Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-08-22
1996-10-15
Gupta, Yogendra N.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514146, 514231, 514312, 514347, 5142315, 514381, 514461, 514464, 514465, 514469, 514470, 514869, 544146, 546153, 546293, 548253, 548254, 549220, 549362, 549434, 549469, A61K 31335, A61K 31535, C07D31908, C07D26530
Patent
active
055654851
ABSTRACT:
Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.
REFERENCES:
Naim et al., Indian J. Chem. Vol. 19B, pp. 622-623 1980.
Crenshaw et al., J. Org. Chem. vol. 47, pp. 101-104 1982.
Michael E. Jung et al., Heterocycles, vol. 30(2) pp. 839-853, 1990.
Saraiva et al., CA114(19): 185076t, 1990.
"Antihypertensive Effects of the Endothelin Receptor Antagonist BQ-123 n Conscious Spontaneously Hypetensive Rats" E. H. Ohlstein, et al. Journal of Cardiovascular Pharmacology, vol. 22, (Suppl. 8), 1993, pp. S321-S324.
"Direct and Sympathetically Mediated Vasoconstriction in Essential Hypertension" W. G. Haynes, et al. J. Clin. Invest., vol. 94, Oct. 1994, pp. 1359-1364.
"Role of Endothelin in Hypertension" B. K. Kramer, et al. Clin. Investig., vol. 72, (1994), pp. 88-93.
"Potential Role of Endothelin in Hypertension" T. F. Luscher, et al. Hypertension, vol. 21, No. 6, Part 1, Jun. 1993, pp. 752-757.
"BQ123, An ET(A) Receptor Antagonist, Attenuates Hypoxic Pulmonary-Hypertension in Rats" Bonvallet, S. T., et al. American Journal of Physiology, vol. 266, No. 4, (Apr. 1994), pp. H1327-1331.
"Endothelin-A Receptor Antagonist Prevents Acute Hypoxia-Induced Pulmonary-Hypertension in the Rat" Oparil, S., et al. American Journal of Physiology-Lung Cellular and Molecular Physiology, vol. 12, No. 1, (Jan. 1995), pp. L95-L100.
"Protection from Pulmonary Hypertension with an Orally Active Endothelin Receptor Antagonist in Hypoxic Rats" American Journal of Physiology-Heart and Circulatory Physiology, vol. 37, No. 2, (Feb. 1995), pp. H828-H835.
"Endothelial Dysfunction and Remodeling of the Pulmonary Ciculation in Chronic Hypoxic Pulmonary-Hypertension" Dinhxuan, A. T., et al. ACP--Applied Cardiopulmonary Pathophysiology, vol. 5, No. 2, (1994), pp. 93-99.
"Cyclosporine-Induced Elevation in Circulating Endothelin-1 in Patients with Solid-Organ Transplants" Grieff, M., et al. Transplantation vol. 54, No. 4, (Oct. 1993), pp. 880-884.
"Cyclosporine-Induced Hypertension After Transplantation" Textor, S. C., et al. Mayo Clinical Proceedings, vol. 69, (1994), pp. 1182-1193.
"A Role of Endogenous Endothelin-1 in Neointimal Formation After Rat Carotid Artery Balloon Angioplasty" Douglas S. A., et al. Circulation Research, vol. 75, (1994), pp. 190-197.
"[125I]-Endothelin-1 Binding to Vasa Vasorum and Regions of Neovascularization in Human and Porcine-Blood Vessels: A Possible Role for Endothelin in Intimal Hyperplasia and Atheroscelerosis" Dashwood, M. R., et al. Journal of Cardiovascular Pharmacology, vol. 22, (Suppl. 8), (1993), pp. S343-347.
"The Endothelin-1 Receptor Antagonist BQ-123 Reduces Infarct Size in a Canine Model of Coronary Occlusion and Reperfusion" Grover, G. J., et al. Cardiovascular Research, vol. 75, No. 9, (Sep. 1993), pp. 1613-1618.
"The Effects of the Endothelin ETa Receptor Antagonist, FR139317, on Infarct Size in a Rabbit Model of Acute Myocardial Ischemia and Reperfusion" McMurdo, L., et al. British Journal of Pharmacology, (1994), vol. 112, pp. 75-80.
"Vasodilator Effects of the Endothelin-1 Receptor Antagonist Bosentan in Patients with Severe Chronic Heart Failure" Kiowski, W., et al. Journal Am. College of Cardiology, Feb. 1995, pp. 296A, abstract No. 779-1.
"Nonpeptide Endothelin Receptor Antagonists. III, Effect of SB 209670 and BQ123 on Acute Renal Failure in Anesthetized Dogs" Brooks, D. P., et al. Journal of Pharmacology and Experimental Therapeutics, vol. 271, (1994), pp. 769-775.
"Reversal of Postischemic Acute Renal Failure with a Selective Endothelin.sub.A Receptor Antagonist in the Rat" Gellai, M., et al. Journal of Clinical Investigator, vol. 93, (1994), pp. 900-906.
"Effects of BQ-123 on Renal-Function and Acute Cyclosporine Induced Renal Dysfunction", Kivlighn, S. D. et al., Kidney International, vol. 45, No. 1, (Jan. 1994), pp. 131-136.
