摘要:
Compounds of the following formula are described: in which n is 0, 1 or 2, R 1 is C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkylthio, C 1-4 alkylsulphonyl, trifluoromethyl, halo or nitro, and R 2 and R 3 are each independently hydrogen or C 1-4 alkyl, and salts thereof. The compounds are useful in the treatment of immediate hypersensitivity conditions and are prepared by reaction of the appropriate formylquinolone with malonic acid, ylid or phosphonate.
摘要:
Compounds of formula wherein R,, R 2 and R 3 are each independently selected from H, OH, C 1 -C 4 alkyl, R 4 -CO and halogen, where R. is C 1 -C 4 alkyl; R 5 and R. are each independently selected from H, C 1 -C 4 alkyl and optionally-substituted phenyl; R 7 is an alkylene group having from 1 to 4 carbon atoms, optionally containing a substituted or unsubstituted phenyl group; p or 0 or 1; and Z is a 1H-tetrazol-5-yl or a -CN group; and salts thereof, may be prepared by reacting a compound of formula. with a compound of formula wherein R 1 -R 7 are as defined in claim 1, in an organic solvent at a temperature in the range of 40-120°C in the presence of a base, and reacting the resulting compound with an alkali metal cyanide orthiocyanate, and optionally reacting the resulting compound with a source of azide ions to produce pharmacologically active compounds of formula I wherein Z is 1H-tetrazol-5-yl.
摘要:
There are described compounds of the formula in which R 1 is hydrogen or C 1-6 alkyl, R 2 is hydrogen, C 1-6 alkyl or C 3-6 alkenyl, X and Y are each oxygen, sulphur, sulphinyl or sulphonyl, n is 2 to 6 and Z ist IH-tetrazol-5-yl, 1H-tetrazol-5-ylthio, 1H-tetrazol-5-ylsulphinyl, 1H-tetrazol-5-yl- sulphonyl, cyano or thiocyano, provided that when both X and Y are oxygen Z is 1H-tetrazol-5-ylthio, 1H-tetrazol-5-yl- sulphinyl, 1H-tetrazol-5-ylsulphonyl or thiocyano; and salts thereof. The compounds in which Z is other than cyano or thiocyano have pharmaceutical activity and inhibit leukotriene action or formation.
摘要:
There are described compounds of the formula in which R' is hydrogen or C 1-6 alkyl, R 2 is hydrogen, C 1-6 alkyl or C 3-6 alkenyl, R 3 is hydrogen or C 1-6 alkyl, R 4 is hydrogen or an N-protecting group, n is 2, 3, 4 or 5, and X is oxygen, sulphur or -CH 2 -, provided that when X is -CH 2 - n is 0; and salts thereof. The compounds in which R 4 is hydrogen have pharmaceutical activity.
摘要:
@ There is described compounds of the formula in which R 1 is hydrogen or C 1-6 alkyl, R 2 is hydrogen, C 1-6 alkyl or C 3-6 alkenyl, and X is -CH = CH- or -(CH 2 ) n - where n is 1 to 3, and Y is -CN or and salts thereof. The compounds in which Y is tetrazolyl possess pharmaceutical activity.
摘要:
Hydantoin compounds are described, having the following formula wherein Ar is phenyl optionally substituted by up to three radicals selected
from the group comprising C 1-6 alkoxy, halogen, 1,3-dioxol-2-yl, hydroxy C 1-4 alkoxy C 1-4 alkyl, phenyl, hydroxyl, nitrile, C 1-4 haloalkyl, C 1-4 alkyl, C 2-4 alkenyloxy, C 1-4 alkoxycarbonyl or phenoxy optionally substituted by C 1-4 haloalkyl, C 1-4 alkoxy or halogen; or is thiophene optionally substituted by phenyl or by one or two C 1-4 alkyl groups; R' and R 2 are independently hydrogen or taken together represent a chemical bond; R 3 is hydrogen, C 1-6 alkyl or C 2-4 alkenyl; and R 4 is C 1-6 alkyl, C 2-4 alkenyl, phenyl or benzyl; provided that R 3 cannot be hydrogen when Ar is unsubstituted phenyl and R 4 is n-butyl.
The compounds are useful in the prophylactic treatment of asthma in mammals.