2,3 Disubstituted- (5,6)-heteroarylfused-pyrimidine-4-ones

A method for treating a condition selected from cerebral deficits subsequent to cardiac bypass surgery and grafting, stroke, cerebral ischemia, spinal cord trauma, head trauma, Alzheimer's Disease, AIDS-induced dementia, migraine headaches, urinary incontinence, psychosis, perinatal hypoxia, hypoxia arrest, hypoglycemic neuronal damage, opiate tolerance, addiction withdrawal, ocular damage, retinopathy, retinal neuropathy, tinnitus, anxiety, emesis, brain edema, or chronic or acute pain in a mammal comprising administering to a mammal in need of such treatment an amount effective in treating such condition of a bicyclic compound or pharmaceutically acceptable salt of said bicyclic compound of the formula ##STR24## wherein ring A is a fused 5 membered heteroaromatic ring which, taken together with the carbon atoms common to both rings of the bicyclic system, has the formula ##STR25## wherein one of said ring positions "F", "G" and "J" is selected from nitrogen, oxygen or sulfur, and the other two of said ring positions "F", "G", and "J" are carbons;

• wherein said fused heteroaromatic rings may optionally be independently substituted on any of the carbon or nitrogen atoms capable or forming an additional bond with a substituent selected from hydrogen, (C.sub.1 -C.sub.6)alkyl, halogen, trifluoromethyl, amino-(CH.sub.2).sub.n --, (C.sub.1 -C.sub.6)alkylamino-(CH.sub.2).sub.n --, di(C.sub.1 -C.sub.6)alkyl-amino-(CH.sub.2).sub.n --, (C.sub.1 -C.sub.6)alkoxy, hydroxy (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-O--(C.sub.1 -C.sub.6)alkyl-, --CN, (C.sub.1 -C.sub.6)alkyl-CO--O--(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6)alkyl-O--CO--O--(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-CO--O--, hydroxy, --NO.sub.2, R.sup.3 --C(.dbd.O)--, R.sup.4 --O--C(.dbd.O)--, di(C.sub.1 -C.sub.6)alkyl-N--C(.dbd.O)--, (C.sub.1 -C.sub.6)cycloalkyl, and R.sup.4 --NH--C(.dbd.O)--, and phenyl optionally substituted with halo, (C.sub.1 -C.sub.6) alkyl, --CN, or --CF.sub.3 ;
• R.sup.1 is substituted phenyl of the formula Ph.sup.1 or heteroaryl wherein said heteroaryl is selected from the group consisting of pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, wherein said heteroaryl may optionally be substituted on any of the atoms capable of forming an additional bond, up to a maximum of three substituents, with a substituent selected from hydrogen, (C.sub.1 -C.sub.6)alkyl, halogen, trifluoromethyl, amino-(CH.sub.2).sub.n --, (C.sub.1 -C.sub.6)alkylamino-(CH.sub.2).sub.n --, di(C.sub.1 -C.sub.6)alkyl-amino-(CH.sub.2).sub.n --, (C.sub.1 -C.sub.6)alkoxy, hydroxy(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-O--(C.sub.1 -C.sub.6)alkyl-, --CN, (C.sub.1 -C.sub.6)alkyl-CO--O--(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6)alkyl-O--CO--O--(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-CO--O--, hydroxy, H--C(.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-C(.dbd.O)--, HO--C(.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-O--C(.dbd.O)--, NH.sub.2 --C(.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-NH--C(.dbd.O), and di(C.sub.1 -C.sub.6)alkyl-NH--C(.dbd.O)--;
• wherein said Ph.sup.1 is a group of the formula ##STR26## R.sup.2 is phenyl of the formula Ph.sup.2 or a five or six membered heterocycle, wherein said six membered heterocycle has the formula ##STR27## wherein "N" is nitrogen;
• wherein said ring positions "K", "L" and "M" may be independently selected from carbon or nitrogen, with the proviso that only one of "K", "L" or "M" can be nitrogen;
• wherein said five membered heterocycle has the formula ##STR28## wherein said ring positions "P," "Q" and "T" may be independently selected from carbon, nitrogen, oxygen or sulfur;
