Patent ID: 6136812
Filing Date: 2000-10-24
Classification: A61K,A61P

Abstract:
A method of treating dyskinesia associated with dopamine agonist therapy in a mammal which comprises administering to said mammal an amount of a compound within group (A), (B), (C), (D), (E), or (F), or a pharmaceutically acceptable salt of said compound, that is effective in treating said dyskinesia, wherein groups (A), (B), (C), (D), (E), and (F) are defined as follows:(A) (S)-3-(2-chloro-phenyl)-2-[2-(5-diethylaminomethyl-2-fluoro-phenyl)-vinyl] -6-fluoro-3H-quinazolin-4-one;(S)-3-(2-chloro-phenyl)-2-[2-(6-diethylaminomethyl-pyridin-2-yl)-vinyl]-6-f luoro-3H-quinazolin-4-one;(S)-3-(2-chloro-phenyl)-2-[2-(4-diethylaminomethyl-pyridin-2-yl)-vinyl]-6-f luoro-3H-quinazolin-4-one;(S)-3-(2-chloro-phenyl)-2-[2-(6-ethylaminomethyl-pyridin-2-yl)-vinyl]-6-flu oro-3H-quinazolin-4-one;(S)-3-(2-bromo-phenyl)-2-[2-(6-diethylaminomethyl-pyridin-2-yl)-vinyl]-6-fl uoro-3H-quinazolin-4-one;(S)-3-(2-chloro-phenyl)-6-fluoro-2-[2-(6-methoxymethyl-pyridin-2-yl)-vinyl] -3H-quinazolin-4-one;(S)-3-(2-chloro-phenyl)-6-fluoro-2-[2-(4-methyl-pyrimidine-2-yl)-vinyl]-6-f luoro-3H-quinazolin-4-one;(S)-3-(2-chloro-phenyl)-6-fluoro-2-{2-[6-(isopropylamino-methyl)-pyridin-2- yl]-ethyl}-3H-quinazolin-4-one;(S)-6-fluoro-2-[2-(2-methyl-thiazol-4-yl)-vinyl]-3-(2-methyl-phenyl)-3H-qui nazolin-4-one;(S)-3-(2-chloro-phenyl)-6-fluoro-2-[2-(2-methyl-thiazol-4-yl)-vinyl]-3H-qui nazolin-4-one;(S)-2-[2-(2-dimethylaminomethyl-thiazol-4-yl)-vinyl]-6-fluoro-3-(2-fluoro-p henyl)-3H-quinazolin-4-one;(S)-3-(2-bromo-phenyl)-6-fluoro-2-[2-(2-methyl-thiazol-4-yl)-vinyl]-3H-quin azolin-4-one;(S)-3-(2-chloro-phenyl)-2-[2-(2-methyl-thiazol-4-yl)-vinyl]-3H-quinazolin-4 -one;(S)-3-(2-chloro-phenyl)-6-fluoro-2-(2-pyridin-2-yl-vinyl)-3H-quinazolin-4-o ne;(S)-3-(2-bromo-phenyl)-2-(2-pyridin-2-yl-vinyl)-3H-quinazolin-4-one;(S)-6-chloro-2-(2-pyridin-2-yl-vinyl)-3-o-tolyl-3H-quinazolin-4-one;(S)-3-(2-chloro-phenyl)-2-[2-(6-methyl-pyridin-2-yl)-vinyl]-3H-quinazolin-4 -one;(S)-6-chloro-2-[2-(6-methyl-pyridin-2-yl)-vinyl]-3-o-tolyl-3H-quinazolin-4- one;(S)-3-(2-chloro-phenyl)-6-fluoro-2-(2-pyridin-2-yl-ethyl)-3H-quinazolin-4-o ne;(S)-6-{2-[3-(2-chloro-phenyl)-6-fluoro-4oxo-3,4-dihydro-quinazolin-2-yl]-vi nyl}-pyridine-2-carbaldehyde;(S)-3-(2-chloro-phenyl)-6-fluoro-2-[2-(6-methylaminomethyl-pyridin-2-yl)-vi nyl]-3H-quinazolin-4-one;(S)-N-(6-{2-(2-chloro-phenyl-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-vi nyl}-pyridin-2-ylmethyl)-N-methyl-acetamide;(S)-6-{2-[3-(2-chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-v inyl}-pyridine-2-carbonitrile;(S)-3-(2-fluoro-phenyl)-2-(2-pyridin-2-yl-vinyl)-3H-quinazolin-4-one;(S)-3-(2-bromo-phenyl)-6-fluoro-2-(2-pyridin-2-yl-vinyl)-3H-quinazolin-4-on e;(S)-3-(4-bromo-2-chloro-phenyl)-6-fluoro-2-(2-pyridin-2-yl-vinyl)-3H-quinaz olin-4-one;(S)-3-(2-chloro-phenyl)-2-[2-(6-diethylaminomethyl-pyridin-2-yl)-vinyl]-3H- quinazolin-4-one;(S)-N-(6-{2-[3-(2-chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl ]-vinyl}-pyridin-2-ylmethyl)-N-ethyl-acetamide;(S)-3-(2-chloro-phenyl)-6-fluoro-2-[2-(6-fluoromethyl-pyridin-2-yl)-vinyl]- 3H-quinazolin-4-one;(S)-3-(2-chloro-phenyl)-6-fluoro-[2-(6-pyrrolidin-1-ylmethyl-pyridin-2-yl)- ethyl]-3H-quinazolin-4-one;(S)-3-(2-chloro-phenyl)-2-[2-(6-{(ethyl-(2-hydroxy-ethyl)-amino]-methyl}-py