Patent ID: 6225329
Filing Date: 2001-05-01
Classification: C07D

Abstract:
A compound of Formula 1 ##STR64##whereinA is together with the double bond in Formula 1 biphenyl, indenyl, fluorenyl or fluorenyl-9-one;R.sub.1 is hydrogen, COR.sub.5, OR.sub.6, CF.sub.3, nitro, cyano, SO.sub.3 H, SO.sub.2 NR.sub.7 R.sub.8, PO(OH).sub.2, CH.sub.2 PO(OH).sub.2, CHFPO(OH).sub.2, CF.sub.2 PO(OH).sub.2, C(.dbd.NH)NH.sub.2, NR.sub.7 R.sub.8 or selected from the following 5-membered heterocycles: ##STR65##or R.sub.1 is ##STR66##wherein R.sub.12, R.sub.13, and R.sub.14 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, aryl, or arylC.sub.1 -C.sub.6 alkyl wherein the alkyl and aryl groups are optionally substituted;R.sub.2 is COR.sub.5, OR.sub.6, CF.sub.3, nitro, cyano, SO.sub.3 H, SO.sub.2 NR.sub.7 R.sub.8, PO(OH).sub.2, CH.sub.2 PO(OH).sub.2, CHFPO(OH).sub.2, CF.sub.2 PO(OH).sub.2, C(.dbd.NH)NH.sub.2, NR.sub.7 R.sub.8, or selected from the following 5-membered heterocycles: ##STR67##R.sub.3, R.sub.16 and R.sub.17 are independently hydrogen, halo, nitro, cyano, trihalomethyl, C.sub.1 -C.sub.6 alkyl, aryl, arylC.sub.1 -C.sub.6 -alkyl, hydroxy, carboxy, carboxyC.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkyloxycarbonyl, aryloxycarbonyl, arylC.sub.1 -C.sub.6 alkyloxycarbonyl, C.sub.1 -C.sub.6 alkyloxy, C.sub.1 -C.sub.6 alkyloxyC.sub.1 -C.sub.6 alkyl, aryloxy, arylC.sub.1 -C.sub.6 alkyloxy, arylC.sub.1 -C.sub.6 alkyloxyC.sub.1 -C.sub.6 alkyl, thio, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylthioC.sub.1 -C.sub.6 alkyl, arylthio, arylC.sub.1 -C.sub.6 alkylthio, arylC.sub.1 -C.sub.6 alkylthioC.sub.1 -C.sub.6 alkyl, NR.sub.7 R.sub.8, C.sub.1 -C.sub.6 alkylaminoC.sub.1 -C.sub.6 alkyl, arylC.sub.1 -C.sub.6 alkylaminoC.sub.1 -C.sub.6 alkyl, di(arylC.sub.1 -C.sub.6 alkyl)aminoC.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkylcarbonyl, C.sub.1 -C.sub.6 alkylcarbonyl-C.sub.1 -C.sub.6 alkyl, arylC.sub.1 -C.sub.6 alkylcarbonyl, arylC.sub.1 -C.sub.6 alkylcarbonylC.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkylcarboxy, C.sub.1 -C.sub.6 alkylcarboxyC.sub.1 -C.sub.6 -alkyl, arylcarboxy, arylcarboxyC.sub.1 -C.sub.6 alkyl, arylC.sub.1 -C.sub.6 alkylcarboxy, arylC.sub.1 -C.sub.6 alkylcarboxyC.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkyl-carbonylamino, C.sub.1 -C.sub.6 alkylcarbonylaminoC.sub.1 -C.sub.6 alkyl, -carbonylNR.sub.7 C.sub.1 -C.sub.6 alkylCOR.sub.11, arylC.sub.1 -C.sub.6 alkylcarbonylamino, arylC.sub.1 -C.sub.6 alkylcarbonyl-aminoC.sub.1 -C.sub.6 alkyl, CONR.sub.7 R.sub.8, or C.sub.1 -C.sub.6 alkylCONR.sub.7 R.sub.8 wherein the alkyl and aryl groups are optionally substituted and R.sub.11 is NR.sub.7 R.sub.8, or C.sub.1 -C.sub.6 alkylNR.sub.7 R.sub.8 ; or R.sub.3 is ##STR68##wherein R.sub.12, R.sub.13, and R.sub.14 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, aryl, or arylC.sub.1 -C.sub.6 alkyl, wherein the alkyl and aryl groups are optionally substituted;R.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, aryl, arylC.sub.1 -C.sub.6 alkyl, NR.sub.7 R.sub.8, or C.sub.1 -C.sub.6 alkyloxy, wherein the alkyl and aryl groups are optionally substituted;R.sub.5 is hydroxy, C.sub.1 -C.sub.6 alkyl, aryl, arylC.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkyloxy, C.sub.1 -C.sub.6 alkyl-oxyC.sub.1 -C.sub.6 alkyloxy, aryloxy, arylC.sub.1 -C.sub.6 alkyloxy, CF.sub.3, or NR.sub.7 R.sub.8, wherein the alkyl and aryl groups are optionally substituted;R.sub.6 is hydrogen, C.sub.1 -C.sub.6 alkyl, aryl, or arylC.sub.1 -C.sub.6 alkyl, wherein the alkyl and aryl groups are optionally substituted;R.sub.7 and R.sub.8 are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl, aryl, arylC.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkylcarbonyl, arylcarbonyl, arylC.sub.1 -C.sub.6 alkylcarbonyl, C.sub.1 -C.sub.6 alkylcarboxy or arylC.sub.1 -C.sub.6 alkylcarboxy wherein the alkyl and aryl groups are optionally substituted; orR.sub.7 and R.sub.8 are taken together with the nitrogen to which they are attached forming a saturated, partially saturated or aromatic cyclic, bicyclic or tricyclic ring system containing from 3 to 14 carbon atoms and from 0 to 3 additional heteroatoms selected from nitrogen, oxygen or sulfur, the ring system being optionally substituted with at least one C.sub.1 -C.sub.6 alkyl, aryl, arylC.sub.1 -C.sub.6 alkyl, hydroxy, oxo, C.sub.1 -C.sub.6 alkyloxy, arylC.sub.1 -C.sub.6 alkyloxy, C.sub.1 -C.sub.6 alkyloxyC.sub.1 -C.sub.6 alkyl, NR.sub.9 R.sub.10 or C.sub.1 -C.sub.6 alkylaminoC.sub.1 -C.sub.6 alkyl, wherein R.sub.9 and R.sub.10 are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl, aryl, arylC.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkylcarbonyl, arylcarbonyl, arylC.sub.1 -C.sub.6 alkylcarbonyl, C.sub.1 -C.sub.6 alkylcarboxy or arylC.sub.1 -C.sub.6 alkylcarboxy, wherein the alkyl and aryl groups are optionally substituted; orR.sub.7 and R.sub.8 are independently a saturated or partially saturated cyclic 5, 6 or 7 membered amine, imide or lactam;or a salt thereof with a pharmaceutically acceptable acid or base, or any optical isomer or mixture of optical isomers, or any tautomeric forms.