• with the proviso that only one of "P," "Q" or "T" can be oxygen or sulfur and at least one of "P," "Q" or "T" must be a heteroatom;
• wherein said Ph.sup.2 is a group of the formula ##STR29## R.sup.3 is hydrogen or (C.sub.1 -C.sub.6) alkyl;
• R.sup.4 is hydrogen or (C.sub.1 -C.sub.6) alkyl;
• R.sup.5 is hydrogen, (C.sub.1 -C.sub.6)alkyl, halo, CF.sub.3, (C.sub.1 -C.sub.6)alkoxy or (C.sub.1 -C.sub.6)alkylthiol;
• R.sup.6 is hydrogen or halo;
• R.sup.7 is hydrogen or halo;
• R.sup.8 is hydrogen or halo;
• R.sup.9 is hydrogen, (C.sub.1 -C.sub.6)alkyl optionally substituted with one to three halogen atoms, halo, CF.sub.3, (C.sub.1 -C.sub.6)alkoxy optionally substituted with one to three halogen atoms, (C.sub.1 -C.sub.6)alkylthiol, R.sup.13 O--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-NH--(CH.sub.2).sub.p --, di(C.sub.1 -C.sub.6)alkyl-N--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.5)cycloalkyl-NH--(CH.sub.2).sub.p --, H.sub.2 N--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-HN--(C.dbd.O)--(CH.sub.2).sub.p --, di(C.sub.1 -C.sub.6)alkyl-N--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.5)cycloalkyl-NH--(C.dbd.O)--(CH.sub.2).sub.p --, R.sup.13 O--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-(O.dbd.C)--O--(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6)alkyl-O--(O.dbd.C)--O--(C.sub.1 -C.sub.6)-alkyl-, ##STR30## hydroxy, H--C(.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-C(.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-O--C(.dbd.O)--, R.sup.4 --(CH.sub.2).sub.p --O--C(.dbd.O)--, amino-(CH.sub.2).sub.p --, hydroxy-(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6)alkyl-O--(C.sub.1 -C.sub.6)alkyl-, and --CN;
• R.sup.10 and R.sup.14 are hydrogen, (C.sub.1 -C.sub.6)alkyl optionally substituted with one to three halogen atoms, halo, CF.sub.3, (C.sub.1 -C.sub.6)alkoxy optionally substituted with one to three halogen atoms, (C.sub.1 -C.sub.6)alkylthiol, R.sup.13 O--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-NH--(CH.sub.2).sub.p --, di(C.sub.1 -C.sub.6)alkyl-N--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.5)cycloalkyl-NH--(CH.sub.2).sub.p --, H.sub.2 N--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-HN--(C.dbd.O)--(CH.sub.2).sub.p --, di(C.sub.1 -C.sub.6)alkyl-N--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.5)cycloalkyl-NH--(C.dbd.O)--(CH.sub.2).sub.p --, R.sup.13 O--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-(O.dbd.C)--O--(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6)alkyl-O--(O.dbd.C)--O--(C.sub.1 -C.sub.6)--alkyl-, (C.sub.1 -C.sub.6)alkyl-(O.dbd.C)--O--, (C.sub.1 -C.sub.6)alkyl-(O.dbd.C)--NH--(CH.sub.2).sub.p --, H(O.dbd.C)--NH--(CH.sub.2).sub.p --, ##STR31## hydroxy, H--C(.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-C(.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-O--C(.dbd.O)--, R.sup.4 --(CH.sub.2).sub.p --O--C(.dbd.O)--, amino-(CH.sub.2).sub.p --, hydroxy-(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-O--(C.sub.1 -C.sub.6)alkyl, --CHO and --CN;
• R.sup.11 is hydrogen or halo;
• R.sup.12 is hydrogen or halo;
• R.sup.13 is hydrogen, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-(C.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-O--(C.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-NH--(C.dbd.O)--, or di(C.sub.1 -C.sub.6)alkyl-N--(C.dbd.O)--;
• R.sup.15 is hydrogen, --CN, (C.sub.1 -C.sub.6)alkyl, halo, CF.sub.3, --CHO or (C.sub.1 -C.sub.6)alkoxy;
• R.sup.16 is hydrogen, --CN, (C.sub.1 -C.sub.6)alkyl, halo, CF.sub.3, --CHO or (C.sub.1 -C.sub.6)alkoxy;
• R.sup.17 is hydrogen, --CN, (C.sub.1 -C.sub.6)alkyl, halo, CF.sub.3, CHO or (C.sub.1 -C.sub.6)alkoxy;
• n is an integer from zero to 3;
• p is an integer from zero to 3;
• wherein the dashed bond represents an optional double bond;
• with the proviso that when R.sup.9 is hydrogen, then one of R.sup.11 and R.sup.12 is other than hydrogen.