ridin-2-yl)-vinyl]-6-fluoro-3H-quinazolin-4-one;(S)-3-(2-chloro-phenyl)-6-fluoro-2-{2-[6-(isopropylamino-methyl)-pyridin-2- yl]-vinyl}-3H-quinazolin-4-one;(S)-3-(2-chloro-phenyl)-6-fluoro-2-{2-[6-(2-methyl-piperidin-1-ylmethyl)-py ridin-2-yl]-vinyl}-3H-quinazolin-4-one;(S)-3-(2-chloro-phenyl)-2-[2-(6-ethoxymethyl-pyridin-2-yl)-vinyl]-6-fluoro- 3H-quinazolin-4-one;(S)-3-)2-chloro-phenyl)-2-{2-[6-(2,5-dihydro-pyrrol-1-ylmethyl)-pyridin-2-y l]-vinyl}-6-fluoro-3H-quinazolin-4-one;(S)-3-(2-chloro-phenyl)-6-fluoro-2-{2-[6-(4-methyl-piperidin-1-ylmethyl)-py ridin-2-yl]-vinyl}-3H-quinazolin-4-one;(S)-6-bromo-2-[2-(6-methyl-pyridin-2-yl)-vinyl]-3-o-tolyl-3H-quinazolin-4-o ne;(S)-6-bromo-2-(2-pyridin-2-yl-vinyl)-3-o-tolyl-3H-quinazolin-4-one;(S)-6-fluoro-3-(2-fluoro-phenyl)-2-(2-pyridin-2-yl-vinyl)-3H-quinazolin-4-o ne;(S)-3-(2-chloro-phenyl)-6-methyl-2-(2-pyridin-2-yl-vinyl)-3H-quinazolin-4-o ne;(S)-3-(2-chloro-phenyl)-2-[2-(6-dimethylaminomethyl-pyridin-2-yl)-vinyl]-6- fluoro-3H-quinazolin-4-one;(S)-6-fluoro-3-(2-fluoro-phenyl)-2-[2-(6-methyl-pyridin-2-yl)-vinyl]-3H-qui nazolin-4-one;(S)-3-(2-chloro-phenyl)-2-[2-(6-{(2-dimethylamino-ethyl)-methyl-amino]-meth yl}-pyridin-2-yl)-vinyl]-6-fluoro-3H-quinazolin-4-one;(S)-3-(2-chloro-phenyl)-6-2-[2-(6-hydroxymethyl-pyridin-2-yl)-vinyl]-3H-qui nazolin-4-one;(S)-acetic acid 6-{2-[3-(2-chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-viny l}-pyridin-2-yl methyl ester;(S)-6-{2-[3-(2-bromo-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-vi nyl}-pyridine-2-carbaldehyde;(S)-3-(2-bromo-phenyl)-2-[2-(6-diethylaminomethyl-pyridin-2-yl)-vinyl]-3H-q uinazolin-4-one;(S)-acetic acid 6-{2-[3-(2-bromo-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quin-azolin-2-yl]-viny l}-pyridin-2-ylmethyl ester;(S)-diethylamino-acetic acid 6-{2-[3-(2-chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-viny l}-pyridin-2-ylmethyl ester;(S)-3-(2-chloro-phenyl)-2-[2-(6-difluoromethyl-pyridin-2-yl)-vinyl]-6-fluor o-3H-quinzaolin-4-one;(S)-3-(2-chloro-phenyl)-2-[2-(6-methoxy-pyridin-2-yl)-vinyl]-3H-quinazolin- 4-one;(S)-2-{2-[3-(2-chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-v inyl}-6-methyl-nicotinonitrile;(S)-2-{2-[3-(2-chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-e thyl}-6-methyl-nicotinonitrile;(S)-3-(2-chloro-phenyl)-6-fluoro-2-(2-pyrimidine-2-yl-ethyl)-3H-quinazolin- 4-one;(S)-3-(2-chloro-phenyl)-2-[2-(4,6-dimethyl-pyrimidine-2-yl)-vinyl]-6-fluoro -3H-quinazolin-4-one;(S)-2-{2-[3-(2-chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-v inyl}-nicotinonitrile;(S)-3-(2-chloro-phenyl)-6-fluoro-2-(2-{6-[(3-methyl-butylamino)-methyl]-pyr idin-2-yl}-ethyl)-3H-quinazolin-4-one;(S)-2-{2-[3-(2-chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-e thyl}-nicotinonitrile;(S)-2-[2-(6-chloro-4-oxo-3-o-tolyl-3,4-dihydro-quinazolin-2-yl)-vinyl]-benz onitrile;(S)-2-{2-[3-(2-chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-v inyl}-4-methyl-benzonitrile;(S)-3-(2-bromo-phenyl)-6-fluoro-2-[2-(6-hydroxymethyl-pyridin-2-yl)-vinyl]- 3H-quinazolin-4-one; and(S)-3-(2-chloro-phenyl)-6-fluoro-2-[2-(6-pyrrolidin-1-ylmethyl-pyridin-2-yl -vinyl]-3H-quinazolin-4-one;(B) (S)-6-fluoro-2-[2-(2-fluoro-phenyl)-vinyl]-3-(2-methyl-pyridin-3-yl)-3H-qu inazolin-4-one;(S)-2-{2-[6-fluoro-3-(2-methyl-pyridin-3-yl)-4-oxo-3,4-dihydro-quinazolin-2 -yl]-vinyl}-benzonitrile;(S)-2-{2-[6-fluoro-3-(2-methylpyridin-3-yl)-4-oxo-3,4-dihydroquinazolin-2-y l]-vinyl}-benzonitrile;(S)-2-{2-[3-(2-chloro-pyridin-3-yl)-6-fluoro-4-oxo-3,4-dihydroquinazolin-2- yl]-vinyl}-benzonitrile;(S)-2-{2-[6-fluoro-3-(2-methyl-pyridin-3-yl)-4-oxo-3,4-dihydro-quinazolin-2 -yl]-vinyl}-4-methyl-benzonitrile;(S)-2-{2-[3-(2-methyl-pyridin-3-yl)-4-oxo-3,4-dihydro-quinazolin-2-yl]-viny l}-benzonitrile;(S)-6-fluoro-3-(2-methyl-pyridin-3-yl)-2-[2-(thiazol-2-yl)-vinyl]-3H-quinaz olin-4-one;(S)-6-fluoro-3-(2-methyl-pyridin-3-yl)-2-[2-(2-methyl-thiazol-4-yl)-vinyl]- 3H-quinazolin-4-one;(S)-6-fluoro-3-(2-methyl-pyridin-3-yl)-2-[2-(4-methyl-thiazol-2-yl)-vinyl]- 3H-quinazolin-4-one;(S)-2-[2-(5-diethylaminomethyl-2-fluoro-phenyl)-vinyl]-6-fluoro-3-(2-methyl -pyridin-3-yl)-3H-quinazolin-4-one;(S)-6-fluoro-2-[2-(2-fluoro-5-pyrrolidin-1-ylmethyl-phenyl)-vinyl]-3-(2-met hyl-pyridin-3-yl)-3H-quinazolin-4-one;(S)-3-(2-chloro-pyridin-3yl)-2-[2-(2-fluoro-phenyl)-vinyl]-3H-quinazolin-4- one;(S)-3-(2-chloro-pyridin-3-yl)-6-fluoro-2-[2-(6-methyl-phenyl-2-yl)-vinyl]-3 H-quinazolin-4-one;(S)-3-(2-chloro-pyridin-3-yl)-6-fluoro-2-[2-(fluoro-phenyl)-vinyl]-3H-quina zolin-4-one;(S)-6-chloro-2-[2-(2-fluoro-phenyl)-vinyl]-3-(2-methyl-pyridin-3-yl)-3H-qui nazolin-4-one;(S)-6-chloro-2-[2-(2-fluoro-phenyl)-vinyl]-3-(3-methyl-1-oxy-pyridin-4-yl)- 3H-quinazolin-4-one;(S)-3-{2-(3-(2-chloro-pyridin-3-yl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2 -yl]-vinyl}-benzaldehyde;(S)-3-{2-[3-(2-chloro-pyridin-3-yl)-4-oxo-3,4-dihydro-quinazolin-2-yl]-viny l}-benzaldehyde;(S)-3-(2-chloro-pyridin-3-yl)-6-fluoro-2-[2-(3-hydroxymethyl-phenyl)-vinyl] -3H-quinazolin-4-one;(S)-3-(2-chloro-pyridin-3-yl)-2-{2-[3(1,4-dioxa-8-aza-spiro[4.5]dec-8-ylmet hyl)-phenyl]-vinyl}-6-fluoro-3-3H-quinazolin-4-one;(S)-3-(2-chloro-pyridin-3-yl)-6-fluoro-2-{2-[3-(4-pyrrolidin-1-yl-piperidin -1-ylmethyl)-phenyl]-vinyl}-3H-quinazolin-4-one;(S)-2-{2-[3-(2-chloro-pyridin-3-yl-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2- yl]-vinyl}-benzonitrile;(S)-2-{2-[3-(2-chloro-pyrdini-3-yl)-4-oxo-3,4-dihydro-quinazolin-2-yl]-viny l}-benzonitrile;(S)-2-[2-(2-fluoro-phenyl)-vinyl]-3-(2-methyl-pyridin-3-yl)-3H-quinazolin-4 -one;(S)-3-(2-chloro-pyridin-3-yl)-6-fluoro-2-[2-hydroxy-phenyl)-vinyl]-3H-quina zolin-4-one;(S)-6-fluoro-3-(2-methyl-pyridin-3-yl)-2-[2-(2-methyl-thiazol-4-yl)-ethyl]- 3H-quinazolin-4-one;(S)-6-fluoro-3-(2-chloro-pyridin-3-yl)-2-[2-(2-dimethylamino-methylthiazol- 4-yl)-vinyl]-3H-quinazolin-4-one;(S)-2-[2-(5-Diethylaminomethyl-2-fluoro-phenyl)-vinyl]-6-fluoro-3-(4-methyl -pyridin-3-yl)-3H-quinazolin-4-one;(S)-4-Diethylaminomethyl-2-{2-[6-fluoro-3-(4-methyl-pyridin-3-yl)-4-oxo-3,4 -dihydro-quinazolin-2-yl]-vinyl}-benzonitrile;(S)-2-[2-(5-Diethylaminomethyl-2-fluoro-phenyl)-vinyl]-6-fluoro-3-(3-methyl -pyrazin-2-yl)-3H-quinazolin-4-one;(S)-6-fluoro-3-(2-methyl-pyridin-3-yl)-2-[2-(2-dimethylamino-methylthiazol- 4-yl)-vinyl]-3H-quinazolin-4-one;(S)-6-fluoro-3-(2-methyl-pyridin-3-yl)-2-[2-(2-methyl-oxazol-4-yl)-vinyl]-3 H-quinazolin-4-one;(S)-6-fluoro-3-(2-chloro-pyridin-3-yl)-2-[2-(thiazol-2-yl)-vinyl]-3H-quinaz