Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2005-10-11
2011-11-29
Chandrakumar, Nizal (Department: 1625)
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
active
08067601
ABSTRACT:
The invention relates to 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea as a crystalline, stoichiometrically defined and non-hygroscopic sulfate salt and a process for its preparation. Further, the present invention relates to the use of said 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea as a crystalline, stoichiometrically defined and non-hygroscopic sulfate salt alone or in combination with other compounds. Further, the present invention relates to formulations of said 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea as a crystalline, stoichiometrically defined and non-hygroscopic sulfate salt in the preparation of pharmaceutical compositions. The invention also relates to the use of such sulfate salts in formulations as neurohormonal antagonists.
REFERENCES:
patent: 6331541 (2001-12-01), Ko et al.
patent: 2007/0043081 (2007-02-01), Bur et al.
patent: 428434 (1991-05-01), None
patent: WO 99/21835 (1999-05-01), None
patent: WO 99/40192 (1999-08-01), None
patent: WO 01/09088 (2001-02-01), None
patent: WO 01/45694 (2001-06-01), None
patent: WO 01/45700 (2001-06-01), None
patent: WO 01/45711 (2001-06-01), None
patent: WO 01/66143 (2001-09-01), None
patent: WO 02/00606 (2002-01-01), None
patent: WO 02/02530 (2002-01-01), None
patent: WO 02/47456 (2002-06-01), None
patent: WO 02/47687 (2002-06-01), None
patent: WO 02/058702 (2002-08-01), None
patent: WO 02/076979 (2002-10-01), None
patent: WO 02/078641 (2002-10-01), None
patent: WO 02/078707 (2002-10-01), None
patent: WO 02/079155 (2002-10-01), None
patent: WO 02/079188 (2002-10-01), None
patent: WO 02/089740 (2002-11-01), None
patent: WO 02/089785 (2002-11-01), None
patent: WO 02/089792 (2002-11-01), None
patent: WO 02/089793 (2002-11-01), None
patent: WO 02/090337 (2002-11-01), None
patent: WO 02/090348 (2002-11-01), None
patent: WO 02/090353 (2002-11-01), None
patent: WO 03/048154 (2003-06-01), None
patent: WO 2004/026836 (2004-04-01), None
patent: WO 2004/043366 (2004-05-01), None
patent: WO 2004/043368 (2004-05-01), None
patent: WO 2004/043369 (2004-05-01), None
patent: WO 2004/043463 (2004-05-01), None
patent: WO 2004/043917 (2004-05-01), None
patent: WO 2004/043948 (2004-05-01), None
patent: WO 2004/073634 (2004-09-01), None
patent: WO 2004/099179 (2004-11-01), None
Clozel et al., The Journal of Pharmacology and Experimental Therapeutics, vol. 311, pp. 204-212 (2004).
Ames, R.S. et al., “Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14” Nature (1999), 401, pp. 282-286.
Bern, H.A. et al., “Neurohormones from fish tails: the caudal neurosecretory system. I. Urophysiology and the caudal neurosecretory system of fishes”, Recent Prog. Horm. Res., (1985), 41, pp. 533-552.
Breu, V. et al., In vitro characterization of Ro-46-2005, a novel synthetic non-peptide antagonist of ETAand ETBreceptors., FEBS Lett., (1993), 334, pp. 210-214.
Cheung, B.M. et al., “Plasma concentration of urotensin II is raised in hypertension”, J. Hypertens., (2004), 22, pp. 1341-1344.
Douglas, S.A., et al., “Differential vasoconstrictor activity of human urotensin-II in vascular tissue isolated from the rat, mouse, dog, pig, marmoset and cynomolgus monkey”, Br. J. Pharmacol., (2000), 131, pp. 1262-1274.
Douglas, S.A. et al., “Human urotensin-II is a potent vasoactive peptide: pharmacological characterization in the rat, mouse, dog and primate”, J. Cardiovasc. Pharmacol., (2000), 36, Suppl 1:S163-S166.
Garlton, J., et al., “Central effects of urotensin-II following ICV administration in rats”, Psychopharmacology (Berlin), (2001), 155, pp. 426-433.
Heller, J. et al., “Increased urotensin II plasma levels in patients with cirrhosis and portal hypertension”, J. Hepatol., (2002), 37, pp. 767-772.
Liu, Q. et al., “Identification of urotension II as the endogenous ligand for the orphan G-protein-coupled receptor GPR14”, Biochem. Biophys. Res. Commun., (1999), 266, pp. 174-178.
Malinowski, M., et al., “A Convenient Preparation of 4-Pyridinamine Derivatives”, J. Prakt, Chem., (1988), 330, pp. 154-158.
Mori, M. et al., “Urotensin II is the endogenous ligand of a G-protein-coupled orphan receptor, SENR (GPR14)”, Biochem. Biophys. Res. Commun., (1999), 265, pp. 123-129.
“Protective Groups in Organic Synthesis”, T.W. Greene, P.G.M. Wuts, Wiley-Interscience, (1999).
Russell, F.D., et al., “Cardiostimulant effects of urotensin-II in human heart in vitro”, Br. J. Pharmacol., (2001), 132, pp. 5-9.
Shenouda, S. et al., “Localization of urotensin-II immunoreactivity in normal human kidneys and renal carcinoma”, J. Histochem. Cytochem, (2002), 50, pp. 885-889.
Silvestre, R.A., et al., “Inhibition of insulin release by urotensin II—a study on the perfused rat pancreas”, Horm Metab Res, (2001), 33, pp. 379-381.
Takahashi, K. et al., “Expression of utotensin II and urotensin II receptor mRNAs in various human tumor cell lines and secretion of urotensin II-like immunoreactivity b SW-13 adrenocortical carcinoma cells”, Peptides, (2001), 22, pp. 1175-1179.
Takahashi, K. et al., “Expression of urotensin II and its receptor in adrenal tumors and stimulation of proliferation of cultured tumor cells by urotensin II”, Peptides, (2003), 24, pp. 301-306.
Totsune, K. et al., “Role of urotensin II in patients on dialysis”, Lancent, (2001), 358, pp. 810-811.
Totsune, K. et al., “Increased plasma urotensin II levels in patients with diabetes mellitus” Clin. Sci., (2003), 104, pp. 1-5.
Tsandis, A. et al., “Urotensin II stimulates collagen synthesis of cardiac fibroblasts and hypertrophic signaling in cardiomyocytes via G(alpha)q- and Ras-dependent pathways”, J. Am. Coll. Cardiol., (2001), 37, p. 164A.
Zou, Y. et al., “Urotensin II induces hypertrophic responses in cultured cardiomyocytes from neonatal rats” FEBS Lett., (2001), 508, pp. 57-60.
Bonard Jean-Michel
Buchmann Stephan
Redey Stéphane
Woinet Bertrand
Actelion Pharmaceticals Ltd.
Chandrakumar Nizal
Hoxie & Associates
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