A method for treating disorders the treatment of which is facilitated by enhanced glutamate nourotransmission in a mammal, comprising administering to a mammal requiring such treatment an amount effective in treating such condition of a bicyclic compound, or pharmaceutically acceptable salt of said bicyclic compound, of the formula ##STR32## wherein ring A is a fused 5 membered heteroaromatic ring which, taken together with the carbon atoms common to both rings of the bicyclic system, has the formula ##STR33## wherein one of said ring positions "F", "G" and "J" is selected from nitrogen, oxygen or sulfur, and the other two of said ring positions "F", "G", and "J" are carbons;

• wherein said fused heteroaromatic rings may optionally be independently substituted on any of the carbon or nitrogen atoms capable of forming an additional bond with a substituent selected from hydrogen, (C.sub.1 -C.sub.6)alkyl, halogen, trifluoromethyl, amino-(CH.sub.2).sub.n --, (C.sub.1 -C.sub.6)alkylamino-(CH.sub.2).sub.n --, di(C.sub.1 -C.sub.6)alkyl-amino-(CH.sub.2).sub.n --, (C.sub.1 -C.sub.6)alkoxy, hydroxy(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-O--(C.sub.1 -C.sub.6)alkyl-, --CN, (C.sub.1 -C.sub.6)alkyl-CO--O--(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6)alkyl-O--CO--O--(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-CO--O--, hydroxy, --NO.sub.2, R.sup.3 --C(.dbd.O)--, R.sup.4 --O--C(.dbd.O)--, di(C.sub.1 -C.sub.6)alkyl-N--C(.dbd.O)--, (C.sub.1 -C.sub.6)cycloalkyl, and R.sup.4 --NH--C(.dbd.O)--, and phenyl optionally substituted with halo, (C.sub.1 -C.sub.6) alkyl, --CN, or --CF.sub.3 ;
• R.sup.1 is substituted phenyl of the formula Ph.sup.1 or heteroaryl wherein said heteroaryl is selected from the group consisting of pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, wherein said heteroaryl may optionally be substituted on any of the atoms capable of forming an additional bond, up to a maximum of three substituents, with a substituent selected from hydrogen, (C.sub.1 -C.sub.6)alkyl, halogen, trifluoromethyl, amino-(CH.sub.2).sub.n --, (C.sub.1 -C.sub.6)alkylamino-(CH.sub.2).sub.n --, di(C.sub.1 -C.sub.6)alkyl-amino-(CH.sub.2).sub.n --, (C.sub.1 -C.sub.6)alkoxy, hydroxy(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-O--(C.sub.1 -C.sub.6)alkyl-, --CN, (C.sub.1 -C.sub.6)alkyl-CO--O--(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6)alkyl-O--CO--O--(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-CO--O--, hydroxy, H--C(.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-C(.dbd.O)--, HO--C(.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-O--C(.dbd.O)--, NH.sub.2 --C(.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-NH--C(.dbd.O), and di(C.sub.1 -C.sub.6)alkyl-NH--C(.dbd.O)--;
• wherein said Ph.sup.1 is a group of the formula ##STR34## R.sup.2 is phenyl of the formula Ph.sup.2 or a five or six membered heterocycle, wherein said six membered heterocycle has the formula ##STR35## wherein "N" is nitrogen;
• wherein said ring positions "K", "L" and "M" may be independently selected from carbon or nitrogen, with the proviso that only one of "K", "L" or "M" can be nitrogen;
• wherein said five membered heterocycle has the formula ##STR36## wherein said ring positions "P," "Q" and "T" may be independently selected from carbon, nitrogen, oxygen or sulfur;
• with the proviso that only one of "P," "Q" or "T" can be oxygen or sulfur and at least one of "P," "Q" or "T" must be a heteroatom;
• wherein said Ph.sup.2 is a group of the formula ##STR37## R.sup.3 is hydrogen or (C.sub.1 -C.sub.6) alkyl;
• R.sup.4 is hydrogen or (C.sub.1 -C.sub.6) alkyl;