olin-4-one;(S)-6-fluoro-3-(4-methyl-pyridin-3-yl)-2-[2-(4-methyl-thiazol-2-yl)-vinyl]- 3H-quinazolin-4-one;(S)-3-(2-chloro-pyridin-3-yl)-6-fluoro-2-[2-(2-hydroxy-phenyl)-vinyl]-3H-qu inazolin-4-one; and(S)-6-fluoro-2-[2-(2-fluoro-5-pyrrolidin-1-ylmethyl-phenyl)-ethyl]-3-(2-met hyl-pyridin-3-yl)-3H-quinazolin-4-one;(C) 3-(2-chloro-phenyl)-6-fluoro-2-(2-pyridin-2-yl-vinyl)-3H-quinazolin-4-one;3-(2-bromo-phenyl)-2-(2-pyridin-2-yl)-3H-quinazolin-4-one;6-chloro-2-(2-pyridin-2-yl-vinyl)-3-o-tolyl-3H-quinazolin-4-one;3-(2-chloro-phenyl)-2-[2-(6-methyl-pyridin-2-yl)-vinyl]-3H-quinazolin-4-one ;6-chloro-2-[2-(6-methyl-pyridin-2-yl)-vinyl]-3-o-tolyl-3H-quinazolin-4-one;3-(2-chloro-phenyl)-6-fluoro-2-(2-pyridin-2-yl-ethyl)-3H-quinazolin-4-one;6-{2-[3-(2-chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-vinyl }-pyridine-2-carbaldehyde;3-(2-chloro-phenyl)-6-fluoro-2-[2-(6-methylaminomethyl-pyridin-2-yl)-vinyl] -3H-quinazolin-4-one;N-(6-{2-[3-(2-chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-vi nyl}-pyridin-2-ylmethyl)-N-methyl-acetamide;3-(2-chloro-phenyl)-2-[2-(4-diethylaminomethyl-pyridin-2-yl)-vinyl]-6-fluor o-3H-quinazolin-4-one;6-{2-[3-(2-chloro-pheny;)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-vinyl }-pyridine-2-carbonitrile;3-(2-fluoro-phenyl)-2-(2-pyridin-2-yl-vinyl)-3H-quinazolin-4-one;3-(2-bromo-phenyl)-6-fluoro-2-(2-pyridin-2-yl-vinyl)-3H-quinazolin-4-one;3-(4-bromo-2-chloro-phenyl)-6-fluoro-2-(2-pyridin-2-yl-vinyl)-3H-quinazolin -4-one;3-(2-chloro-phenyl)-2-[2-(6-diethylaminomethyl-pyridin-2-yl)-vinyl)-3H-quin azolin-4-one;N-(6-{2-[3-(2-chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-vi nyl}-pyridin-2-ylmethyl)-N-ethyl-acetamide;3-(2-chloro-phenyl)-6-fluoro-2-[2-(6-fluoromethyl-pyridin-2-yl)-vinyl]-3H-q uinazolin-4-one;3-(2-chloro-phenyl)-6-fluoro-2-[2-(6-pyrrolidin-1-ylmethyl-pyridin-2-yl)-et hyl]-3H-quinazolin-4-one;3-(2-chloro-phenyl)-2-[2-(6-{(ethyl-(2-hydroxy-ethyl)-amino]-methyl}-pyridi n-2-yl)-vinyl]-6-fluoro-3H-quinazolin-4-one;3-(2-chloro-phenyl)-6-fluoro-2-{2-[6-(isopropylamino-methyl)-pyridin-2-yl]- vinyl}-3H-quinazolin-4-one;3-(2-chloro-phenyl)-6-fluoro-2-{2-[6-(2-methyl-piperidin-1-ylmethyl)-pyridi n-2-yl]-vinyl}-3H-quinazolin-4-one;3-(2-chloro-phenyl)-2-[2-(6-ethylaminomethyl-pyridin-2-yl)-vinyl]-6-fluoro- 3H-quinazolin-4-one;3-(2-chloro-phenyl)-2-[2-(6-ethoxymethyl-pyridin-2-yl)-vinyl]-6-fluoro-3H-q uinazolin-4one;3-(2-chloro-phenyl)-2-{2-[6-(2,5-dihydro-pyrrol-1-ylmethyl)-pyridin-2-yl]-v inyl}-6-fluoro-3H-quinazolin-4-one;3-(2-chloro-phenyl)-6-fluoro-2-{2-[6-(4-methyl-piperidin-1-ylmethyl)-pyridi n-2-yl]-vinyl}-3H-quinazolin-4-one;6-bromo-2-[2-(6-methyl-puridin-2-yl)-vinyl]-3-o-tolyl-3H-quinazolin-4-one;6-bromo-2-(2-pyridin-2-yl-vinyl)-3-o-tolyl-3H-quinazolin-4-one;6-fluoro-3-(2-fluoro-phenyl)-2-(2-pyridin-2-yl-vinyl)-3H-quinazolin-4-one;1-benzyl-5-(2-methyl-[1,3]dioxolan-2-yl)-2-oxo-2,3-dihydro-1H-indole-3-carb oxylic acid (3-phenylcarbamoyl-phenyl)-amide;3-(2-chloro-phenyl)-6-methyl-2-(2-pyridin-2-yl-vinyl)-3H-quinazolin-4-one;3-(2-chloro-phenyl)-2-[2-(6-dimethylaminomethyl-pyridin-2-yl)-vinyl]-6-fluo ro-3H-quinazolin-4-one;6-fluoro-3-(2-fluoro-phenyl)-2-[2-(6-methyl-pyridin-2-yl)-vinyl]-3H-quinazo