Claims
- 1. A pharmaceutical composition containing as one of plural components and as sole essential active ingredient, a cerebral-blood-flow-increasing amount of a compound of the formula ##STR3## wherein R.sub.1 is a member selected from the group consisting of .omega.-hydroxyalkyl having from 5 to 8 carbon atoms and in which the hydroxyl is separated from the xanthine nucleus by at least two carbon atoms, unbranched (.omega.-1)-hydroxyalkyl having 5 to 8 carbon atoms, branched (.omega.-1)-hydroxyalkyl having from 5 to 8 carbon atoms and in which the hydroxyl is separated from the xanthine nucleus by at least two carbon atoms, methyl and --H;
- R.sub.2 is a member selected from the group consisting of .omega.-hydroxyalkyl having from 5 to 8 carbon atoms and in which the hydroxyl is separated from the xanthine nucleus by at least two carbon atoms, unbranched (.omega.-1)-hydroxyalkyl having from 5 to 8 carbon atoms, branched (.omega.-1)-hydroxyalkyl having from 5 to 8 carbon atoms and in which the hydroxyl is separated from the xanthine nucleus by at least two carbon atoms, and methyl; and
- R.sub.3 is a member selected from the group consisting of unbranched .omega. or (.omega.-1)-hydroxyalkyl having from 5 to 8 carbon atoms, branched (.omega.-1)-hydroxyalkyl having from 5 to 8 carbon atoms and in which the hydroxyl is separated from the xanthine nucleus by at least two carbon atoms, methyl and --H;
- one and only one of R.sub.1, R.sub.2 and R.sub.3 being .omega.- or (.omega.-1)-hydroxyalkyl.
- 2. A pharmaceutical composition as claimed in claim 1 wherein one of the groups R.sub.1, R.sub.2 and R.sub.3 is a hydroxyalkyl group having from 5 to 8 carbon atoms in which the carbon atom to which the hydroxy group is bound is separated from the xanthine nucleus by at least 2 carbon atoms, and each other of said groups is methyl.
- 3. A pharmaceutical composition as claimed in claim 1 wherein either R.sub.1 or R.sub.3 is a hydroxyalkyl group having from 5 to 8 carbon atoms and wherein R.sub.2 and the other one of R.sub.1 and R.sub.3 is methyl.
- 4. A pharmaceutical composition as claimed in claim 1 wherein the hydroxyl of the hydroxyalkyl group is in the .omega.- or (.omega.-1)-position.
- 5. A pharmaceutical composition as claimed in claim 1 wherein the hydroxyl group of the hydroxyalkyl is in the (.omega.-1)-position and the hydroxyalkyl group is unbranched.
- 6. A pharmaceutical composition as claimed in claim 1 wherein the compound is 1-(5-hydroxylhexyl)-3,7-dimethylxanthine.
- 7. A pharmaceutical composition as claimed in claim 1 in dosage unit form containing up to 1000 mg of the compound.
- 8. A composition according to claim 1 containing (a) carrier, diluent or excipient and (b) the essential ingredient in an essentially non-toxic concentration which is effective for increasing cerebral blood flow of a subject to which the composition is administered.
- 9. A pharmaceutically-acceptable composition according to claim 1 containing
- (a) a pharmaceutically-acceptable diluent for active ingredient in the composition and
- (b) a sufficient concentration of active ingredient to counteract insufficiency of cerebral blood circulation in a host to which the composition is administered; the essential active ingredient of the composition being a compound of the formula ##STR4## wherein one of R.sub.1 and R.sub.3 is unbranched (.omega.-1)-monohydroxyalkyl having from 5 to 8 carbon atoms and the other is methyl.
- 10. A pharmaceutically-acceptable composition as claimed in claim 9 wherein the compound is 1-(5-hydroxyhexyl)-3,7-dimethylxanthin.
- 11. A pharmaceutically-acceptable composition according to claim 9 in the form of an injectable solution of the essential active ingredient in sterile water.
- 12. A sterile aqueous pharmaceutically-acceptable composition according to claim 9 in dosage unit form containing
- (a) a pharmaceutically-acceptable diluent for active ingredient in the composition and
- (b) from 10 to 1000 milligrams of the essential active ingredient.