• R.sup.5 is hydrogen, (C.sub.1 -C.sub.6)alkyl, halo, CF.sub.3, (C.sub.1 -C.sub.6)alkoxy or (C.sub.1 -C.sub.6)alkylthiol;
• R.sup.6 is hydrogen or halo;
• R.sup.7 is hydrogen or halo;
• R.sup.8 is hydrogen or halo;
• R.sup.9 is hydrogen, (C.sub.1 -C.sub.6)alkyl optionally substituted with one to three halogen atoms, halo, CF.sub.3, (C.sub.1 -C.sub.6)alkoxy optionally substituted with one to three halogen atoms, (C.sub.1 -C.sub.6)alkylthiol, R.sup.13 O--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-NH--(CH.sub.2).sub.p --, di(C.sub.1 -C.sub.6)alkyl-N--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.5)cycloalkyl-NH--(CH.sub.2).sub.p --, H.sub.2 N--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-HN--(C.dbd.O)--(CH.sub.2).sub.p --, di(C.sub.1 -C.sub.6)alkyl-N--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.5)cycloalkyl-NH--(C.dbd.O)--(CH.sub.2).sub.p --, R.sup.13 O--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-(O.dbd.C)--O--(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6)alkyl-O--(O.dbd.C)--O--(C.sub.1 -C.sub.6)-alkyl-, ##STR38## hydroxy, H--C(.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-C(.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-O--C(.dbd.O)--, R.sup.4 --(C.sub.2).sub.p --O--C(.dbd.O)--, amino-(CH.sub.2).sub.p --, hydroxy-(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6)alkyl-O--(C.sub.1 -C.sub.6)alkyl-, and --CN;
• R.sup.10 and R.sup.14 are hydrogen, (C.sub.1 -C.sub.6)alkyl optionally substituted with one to three halogen atoms, halo, CF.sub.3, (C.sub.1 -C.sub.6)alkoxy optionally substituted with one to three halogen atoms, (C.sub.1 -C.sub.6)alkylthiol, R.sup.13 O--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-NH--(CH.sub.2).sub.p --, di(C.sub.1 -C.sub.6)alkyl-N--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.5)cycloalkyl-NH--(CH.sub.2).sub.p --, H.sub.2 N--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-HN--(C.dbd.O)--(CH.sub.2).sub.p --, di(C.sub.1 -C.sub.6)alkyl-N--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.5)cycloalkyl-NH--(C.dbd.O)--(CH.sub.2).sub.p --, R.sup.13 O--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-(O.dbd.C)--O--(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6)alkyl-O--(.dbd.C)--O--(C.sub.1 -C.sub.6)-alkyl-, (C.sub.1 -C.sub.6)alkyl-(O.dbd.C)--O--, (C.sub.1 -C.sub.6)alkyl-(O.dbd.C)--NH--(CH.sub.2).sub.p --, H(O.dbd.C)--NH--(CH.sub.2).sub.p --, ##STR39## hydroxy, H--C(.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-C(.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-O--C(.dbd.O)--, R.sup.4 --(CH.sub.2).sub.p --O--C(.dbd.O)--, amino-(CH.sub.2).sub.p --, hydroxy-(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-O--(C.sub.1 -C.sub.6)alkyl, --CHO and --CN;
• R.sup.11 is hydrogen or halo;
• R.sup.12 is hydrogen or halo;
• R.sup.13 is hydrogen, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-(C.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-O--(C.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-NH--(C.dbd.O)--, or di(C.sub.1 -C.sub.6)alkyl-N--(C.dbd.O)--;
• R.sup.15 is hydrogen, --CN, (C.sub.1 -C.sub.6)alkyl, halo, CF.sub.3, --CHO or (C.sub.1 -C.sub.6)alkoxy;
• R.sup.16 is hydrogen, --CN, (C.sub.1 -C.sub.6)alkyl, halo, CF.sub.3, --CHO or (C.sub.1 -C.sub.6)alkoxy;
• R.sup.17 is hydrogen, --CN, (C.sub.1 -C.sub.6)alkyl, halo, CF.sub.3, CHO or (C.sub.1 -C.sub.6)alkoxy;
• n is an integer from zero to 3;
• p is an integer from zero to 3;
• wherein the dashed bond represents an optional double bond;
• with the proviso that when R.sup.9 is hydrogen, then one of R.sup.11 and R.sup.12 is other than hydrogen.