"Endotoxin-Mediated Changes In Plasma Endothelin Concentrations, Renal Endothelin Receptor And Renal-Function", Nambi, P. et al., vol. 48, No. 3, (Mar. 1994), pp. 147-156.
"Effect of Total-Body Cold-Exposure on Plasma-Concentrations of Vonwillebrand-Factor, Endothelin-1 Thrombomodulin in Systemic Lupus-Erythematosus Patients with or without Raynauds-Phenomeon", Matsuda, J.,et al. Acta Haematologica, vol. 88, No. 4, (1992), pp. 189-193.
"Localization of Endothelin-1 and Its Binding-Sites in Scleroderma Skin" Vancheeswaran, R., et al. Journal of Rheumatology, vol. 21, No. 7, (Jul. 1994), pp. 1268-1276.
"Increased Endothelin-1 Production in Fibroblasts Derived from Patients with Systemic-Sclerosis" Kawaguchi, Y., et al. Annals of the Rheumatic Diseases, vol. 53, No. 8, (Aug. 1994), pp. 506-510.
"Characterization of Endothelin-Binding Sites in Human Skin and Their Regulation in Primary Raynauds-Phenomenon and Systemic-Sclerosis" Knock G. A., et al. Journal of Investigative Dermatology, vol. 101, No. 1, (Jul. 1993), pp. 73-78.
"Raynaud-Phenomenon" Coffman, J. D., et al. Current Opinion in Cardiology, vol. 8, No. 5, (Sep. 1993), pp. 821-828.
"Parameters of Vascular Function in Idiopathic and Silica-Induced Systemic-Sclerosis" Haustein, U. F., et al. Hautarzt, vol. 44, No. 11, (Nov. 1993), pp. 717-722.
"Circulating Endothelin-1 Levels in Systemic-Sclerosis Subsets--A Marker of Fibrosis or Vascular Dysfunction" Vancheeswaran, R., et al. Journal of Rheumatology, vol. 21, No. 10, (Oct. 1994), pp. 1838-1844.
"Endothelin and Collagen Vascular Disease: A Review with Special Reference to Raynauds-Phenomenon and Systemic-Sclerosis" Yamane, K. Internal Medicine, vol. 33, No. 10, (Oct. 1994), pp. 579-582.
"A Pathogenic Role for Endothelin in Raynauds-Phenomenon" Bottomley, W., et al. Acta Dermato-Venereologica, vol. 74, No. 6, (Nov. 1994), pp. 433-434.
"BQ 123, A Peptidic Endothelin ETA Receptor Antagonist, Prevents the Early Cerebral Vasospasm Following Subarachnoid Hemorrhage After Interacisternal but not Intravenous-Injection" Clozel, M., et al. Life Sciences, vol. 52, No. 9, (1993), pp. 825-834.
"An Endothelin ET(A) Receptor Antagonist, FR139317, Ameliorates Cerebral Vasospasm in Dogs" Nirei, H., et al. Life Sciences, vol. 52, No. 23, (1993), pp. 1869-1874.
"Reversal of Subarachnoid Hemorrhage-Induced Vasoconstriction with an Endothelin Receptor Antagonist" Foley, P. L. et al. Neurosurgery, vol. 34, No. 1, (Jan. 1994), pp. 108-113.
"Endothelin Levels Increase in Rat Focal and Global-Ischemia" Barone, F. C., et al. Journal of Cerebral Blood Flow and Metabolism, vol. 14, No. 2, (Mar. 1994), pp. 337-342.
"Endothelin ET(A) and ET(B) Receptors in Subarachnoid Hemorrhage-Induced Cerebral Vasospasm" Zuccarello, M., et al. European Journal of Pharmacology, vol. 259, No. 1, (Jun. 23 1994), pp. R1-R2.
"Changes of Endothelin Concentration in Cerebrospinal-Fluid and Plasma of Patients with Aneurysmal Subarachnoid Hemorrhage" Shirakami, G., et al. Acta Anaesthesiologica Scandinavica, vol. 38, No. 5, (Jul. 1994), pp. 457-461.
"Prevention of Delayed Vasospasm by an Endothelin ET(A) Receptor Antagonist, BQ-123--Change of ET(A) Receptor Messenger-RNA Expression in a Canine Subarachnoid Hemorrhage Model" Itoh, S., et al., Journal of Neurosurgery, vol. 81, No. 5, (Nov. 1994), pp. 759-764.
"Endothelin Concentrations in Patients with Aneurysmal Subarachnoid Hemorrhage--Correlation with Cerebral Vasospasm, Delayed Ischemic Neurological Deficits, and Volume of Hematoma" Seifert V., et al. Journal of Neurosurgery, vol. 82, No. 1, (Jan. 1995), pp. 55-62.
Bagley Scott W.
Broten Theodore P.
Chakravarty Prasun K.
Dhanoa Daljit S.
Fitch Kenneth J.
Camara Valerie J.
Daniel Mark R.
Gupta Yogendra N.
Merck & Co. , Inc.
LandOfFree
Biphenyl compounds useful or endothelin antagonists does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Biphenyl compounds useful or endothelin antagonists, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Biphenyl compounds useful or endothelin antagonists will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1246555