Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-04-15
1998-09-08
Dentz, Bernard
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514300, 514302, 514380, 544238, 546113, 546114, 546116, 548245, 548246, A61K 31435, C07D49504
Patent
active
058045856
ABSTRACT:
Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds that include those of the formula: ##STR1## where X is selected from groups that include O, S, and NH; Y is selected from O.sup.+ and N, and R.sup.1 and R.sup.2 are each selected independently from among alkyl, lower alkenyl, lower alkynyl, lower haloalkyl, halide, pseudohalide or H, except that R.sup.2 is not halide. R.sup.3, R.sup.4 and R.sup.5 are selected from among groups that include hydrogen, halide, alkoxy, alkyl, haloalkyl; and R.sup.7 is selected from groups that include (CH.sub.2).sub.r R.sup.18, in which r is 0 to 6 and R.sup.18 is selected from groups that include aryl, particularly pyrmidinyl and phenyl. The methods are effected by contacting endothelin receptors with one or more of the compounds or with compositions containing one or more of the compounds prior to, simultaneously with, or subsequent to contacting the receptors with an endothelin peptide.
REFERENCES:
patent: 2888455 (1959-05-01), Kano et al.
patent: 3300488 (1967-01-01), Onoue et al.
patent: 3660383 (1972-05-01), Sumimoto et al.
patent: 3821087 (1974-06-01), Knazek et al.
patent: 3883393 (1975-05-01), Knazek et al.
patent: 4044126 (1977-08-01), Cook et al.
patent: 4161599 (1979-07-01), Maffrand
patent: 4191554 (1980-03-01), Gregory
patent: 4311845 (1982-01-01), Braye et al.
patent: 4364923 (1982-12-01), Cook et al.
patent: 4375544 (1983-03-01), Meth-Cohn et al.
patent: 4406898 (1983-09-01), Lunn et al.
patent: 4414209 (1983-11-01), Cook et al.
patent: 4485108 (1984-11-01), Jozic
patent: 4522811 (1985-06-01), Eppstein et al.
patent: 4577014 (1986-03-01), Lunn et al.
patent: 4752613 (1988-06-01), Floyd et al.
patent: 4997836 (1991-03-01), Sugihara et al.
patent: 5026700 (1991-06-01), Harrison et al.
patent: 5082838 (1992-01-01), Naka et al.
patent: 5114918 (1992-05-01), Ishikawa et al.
patent: 5187195 (1993-02-01), Oohata et al.
patent: 5198548 (1993-03-01), Beylin et al.
patent: 5208243 (1993-05-01), Peglion et al.
patent: 5230999 (1993-07-01), Suzuki et al.
patent: 5240910 (1993-08-01), Lam et al.
patent: 5248807 (1993-09-01), Fujimoto et al.
patent: 5260278 (1993-11-01), Cody et al.
patent: 5270313 (1993-12-01), Burri et al.
patent: 5292740 (1994-03-01), Burri et al.
patent: 5324839 (1994-06-01), Clemence et al.
patent: 5334598 (1994-08-01), Bagley et al.
patent: 5352659 (1994-10-01), Wakimasu et al.
patent: 5352800 (1994-10-01), Bills et al.
patent: 5378715 (1995-01-01), Stein et al.
patent: 5382569 (1995-01-01), Cody et al.
patent: 5389620 (1995-02-01), Ishikawa et al.
patent: 5389633 (1995-02-01), Miyake et al.
patent: 5407941 (1995-04-01), Carceller et al.
patent: 5420123 (1995-05-01), Murugesan et al.
patent: 5420129 (1995-05-01), Breu et al.
patent: 5420131 (1995-05-01), Carceller et al.
patent: 5420133 (1995-05-01), Dhanoa et al.
patent: 5420138 (1995-05-01), Corbier et al.
patent: 5420275 (1995-05-01), Masuya et al.
patent: 5430022 (1995-07-01), Hemmi et al.
patent: 5439887 (1995-08-01), Hamon et al.
patent: 5444152 (1995-08-01), Ishikawa et al.
patent: 5464853 (1995-11-01), Chan et al.
patent: 5470833 (1995-11-01), Ishikawa et al.
patent: 5492892 (1996-02-01), Anderson et al.
patent: 5514691 (1996-05-01), Chan et al.
patent: 5514696 (1996-05-01), Murugesan et al.
patent: 5565485 (1996-10-01), Bagley et al.
patent: 5585397 (1996-12-01), Tung et al.
patent: 5589478 (1996-12-01), Yamada et al.
patent: 5591728 (1997-01-01), de Nanteuil et al.
patent: 5599811 (1997-02-01), Berryman et al.
patent: 5612359 (1997-03-01), Murugesan
patent: 5641793 (1997-06-01), Bradbury
patent: 5668137 (1997-09-01), Phillips et al.
patent: 5668176 (1997-09-01), Bagley et al.
Raju et al., Amide bond surrogates: a study in thiophenesulfonamide based endothelin receptor antagonists, Bioorganic Medicinal Chem. LETT. 7(7):939-944 (1997).
