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US 2010/0063285 A1Published application
Antifungal triazole derivatives, method for the preparation thereof and pharmaceutical composition containing same
AssigneeDaewoong Pharmaceutical Co., Ltd.
InventorsJoon Seok Park, Kyung A Yu, Yun Soo Yoon, Mi Ryeong Han
Life of this patent
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Abstract
The present invention relates to triazole derivaties, a method for the preparation thereof, and a pharmaceutical composition containing the same as an active ingredient. The inventive triazole derivaties have an excellent antifungal activity against various pathogens.
Claims7
A compound of formula (I), or an isomer or pharmaceutically acceptable salt thereof:
- wherein,
- Ar is phenyl substituted with at least one halogen or C1-C4 haloalkyl;
- R1 is hydrogen, fluorine or C1-C4 alkyl;
- R2, R3 and R4 are each independently hydrogen, halogen, C1-C4 alkyl, C1-C4 haloalkyl, C3-C6 cycloalkyl, C1-C4 alkoxy, nitro, cyano, amino, hydroxy, —NR5R6, —CONR5R6, —CH2—CO—R5, —CH2—OCO—R5, —CO—R5, —COOR5, —C(═NR5)NHR7, —C(═NR7)OR7, —SOZR7, —NR5SO2R7 or aryl C1-C4 alky, the aryl moiety being phenyl or naphtyl unsubstituted or substituted with at least one halogen, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 haloalkoxy, nitro, cyano, hydroxy or hydroxymethyl, wherein R4 may represent two or more substituents independently selected from the above-mentioned substituents;
- X is C1-C4 alkyl, C1-C4 alkenyl or C1-C4 alkynyl unsubstituted or substituted with at least one halogen;
- O;
- NR2;
- CONR2;
- R2—O;
- R2—NR3;
- R2—OR3;
- R2—CO—R3;
- or Q-P unsaturated or substituted with O or C1-C4alky;
- Q being a linker, CO or C1-C4 alkyl, and P being a 5- to 7-membered heterocyclic ring containing at least one nitrogen or oxygen atom;
- and
- A, B, D, E and G are each independently nitrogen or carbon fused together to form a phenyl, pyridine, pyrimidine or triazine group, which is optionally fused with X to form a ring,
- in which
- R5 is hydrogen, C1-C4 alkyl, C3-C6 cycloalkyl, —COCF3, or the aryl C1-C4 alkyl defined for R2;
- R6 is hydrogen, —CONH2, —COCH3, —CN, or —(C1-C4 alkyl)-NH2;
- R7 is C1-C4 alkyl, C3-C6 cylcoalkyl, or the aryl C1-C4 alkyl defined for R2;
- and
- Z is 0, 1, or 2.
19 more elements
Dependencies are inferred from the claim text.