Patents by Inventor Jeff A. Zablocki

Jeff A. Zablocki has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Process for preparing an A2A-adenosine receptor agonist and its polymorphs
    Patent number: 7956179
    Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
    Type: Grant
    Filed: January 13, 2010
    Date of Patent: June 7, 2011
    Assignee: Gilead Sciences, Inc.
    Inventors: Jeff Zablocki, Elfatih Elzein
  • A2B ADENOSINE RECEPTOR ANTAGONISTS
    Publication number: 20110130362
    Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.
    Type: Application
    Filed: January 28, 2011
    Publication date: June 2, 2011
    Applicant: Gilead Sciences, Inc.
    Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
  • Quinazolinone derivatives as ALDH-2 inhibitors
    Patent number: 7951813
    Abstract: Disclosed are novel quinazolinone derivatives of formula: wherein: R1 is optionally substituted phenyl or optionally substituted heteroaryl; R2 is 3-hydroxy, 4-hydroxy, 3-NHR4 or 4-NHR4, in which R4 is hydrogen, —C(O)R5, —C(O)NHR6, or —SO2R6; in which R5 is optionally substituted lower alkyl or optionally substituted lower alkoxy; and R6 is optionally substituted lower alkyl; R3 is hydrogen, lower alkyl, lower alkoxy, or halo; V is oxygen, sulfur, or —NH—; and W is lower alkylene of 1-3 carbon atoms, which are useful as ALDH-2 inhibitors for treating mammals for various disease states, such as treatment for cocaine dependency and alcohol dependency.
    Type: Grant
    Filed: April 3, 2008
    Date of Patent: May 31, 2011
    Assignee: Gilead Sciences, Inc.
    Inventors: Matthew Abelman, Michael Organ, Jeff Zablocki, Wing Ming Keung, Guoxin Tao
  • Partial and full agonists of Aadenosine receptors
    Patent number: 7939509
    Abstract: Disclosed are novel compounds a compound of Formula I that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular dyslipidemia, diabetes, decreased insulin sensitivity, Polycystic Ovarian Syndrome, Stein-Leventhal syndrome, and obesity.
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: May 10, 2011
    Assignee: Gilead Sciences, Inc.
    Inventors: Arvinder Dhalla, Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki
  • Pyridol[2,3-B]pyrazinones for use as stearoyl CoA desaturase inhibitors
    Patent number: 7893066
    Abstract: The present invention discloses pyrido[2,3-B]pyrazinones having the structure of Formula I for use as inhibitors of stearoyl-CoA desaturase. 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, oily skin conditions, metabolic syndrome, and the like.
    Type: Grant
    Filed: April 9, 2008
    Date of Patent: February 22, 2011
    Assignee: Gilead Palo Alto, Inc.
    Inventors: Dmitry Koltun, Jeff Zablocki, Eric Parkhill, Andrei Glushkov, Natalya Vasilevich, Timur Zilbershtein, Alexey Ivanov, Jeffrey Chisholm
  • FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS
    Publication number: 20110021521
    Abstract: The present invention relates to compounds that are 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 W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Application
    Filed: July 26, 2010
    Publication date: January 27, 2011
    Applicant: Gilead Palo Alto, Inc.
    Inventors: Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
  • HETEROCYCLIC COMPOUNDS USEFUL AS STEAROYL CoA DESATURASE INHIBITORS
    Publication number: 20100267748
    Abstract: The present invention discloses 1H-pyrido[1,2-a]pyrimidin-4(9aH)-one derivatives or 1H-pyrimido[1,2-a]pyrimidin-4(9aH)-one 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, cancer, diabetes, obesity, metabolic syndrome and the like.
    Type: Application
    Filed: October 14, 2009
    Publication date: October 21, 2010
    Applicant: Gilead Palo Alto, Inc.
    Inventors: Dmitry Koltun, Alexey Ivanov, Natalya Vasilevich, Jeff Zablocki
  • PROCESS FOR PREPARING AN A2A-ADENOSINE RECEPTOR AGONIST AND ITS POLYMORPHS
    Publication number: 20100267953
    Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
    Type: Application
    Filed: April 22, 2010
    Publication date: October 21, 2010
    Inventors: Jeff Zablocki, Elfaith Elzein
  • 3-HYDROQUINAZOLIN-4-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS
    Publication number: 20100267752
    Abstract: The present invention discloses 3-hydroquinazolin-4-one derivatives for use as inhibitors of stearoyl-CoA desaturase. 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, cancer, cardiovascular disease, diabetes, obesity, metabolic syndrome and the like.
    Type: Application
    Filed: October 14, 2009
    Publication date: October 21, 2010
    Applicant: Gilead Palo Alto, Inc.
    Inventors: Andrei Glushkov, Dmitry Koltun, Elena Mayboroda, Eric Parkhill, Natalya Vasilevich, Jeff Zablocki
  • Aadenosine receptor antagonists
    Patent number: 7795269
    Abstract: Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.
