Claims for Patent: 4,576,947

Summary for Patent: 4,576,947

Title:	Pharmaceutical compositions
Abstract:	A pharmaceutical composition containing as an essential ingredient a compound of the formula ##STR1## wherein one of the groups R.sub.1, R.sub.2 and R.sub.3 is an .omega.- or (.omega.-1)-hydroxyalkyl group having from 5 to 8 carbon atoms in which the hydroxy group is separated from the xanthine nucleus by at least 2 carbon atoms, radicals R.sub.1 and R.sub.3 which are no hydroxylalkyl group, are hydrogen or methyl and equal or different, and R.sub.2 is said hydroxyalkyl group or methyl, a compound of formula (I) and a pharmaceutical product for treatment of diseases involving insufficiency of cerebral blood flow.
Inventor(s):	Hinze; Heinz-Joachim (Auringen, DE), Soder; Alfons (Frankfurt-Schwanheim, DE), Popendiker; Kurt (Wiesbaden, DE)
Assignee:	Hoechst Aktiengesellschaft (Frankfurt, DE)
Application Number:	06/543,114
Patent 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.

Details for Patent 4,576,947

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Merck Sharp & Dohme Corp.	ZOSTAVAX	zoster vaccine live	For Injection	125123	05/25/2006		2003-03-18