Antifungal triazole derivatives
AssigneeDaewoong Pharmaceutical Co., Ltd.
InventorsJoon Seok Park, Kyung A Yu, Yun Soo Yoon, Mi Ryeong Han, Ji Duck Kim
Life of this patent
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Abstract
Disclosed are novel triazole derivatives. Exhibiting excellent antifungal activity and in vivo safety, they are useful for the treatment or prevention of fungal infections caused by a wide spectrum of fungi.
Claims18
A compound, represented by the following Chemical Formula 1, or a pharmaceutically acceptable salt thereof:
- wherein,
- Ar is phenyl which is substituted with one to five halogens;
- B is phenyl, pyridinyl or pyrimidinyl, which is unsubstituted or substituted with one or two R3 groups;
- R1 is hydrogen or C1-4 alkyl;
- R2 is O, NH or NCH3;
- and
- R3 is independently halogen, C1-4 alkyl, C1-4 haloalkyl, or cyano.
A method for the preparation of a compound represented by Chemical Formula 1, comprising reacting a compound represented by Chemical Formula 2 having the following structure with a compound represented by Chemical Formula 3a, 3b, 3c or 3d each having the following structures:
- wherein, in the Chemical Formulae 1, 2, 3a, 3b, 3c and 3d, A is
- Ar is phenyl which is substituted with one to five halogens;
- B is phenyl, pyridinyl or pyrimidinyl, which is unsubstituted or substituted with one or two R3 groups;
- R1 is hydrogen or C1-4 alkyl;
- R2 is O, NH or NCH3;
- and
- R3 is independently halogen, C1-4 alkyl, C1-4 haloalkyl or cyano.
A method for the preparation of a compound represented by Chemical Formula 1, comprising reacting a compound represented by Chemical Formula 4 having the following structure with a compound represented by Chemical Formula 5a or 5b each having the following structures:
- wherein, in the Chemical Formulae 1, 4, 5a and 5b,
- A is
- Ar is phenyl which is substituted with one to five halogens;
- B is phenyl, pyridinyl or pyrimidinyl, which is unsubstituted or substituted with one or two R3 groups;
- R1 is hydrogen or C1-4 alkyl;
- R2 is NH;
- R3 is independently halogen, C1-4 alkyl, C1-4 haloalkyl, or cyano.
A method for the preparation of a compound represented by Chemical Formula 1, comprising reacting a compound represented by Chemical Formula 1e or 1f having the following structures with a compound represented by Chemical Formula 6 having the following structure:
- wherein, in the Chemical Formulae 1, 1e, 1f, and 6,
- Ar is phenyl which is substituted with one to five halogens;
- B is phenyl, pyridinyl or pyrimidinyl, which is unsubstituted or substituted with one or two R3 groups;
- A is
- R1 is hydrogen or C1-4 alkyl;
- R2 is NCH3,
- R3 is independently halogen, C1-4 alkyl, C1-4 haloalkyl or cyano;
- R4 is CH3, and
- X is halogen.
Dependencies are inferred from the claim text.