- 13. A solid pharmaceutically-acceptable composition according to claim 9 in dosage unit form containing
- (a) a pharmaceutically-acceptable diluent for active ingredient in the composition and
- (b) from 10 to 1000 milligrams of the essential active ingredient.
- 14. A sterile aqueous composition according to claim 9.
- 15. A solid composition according to claim 9.
- 16. A sterile aqueous composition according to claim 10.
- 17. A solid composition according to claim 10.
- 18. A composition according to claim 1 wherein R.sub.3 is .omega.-hydroxyhexyl.
- 19. A pharmaceutical composition as claimed in claim 8 wherein one of the groups R.sub.1, R.sub.2 and R.sub.3 is a hydroxyalkyl group having from 5 to 8 carbon atoms in which the carbon atom to which the hydroxy group is bound is separated from the xanthine nucleus by at least 2 carbon atoms and each other of said groups is methyl.
- 20. A non-toxic pharmaceutical composition comprising active component in addition to carrier, diluent or excipient and characterized by the active component which consists essentially of a cerebral-blood-flow-increasing amount of a compound of the formula ##STR5## wherein R.sub.1 is a member selected from the group consisting of .omega.-hydroxyalkyl having from 5 to 8 carbon atoms and in which the hydroxyl is separated from the xanthine nucleus by at least two carbon atoms, unbranched (.omega.-1)-hydroxyalkyl having 5, 7 or 8 carbon atoms, branched (.omega.-1)-hydroxyalkyl having from 5 to 8 carbon atoms and in which the hydroxyl is separated from the xanthine nucleus by at least two carbon atoms, methyl and --H;
- R.sub.2 is a member selected from the group consisting of .omega.-hydroxyalkyl having from 5 to 8 carbon atoms and in which the hydroxyl is separated from the xanthine nucleus by at least two carbon atoms unbranched (107 -1)-hydoxyalkyl having from 5 to 8 carbon atoms, branched (.omega.-1)-hydroxyalkyl having from 5 to 8 carbon atoms and in which the hydroxyl is separated from the xanthine nucleus by at least two carbon atoms, and methyl; and
- R.sub.3 is a member selected from the group consisting of .omega.-hydroxyhexyl, unbranched (.omega.-1)-hydroxyalkyl having from 5 to 8 carbon atoms, branched (.omega.-1)-hydroxyalkyl having from 5 to 8 carbon atoms and in which the hydroxy is separated from the xanthine nucleus by at least two carbon atoms, methyl and --H;
- one and only one of R.sub.1, R.sub.2 and R.sub.3 being .omega.- or (.omega.-1)-hydroxyalkyl.
Priority Claims (3)
Number |
Date |
Country |
Kind |
1810705 |
Feb 1972 |
DEX |
|
2207860 |
Feb 1972 |
DEX |
|
2335170 |
Jul 1973 |
DEX |
|
Parent Case Info
This application is a continuation of application Ser. No. 774,648, filed Mar. 4, 1977 now abandoned, which is a continuation-in-part application of U.S. application Ser. No. 485,870, filed July 5, 1974 now abandoned, which again is a continuation-in-part application of U.S. application Ser. No. 330,653, filed Feb. 8, 1973 now abandoned.
US Referenced Citations (4)
Number |
Name |
Date |
Kind |
2953493 |
Schroeder et al. |
Sep 1960 |
|
3632742 |
Eckert et al. |
Jan 1972 |
|
3864469 |
Reiser et al. |
Feb 1975 |
|
4515795 |
Hinze et al. |
May 1985 |
|
Non-Patent Literature Citations (2)
Entry |
Archiv. der Pharmazie, vol. 299, (1966), pp. 448-456. |
Dissertationes Pharmaceuticae et Pharmacological, vol. XX, pp. 497-505, (1968). |
Continuations (1)
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Number |
Date |
Country |
Parent |
774648 |
Mar 1977 |
|
Continuation in Parts (2)
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Number |
Date |
Country |
Parent |
485870 |
Jul 1974 |
|
Parent |
330653 |
Feb 1973 |
|