Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-10-14
1999-04-06
Fan, Jane
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
5462704, A61K 3144, C07D41704
Patent
active
058918922
ABSTRACT:
Novel small molecular biaryl compounds as inhibitors of endothelin converting enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cerebral ischemia, cerebral infarction, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, stroke, benign prosthatic hyperplasia (BPH), and diabetes.
REFERENCES:
patent: 4594443 (1986-06-01), Bianchi et al.
patent: 4904675 (1990-02-01), Winter-Mihaly et al.
patent: 4968817 (1990-11-01), Brima
Stein et al., "The Discovery of Sulfonamide Endothelin Antagonists and the Development of the Orally Active ET.sub.A Antagonist 5-(Dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamide", J. Med. Chem., 1994, 37:3, 329-331.
Foley et al., "Reversal of Subarachnoid Hemorrhage-induced Vasoconstriction with an Endothelin Receptor Anatagonist", Neurosurgery, 1994, 34:1, 108-113.
Rio and Hardy, "Triphenyl-3,4,5 H-5 furannone-2, acide cis-benzoyl-3 diphenyl-2,3 acrylique et derives", Bulletin de la Societe Chimique de France, 1970, 10, 3572-3578.
Patwardhan and Bagawant, "Claisen-Stobbe Reaction of Phenylacetic Esters & Diketones", Indian Journal of Chemistry, 1973, 11:9, 1333-1334.
McEvoy and Allen, "6-(Substituted phenyl)-5-substituted-4,5-dihydro-3(2H)-pyridazinones. Antihypertensive Agents", J. Med. Chem., 1974, 17:3, 281-286.
Dikshit et al., "Synthesis and biological activity of 2,3- and 3,4-diarylfurans and 2,3,4-triaryl-2,5-dihydrofurans", Indian Journal of Chemistry, 1990, 29B, 954-960.
Krapf et al., "Thermische Umwandlung der labilen 1:1-Addukte aus Diphenylcyclopropenon bzw. Diphenylcyclopropenthion und Ketenacetalen", Chem. Ber., 1976, 109, 576-596.
Schmand et al., "Synthese eines 1,5-Naphthochinons; zur Struktur des Naphthazarins und zur Stabilitat von Chinonen", Liebigs Ann. Chem., 1976, 1560-1576.
Rohrscheidt and Fritz, "Zum Mechanismus der Aminabspaltung bei der Bildung von Pyrrolinonen aus N'-(1-Alkenyl)hydraziden and durch Brunnersche Oxindolsynthese", Liebigs Ann. Chem., 1878, 680-693.
Padwa et al., "Migratory Aptitude Studies in the Photochemical Rearrangement of 2(5H)-Furanones", J. Am. Chem. Soc., 1978, 100:26, 8247-8259.
Chelain et al., "Reaction of Aminocarbene Complexes of Chromium with Alkynes. 1. Formation and Rearrangement of Ketene and Nitrogen Ylide Complexes", J. Am. Chem. Soc., 1992, 114, 8088-8098.
Weinberg and Miller, "Decomposition of 5-Aryl-5-(tert-butylperoxy)-3,4-diphenyl-2(5H)-furanones", J. Org. Chem., 1979, 44:25, 4722-4725.
Daroca et al., "Reactivity of Pyrrole Pigments. Part 5: Electrophilic Substitution--Nitration and Bromination-of Some Pyrromethenones and 5-Arylmethylene-3,4-dimethyl-3-pyrrolin-2-ones", Monatschefte fur Chemie, 1984, 115, 357-373.
Falsone and Wingen, "Synthese von 2-Oxo-5H-furanen unter Wittig-Horner Bedingungen", Arch. Pharm., 1984, 317, 802-806.
Verma et al., "Smooth Conversion of 3,4-Diarylcoumarins and 3,4,5-Triaryl-2(5H)-furanones to 2H-Chromene and 2,5-Dihydrofuran Derivatives with Dimethyl Sulfide-Borane Complex", Synthesis, 1988, 1, 68-70.
Pratapan et al., "Substituent Effects in the Photochemistry of 5-Aryl-3,3-diphenyl-2(3H)-furanones. Steady-State and Laser Flash Photolysis Studies", J. Org. Chem., 1988, 53, 5826-5831.
Krafft and Pankowski, "Butenolide synthesis using acyl cobalt complexes", Tetrahedron Letters, 1990, 31:36, 5139-5142.
Alcaide and Rodriguez-Lopez, "Reaction of N-Trimethylsilyl Benzil Monoimine with Simple Lithium Ester Enolates. A Synthetic Tool for the Regioselective One-Pot Preparation of Novel Polyfunctional Pyrrolines", J. Chem. Soc.-Perkin Trans., 1990, 1, 2451-2457.
Dinulescu et al., "IX. Reaction of 1-chloro-1,2-diphenyl-3-aryl-.pi.-allylpalladium complexes with carbon monoxide", Journal of Organonmetallic Chemistry, 1977, 140, 91-96.
