C1-C6alkyl,—(CH2)m-phenyl,—(CH2)m-heterocycle,—C1-C6alkyl,—C1-C4alkylNH—COOCH2-benzyl, or—C1-C4alkyl-S—CH3; R13 represents:
—NH—CO2C(CH3)3,—CN,—COOH, or—CO2R11; R14 and R15, independently from each other, represent:
—H,—C1-C6alkyl,—(CH2)m-aryl,—(CH2)m-cycloalkyl,—(CH2)m-heterocycle,—(CH2)m—W—R10,—(CH2)m—CN,taken together with the nitrogen atom to which they are attached form an optionally substituted 5- to 8-membered heteromonocycle having from one to three additional heteroatoms selected from the group consisting of nitrogen, oxygen and sulphur, ortaken together with the nitrogen atom to which they are attached form an optionally substituted 5- to 8-membered heteromonocycle which is fused to one or two optionally substituted saturated or unsaturated rings or to other optionally substituted heterocycles having from one to three heteroatoms selected from the group consisting of nitrogen, oxygen and sulphur; and m represents an integer from 0 to 6; wherein aryl is:
phenyl,naphthyl,biphenyl,tetrahydro-naphthyl, orfluorenyl; heterocycle is a 5-, 6- or 7-membered saturated or unsaturated ring containing from one to three heteroatoms selected from the group consisting of nitrogen, oxygen and sulphur, and including any bicyclic group in which any of the above heterocyclic rings is fused to a benzene ring or another heterocyclic; and cycloalkyl is a saturated or unsaturated hydrocarbon ring including bicyclic groups in which the above ring is connected to a benzene, heterocyclic or other hydrocarbon ring. |