lin-4-one;3-(2-chloro-phenyl)-2-[2-(6-{[(2-dimethylamino-ethyl)-methyl-amino]-methyl} -pyridin-2-yl)-vinyl]-6-fluoro-3H-quinazolin-4-one;3-(2-chloro-phenyl)-6-fluoro-2-[2-(6-hydroxymethyl-pyridin-2-yl)-vinyl]-3H- quinazolin-4-one;acetic acid 6-{2-[3-(2-chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-viny l}-pyridin-2-ylmethyl ester;6-{2-[3-(2-bromo-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-vinyl} -pyridine-2-carbaldehyde;3-(2-bromo-phenyl)-2-[2-(6-diethylaminomethyl-pyridin-2-yl)-vinyl]-6-fluoro -3H-quinazolin-4-one;3-(2-bromo-phenyl)-2-[2-(6-diethylaminomethyl-pyridin-2-yl)-vinyl]-3H-quina zolin-4-one;acetic acid 6-{2-[3-(2-bromo-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-vinyl }-pyridin-2-ylmethyl ester;3-(2-chloro-phenyl)-6-fluoro-2-[2-(6-methoxymethyl-pyridin-2-yl)-vinyl]-3H- quinzolin-4-one;diethylamino-acetic acid 6-{2-[3-(2-chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-viny l}-pyridin-2-ylmethyl ester;6-fluoro-3-(2-methyl-pyridin-3-yl)-2-[2-(2-methyl-thiazol-4-yl)-vinyl]-3H-q uinazolin-4-one;3-(2-bromo-phenyl)-6-fluoro-2-[2-(6-hydroxymethyl-pyridin-2-yl)vinyl]-3H-qu inazolin-4-one; and,3-(2-chloro-phenyl)-6-fluoro-2-[2-(6-pyrrolidin-1-ylmethyl-pyridin-2-yl)-vi nyl]-3H-quinazolin-4-one;(D) 6-Chloro-3-(2-chloro-phenyl)-2-[2-hydroxy-2-(6-methyl-pyridin-2-yl)-vinyl] -3H-quinazolin-4-one; 2-{2-[3-(2-Chloro-phenyl)-4-oxo-3,4-dihydro-quinazolin-2-yl]-1-hydroxy-vin yl}-nicotinonitrile;2-{2-[3-(2-Chloro-pyrid-3-yl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-1 -hydroxy-vinyl}-nicotinonitrile;2-{2-[6-Chloro-3-(2-methyl-phenyl)-4-oxo-3,4-dihydro-quinazolin-2-yl]-1-hyd roxy-vinyl]-nicotinonitrile;3-(2-Chloro-phenyl)-2-[2-(3-diethylaminomethyl-phenyl)-2-hydroxy-ethoxy]-6- fluoro-3H-quinazolin-4-one;3-(2-Chloro-phenyl)-6-fluoro-2-[2-(3-pyrrolidin-1-ylmethyl-phenyl)-2-hydrox y-ethyl]-3H-quinazolin-4-one;3-(2-Chloro-pyrid-3-yl)-2-[2-(3-diethylaminomethyl-phenyl)-2-hydroxy-ethyl] -6-fluoro-3H-quinazolin-4-one;2-[2-(3-Diethylaminomethyl-phenyl)-2-hydroxy-ethyl]-6-fluoro-3-(2-fluoro-ph enyl)-3H-quinazolin-4-one;2-[2-(3-Diethylaminomethyl-phenyl)-2-hydroxy-ethyl]-3-(2-fluoro-phenyl)-3H- quinazolin-4-one;3-(2-chloro-phenyl)-2-[2-(6-diethylaminomethyl)-pyridin-2-yl)-2-hydroxy-vin yl]-6-fluoro-3H-quinazolin-4-one;2-[2-[3-(2-Chloro-pyrid-3-yl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-1 -hydroxy-vinyl}-6-methyl-nicotinonitrile;2-{2-[3-(2-Chloro-phenyl)-4-oxo-3,4-dihydro-quinazolin-2-yl]-1-hydroxy-viny l)-6-methyl-nicotinonitrile;2-{2-[6-Chloro-3-(2-chloro-phenyl)-4-oxo-3,4-dihydro-quinazolin-2-yl]-1-hyd roxy-vinyl}-6-methyl-nicotinonitrile;2-{2-[3-(2-Chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-1-hyd roxy-vinyl}-6-fluoro-nicotinonitrile;2-{2-[3-(2-Chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-1-hyd roxy-vinyl}-4-fluoro-benzonitrile;2-{2-[3-(2-Chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-1-hyd roxy-vinyl}-4-methyl-benzonitrile;2-{2-[3-(2-Chloro-phenyl)-4-oxo-3,4-dihydro-thieno[3,2d]pyrimidin-2-yl]-1-h ydroxy-vinyl}-6-methyl-nicotinonitrile;2-{2-[3-(2-methyl-phenyl)-4-oxo-3,4-dihydro-thieno[3,2d]pyrimidin-2-yl]-1-h ydroxy-vinyl}-6-methyl-nicotinonitrile;2-{2-[3-(2-Chloro-pyrid-3yl)-4-3,4-dihydro-thieno[3,2-d]pyrimidin-2-yl]-1-h