Robert Lynn Roden

US Patent:

20080145433, Jun 19, 2008

Filed:

Nov 6, 2007

Appl. No.:

11/935474

Inventors:

Michael J. Gerber - Denver CO, US
Richard J. Gorczynski - Westminster CO, US
Robert L. Roden - Broomfield CO, US
Praful K. Shah - Superior CO, US

Assignee:

GILEAD COLORADO, INC. - Westminster CO

International Classification:

A61K 9/14
A61K 31/44
A61P 3/10

US Classification:

424489, 514348

Abstract:

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 μm 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.

US Patent:

20090054473, Feb 26, 2009

Filed:

Aug 22, 2008

Appl. No.:

12/196635

Inventors:

Robert L. Roden - Broomfield CO, US
Richard J. Gorczynski - Westminster CO, US
Michael J. Gerber - Denver CO, US

Assignee:

Gilead Colorado, Inc. - Westminster CO

International Classification:

A61K 31/513
A61P 3/00

US Classification:

514274

Abstract:

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 (ET) 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 ETreceptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETreceptor 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 ETreceptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETreceptor antagonist.

US Patent:

20090221549, Sep 3, 2009

Filed:

Feb 16, 2007

Appl. No.:

12/279037

Inventors:

Michael J. Gerber - Denver CO, US
Richard J. Gorczynski - Westminster CO, US
Robert L. Roden - Broomfield CO, US

Assignee:

Gilead Colorado, Inc. - Westminster

International Classification:

A61K 31/554
A61K 31/505
A61K 31/5415
A61K 31/55
A61K 31/551
A61K 31/495
A61P 9/12

US Classification:

51421107, 514274, 5142235, 51421207, 514221, 51425212

Abstract:

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. Further provided is a new use of darusentan in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy, wherein the composition is administered adjunctively with at least one diuretic and at least one antihypertensive drug selected from ACE inhibitors, angiotensin II receptor blockers, beta-adrenergic receptor blockers and calcium channel blockers.

US Patent:

20070196510, Aug 23, 2007

Filed:

Aug 24, 2006

Appl. No.:

11/509895

Inventors:

Michael J. Gerber - Denver CO, US
Richard J. Gorczynski - Westminster CO, US
Robert L. Roden - Broomfield CO, US

International Classification:

A61K 33/24
A61K 31/554
A61K 31/549
A61K 31/455
A61K 31/4184
A61K 31/41
A61K 31/401

US Classification:

424617, 514355, 514423, 514381, 5142235, 514471, 514571, 514412, 514651, 514278, 514738, 514411, 51421107

Abstract:

A method is provided for lowering blood pressure in a patient having clinically diagnosed resistant hypertension. The method comprises administering darusentan to the patient adjunctively with a baseline antihypertensive regimen that comprises administration of at least one diuretic and at least two antihypertensive drugs selected from at least two of (a) ACE inhibitors and angiotensin II receptor blockers, (b) beta-adrenergic receptor blockers and (c) calcium channel blockers. The darusentan is orally administered at a dose and frequency effective, in combination with the baseline regimen, 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.