A method for treating a condition selected from cerebral deficits subsequent to cardiac bypass surgery and grafting, stroke, cerebral ischemia, spinal cord trauma, head trauma, Alzheimer's Disease, AIDS-induced dementia, migraine headaches, urinary incontinence, psychosis, perinatal hypoxia, hypoxia arrest, hypoglycemic neuronal damage, opiate tolerance, addiction withdrawal, ocular damage, retinopathy, retinal neuropathy, tinnitus, anxiety, emesis, brain edema, or chronic or acute pain in a mammal comprising administering to a mammal in need of such treatment an AMPA receptor antagonizing effective amount of a bicyclic compound or pharmaceutically acceptable salt of said bicyclic compound, of the formula ##STR40## wherein ring A is a fused 5 membered heteroaromatic ring which, taken together with the carbon atoms common to both rings of the bicyclic system, has the formula ##STR41## wherein one of said ring positions "F", "G" and "J" is selected from nitrogen, oxygen or sulfur, and the other two of said ring positions "F", "G", and "J" are carbons;

• wherein said fused heteroaromatic rings may optionally be independently substituted on any of the carbon or nitrogen atoms capable of forming an additional bond with a substituent selected from hydrogen, (C.sub.1 -C.sub.6)alkyl, halogen, trifluoromethyl, amino-(CH.sub.2).sub.n --, (C.sub.1 -C.sub.6)alkylamino-(CH.sub.2).sub.n --, di(C.sub.1 -C.sub.6)alkyl-amino-(CH.sub.2).sub.n --, (C.sub.1 -C.sub.6)alkoxy, hydroxy (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-O--(C.sub.1 -C.sub.6)alkyl-, --CN, (C.sub.1 -C.sub.6)alkyl-CO--O--(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6)alkyl-O--CO--O--(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-CO--O--, hydroxy, --NO.sub.2, R.sup.3 --C(.dbd.O)--, R.sup.4 --O--C(.dbd.O)--, di(C.sub.1 -C.sub.6)alkyl-N--C(.dbd.O)--, (C.sub.1 -C.sub.6)cycloalkyl, and R.sup.4 --NH--C(.dbd.O)--, and phenyl optionally substituted with halo, (C.sub.1 -C.sub.6) alkyl, --CN, or --CF.sub.3 ;
• R.sup.1 is substituted phenyl of the formula Ph.sup.1 or heteroaryl wherein said heteroaryl is selected from the group consisting of pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, wherein said heteroaryl may optionally be substituted on any of the atoms capable of forming an additional bond, up to a maximum of three substituents, with a substituent selected from hydrogen, (C.sub.1 -C.sub.6)alkyl, halogen, trifluoromethyl, amino-(CH.sub.2).sub.n --, (C.sub.1 -C.sub.6)alkylamino-(CH.sub.2).sub.n --, di(C.sub.1 -C.sub.6)alkyl-amino-(CH.sub.2).sub.n --, (C.sub.1 -C.sub.6)alkoxy, hydroxy(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-O--(C.sub.1 -C.sub.6)alkyl-, --CN, (C.sub.1 -C.sub.6)alkyl-CO--O--(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6)alkyl-O--CO--O--(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-CO--O--, hydroxy, H--C(.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-C(.dbd.O)--, HO--C(.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-O--C(.dbd.O)--, NH.sub.2 --C(.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-NH--C(.dbd.O), and di(C.sub.1 -C.sub.6)alkyl-NH--C(.dbd.O )--;
• wherein said Ph.sup.1 is a group of the formula ##STR42## R.sup.2 is phenyl of the formula Ph.sup.2 or a five or six membered heterocycle, wherein said six membered heterocycle has the formula ##STR43## wherein "N" is nitrogen;
• wherein said ring positions "K", "L" and "M" may be independently selected from carbon or nitrogen, with the proviso that only one of "K", "L" or "M" can be nitrogen;
• wherein said five membered heterocycle has the formula ##STR44## wherein said ring positions "P," "Q" and "T" may be independently selected from carbon, nitrogen, oxygen or sulfur;
• with the proviso that only one of "P," "Q" or "T" can be oxygen or sulfur and at least one of "P," "Q" or "T" must be a heteroatom;
