Claims
- 1. A compound of the formula ##STR6## or a pharmaceutically acceptable addition salt thereof, wherein R.sub.1 is hydrogen or lower alkyl; Ar and Ar.sup.1 are each independently phenyl, phenyl substituted by halogen, hydroxy, thiol, lower alkoxy, lower thioalkoxy, lower alkanoyloxy, lower alkyl, nitro, amino, low S(O).sub.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.sub.2 R.sub.3, --OR.sub.2, or --SR, in which R.sub.2 and R.sub.3 are independently hydrogen, lower alkyl or phenyl lower alkyl; Z is hydrogen or halogen; R.sub.2 ' and R.sub.3 ' 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.sub.2 ' and R.sub.3 ' may be linked together to form a five-membered alkylidene ring having a total of up to 20 carbons, and R.sub.5 ' is hydrogen; alkanoyl having two to twelve carbons in a straight or branched alkyl chain which may be substituted by amino, benzoyl or benzoyl substituted by lower alkyl, lower alkoxy, halogen, or trifluromethyl; phosphate; hydrogen phosphate; dihydrogen phosphate; an alkali or dialkali or dialkali metal phosphate; with the overall proviso that A cannot be a branched alkylene of two to eight carbon atoms.
- 2. A compound as claimed in claim 1, wherein R.sup.1 and X are hydrogen or methyl; R.sub.2 ' and R.sub.3 ' are hydrogen, acetyl, benzoyl or when taken together form isopropylidene; R.sub.5 ' is hydrogen, phosphate, hydrogen phosphate, dihydrogen phosphate, sodium phosphate or disodium phosphate; Z is hydrogen or fluorine.
- 3. A compound as claimed in claim 2, wherein R.sub.1 ', R.sub.2 ',R.sub.3 ',R.sub.5 ', X, and Z are hydrogen.
- 4. A compound as claimed in claim 3, wherein Y is hydrogen, halogen or --NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 are independently hydrogen, lower alkyl or phenyl lower alkyl.
- 5. A compound as claimed in claim 4, wherein Y is hydrogen, chlorine or amino and A is straight of branched alkylene from 1 to 4 carbon atoms.
- 6. A compound as claimed in claim 5, wherein A is methylene, and Ar and Ar.sup.1 are phenyl.
- 7. A compound as claimed in claim 6 and being N.sup.6 -(2,2-diphenylethyl)adenosine.
- 8. A compound as claimed in claim 5 and being N.sup.6 -(3,3-diphenylpropyl)adenosine.
- 9. A compound as claimed in claim 6 and being N.sup.6 -(2,2-diphenylethyl)-2-chloroadenosine.
- 10. A compound as claimed in claim 6 and being N.sup.6 -(2,2-diphenylethyl)-2-aminoadenosine.
- 11. A compound as claimed in claim 5 and being N.sup.6 -(2,2-diphenylpropyl)adenosine.
- 12. A pharmaceutical composition comprising a therapeutically effective amount for antipsychotic activity of a compound as claimed in claim 1 and a pharmaceutically acceptable carrier.
- 13. A method for treating psychosis in a mammal suffering therefrom comprising administering an anti psychotic effective amount to such mammal a compound of the formula ##STR7## or a pharmaceutically acceptable addition salt thereof, wherein R.sub.1 is hydrogen or lower alkyl; Ar and Ar.sub.1 are each independently phenyl phenyl substituted by halogen, hydroxy thiol, lower alkoxy, lower thioalkoxy, lower alkanoyloxy, lower alkyl, nitro, amino, lower S(O).sub.n -alkyl in which n is zero, one, or two, sulfonamide or trifluromenthyl, 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 2R 3, --OR 2, or --SR 2 in which R.sub.2 and R.sub.3 are independently hydrogen, lower alkyl or phenyl lower alkyl; Z is hydrogen or halogen; R.sub.2 ' and R.sub.3 ' 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 trifluromethyl; R.sub.2 ' and R.sub.3 ' may be linked together to from a five-membered alkylidene ring having a total up to 20 carbons, and R.sub.5 ' is hydrogen, alkanoyl having two to twelve carbons in a straight or branched alkyl chain which may be substituted by amino, benzoyl or benzoyl substituted by lower alkyl; lower alkoxy, halogen, or trifluromethyl; phosphate; hydrogen phosphate; dihydrogen phosphate; an alkali or dialkali metal phosphate; ammonium or diammonium phosphate; with the overall proviso that A cannot be a branched alkylene of two to eight carbon atoms in unit dosage forms.
- 14. A pharmaceutical composition for treating psychosis comprising an antipsychotic effective amount of a compound as claimed in claim 1 in unit dosage form.
Parent Case Info
This is a continuation of application Serial No. 06/621,943 filed June 22, 1984, now abandoned, which is a CIP of Ser. No. 519,284 filed 8/1/83, now abandoned.
US Referenced Citations (4)
Foreign Referenced Citations (2)
Number |
Date |
Country |
0040325 |
Nov 1981 |
EPX |
2406587 |
Aug 1975 |
DEX |
Continuations (1)
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Number |
Date |
Country |
Parent |
621943 |
Jun 1984 |
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Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
519284 |
Aug 1983 |
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