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
Abstract: Phosphonate substituted compounds with HIV protease inhibitory properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit HIV protease activity and/or are useful therapeutically for the treatment of AIDS and other antiviral infections, as well as in assays for the detection of HIV protease.
Type:
Grant
Filed:
April 25, 2003
Date of Patent:
January 19, 2010
Assignee:
Gilead Sciences, Inc.
Inventors:
Murty N. Arimili, Xiaowu Chen, Maria Fardis, Gong-Xin He, Haolun Jin, Choung U. Kim, William A. Lee, Kuei-Ying Lin, Hongtao Liu, Richard L. Mackman, Michael L. Mitchell, Hyung-Jung Pyun, Mark Sparacino, Sundaramoorthi Swaminathan, Jianying Wang, Matthew A. Williams, Lianhong Xu, Zheng-Yu Yang, Richard H. Yu, Jiancun Zhang, Lijun Zhang
Abstract: The invention is related to phosphorus substituted anti-viral inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
July 18, 2005
Date of Patent:
January 5, 2010
Assignee:
Gilead Sciences, Inc.
Inventors:
Kleem Chaudhary, Melissa Fleury, Choung U. Kim, Darren J. McMurtrie, Xiaoning C. Sheng
Abstract: This invention is concerned with human organic anion transporter (“hOAT”). Isolated nucleic acid encoding hOAT is provided, along with isolated hOAT polypeptide. hOAT nucleic acid and/or hOAT polypeptide are employed in transgenic animals, recombinant cells, replicable vectors and analytical procedures for identifying hOAT agonists or antagonists, assays for identifying hOAT alleles and/or isotypes, screening tests for nephrotoxic or neurologically active compounds, and determination of drug-drug interactions within the kidney or brain.
Abstract: The invention provides compounds with activity against infectious diseases. The compounds of the invention may inhibit retroviral reverse transcriptases and thus inhibit the replication, of the virus. The compounds of the invention may be useful for treating human patients infected with a human retrovirus, such as human immunodeficiency virus (strains of HIV-l or HIV-2) or human T-cell leukemia virus (HTLV-1 or HTLV-II) which results in acquired immunodeficiency syndrome (AIDS) and/or related diseases.