• wherein said Ph.sup.2 is a group of the formula ##STR45## R.sup.3 is hydrogen or (C.sub.1 -C.sub.6)alkyl;
• R.sup.4 is hydrogen or (C.sub.1 -C.sub.6)alkyl;
• R.sup.5 is hydrogen, (C.sub.1 -C.sub.6)alkyl, halo, CF.sub.3, (C.sub.1 -C.sub.6)alkoxy or (C.sub.1 -C.sub.6)alkylthiol;
• R.sup.6 is hydrogen or halo;
• R.sup.7 is hydrogen or halo;
• R.sup.8 is hydrogen or halo;
• R.sup.9 is hydrogen, (C.sub.1 -C.sub.6)alkyl optionally substituted with one to three halogen atoms, halo, CF.sub.3, (C.sub.1 -C.sub.6)alkoxy optionally substituted with one to three halogen atoms, (C.sub.1 -C.sub.6)alkylthiol, R.sup.13 O--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-NH--(CH.sub.2).sub.p --, di(C.sub.1 -C.sub.6)alkyl-N--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.5)cycloalkyl-NH--(CH.sub.2).sub.p --, H.sub.2 N--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-HN--(C.dbd.O)--(CH.sub.2).sub.p --, di(C.sub.1 -C.sub.6)alkyl-N--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.5)cycloalkyl-NH--(C.dbd.O)--(CH.sub.2).sub.p --, R.sup.13 O--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl--(O.dbd.C)--O--(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6)alkyl-O--(O.dbd.C)--O--(C.sub.1 -C.sub.6)-alkyl-, ##STR46## hydroxy, H--C(.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-C(.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-O--, C(.dbd.O)--, R.sup.4 --(CH.sub.2).sub.p --O--C(.dbd.O)--, amino-(CH.sub.2).sub.p --, hydroxy-(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6)alkyl-O--(C.sub.1 -C.sub.6)alkyl-, and --CN;
• R.sup.10 and R.sup.14 are hydrogen, (C.sub.1 -C.sub.6)alkyl optionally substituted with one to three halogen atoms, halo, CF.sub.3, (C.sub.1 -C.sub.6)alkoxy optionally substituted with one to three halogen atoms, (C.sub.1 -C.sub.6)alkylthiol, R.sup.13 O--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-NH--(CH.sub.2).sub.p --, di(C.sub.1 -C.sub.6)alkyl-N--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.5)cycloalkyl-NH--(CH.sub.2).sub.p --, H.sub.2 N--(C.dbd.O)--, (CH.sub.2 .sub.p --, (C.sub.1 -C.sub.6)alkyl-HN--(C.dbd.O)--(CH.sub.2).sub.p --, di(C.sub.1 -C.sub.6)alkyl-N--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)cycloalkyl-NH--(C.dbd.O)--(CH.sub.2 (.sub.p --, R.sup.13 O--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-(O.dbd.C)--O--(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-O--(O.dbd.C)--O--(C.sub.1 -C.sub.6)--alkyl-, (C.sub.1 -C.sub.6)alkyl-(O.dbd.C)--O--, (C.sub.1 -C.sub.6)alkyl-(O.dbd.C)--NH--(CH.sub.2).sub.p --, alkyl-(O.dbd.C)--N--(CH.sub.2).sub.p --, H(O.dbd.C)--N--(CH.sub.2).sub.p - - ##STR47## hydroxy, H--C(.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-C(.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-O--C(.dbd.O)--, R.sup.4 --(CH.sub.2).sub.p --O--C(.dbd.O)--, amino-(CH.sub.2).sub.p --, hydroxy-(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-O--(C.sub.1 -C.sub.6)alkyl, --CHO and --CN;
• R.sup.11 is hydrogen or halo;
• R.sup.12 is hydrogen or halo;
• R.sup.13 is hydrogen, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-(C.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-O--(C.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-NH--(C.dbd.O--, or di(C.sub.1 -C.sub.6)alkly-N--(C.dbd.O)--;
• R.sup.15 is hydrogen --CN, (C.sub.1 -C.sub.6)alkyl, halo, CF.sub.3, --CHO or (C.sub.1 -C.sub.6)alkoxy;
• R.sup.16 is hydrogen, --CN, (C.sub.1 -C.sub.6)alkyl, halo, CF.sub.3, --CHO or (C.sub.1 -C.sub.6)alkoxy;
• R.sup.17 is hydrogen, --CN, (C.sub.1 -C.sub.6)alkyl, halo, CF.sub.3, CHO or (C.sub.1 -C.sub.6)alkoxy;
• n is an integer from zero to 3;
• p is an integer from zero to 3;
• wherein the dashed bond represents an optional double bond;
• with the proviso that when R.sup.9 is hydrogen, then one of R.sup.11 and R.sup.12 is other than hydrogen.