Raju et al., Search for surrogates: a study of endothelin receptor antagonist structure activity relationships, Bioorganic Medicinal Chem. LETT. 7(7): 933-938 (1997).
Raju et al., Thiophenesulfonamides as endothelin receptor antagonists, Bioorganic Medicinal Chem. LETT. 6(22):2651-2656 (1996).
Wu et al., Discovery of TBC11251, a potent, long acting, orally active endothelin receptor-A selective antagonist, J. Medicinal Chem. 40(11):1690-1697 (1997).
Wu et al., Structure-activity relationships of N-2-aryl-3(isoazolylsulfamoyl)-2-thiophenecarboxamides as selective endothelin receptor-A antagonists, J. Medicinal Chem. 40(11);1682-1689 (1997).
Anagnostou et al., Erythropoietin has mitogenic and positive chemotactic effects on endothelial cells, Proc. Natl. Acad. Sci. USA 87:5978-5982 (1990).
Arai et al., Cloning and expression of a cDNA encoding an endothelin receptor, Nature 348:730-732 (1990). by .sup.1 H NMR, Int. J. Peptide Protein Res. 37:315-324 (1991).
Benigni, et al., A specific endothelin subtype A receptor antagonist protects against injury in renal disease progression, Kidney Int. 44:440-444 (1993).
Bolger et al., Vascular activity, tissue levels, and binding sites for endothelin: A comparison in the spontaneously hypertensive and Wistar-Kyoto rats,Can. J. Physiol. Pharmacol, 69: 406-413 (1991).
Bolger et al., Characterization of binding of the Ca.sup.++ channel Pharmacol Exp. Therap. 225:291-309 (1983).
Borges et al., Tissue selectivity of endothelin, Eur. J. Pharmacol. 165-223-230 (1989).
Brooks et al., Effect of nifedipine on cyclosporine A-induced nephrotoxicity, urinary endothelin excretion and renal endothelin receptor number, Eur. J. Pharmacol. 194:115-117 (1991).
Buemi et al., Influence of recombinant erythropoietin on the production of endothelin-1 from human umbilical artery, Nephron 64(1):165-166 (1993).
Cardell et al., Two functional endothelin receptors in guinea-pig pulmonary arteries, Neurochem. Int. 18(4):571-574 (1991).
Carlini et al., Intravenous erythropoietin (rHuEPO) administration increases plasma endothelin and blood pressure in hemodialysis patients, Am. J. Hyper. 6:103-107 (1993).
Clarke et al., Endothelin is a potent long-lasting vasoconstrictor in men, Am. J. Physiol. 257 (6 pt 2):H2033-H2035 (1989).
Clozel et al., Pathophysical role of endothelin revealed by the first orally active endothelin receptor antagonist, Nature 365:759-761 (1993).
Cody et al., The rational design of a highly potent combined ET.sub.A and ET.sub.B receptor antagonist (PD145065) and related analogues, Med. Chem. Res. 3:154-162 (1993).
Cooper et al., A novel approach to molecular similarity, J. Comput.-Aided Mol Design 3:253-259 (1989).
De Nucci et al., Presor effects of circulating endothelin are limited by its removal in the pulmonary circulation and by the release of prostacyclin and endothelium-derived relaxing factor, Proc. Natl. Acad. Sci. USA 85:9797 (1988).
De Castiglione et al., Alanine scan of endothelin, in Peptides: Chemistry and Biology, Proc. Amer. Rept. Symp. (Twelfth), (J.A. Smith and J.E. Rivier, Eds.) ESCOM, Leiden, 1992, pp. 402-403.
Doherty, Endothelin: A new challenge, J. Med. Chem. 35(9):1493-1508 (1992).
Eschbach et al., Recombinant human erythropoietin in anemic patients with end stage renal disease; results of a phase III multicenter clinical trial, Ann. Intern. Med. 111:992-1000 (1989).
Filep et al., Endothelin-1 induces prostaglandin release from bovine aortic endothelial cells, Biochem. Biophys. Res. Comm. 177(1):171-176 (1991).
Fujimoto et al., A novel non-peptide endothelin antagonist isolated from bayberry, FEBS Lttrs. 305(1):41-44 (1992).
Furchgott et al., The obligatory role of endothelial cells in the relaxation of arterial smooth muscle by acetylcholine, Nature 288:373-376 (1980).
Galantino et al., D-Amino acid scan of endothelin, Peptides: Chemistry & Biology, Proc. Amer. Report. Symp. (Twelfth), J.A. Smith and J.E. Rivier, Eds., ESCOM, Leiden, 1992, pp. 404-405. Leu.sup.11 ! substance P on endothelin-1 binding sites in rat cardiac membranes, Biochem. Biophys. Res. Commun. 179(1):130-133 (1991).
Heidenreich et al., Erythropoietin induces contraction of isolated renal small resistance ves
Dentz Bernard
Seldman Stephanie L.
Texas Biotechnology Corporation
LandOfFree
Thieno-pyridine sulfonamides derivatives thereof and related com does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Thieno-pyridine sulfonamides derivatives thereof and related com, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Thieno-pyridine sulfonamides derivatives thereof and related com will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1282380