Patents Assigned to Gilead Colorado, Inc.
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Publication number: 20130116257Abstract: A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years.Type: ApplicationFiled: December 21, 2012Publication date: May 9, 2013Applicant: GILEAD COLORADO, INC.Inventor: GILEAD COLORADO, INC.
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Patent number: 8377933Abstract: A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years.Type: GrantFiled: June 16, 2011Date of Patent: February 19, 2013Assignee: Gilead Colorado, Inc.Inventors: Michael J. Gerber, Christopher Dufton
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Patent number: 8217155Abstract: The invention relates to derivatives and metabolites of ambrisentan, including compounds of general Formula (I) or salts, hydrates, solvates, racemates, or optical isomers thereof, wherein R1 is —OH or —OCH3; R2 is —H, lower alkyl (e.g. C1-C4 alkyl) or glycosidyl; and R3 and R4 are independently —CH3, —C(O)H or —CH2OR6, wherein R6 is —H or a hydrocarbyl group having 1 to 20 carbon atoms.Type: GrantFiled: July 31, 2008Date of Patent: July 10, 2012Assignees: Gilead Colorado, Inc., Abbott GmbH & Co. KGInventors: Lawrence S. Melvin, Jr., Martina Ullrich, Hans-Guenther Hege, Jürgen Weymann
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Publication number: 20100292320Abstract: The present disclosure provides a compound of general Formula (I) having enzyme inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: ApplicationFiled: December 12, 2008Publication date: November 18, 2010Applicant: Gilead Colorado, Inc.Inventor: Lawrence S. Melvin, JR.
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Publication number: 20100204163Abstract: The invention relates to derivatives and metabolites of ambrisentan, including compounds of general Formula (I) or salts, hydrates, solvates, racemates, or optical isomers thereof, wherein R1 is —H or —OCH3; R2 is —H, lower alkyl (e.g. C1-C4 alkyl) or glycosidyl; and R3 and R4 are independently —CH3, —C(O)H or —CH2OR6, wherein R6 is —H or a hydrocarbyl group having 1 to 20 carbon atoms. In some embodiments, compounds of Formula (I) exhibit selective affinity for ETA receptors and serve as endothelin receptor antagonists. In some embodiments, the compounds correspond to metabolites of ambrisentan produced by the enzymatic action of cytochrome P450 or uridine diphosphate glucuronosyl transferase enzymes, for example as elucidated in pre-clinical or clinical studies.Type: ApplicationFiled: July 31, 2008Publication date: August 12, 2010Applicant: Gilead Colorado, Inc.Inventors: Lawrence S. Melvin, JR., Martina Ullrich, Hans-Guenther Hege, Jürgen Weymann
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Publication number: 20090221549Abstract: A new use of darusentan is provided in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy with one or more drugs. The composition comprises darusentan in an amount providing a therapeutically effective daily dose; wherein (a) the composition is orally deliverable and/or (b) the daily dose of darusentan is effective to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures.Type: ApplicationFiled: February 16, 2007Publication date: September 3, 2009Applicant: Gilead Colorado, Inc.Inventors: Michael J. Gerber, Richard J. Gorczynski, Robert L. Roden
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Publication number: 20090054473Abstract: A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.Type: ApplicationFiled: August 22, 2008Publication date: February 26, 2009Applicant: Gilead Colorado, Inc.Inventors: Robert L. Roden, Richard J. Gorczynski, Michael J. Gerber
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Publication number: 20080145433Abstract: A solid discrete orally deliverable pharmaceutical dosage form comprises darusentan and one or more pharmaceutically acceptable excipients; wherein (a) the darusentan is in solid particulate form having a mean particle size of about 5 to about 200 ?m and is present in the dosage form in an amount of about 1 to about 600 mg; and (b) the dosage form exhibits at least about 90% dissolution of the darusentan in 30 minutes in a standard in vitro dissolution test. A method for lowering blood pressure, for example in a patient having resistant hypertension, comprises administering such a dosage form once daily to the patient.Type: ApplicationFiled: November 6, 2007Publication date: June 19, 2008Applicant: GILEAD COLORADO, INC.Inventors: Michael J. Gerber, Richard J. Gorczynski, Robert L. Roden, Praful K. Shah