ydroxy-vinyl}-4-methyl-benzonitrile;2-{2-[3-(2-Chloro-phenyl)-4-oxo-3,4-dihydro-thieno[3,2-d]pyrimidin-2-yl]-1- hydroxy-vinyl}-4-fluoro-benzonitrile;2-{2-[3-(2-Fluoro-phenyl)-4-oxo-3,4-dihydro-thieno[3,2-d]pyrimidin-2-yl]-1- hydroxy-vinyl}-4-methyl-benzonitrile;2-{2-[3-(2-Chloro-phenyl)-4-oxo-3,4-dihydro-thieno[3,2-d]pyrimidin-2-yl]-1- hydroxy-vinyl}-benzonitrile; and,2-{2-[3-(2-Chloro-pyrid-3yl)-4-oxo-3,4-dihydro-thieno[3,2-d]pyrimidin-2-yl] -1-hydroxy-vinyl}-benzonitrile;3-(2-chloro-phenyl)-6-fluoro-2-[2-hydroxy-2-(2-methyl-thiazol-4-yl)-vinyl]- 3H-quinazolin-4-one;3-(2-chloro-phenyl)-6-fluoro-2-[2-hydroxy-2-(6-methyl-pyridin-2-yl)-vinyl]- 3H-quinazolin-4-one;2-{2-[3-(2-chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-1-hyd roxy-vinyl}-6-methyl-nicotinonitrile;2-{2-[3-(2-chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-1-hyd roxy-vinyl}-nicotinonitrile;2-{2-[3-(2-chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl]-1-hyd roxy-vinyl}-benzonitrile;2-{2-[3-(2-chloro-pyridin-3-yl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl] -1-hydroxy-vinyl}-6-methyl-nicotinonitrile;3-(2-chloro-phenyl)-6-fluoro-2-(2-hydroxy-2-pyridin-2-yl-vinyl)-3H-quinazol in-4-one;2-{2-[6-fluoro-3-(2-methyl-pyridin-3-yl)-4-oxo-3,4-dihydro-quinazolin-2-yl] -1-hydroxy-vinyl}-benzonitrile;2-{2-[3-(2-chloro-pyridin-3-yl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-yl] -1-hydroxy-vinyl}-benzonitrile;3-(2-chloro-phenyl)-6-fluoro-2-[2-(2-fluoro-phenyl)-2-hydroxy-ethyl]-3H-qui nazolin-4-one;(E) 3-(2-chloro-phenyl)-6-fluoro-2-[(pyridin-2-ylmethyl)-amino]-3H-quinazolin- 4-one;6-fluoro-3-(2-methyl-phenyl)-2-[(pyridin-2-ylmethyl)-amino]-3H-quinazolin-4 -one;3-(2-chloro-phenyl)-6-fluoro-2-[(2-flurophenyl-methyl)-amino]-3H-quinazolin -4-one;3-(2-chloro-phenyl)-2-[(2-cyanophenyl-methyl)-amino]-6-fluoro-3H-quinazolin -4-one;3-(2-chloro-phenyl)-2-[(6-diethylaminomethylpyridin-2-ylmethyl)-amino]-6-fl uoro-3H-quinazolin-4-one;3-(2-chloro-phenyl)-6-fluoro-2-[(6-pyrrolidin-1-ylmethyl-pyridin-2-ylmethyl )-amino]-3H-quinazolin-4-one;3-(2-chloro-phenyl)-2-[(3-pyrrolidin-1-ylmethyl-phenylamino)-methyl]-3H-thi eno[3,2-d]pyrimidin-4-one;3-(2-methyl-phenyl)-2-[(3-pyrrolidin-1-ylmethyl-phenylamino)-methyl]-3H-thi eno[3,2-d]pyrimidin-4-one;3-(2-chloro-phenyl)-2-[(2-fluoro-phenylamino)-methyl]-3H-thieno[3,2d]pyrimi din-4-one;3-(2-chloro-pyrid-3-yl)-2-[(3-pyrrolidin-1-ylmethyl-phenylamino)-methyl]-3H -thieno[3,2-d]pyrimidin-4-one;2-{[3-(2-chloro-pyrid-3-yl)-4-oxo-3,4-dihydro-thieno[3,2-d]pyrimidin-2-ylme thyl]-amino}-benzonitrile;3(2-chloro-phenyl)-2-[(3-pyrrolidin-1-ylmethyl-phenylamino)-methyl]-3H-quin azolin-4-one;6-chloro-3-(2-chloro-phenyl)-2-[(3-pyrrolidin-1-ylmethyl-phenylamino)-methy l]-3H-quinazolin-4-one;6-chloro-3-(2-chloro-phenyl)-2-[(3-diethylaminomethyl-phenylamino)-methyl]- 3H-quinazolin-4-one;6-chloro-3-(2-chloro-pyrid-3-yl)-2-[(3-diethylaminomethyl-phenylamino)-meth yl]-3H-quinazolin-4-one;6-chloro-3-(2-trifluoromethyl-phenyl)-2-[(3-diethylaminomethyl-phenylamino) -methyl]-3H-quinazolin-4 -one;2-{[3-(2-chloro-pyridin-3-yl)-4-oxo-3,4-dihydro-quinazolin-2-ylmethyl]-amin o}-benzonitrile;2-{[3-(2-methyl-pyridin-3-yl)-4-oxo-3,4-dihydro-quinazolin-2-ylmethyl]-amin o}-benzonitrile;2-{[6-fluoro-3-(2-methyl-phenyl)-4-oxo-3,4-dihydro-quinazolin-2-ylmethyl]-a