Claims
- 1. A trans-(.+-.)-racemate containing trans-(-) and trans-(+) enantiomers of the formulas ##STR14## wherein R is C.sub.1-3 straight-chain alkyl or allyl and R.sup.1 is H, C.sub.1-3 alkyl, O--C.sub.1-3 alkyl, NH.sub.2, NHC.sub.1-3 alkyl, N(C.sub.1-3 alkyl).sub.2, 1-pyrrolidinyl, 1-piperidinyl or NHCOC.sub.1-3 alkyl; and pharmaceutically-acceptable acid addition salts thereof.
- 2. A trans-(-)-4aR,8aR enantiomer or a salt thereof according to claim 1.
- 3. A racemate according to claim 1 in which R is n-propyl.
- 4. A 4aR,8aR-enantiomer according to claim 2 in which R is n-propyl.
- 5. A racemate according to claim 1 in which R is C.sub.1-3 straight-chain alkyl or allyl and R.sup.1 is NH.sub.2, C.sub.1-3 alkyl, NHC.sub.1-3 alkyl, N(C.sub.1-3 alkyl).sub.2, NHCOC.sub.1-3 alkyl, 1-pyrrolidinyl or H, or an acid addition salt thereof formed with a pharmaceutically-acceptable acid.
- 6. A 4aR,8aR enantiomer according to claim 2 in which R is C.sub.1-3 straight-chain alkyl or allyl and R.sup.1 is NH.sub.2, NHC.sub.1-3 alkyl, N(C.sub.1-3 alkyl).sub.2, NHCOC.sub.1-3 alkyl, 1-pyrrolidinyl, 1-piperidinyl, C.sub.1-3 alkyl, OH or H, or a pharmaceutically-acceptable acid addition salt thereof.
- 7. A racemate according to claim 5 in which R.sup.1 is NH.sub.2.
- 8. A 4aR,8aR enantiomer according to claim 6 in which R.sup.1 is NH.sub.2.
- 9. A hydrohalide salt of a racemate according to claim 1.
- 10. A hydrohalide salt of a 4aR,8aR enantiomer according to claim 2.
- 11. A racemate according to claim 1 in which R is H.
- 12. A 4aR,8aR enantiomer according to claim 2 in which R is H.
- 13. A racemate according to claim 1, said racemate being trans-(.+-.)-2-amino-5-n-propyl-4,4a,5,6,7,8,8a,9-octahydro-oxazolo[4,5-g]quinoline.
- 14. A racemate according to claim 1, said racemate being trans-(.+-.)-5-n-propyl-4,4a,5,6,7,8,8a,9-octahydro-oxazolo[4,5-g]quinoline.
- 15. A racemate according to claim 1, said racemate being trans-(.+-.)-2-methyl-5-n-propyl-4,4a,5,6,7,8,8a,9-octahydro-oxazolo[4,5-g]quinoline.
- 16. A dihydrohalide salt of the racemate of claim 13.
- 17. A method of inhibiting the secretion of prolactin in a mammal which consists of administering to a mammal having a physiologic condition characterized in part by elevated prolactin levels an amount of a racemic drug according to claim 6 effective to reduce prolactin secretion.
- 18. A method of treating hypertension in mammals which consist of administering to a hypertensive mammal a blood-pressure lowering dose of a racemate according to claim 5.
- 19. A method of treating depression in mammals which consists of administering to a mammal in a depressed state, a depression alleviating dose of a racemate according to claim 5.
- 20. A method of treating anxiety in mammals which consist of administering to an anxious mammal an anxiety relieving dose of a racemate according to claim 5.
- 21. A method for potentiating sexual behavior in mammals in need of such potentiation which comprises administering to said mammals an effective dose of a trans-(.+-.)-racemate of claim 5.
- 22. A method for treating sexual dysfunction in mammals suffering from such dysfunction and in need of treatment which comprises administering to said mammals an effective dose of a trans-(.+-.)-racemate of claim 5.
- 23. A method of restoring potency in impotent male mammals in need of treatment which comprises administering to such impotent male mammals a potency restoring dose of a trans-(.+-.)-racemate of claim 5.
- 24. A method of treating Parkinson's Syndrome consisting of administration to a mammal suffering from Parkinson's Syndrome and in need of treatment an effective dose of a 4aR,8aR enantiomeric drug according to claim 6.