    Type: Grant
    Filed: December 3, 2007
    Date of Patent: September 14, 2010
    Assignee: Gilead Palo Alto, Inc.
    Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
  • A2B Adenosine Receptor Antagonists
    Publication number: 20100222300
    Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.
    Type: Application
    Filed: May 10, 2010
    Publication date: September 2, 2010
    Applicant: Gilead Palo Alto, Inc.
    Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
  • PARTIAL AND FULL AGONISTS OF A1 ADENOSINE RECEPTORS
    Publication number: 20100210579
    Abstract: Disclosed are novel compounds a compound of Formula I that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular dyslipidemia, diabetes, decreased insulin sensitivity, Polycystic Ovarian Syndrome, Stein-Leventhal syndrome, and obesity.
    Type: Application
    Filed: March 15, 2010
    Publication date: August 19, 2010
    Applicant: Gilead Palo Alto, Inc.
    Inventors: Arvinder Dhalla, Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki
  • Substituted bicyclic and tricyclic thieno[2,3-d]pyrimidines as Aadenosine receptor antagonists
    Patent number: 7776868
    Abstract: The present invention relates to novel compounds that are A2A adenosine receptor antagonists having the structure of Formula I and to their use in treating mammals for various disease states, such as obesity, CNS disorders, including the “movement disorders” (Parkinson's disease, Huntington's Chorea, and catelepsy), and cerebral ischemia, excitotoxicity, cognitive and physiological disorders, depression, ADHD, and drug addiction (alcohol, amphetamine, cannabinoids, cocaine, nicotine, and opioids) and to their use in the enhancement of immune response. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: November 29, 2007
    Date of Patent: August 17, 2010
    Assignee: Gilead Palo Alto, Inc.
    Inventors: Tetsuya Kobayashi, Rao Kalla, Elfatih Elzein, Jeff Zablocki, Brent Blackburn
  • BICYCLIC NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS FOR USE AS STEAROYL CoA DESATURASE INHIBITORS
    Publication number: 20100204238
    Abstract: The present invention discloses bicyclic nitrogen-containing heterocyclic compounds for use as inhibitors of stearoyl-CoA desaturase. 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, oily skin conditions, metabolic syndrome, and the like.
    Type: Application
    Filed: April 26, 2010
    Publication date: August 12, 2010
    Applicant: Gilead Palo Alto, Inc.
    Inventors: Jeffrey Chisholm, Dmitry Koltun, Jeff Zablocki, Eric Parkhill, Andrey Glushkov, Natalya Vasilevich, Timur Zilbershtein, Alexey Ivanov
  • SUBSTITUTED HETEROCYCLIC COMPOUNDS
    Publication number: 20100197684
    Abstract: The present invention relates to novel heterocyclic compounds 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 Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: February 9, 2010
    Publication date: August 5, 2010
    Applicant: Gilead Palo Alto, Inc.
    Inventors: Matthew Abelman, Robert Jiang, Jeff Zablocki
  • PROCESS FOR PREPARING AN A2A-ADENOSINE RECEPTOR AGONIST AND ITS POLYMORPHS
    Publication number: 20100179313
    Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
    Type: Application
    Filed: January 13, 2010
    Publication date: July 15, 2010
    Inventors: Jeff Zablocki, Elfaith Elzein
  • N-PYRAZOLE A2A RECEPTOR AGONISTS
    Publication number: 20100160620
    Abstract: 2-adenosine N-pyrazole compounds having the following formula: and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.
    Type: Application
    Filed: December 14, 2009
    Publication date: June 24, 2010
    Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle, Luiz Belardinelli
  • A2B adenosine receptor antagonists
    Patent number: 7741331
    Abstract: Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.
    Type: Grant
    Filed: December 5, 2007
    Date of Patent: June 22, 2010
    Assignee: Gilead Palo Alto, Inc.
    Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
  • Pyrido[2,3-B] pyrazin-3(4H)-ones for use as stearoyl CoA desaturase inhibitors
    Patent number: 7732453
    Abstract: The present invention discloses pyrido[2,3-B]pyrazin-3(4h)-ones for use as inhibitors of stearoyl-CoA desaturase. 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, oily skin conditions, metabolic syndrome, and the like.
    Type: Grant
    Filed: October 5, 2007
    Date of Patent: June 8, 2010
    Assignee: Gilead Palo Alto, Inc.
    Inventors: Dmitry Koltun, Jeff Zablocki, Eric Parkhill, Andrey Glushkov, Natalya Vasilevich, Timur Zilbershtein, Alexey Ivanov
  • Process for preparing an A-adenosine receptor agonist and its polymorphs
    Patent number: 7732595
    Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph. The A2A-adenosine receptor agonist has the following formula: This compound is prepared by reacting the ethyl ester with methylamine in a sealed pressure reactor.
    Type: Grant
    Filed: February 2, 2007
    Date of Patent: June 8, 2010
    Assignee: Gilead Palo Alto, Inc.
    Inventors: Jeff Zablocki, Elfatih Elzein