Chan et al., "Solvent chelation and concentration effects on the benzannulation reaction of chromium carbene complexes and acetylenes", Journal of Organometallic Chemistry, 1987, 334, 9-56.
Pennanen, "Studies on the furan series. Part VIII. The reaction of ynamines with acyloins. A convenient preparation of 4,5-di(2-furyl and 2-thienyl)-2(5H)-furanones and -furans", Heterocycles, 1977, 6:6, 701-706. N-Acyl-N'-enylhydrazines to pyrrolidinones", Heterocycles, 1992, 33:1, 91-95.
Dotz et al., "LVII. Amidinocarben-Chelatkomplexe des Chroms und Molybdans: Synthese, Struktur und Cycloadditionen mit Alkinen", Journal of Organometallic Chemistry, 1993, 459, 169-176.
Herndon and Zora, "Reaction of Cyclopropylcarbene-Molybdenum Complexes with Alkynes: Formation of Cycloheptadienones under Mild Conditions", Synlett, 1993, 5, 363-364.
Tyvorskii and Kukharev "Reaction of alkyl- and phenyl-substituted 5-aminomethyl-2(5H)-furanones with dimethylamine", Russian Journal of Organic Chemistry, 1993, 29:5(2), 840-843.
Clozel et al., "Pathophysiological role of endothelin revealed by the first orally active endothelin receptor antagonist", Nature, 1993, 365, 759-761.
Ohno, "Effects of Endothelin-specific Antibodies and Endothelin in Spontaneously Hypertensive Rats", J. Tokyo Women's Medical College, 1991, 61:10-11, 951-959.
Lerman et al., "Endothelin Has Biological Actions at Pathophysiological Concentrations", Circulation, 1991, 83:5, 1808-1814.
Rodeheffer et al., "Circulating plasma endothelin correlates with the severity of congestive heart failure in humans", Am. J. Hypertension, 1991, 4:9A-10A.
Arai et al., "Cloning and expression of a cDNA encoding an endothelin receptor", Nature, 1990, 348, 730-732.
Sakurai et al., "Cloning of a cDNA encoding a non-isopeptide-selective subtype of the endothelin receptor", Nature, 1990, 348, 732-735.
Lin et al., "Cloning and functional expression of a vascular smooth muscle endothelin 1 receptor", Proc. Natl. Acad. Sci. USA, 1991, 88, 3185-3189.
Sakamoto et al., "Cloning and functional expression of human cDNA for the ET.sub.B endothelin receptor", Biochem. Biophys. Res. Chem., 1991, 178:2, 656-663.
Hosoda et al., "Cloning and expression of human endothelin-1 receptor cDNA", FEBS Lett., 1991, 287:1,2; 23-26.
Takayanagi et al., "Presence of non-selective type of endothelin receptor on vascular endothelium and its linkage to vasodilation", FEBS Lett., 1991, 282:1, 103-106.
Panek et al., "Endothelin and structurally related analogs distinguish between endothelin receptor subtypes", Biochem. Biophys. Res. Chem., 1992, 183:2, 566-571. agonistic activity", Biochem. Biophys. Res. Chem., 1991, 179:1, 286-292.
Nakagawa et al., "Measurement of Immunoreactive Endothelin-1 in Plasma of a Patient with Malignant Hemangioendothelioma", Nippon Hifuka Gakkai Zasshi, 1990, 100, 1453-1456.
Norguchi et al., "An Endothelin (ET).sub.A Receptor Antagonists, BQ-123, Blocks ET-1 Induced Bronchoconstriction and Tracheal Smooth Muscle (TSM) Contraction in Allergic Sheep", Am. Rev. Respir. Dis., 1992, 145 (4 Part 2), A858.
Clark et al., "Plasma endothelin levels in preeclampsia: Elevation and correlation with uric acid levels and renal impairment", Am. J. Obstet Gynecol., 1992, 166:3, 962-968.
Pittet et al., "Elevated Plasma Endothelin-1 Concentrations Are Associated with the Severity of Illness in Patients with Sepsis", Ann. Surg., 1991, 213:3, 261-264.
Gandhi et al., "Endothelin, a Potent Peptide Agonist in the Liver", J. Biol. Chem., 1990, 265:29, 17432-17435.
Kanno et al., "Endothelin-1 and Vasculitis", J. Amer. Med. Assoc., 1990, 264:22, 2868.
Zamora et al., "Serum endothelin-1 concentrations and cold provocation in primary Raynaud's phenomenon", Lancet, 1990, 336, 1144-1147.
Tahara et al., "Circulating Immunoreactive Endothelin in Patients Undergoing Percutaneous Transluminal Coronary Angioplasty", Metabolism, 1991, 40:12, 1235-1237.
Stewart e
Cheng Xue-Min
Massa Mark Alan
Patt William Chester
Anderson Elizabeth M.
Fan Jane
Warner-Lambert & Company
LandOfFree
Small molecule biaryl compounds as inhibitors of endothelin conv does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Small molecule biaryl compounds as inhibitors of endothelin conv, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Small molecule biaryl compounds as inhibitors of endothelin conv will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1371663