mino}-nicotinonitrile;2-{[3-(2-chloro-phenyl)-4-oxo-3,4-dihydro-quinazolin-2-ylmethyl]-amino}-nic otinonitrile;2-{[3-(2-chloro-pyridin-3-yl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-ylmet hyl]-amino}-benzonitrile;3-{[3-(2-chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-ylmethyl]-a mino}-benzonitrile;3-(2-chloro-phenyl)-2-[(3-diethylaminomethyl-phenylamino)-methyl]-6-fluoro- 3H-quinazolin-4-one;3-(2-chloro-phenyl)-6-fluoro-2-(pyrimidin-2-ylaminomethyl)-3H-quinazolin-4- one;3-(2-chloro-pyridin-3-yl)-6-fluoro-2-(m-tolylamino-methyl)-3H-quinazolin-4- one;3-(2-chloro-pyridin-3-yl)-6-fluoro-2-[(6-methyl-pyridin-2-ylamino)-methyl]- 3H-quinazolin-4-one;3-(2-chloro-phenyl)-6-fluoro-2-(pyridin-2-ylaminomethyl)-3H-quinazolin-4-on e;3-(2-chloro-pyridin-3-yl)-6-fluoro-2-[(3-pyrrolidin-1-ylmethyl-phenylamino) -methyl]-3H-quinazolin-4-one;6-fluoro-3-(2-methyl-pyridin-3-yl)-2-[(3-pyrrolidin-1-ylmethyl-phenylamino) -methyl]-3H-quinazolin-4-one;3-(2-chloro-phenyl)-6-fluoro-2-[(2-fluoro-benzylamino)-methyl]-3H-quinazoli n-4-one;N-(3-{[3-3-(2-chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-ylmeth yl]-amino}-phenyl)-acetamide;3-(2-chloro-phenyl)-6-fluoro-2-[(3-pyrrolidin-1-ylmethyl-phenylamino)-methy l]-3H-quinazolin-4-one;2-{[3-(2-chloro-phenyl)-6-fluoro-4-oxo-3,4-dihydro-quinazolin-2-ylmethyl]-a mino}-nicotinonitrile;3-(2-chloro-pyridin-3-yl)-6-fluoro-2-[(2-fluoro-phenylamino)-methyl]-3H-qui nazolin-4-one;3-(2-chloro-phenyl)-6-fluoro-2-[(2-fluoro-phenylamino)-methyl]-3H-quinazoli n-4-one;3-(2-chloro-phenyl)-6-fluoro-2-[(6-methyl-pyridin-2-ylamino)-methyl]-3H-qui nazolin-4-one; and,(F) an atropisomer of the formula ##STR8## wherein either V, X, Y and Z are all carbon or one of them is nitrogen and the others are carbon;each of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 is selected, independently, from hydrogen, halogen, (C.sub.1 -C.sub.6)alkyl, trifluoromethyl, cyano, (C.sub.1 -C.sub.6)alkosy, (C.sub.1 -C.sub.6)alkylthio and C(.dbd.O)--)--(C.sub.1 -C.sub.6)alkyl, with the proviso that: (a) R.sup.1 can not be the same as R.sup.5, when each of V, X, and Z is carbon; (b) at least one of R.sup.1 and R.sup.5 must be other than hydrogen; and (c) when V, X, Y or Z is nitrogen, then R.sup.5, R.sup.4, R.sup.3 or R.sup.2 respectively, is absent;ring A is a fused heteroaromatic ring, wherein said heteroaromatic ring is a 5 or 6 membered heteroaromatic ring, wherein said 6 membered heteroaromatic ring, taken together with the carbon atoms common to both rings of the bicyclic system, has the formula ##STR9## and wherein said 5 membered heteroaromatic ring, taken together with the carbon atoms common to both rings of the bicyclic system, has the formula ##STR10## wherein said ring positions ""A"", ""B"", ""D"" and ""E"" may be independently selected from carbon or nitrogen;wherein said ring positions ""F"", ""G"" and ""J"" may be independently selected from carbon, nitrogen, oxygen or sulfur, with the proviso that: (a) if more than two of ""F"", ""G"" or ""J"" is a heteroatom then said 5 membered heteroaromatic ring isselected from the group consisting of (1,2,3)-triazole, (1,2,3)-thiadiazole, (1,2,5)-thiadiazole, and (1,2,5-oxadiazole; and (b) if two of ""F"", ""G"" or ""J"" are heteroatoms, only one of