Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-11-21
1998-11-10
Jordan, Kimberly
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
A61K 3144
Patent
active
058344969
ABSTRACT:
Methods and compositions are disclosed utilizing the optically pure S(-) isomer of felodipine. This compound is a potent drug for the treatment of hypertension while avoiding the concomitant liability of adverse effects associated with the racemic mixture of felodipine. The S(-) isomer of felodipine is also useful for the treatment of angina and such other conditions as may be related to the activity of S(-) felodipine as a calcium channel antagonist such as cerebral ischemia, cerebral disorders, arrhythmias, cardiac hypertrophy, coronary vasospasm, myocardial infarction, renal impairment and acute renal failure, without the concomitant liability of adverse effects associated with the administration of the racemic mixture of felodipine.
REFERENCES:
patent: 4264611 (1981-04-01), Berntsson et al.
patent: 4803081 (1989-02-01), Falk et al.
patent: 4849433 (1989-07-01), Wehinger et al.
patent: 4918076 (1990-04-01), Opitz et al.
patent: 4942040 (1990-07-01), Ragnarsson et al.
patent: 4992445 (1991-02-01), Lawter et al.
patent: 5015479 (1991-05-01), Mulligan et al.
Ariens, 1991, "Racemic Therapeutics--ethical and regulatory aspects", Eur J Clin Pharmacol 41:89-93.
Yedinak and Lopez, 1991, "Felodipine: A new dihydropyridine calcium-channel antagonist", DIPC 25:1193-1206.
Ariens, 1990, "Stereoselectivity in pharmacodynamics and pharmacokinetics", Schweiz Med Wschr 120(5):131-134.
Cerasola et al., 1990, "Reversal of cardiac hypertrophy and left ventricular function with the calcium antagonist felodipine in hypertensive patients", J Hum Hypertens 4:703-708.
Ardissino et al., 1989, "Effect of felodipine on hyperventilation-induced ischemic attacks in variant angina pectoris", Am J Cardiol 63(1):104-107.
Colucci et al., 1987, "Usefulness of calcium antagonists for congestive heart failure", Am J Cardiol 59(3):52B-58B.
Been et al., 1985, "Electrophysiological effects of felodipine", Drugs 29(Suppl 2):76-80.
Day et al., 1987, "Clinical Pharmacology of Non-Steroidal Anti-Inflammatory Drugs", Pharmac. Ther. 33:383-433.
Blychert, E et al., "A population study of the pharmacokinetics of felodipine", Br. J. Clin. Pharmac. 31:15-24 (1991).
Eriksson, U.G. et al., "Pharmacokinetics of the enantiomers of felodipine in the dog after oral and intravenous administration of a pseudoracemic mixture", Xenobiotica 21(1): 75-84 (1991).
Eriksson, U.G. et al., "Stereoselective Metabolism of Felodipine in Liver Microsomes from Rat, Dog, and Human", Drug Metabolism and Disposition 19(5): 889-894 (1991).
Goldmann, S. and Stoltefuss, J., "1,4-Dihydropyridines: Effects of Chirality and Conformation on the Calcium Antagonist and Calcium Agonist Activities", Angew. Chem. Int. Ed. Engl. 30: 1559-1578 (1991).
Eltze, M. et al., "Stereoselective Inhibition of Thromboxane-Induced Coronary Vasoconstriction by 1,4-Dihydropyridine Calcium Channel Antagonists", Chirality 2: 233-240 (1990).
Soons, P.A. et al., "Enantioselective Determination of Felodipine and Other Chiral Dihydropyridine Calcium Entry Blockers in Human Plasma", Journal of Chromotography 528: 343-356 (1990).
Soons, P.A. et al., "Stereoselective Kinetics of Felodipine and Nitrendipine in Man", Clin. Pharmacol. Ther. 158 Abstract No. PII-40 (1990).
Thulin, T., "Calcium Antagonists--Assessment of Side Effects", Scand. J. Prim. Health Care Suppl. 1: 81-84 (1990).
Lamm, B. and Simonsson, R., "Synthesis of the Enantiomers of Felodipine and Determination of Their Absolute Configuration", Tetrahedron Letters 30(46): 6423-6426 (1989).
Scripp's Product Report, "Felodipine--A review of the scientific literature on felodipine, a calcium channel blocker with antihypertensive properties", PJB Publications Ltd. (1989).
Jordan Kimberly
Sepracor Inc.
LandOfFree
Methods for treating hypertension using optically pure S(-) felo 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 treating hypertension using optically pure S(-) felo, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Methods for treating hypertension using optically pure S(-) felo will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1517170