Patent ID: 6242446
Filing Date: 2001-06-05
Classification: A61K,Y10S

Abstract:
A method for the treatment or prophylaxis of attention deficit disorder in a patient in need thereof which comprises administering an effective amount of a neurokinin-1 receptor antagonist which is selected from the group consisting of:4-(3-(1,2,4-triazolo)methyl)-2(S)-(3,5-bis(trifluoromethyl)benzyloxy)-3(S)- phenyl-morpholine;4-(3-(1,2,4-triazolo)methyl)-2(S)-(3,5-bis(trifluoromethyl)benzyloxy)-3(R)- phenyl-morpholine;4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methyl)-2(S)-(3,5-bis(trifluoromethyl)benz yloxy)-3(S)-phenyl-morpholine; and2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluorophenyl) -4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methyl)morpholine;2-(R)-2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-4-(5-(dimethylam ino)methyl-1,2,3-triazol-4-yl)methyl-3-(S)-phenylmorpholine;(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-4-((dimethylaminomethyl)-1,2 ,3-triazol-4-yl)methyl)-3-(S)-(4-fluorophenyl)morpholine;2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)-pheny l-4-(3-(1-monophosphoryl-5-oxo-1H-1,2,4-triazolo)methyl)morpholine;2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluorophenyl) -4-(4-morpholinobut-2-yn-yl)morpholine;2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-4-(4-N,N-dimethylamino but-2-yn-yl)-3-(S)-(4-fluorophenyl)morpholine;4-(4-azetidinylbut-2-yn-yl)-2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)e thoxy)-3-(S)-(4-fluorophenyl)morpholine;2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluorophenyl) -4-(4-imidazolylbut-2-yn-yl)morpholine;2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluorophenyl) -4-(4-(N-methylpiperazinyl)but-2-yn-yl)morpholine;4-(4-bis(2-methoxyethyl)aminobut-2-yn-yl)-2-(R)-(1-(R)-(3,5-bis(trifluorome thyl)phenyl)ethoxy)-3-(S)-(4-fluorophenyl)morpholine;2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluorophenyl) -4-(4-pyrrolidinobut-2-yn-yl)morpholine;3-(S)-(4-fluorophenyl)-2-(R)-(1-(R)-(3-fluoro-5-(trifluoromethyl)-phenyl)et hoxy)-4-(4-morpholinobut-2-yn-yl)morpholine;3-(S)-(4-fluorophenyl)-4-(4-morpholinobut-2-yn-yl)-2-(R)-(1-(R)-(3-(trifluo romethyl)phenyl)ethoxy)morpholine;4-(4-azetidinylbut-2-yn-yl)-3-(S)-(4-fluorophenyl)-2-(R)-(1-(R)-(3-(trifluo romethyl)phenyl)ethoxy)morpholine;2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-4-(4-(N-(2-methoxyethy l)-N-methyl)aminobut-2-yn-yl)-3-(S)-phenylmorpholine;2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-4-(4-(N-cyclopropyl-N- (2-methoxyethyl)amino)but-2-yn-yl)-3-(S)-phenylmorpholine;2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-4-(4-(N-isopropyl-N-(2 -methoxyethyl)amino)but-2-yn-yl)-3-(S)-phenylmorpholine;4-(4-(N,N-dimethylamino)but-2-yn-yl)-3-(S)-(4-fluorophenyl)-2-(R)-C1-(S)-(3 -fluoro-5-(trifluoromethyl)phenyl-2-hydroxyethoxy)morpholine;4-(4-azetidinylbut-2yn-yl)-3-(S)-(4-fluorophenyl)-2-(R)-(1-(S)-(3-fluoro-5- (trifluoromethyl)phenyl)-2-hydroxyethoxy)morpholine;2-(R)-(1-(S)-(3,5-bis(trifluoromethyl)phenyl)-2-hydroxyethoxy)-4-(4-(N,N-di methylamino)but-2-yn-yl)-3-(S)-(4-fluorophenyl)morpholine;4-(4-azetidinylbut-2-yn-yl)-2-(R)-(1-(S)-(3,5-bis(trifluoromethyl)-phenyl-2 -hydroxyethoxy)-3-(S)-(4-fluorophenyl)morpholine;4-(4-N-bis(2-methoxy)ethyl-N-methylamino)but-2-yn-yl)-2-(R)-(1-(R)-(3,5-bis (trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluorophenyl)morpholine;2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluorophenyl) -4-(4-(2-(S)-(methoxymethyl)pyrrolidino)but-2-yn-yl)morpholine;4-(4-(7-azabicyclo[2.2. 1]heptano)but-2-yn-yl)-2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy )-3-(S)-(4-fluorophenyl)morpholine;2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-4-(4-diisopropylaminob ut-2-yn-yl)-3-(S)-(4-fluorophenyl)morpholine;2-(R)-(1-(R)-(3-fluoro-5-(trifluoromethyl)phenyl)ethoxy)-4-(4-(2-(S)-(metho xymethyl)pyrrolidino)but-2-yn-yl)-3-(S)-phenylmorpholine;2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluorophenyl) -4-(4-(2-(S)-(hydroxymethyl)pyrrolidino)but-2-yn-yl)morpholine;(2S,3S)-cis-3-(2-methoxybenzylamino)-2-phenylpiperidin;(3aS,4S,7aS)-7,7-diphenyl-4-(2-methoxphenyl)-2-[(2S)-(2-methoxyphenyl)propi onyl]perhydroisoindol-4-ol;(3S,5R,6S)-3-[2-cyclopropoxy-5-(trifluoromethoxy)phenyl]-6-phenyl-1-oxa-7-a za-spiro[4.5]decane;(3R,5R,6S)-3-[2-cyclopropoxy-5-(trifluoromethoxy)phenyl]-6-phenyl-1-oxa-7-a za-spiro[4.5]decane;(2R*,4S*)-2-benzyl-1-(3,5-dimethylbenzoyl)-N-(4-quinolinylmethyl)-4-piperid ineamine;2S,3S)-3-(2-methoxy-5-trifluoromethoxybenzyl)-amino-2-phenylpiperidine;[2-methoxy-5-(5-triflouromethyl-tetrazol-1-yl)-benzyl]-(2S-phenylpiperidin- 3S-yl)-amine;[5-(5-methyl-tetrazol-1-yl)-benzofuran-7-ylmethyl]-(2S-phenylpiperidin-3S-y l)-amine;or a pharmaceutically acceptable salt thereof.