Patents Assigned to Gilead Palo Alto, Inc.
-
Publication number: 20100113463Abstract: The present invention discloses pteridinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome and the like.Type: ApplicationFiled: January 7, 2010Publication date: May 6, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Jeffrey Chisholm, Dmitry Koltun, Jeff Zablocki, Eric Parkhill, Andrey Glushkov, Natalya Vasilevich, Timur Zilbershtein, Andrew Cole, Tsung Lin, Ian Henderson
-
Publication number: 20100113514Abstract: The present invention relates to sodium channel inhibitors of Formula : in which R1, R2, R3, R4, R5, R6, and R7 are as defined above, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes.Type: ApplicationFiled: October 28, 2009Publication date: May 6, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Matthew Abelman, Nancy Chu, Robert Jiang, Kwan Leung, Jeff Zablocki
-
Publication number: 20100113461Abstract: The present invention relates to compounds that are late sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein R1, R2, R3, and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: October 27, 2009Publication date: May 6, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Dmitry Koltun, Eric Parkhill, Jeff Zablocki
-
Publication number: 20100105695Abstract: The invention is directed to methods for enhancing endogenous insulin levels in a patient in need thereof which method comprises administering to the patient an insulin secretion-enhancing amount of racemic ranolazine or the R- or S-enantiomer of ranolazine. It is also directed to methods of treatment comprising racemic ranolazine or the R- or S-enantiomer of ranolazine for enhancing endogenous insulin levels in a patient in need thereof. It is also directed to a composition comprising an insulin secretion-enhancing amount of racemic ranolazine or the R- or S-enantiomer of ranolazine and at least one anti-diabetic agent.Type: ApplicationFiled: January 4, 2010Publication date: April 29, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Arvinder Dhalla, Luiz Belardinelli, John Shryock, Kwan Leung, Dewan Zeng
-
Publication number: 20100105706Abstract: The present invention relates to methods of preventing airway remodeling using A2B adenosine receptor antagonists. This invention finds utility in the treatment and prevention of asthma, COPD, pulmonary fibrosis, emphysema, and other pulmonary diseases. The invention also relates to pharmaceutical compositions for use in the method.Type: ApplicationFiled: October 26, 2009Publication date: April 29, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Dewan Zeng, Michael R. Blackburn, Luiz Belardinelli
-
Patent number: 7683037Abstract: The present invention relates to methods for myocardial imaging by administering at least one 2-adenosine N-pyrazole, 2-adenosine C-pyrazole or a combination thereof A2A adenosine receptor agonist to a human undergoing myocardial imaging. The invention also relates to methods of producing coronary vasodilation without significant peripheral vasodilation by administering at least one 2-adenosine N-pyrazole, 2-adenosine C-pyrazole or a combination thereof adenosine A2A adenosine receptor agonist to a human.Type: GrantFiled: July 29, 2003Date of Patent: March 23, 2010Assignee: Gilead Palo Alto, Inc.Inventor: Luiz Belardinelli
-
Publication number: 20100056538Abstract: Disclosed are prodrugs of A2B adenosine receptor antagonists, and their use in treating mammals for various disease states.Type: ApplicationFiled: November 13, 2009Publication date: March 4, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Rao Kalla, Dmitry Koltun, Jeff Zablocki, Elfatih Elzein
-
Patent number: 7671192Abstract: Synthesis methods suitable for large scale manufacture of the A2A-adenosine receptor agonist (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide and precursors thereof.Type: GrantFiled: May 17, 2007Date of Patent: March 2, 2010Assignee: Gilead Palo Alto, Inc.Inventors: Jeff Zablocki, Elfatih Elzein
-
Patent number: 7662819Abstract: The present invention discloses pteridinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome and the like.Type: GrantFiled: October 5, 2007Date of Patent: February 16, 2010Assignee: Gilead Palo Alto, Inc.Inventors: Jeffrey Chisholm, Dmitry Koltun, Jeff Zablocki, Eric Parkhill, Andrey Glushkov, Natalya Vasilevich, Timur Zilbershtein, Andrew Cole, Tsung Lin, Ian Henderson
-
Publication number: 20100035890Abstract: Disclosed are methods for treating patients suffering from cardiovascular diseases comprising administering an intravenous (IV) infusion of ranolazine. In one embodiment, the IV infusion of ranolazine is followed by an orally administered sustained release ranolazine dosage formulation to maintain human ranolazine plasma levels at therapeutic levels in patients.Type: ApplicationFiled: October 15, 2009Publication date: February 11, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Louis Lange, Markus Jerling, Andrew Wolff
-
Patent number: 7655637Abstract: 2-adenosine N-pyrazole compounds having the following formula: wherein R1?CH2OH; R2 is hydrogen; R3 is selected from the group consisting of CO2R20; —CONR7R8 ,and aryl wherein the aryl substituent is optionally substituted with one substituent selected from the group consisting of halo, C 1-3alkyl and OR20;R4 is hydrogen; R7 is selected from hydrogen, and C1-3alkyl; R8 is hydrogen; and R20 is selected from hydrogen and methyl as well as methods for using the compositions as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart are disclosed.Type: GrantFiled: October 27, 2006Date of Patent: February 2, 2010Assignee: Gilead Palo Alto, Inc.Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata Palle, Luiz Belardinelli
-
Patent number: 7655636Abstract: The present invention relates to methods for producing coronary vasodilation with little peripheral vasodilation by administering doses of a pharmaceutical composition including regadenoson, named (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide, — an adenosine A2A receptor agonist — to a human in an amount sufficient to increase the average coronary peak flow velocity by at least about 16.5 cm/sec.Type: GrantFiled: October 19, 2005Date of Patent: February 2, 2010Assignee: Gilead Palo Alto, Inc.Inventors: Toufigh Gordi, Ann Walls Olmsted, Hsiao Dee Lieu, Luiz Belardinelli
-
Patent number: 7655638Abstract: Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.Type: GrantFiled: November 15, 2006Date of Patent: February 2, 2010Assignee: Gilead Palo Alto, Inc.Inventors: Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki
-
Patent number: 7625881Abstract: Disclosed are prodrugs of A2B adenosine receptor antagonists, having the following structure and their use in treating mammals for various disease states.Type: GrantFiled: June 14, 2006Date of Patent: December 1, 2009Assignee: Gilead Palo Alto, Inc.Inventors: Rao Kalla, Dmitry Koltun, Jeff Zablocki, Elfatih Elzein
-
Patent number: 7601721Abstract: Disclosed are novel piperazine and piperazine derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, diabetes, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction.Type: GrantFiled: September 17, 2007Date of Patent: October 13, 2009Assignee: Gilead Palo Alto, Inc.Inventors: Jeff Zablocki, Dmitry Koltun