N6 -substituted adenosines for treating pain

Claim 1

A method for treating pain in a mammal suffering therefrom, which comprises administering to such mammal an analgesic effective amount of a compound of the formula ##STR6## or a pharmaceutically acceptable addition salt thereof, wherein R 1 is hydrogen or lower alkyl; Ar and Ar 1 are each independently phenyl, phenyl substituted by halogen, hydroxy, thiol, lower alkoxy, lower thioalkoxy, lower alkanoyloxy, lower alkyl, nitro, amino, lower S(O) n -alkyl in which n is zero, one, or two, sulfonamide or trifluoromethyl, or 2-, 3-, or 4-pyridyl, 2- or 3-thienyl or -furanyl; A is straight or branched alkylene of one to eight carbon atoms which may be interrupted by oxygen, sulfur, or NH between two and seven carbons of the alkylene chain; X is hydrogen, hydroxy, lower alkyl, lower carboalkoxy, or lower alkanoyloxy; Y is hydrogen, halogen, --NR 2 R 3 , --OR 2 or --SR 2 in which R 2 and R 3 are independently hydrogen, lower alkyl or phenyl lower alkyl; Z is hydrogen or halogen; R 2 ', R 3 ', and R 5 ' are each independently hydrogen, alkanoyl having two to twelve carbon atoms in a straight or branched alkyl chain which may be substituted by amino, benzoyl or benzoyl substituted by lower alkyl, lower alkoxy, halogen, or trifluoromethyl; R 2 ' and R 3 ' may be linked together to form a five-membered alkylidene ring having a total of up to twenty carbons, and with the proviso R 5 ' may also be phosphate, hydrogen phosphate, dihydrogen phosphate, an alkali or dialkali metal phosphate, or ammonium or diammonium phosphate.

Claim 2

A method for treating pain in a mammal suffering therefrom, which comprises administering to such mammal an analgesic effective amount of a compound of the formula ##STR6## or a pharmaceutically acceptable addition salt thereof, wherein R 1 is hydrogen or lower alkyl; Ar and Ar 1 are each independently phenyl, phenyl substituted by halogen, hydroxy, thiol, lower alkoxy, lower thioalkoxy, lower alkanoyloxy, lower alkyl, nitro, amino, lower S(O) n -alkyl in which n is zero, one, or two, sulfonamide or trifluoromethyl, or 2-, 3-, or 4-pyridyl, 2- or 3-thienyl or -furanyl; A is straight or branched alkylene of one to eight carbon atoms which may be interrupted by oxygen, sulfur, or NH between two and seven carbons of the alkylene chain; X is hydrogen, hydroxy, lower alkyl, lower carboalkoxy, or lower alkanoyloxy; Y is hydrogen, halogen, --NR 2 R 3 , --OR 2 or --SR 2 in which R 2 and R 3 are independently hydrogen, lower alkyl or phenyl lower alkyl; Z is hydrogen or halogen; R 2 ', R 3 ', and R 5 ' are each independently hydrogen, alkanoyl having two to twelve carbon atoms in a straight or branched alkyl chain which may be substituted by amino, benzoyl or benzoyl substituted by lower alkyl, lower alkoxy, halogen, or trifluoromethyl; R 2 ' and R 3 ' may be linked together to form a five-membered alkylidene ring having a total of up to twenty carbons, and with the proviso R 5 ' may also be phosphate, hydrogen phosphate, dihydrogen phosphate, an alkali or dialkali metal phosphate, or ammonium or diammonium phosphate.