A method for treating disorders the treatment of which is facilitated by enhanced glutamate neurotransmission in a mammal, comprising administering to a mammal requiring such treatment an AMPA receptor antagonizing effective amount of a bicyclic compound, or pharmaceutically acceptable salt of said bicyclic compound, of the formula ##STR48## wherein ring A is a fused 5 membered heteroaromatic ring which, taken together with the carbon atoms common to both rings of the bicyclic system, has the formula ##STR49## wherein one of said ring positions "F", "G" and "J" is selected from nitrogen, oxygen or sulfur, and the other two of said ring positions "F", "G", and "J" are carbons;

• wherein said fused heteroaromatic rings may optionally be independently substituted on any of the carbon or nitrogen atoms capable of forming an additional bond with a substituent selected from hydrogen, (C.sub.1 -C.sub.6)alkyl, halogen, trifluoromethyl, amino-(CH.sub.2).sub.n --, (C.sub.1 -C.sub.6)alkylamino-(CH.sub.2).sub.n --, di(C.sub.1 -C.sub.6)alkyl-amino-(CH.sub.2).sub.n --, (C.sub.1 -C.sub.6)alkoxy, hydroxy (C.sub.l -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-O--(C.sub.1 -C.sub.6)alkyl-, --CN, (C.sub.1 -C.sub.6)alkyl-CO--O--(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6)alkyl-O--CO--O--(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-CO--O--, hydroxy, --NO.sub.2, R.sup.3 --C(.dbd.O)--, R.sup.4 --O--C(.dbd.C)--, di(C.sub.1 -C.sub.6)alkyl-N--C(.dbd.O)--, (C.sub.1 -C.sub.6)cycloalkyl, and R.sup.4 --NH--C(.dbd.O)--, and phenyl optionally substituted with halo, (C.sub.1 -C.sub.6)alkyl, --CN, or --CF.sub.3 ;
• R.sup.1 is substituted phenyl of the formula Ph.sup.1 or heteroaryl wherein said heteroaryl is selected from the group consisting of pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, wherein said heteroaryl may optionally be substituted on any of the atoms capable of forming an additional bond, up to a maximum of three substituents, with a substituent selected from hydrogen, (C.sub.1 -C.sub.6)alkyl, halogen, trifluoromethyl, amino-(CH.sub.2).sub.n --, (C.sub.1 -C.sub.6)alkyl-amino-(CH.sub.2).sub.n --, di(C.sub.1 -C.sub.6)alkyl-amino-(C.sub.2).sub.n --, C.sub.1 -C.sub.6)alkoxy, hydroxy(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-O--(C.sub.1 -C.sub.6)alkyl-, --CN, (C.sub.1 -C.sub.6)alkyl--CO--O--(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6)alkyl-O--CO--O--(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-CO--O--, hydroxy, H--C(.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-C(.dbd.O)--, HO--C(.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-O--C(.dbd.O)--, NH.sub.2 --C(.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-NH--C(.dbd.O), and di(C.sub.1 -C.sub.6)alkyl-NH--C(.dbd.O)--;
• wherein said Ph.sup.1 is a group of the formula ##STR50## R.sup.2 is phenyl of the formula Ph.sup.2 or a five or six membered heterocycle, wherein said six membered heterocycle has the formula ##STR51## wherein "N"is nitrogen;
• wherein said ring positions "K", "L" and "M" may be independently selected from carbon or nitrogen, with the proviso that only one of "K", "L" or "M" can be nitrogen;
• wherein said five membered heterocycle has the formula ##STR52## wherein said ring positions "P," "Q" and "T" may be independently selected from carbon, nitrogen, oxygen or sulfur;
• with the proviso that only one of "P," "Q" or "T" must be a heteroatom;
• wherein said Ph.sup.2 is a group of the formula ##STR53## R.sup.3 is hydrogen or (C.sub.1 -C.sub.6) alkyl;
• R.sup.4 is hydrogen or (C.sub.1 -C.sub.6) alkyl;