said heteroatoms may be oxygen or sulfur;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, (C.sub.1 -C.sub.6)alkyl--CO--O--, hydroxy, --NO.sub.2, R.sup.15 --C(.dbd.O)--, R.sup.15 --O--C(.dbd.O)--, di(C.sub.1 -C.sub.6)alkyl--N--C(.dbd.O)--, (C.sub.3 -C.sub.7)cycloalkyl, and R.sup.15 --NH--C(.dbd.O)--, and phenyl optionally substituted with halo, C.sub.1 -C.sub.6)alkyl, --CN, or --CF.sub.3 ;R.sup.6 is phenyl of the formual Ph.sup.1 or a five or six membered heterocycle, wherein said 6-membered heterocycle has the formula ##STR11## wherein ""N"" is nitrogen; wherein said ring positions ""K"", ""L"" and ""M"" may be independently selcted 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 formual ##STR12## 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"" ""T"" can be oxygen or sulfur and at least on of ""P"", ""Q"" or ""T"" must be a heteroatom;wherein said Ph.sup.1 is a group of the formula ##STR13## wherein each R.sup.15 is, independently, hydrogen or (C.sub.1 -C.sub.6)alkyl;each of R.sup.9, R.sup.10 and R.sup.11 is selected, independently, from 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)alkyl optionally one to three halogen atoms, (C.sub.1 -C.sub.6)alkylthiol, R.sup.16 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.3 -C.sub.7)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--NH--(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.3 -C.sub.7)cycloalkyl--NH--(C.dbd.O)--(CH.sub.2).sub.p --, R.sup.16 O--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl--(O.dbd.O)--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.)--NH--(CH.sub.2).sub.p --, H(O.dbd.C)--NH--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl--(O.dbd.C)--N--[(C.sub.1 -C.sub.6)alkyl](CH.sub.2).sub.p --, H(O.dbd.C)--N--[(C.sub.1 -C.sub.6)alkyl](CH.sub.2).sub.p --, 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.15 --(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 cyano;each of R.sup.7, R.sup.12 and R.sup.13 is selected, independently, from hydrogen, (C.sub.1 -C.sub.6)alkyl optionally substituted with one to threee halogen atoms, halogen, 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.16 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.3 -C.sub.7)cycloalkyl--NH--(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.3 -C.sub.7)cycloalkyl--NH--(C.dbd.O)--CH.sub.2).sub.p --, R.sup.16 O--(C.dbd.O)--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl--(O.dbd.O)--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.)--NH--(CH.sub.2).sub.p --, H(O.dbd.C)--NH--(CH.sub.2).sub.p --, (C.sub.1 -C.sub.6)alkyl--(O.dbd.C)--N--[(C.sub.1 -C.sub.6)alkyl](CH.sub.2).sub.p --, H(O.dbd.C)--N--[(C.sub.1 -C.sub.6)alkyl](CH.sub.2).sub.p --, 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.15 --(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 cyano;each R.sup.14 is, independently, hydrogen or halogen;each R.sup.16 is, independently, 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)--;each is hydrogen, cyano, (C.sub.1 -C.sub.6)alkyl, halogen, trifluoromethyl, --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; andwherein the dashed bond represented an optiona double bond;with the proviso that when R.sup.11 is hydrogen, one of R.sup.13 and R.sup.14 is other than hydrogen.