- 25. A method of inhibiting the secretion of prolactin in a mammal which consists of administering to a mammal having a physiologic condition characterized in part by elevated prolactin levels, an amount of a 4aR,8aR enantiomeric drug according to claim 6 effective to reduce prolactin secretion.
- 26. A method of treating hypertension in mammals which consist of administering to a hypertensive mammal a blood-pressure lowering dose of a 4aR,8aR enantiomer according to claim 6.
- 27. A method of treating depression in mammals which consists of administering to a mammal in a depressed state, a depression alleviating dose of a 4aR,8aR enantiomer according to claim 6.
- 28. A method of treating anxiety in mammals which consist of administering to an anxious mammal an anxiety relieving dose of a 4aR,8aR enantiomer according to claim 6.
- 29. A method for potentiating sexual behavior in mammals in need of such potentiation which comprises administering to said mammals an effective dose of a 4aR,8aR enantiomer of claim 6.
- 30. A method for treating sexual dysfunction in mammals suffering from such dysfunction and in need of treatment which comprises administering to said mammals an effective dose of a 4aR,8aR enantiomer of claim 6.
- 31. A method of restoring potency in impotent male mammals in need of treatment which comprises administering to such impotent male mammals a potency restoring dose of a 4aR,8aR enantiomer of claim 6.
- 32. A pharmaceutical formulation in unit dosage form adapted for administration to counter depression, alleviate anxiety, reduce elevated blood pressure, lower excessively high prolactin levels, treat Parkinson's Syndrome, potentiate sexual behaviour, treat sexual dysfunction or restore sexual potency comprising per dosage unit, a standard pharmaceutical excipient plus an amount of a drug according to claim 5 to inhibit the secretion of prolactin, to relieve anxiety, to counter depression, to lower blood pressure of hypertensives, to treat Parkinson's Syndrome, to potentiate sexual behaviour, to treat sexual dysfunction or to restore sexual potency.
- 33. A pharmaceutical formulation in unit dosage form adapted for administration to counter depression, alleviate anxiety, reduce elevated blood pressure, lower excessively high prolactin levels, treat Parkinson's Syndrome, potentiate sexual behaviour, treat sexual dysfunction or restore sexual potency comprising per dosage unit, a standard pharmaceutical excipient plus an amount of a drug according to claim 6 to inhibit the secretion of prolactin, to relieve anxiety, to counter depression, to lower blood pressure of hypertensives to treat Parkinson's Syndrome, to potentiate sexual behaviour, to treat sexual dysfunction or to restore sexual potency.
- 34. A formulation according to claim 33 in which trans-(.+-.)-2-amino-5-n-propyl-4,4a, 5,6,7,8,8a,9-octahydro-oxazolo[4,5-g]quinoline or a pharmaceutically-acceptable acid addition salt thereof is the active D-2 agonist.
- 35. A racemate of the formula ##STR15## wherein R is C.sub.1-3 straight chain alkyl, allyl, benzyl or H, and acid addition salts thereof.
- 36. A 4aR,8aR enantiomer of the formula ##STR16## wherein R is C.sub.1-3 straight chain alkyl, allyl, benzyl or H, and acid addition salts thereof.
- 37. A trans-(.+-.)-racemate containing trans-(-) and trans-(+) enantiomers of the formulas ##STR17## wherein R is H or benzyl, and R.sup.1 is Cl, Br, or OH.
Parent Case Info
This application is a division of application Ser. No. 743,198, filed June 10, 1985, now U.S. Pat. No. 4,659,832, which is a continuation-in-part of application Ser. No. 637,232, filed Aug. 2, 1984, now abandoned.
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
4230861 |
Kornfeld et al. |
Oct 1980 |
|
Non-Patent Literature Citations (3)
Entry |
March, Advanced Organic Chemistry, 2nd Ed., 1977, pp. 381-383, 477-478, 1127, 658-659. |
Newkome and Puadler, Contemporary Heterocyclic Chemistry, (1982), pp. 37-38. |
Organic Reactions (Eds. Roger Adams et al.), vol. 10, p. 148. |
Divisions (1)
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Number |
Date |
Country |
Parent |
743198 |
Jun 1985 |
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Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
637232 |
Aug 1984 |
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