C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/305, 260/304
C07D 411/14 (2006.01) C07D 231/12 (2006.01) C07D 233/54 (2006.01) C07D 233/84 (2006.01) C07D 249/08 (2006.01) C07D 249/12 (2006.01) C07D 317/20 (2006.01) C07D 317/24 (2006.01) C07D 521/00 (2006.01)
Patent
CA 1117534
ABSTRACT OF THE DISCLOSURE Novel 1H-imidazoles and 1H-1,2,4-triazole derivatives have been found useful as antifungal and antibacterial agents. These compounds may structurally be represented by the following formula: Image (I) and the pharmaceutically acceptable acid addition salts and stereo- chemically isomeric forms thereof, wherein: Q is a member selected from the group consisting of CH and N; Ar is a member selected from the group consisting of phenyl and substituted phenyl, said substituted phenyl having from 1 to 3 substituents independently selected from the group con- sisting of halo, lower alkyl and lower alkyloxy; and the radical Y is a member selected from the group consisting of: a 1H-pyrrol-1-yl radical of the formula Image (a); a 1H-pyrazol-1-yl radical of the formula Image (b) wherein R1 is selected from the group consisting of hydrogen, lower alkyl, lower alkylthio and phenyl, and, R2 is selected from the group consisting of hydrogen, lower alkyl and phenyl; a 1H-imidazol-1-yl radical of the formula Image (c) wherein R3 is selected from the group consisting of hydrogen, lower alkyl, phenyl, lower alkylthio, lower alkylsulfinyl and lower alkylsulfonyl, R4 is selected from the group consisting of hydrogen, lower alkyl and phenyl, and, R5 is selected from the group con- sisting of hydrogen and phenyl; 1a a 1H-1,2,4-triazol-1-yl radical of the formula Image (d) wherein R6 is selected from the group consisting of hydrogen and lower alkylthio, and R7 is selected from the group consisting of hydrogen, lower alkyl and phenyl: a 4H-1,2,4-triazol-4-yl radical of the formula Image (e) wherein R8 is selected from the group consisting of hydrogen, lower alkyl, lower alkyloxy, lower alkylthio, lower alkylsulfinyl and lower alkylsulfonyl, and, R9 is selected from the group consisting of hydrogen and lower alkyl: a 2,3-dihydro-4H-1,2,4-triazol-1-yl radical of the formula Image (f) 1b wherein X is selected from the group consisting of O and S, and, R10 and R11 are each independently selected from the group consisting of hydrogen and lower alkyl, provided that when said X is S then said R11 is hydrogen; a 1H-1,2,3,4-tetrazol-1-yl radical of the formula Image (g);and a 4,5-dihydro-5-thioxo-1H-1,2,3,4-tetrazol-1-yl radical of the formula Image (h). It is understood that radicals of formula (f) wherein R11 stands for hydrogen, as well as the radical of formula (h) may also exist under their tautomeric anol, respectively indicated in the above structures, are naturally intended to be within the scope of formula (I). 1c
295742
Backx Leo J.j.
Heeres Jan
Mostmans Joseph H.
Gowling Lafleur Henderson Llp
Janssen Pharmaceutica Naamloze Vennootschap
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