• R.sup.5 is hydrogen, (C.sub.1 -C.sub.6)alkyl, halo, CF.sub.3, (C.sub.1 -C.sub.6)alkoxy or (C.sub.1 -C.sub.6)alkylthiol;
• R.sup.6 is hydrogen or halo;
• R.sup.7 is hydrogen or halo;
• R.sup.8 is hydrogen or halo;
• R.sup.9 is hydrogen, (C.sub.1 -C.sub.6)alkyl optionally substituted with one to three halogen atoms, halo, CF.sub.3, (C.sub.1 -C.sub.6)alkoxy optionally substituted with one to three halogen atoms, (C.sub.1 -C.sub.6)alkylthiol, R.sup.13 O--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-NH--(CH.sub.2).sub.p --, di(C.sub.1 -C.sub.6)alkyl-N--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.5)cycloalkyl-NH--(CH.sub.2).sub.p --, H.sub.2 N--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-HN--(C.dbd.O)--(CH.sub.2).sub.p --, di(C.sub.1 -C.sub.6)alkyl-N--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.5))cycloalkyl-NH--(C.dbd.O)--(CH.sub.2).sub.p --, R.sup.13 O--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-(O.dbd.C)--O--(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6)alkyl-O--(O.dbd.C)--O--(C.sub.1 -C.sub.6)-alkyl-, ##STR54## hydroxy, H--C(.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-C(.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-O--C(.dbd.O)--, R.sup.4 --(CH.sub.2).sub.p --O--C(.dbd.O)--, amino-(CH.sub.2).sub.p --, hydroxy-(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6)alkyl-O--(C.sub.1 -C.sub.6)alkyl-, and --CN;
• R.sup.10 and R.sup.14 are hydrogen, (C.sub.1 -C.sub.6)alkyl optionally substituted with one to three halogen atoms, halo, CF.sub.3, (C.sub.1 -C.sub.6)alkoxy optionally substituted with one to three halogen atoms, (C.sub.1 -C.sub.6)alkylthiol, R.sup.13 --(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-NH--(CH.sub.2).sub.p --, di(C.sub.1 -C.sub.6)alkyl-N--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.5)cycloalkyl-NH--(CH.sub.2).sub.p --, H.sub.2 N--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-HN--(C.dbd.O)--(CH.sub.2).sub.p --, di(C.sub.1 -C.sub.6)alkyl-N--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.5)cycloalkyl-NH--(C.dbd.O)--(CH.sub.2).sub.p --, R.sup.13 O--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-(O.dbd.C)--O--(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6)alkyl-O--(O.dbd.C)--O--(C.sub.1 -C.sub.6)-alkyl-, (C.sub.1 -C.sub.6)alkyl-(O.dbd.C)--O--, (C.sub.1 -C.sub.6)alkyl-(O.dbd.C)--NH--(CH.sub.2).sub.p --, H(O.dbd.C)--NH--(CH.sub.2).sub.p --, ##STR55## hydroxy, H--C(.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl-C(.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-O--C(.dbd.O)--, R.sup.4 --(CH.sub.2).sub.p --O--C(.dbd.O)--, amino-(CH.sub.2).sub.p --, hydroxy-(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-O--(C.sub.1 -C.sub.6)alkyl, --CHO and --CN,
• R.sup.11 is hydrogen or halo;
• R.sup.12 is hydrogen or halo;
• R.sup.13 is hydrogen, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl-(C--O)--, (C.sub.1 -C.sub.6)alkyl-O--(C.dbd.O)--, (C.sub.1 -C.sub.6)alkyl-NH--(C.dbd.C)--, or di(C.sub.1 -C.sub.6)alkyl-N--(C.dbd.O)--;
• R.sup.15 is hydrogen, --CN, (C.sub.1 -C.sub.6)alkyl, halo, CF.sub.3, --CHO or (C.sub.1 -C.sub.6)alkoxy;
• R.sup.16 is hydrogen, --CN, (C.sub.1 -C.sub.6)alkyl, halo, CF.sub.3, --CHO or (C.sub.1 -C.sub.6)alkoxy;
• R.sup.17 is hydrogen, --CN, (C.sub.1 -C.sub.6)alkyl, halo, CF.sub.3, CHO or (C.sub.1 -C.sub.6)alkoxy;
• n is an integer from zero to 3;
• p is an integer from zero to 3;
• wherein the dashed bond represents an optional double bond;
• with the proviso that when R.sup.9 is hydrogen, then one of R.sup.11 and R.sup.12 is other than hydrogen.