Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1992-01-13
1993-07-27
Waddell, Frederick E.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514816, A61K 31495, A61K 3150
Patent
active
052310965
ABSTRACT:
A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: ##STR1## ,pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R.sub.1 and R.sub.4 are independently selected from the group consisting of H and alkyl radicals having 1 to 4 carbon atoms; the R.sub.2 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the R.sub.3 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the 2-imidazolin-2-ylamino group may be in any of the 5-, 6, 7- or 8- positions of the quinoxaline nucleus; and R.sub.5, R.sub.6 and R.sub.7 each is located in one of the remaining 5-, 6-, 7- or 8- positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals having 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as reduction in peripheral pain, anesthetization of the central nervous system, constriction of one or more blood vessels, reduction in or prevention of at least one effect of ischemia, decongestion of one or more nasal passages, and reduction of at least one effect of an inflammatory disorder.
REFERENCES:
patent: 3890319 (1975-06-01), Danielewicz et al.
Fielding, "Clonidine: New Research in Psychotropic Drug Pharmacology", Medicinal Research Reviews, vol. 1, No. 1 pp. 97-123 (1981).
Isom et al, "a2-Adrenergic Receptors Accelerate Na/H Exchange in Neuroblastoma X Glioma Cells", The Journal of Biological Chemistry vol. 262, No. 14, Issue of May 15, 1987, pp. 6750-6757.
Pieter, et al, "Clonidine and Some Bridge Analogues; Cardiovascular Effects and Nuclear Magnetic Resonance Data (.sup.1 H/.sup.13)", Eur. J. Med. Chem, Jul.-Aug. 1980, vol. 4, pp. 323-329.
Gellai et al, "Renal Effects of Selective Alpha-1 and Alpha-2 Adrenoceptor Agonists in Conscious, Normotensive Rats", The Journal of Pharmacology, vol. 240, 1986.
Jarrot, "Clonidine and Related Compounds", Handbook of Hypertension, vol. 5, 1984.
Bloor et al, "Reduction in Halothane Anesthetic Requirement by Clonidine, an Alpha-Adrenergic Agonist", Anesthesia & Analgesia, vol. 61, No. 9, Sep. 1982 (741-745).
Zwieten et al, "Central & Periphera a-Adrenoceptors. Pharmacological Aspects & Clinical Potential", Advances in Drug Research vol. 13, 1984 (209-254).
Gellai et al, "Mechanism of a2-adrenoceptor agonist-induced diuresis" American Physiological Society 1988, F317-F323, vol. 24.
a2-Adrenergic Agonists: A Newer Class of Antidiarrheal Drug Gastroenterology 1986, vol. 91, pp. 769-775.
Mittag, "Ocular Effects of Selective Alpha-Adrenergic Agents: A New Drug Paradox?", Annals of Ophthalmology Mar. 1983.
Jumblatt et al, "Alpha-2 Adrenergic Modulation of Norepinephrine Secretion in the Perfused Rabbit Iris-Ciliary Body", Current Eye Research, 1987, vol. 6, pp. 767-777.
Burke et al, "Ocular Effects of a Relatively Selective a2 Agonist (UK-14,304-18) in cats, rabbits, and monkeys", Current Eye Research, 1986, vol. 5, pp. 665-676.
Fondacaro et al, "Selective Alpha-2 Adrenoceptor Agonists Alter Fluid and Electrolyte Transport in Mammalian Small Intestine American Society for Pharmacology", vol. 247, 1987.
Langer et al, "Pharmacologic and Therapeutic Significance of a-Adrenoceptor Subtypes", Journal of Cardiovascular Pharmacology, vol. 7, Supp.8 (S1-S8) (1985).
Nielsen et al, "Postjunctional a.sub.2 ]adrenoceptors mediate vasoconstrictio in human subcutaneous resistance vessels", Br. J. Pharmacol (1989), 97, (829-834).
B. Bloor, "Clonidine and Other Alpha.sub.2 Adrenergic Agonists: An Important New Drug Class for the Perioperative Period", Seminars in Anesthesia, vol. VII, No. 3 (Sep.), 1988: (pp. 170-177).
Sato et al, "Adrenergic Excitation of Cutaneous Pain Receptors Induced by Peripheral Nerve Injury", Science, vol. 251, (Mar.), 1991), (pp. 1608-1610).
Bendele, et al, "Anti-Inflammatory Activity of Pergolide in Rats", Pharmacol (Aug.) 1991, (p. 152), 82.
Scrip Product Information, Scrip No. 1466 Nov. 22, 1989 (p. 28).
Hieble, et al, "A Potent Peripherally Acting, A.sub.2 Adrenoceptor Agonist", The Pharmologist (1991), vol. 33, #3 (p. 214).
The Pharmacological Basis of Therapeutics, Gilman & Goodmen, 1985, "Therapeutic Uses of Sympathomimetic Drugs", (pp. 174-179), 7th Edition, Chapter 8.
Burke James A.
Garst Michael E.
Gluchowski Charles
Wheeler Larry A.
Allergan Inc.
Jordan Kimberly R.
Uxa, Jr. Frank J.
Waddell Frederick E.
LandOfFree
Methods for using (2-imidazolin-2-ylamino) quinoxaline derivativ does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Methods for using (2-imidazolin-2-ylamino) quinoxaline derivativ, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Methods for using (2-imidazolin-2-ylamino) quinoxaline derivativ will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2342417