Abstract: This invention is in the area of methods and compositions for the inhibition of the expression of VCAM-1 and, in particular, for the treatment of diseases mediated by VCAM-1, including cardiovascular and inflammatory diseases.
Abstract: A probucol or a probucol derivative can be efficiently converted to a monoester or monoether of probucol by reacting the free hydroxyl-containing probucol or a derivative thereof (by which is meant a probucol compound with at least one substituent that is different from that on the parent probucol molecule but which maintains the two free hydroxyl groups) with a Grignard reagent or a lithium reagent that produces a magnesium bromide or lithium salt of probucol or the probucol derivative. The probucol compound anion anion is then reacted with an ester or ether forming compound.
Abstract: This invention is in the area of regulatory DNA sequences and their methods of use. Specifically, DNA sequences found in the regulatory region of cytoprotective genes are described that are termed cytoprotective response elements. DNA constructs also are provided that include cytoprotective response elements operably linked to heterologous protein coding sequence, as well as cells and non-human organisms that include the cytoprotective response elements optionally operably linked to a heterologous protein coding sequence, and a method for screening for a compound that increases mRNA or protein regulated by a cytoprotective response element. It has been discovered that the cytoprotective response elements mediate the coordinate activation of certain genes that protect cells from damaging effects of oxidative stress, and that they do so, for example during conditions of hemodynamic shear stress.
Type:
Grant
Filed:
October 16, 2002
Date of Patent:
July 24, 2007
Assignee:
Atherogenics, Inc.
Inventors:
Charles Kunsch, Signe E. Varner, Xilin Chen, Jayraz Luchoomun
Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.
Type:
Application
Filed:
December 15, 2006
Publication date:
April 26, 2007
Applicant:
AtheroGenics, Inc.
Inventors:
Kimberly Worsencroft, Liming Ni, Zhihong Ye, Charles Meng, M. Weingarten, Jacob Simpson, James Sikorski
Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.
Type:
Grant
Filed:
December 19, 2002
Date of Patent:
April 10, 2007
Assignee:
AtheroGenics, Inc.
Inventors:
James A. Sikorski, Charles Q. Meng, M. David Weingarten
Abstract: This invention is in the area of methods and compositions for the inhibition of the expression of VCAM-1 and, in particular, for the treatment of diseases mediated by VCAM-1, including cardiovascular and inflammatory diseases.
Abstract: It has been discovered that certain selected ethers of probucol, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may also improve HDL functionality by (a) increasing clearance of cholesteryl esters, (b) increasing HDL-particle affinity for hepatic cell surface receptors or (c) increasing the half life of apoAI-HDL.
Type:
Grant
Filed:
July 8, 2004
Date of Patent:
February 27, 2007
Assignee:
Atherogenics, Inc.
Inventors:
James A. Sikorski, Jayraz Luchoomun, Charles Q. Meng, Uday Saxena
Abstract: The use of compounds of the formula and pharmaceutically acceptable salts thereof, alone or in combination for the treatment of transplant rejection, wherein the substituents are further defined in the application.
Type:
Application
Filed:
April 18, 2006
Publication date:
August 24, 2006
Applicant:
AtheroGenics, Inc.
Inventors:
David Edwards, Patricia Somers, Mitchell Glass
Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.
Type:
Grant
Filed:
December 19, 2002
Date of Patent:
August 22, 2006
Assignee:
Atherogenics, Inc.
Inventors:
James A. Sikorski, Charles Q. Meng, M. David Weingarten, Kimberly J. Worsencroft, Liming Ni
Abstract: The use of compounds of the formula and pharmaceutically acceptable salts thereof, alone or in combination for the treatment of transplant rejection, wherein the substituents are further defined in the application.
Type:
Grant
Filed:
December 23, 2003
Date of Patent:
August 8, 2006
Assignee:
AtheroGenics, Inc.
Inventors:
Mitchell Glass, Patricia K. Somers, David B. Edwards
Abstract: It has been discovered certain 1,3-bis-(substituted-phenyl)-2-propen-1-ones, including compounds of formula (I) inhibit the expression of VCAM-1, and thus can be used to treat a patient with a disorder mediated by VCAM-1. Examples of inflammatory disorders that are mediated by VCAM-1 include, but are not limited to arthritis, asthma, dermatitis, cystic fibrosis, post transplantation late and chronic solid organ rejection, multiple sclerosis, systemic lupus erythematosis, inflammatory bowel diseases, autoimmune diabetes, diabetic retinopathy, rhinitis, ischemia-reperfusion injury, post-angioplasty restenosis, chronic obstructive pulmonary disease (COPD), glomerulonephritis, Graves disease, gastrointestinal allergies, conjunctivitis, atherosclerosis, coronary artery disease, angina and small artery disease.
Type:
Grant
Filed:
May 21, 2003
Date of Patent:
July 18, 2006
Assignee:
Atherogenics, Inc.
Inventors:
Charles Q. Meng, Liming Ni, James A. Sikorski, Lee K. Hoong
Abstract: A method to enhance the cytotoxic activity of an antineoplastic drug comprising administering an effective amount of the antineoplastic drug to a host exhibiting abnormal cell proliferation in combination with an effective cytotoxicity-increasing amount of an antioxidant. The invention also includes a method to decrease the toxicity to an antineoplastic agent or increase the therapeutic index of an antineoplastic agent administered for the treatment of a solid growth of abnormally proliferating cells, comprising administering an antioxidant prior to, with, or following the antineoplastic treatment.
Type:
Grant
Filed:
February 7, 2001
Date of Patent:
July 4, 2006
Assignee:
Atherogenics, Inc.
Inventors:
Rebecca Chinery, R. Daniel Beauchamp, Robert J. Coffey, Russell M. Medford, Brian E. Wadzinski
Abstract: Isolated nucleic acid molecules encoding human MEKK1, and isolated human MEKK1 proteins, are provided. The invention further provides antisense nucleic acid molecules, recombinant expression vectors containing a nucleic acid molecule of the invention, host cells into which the expression vectors have been introduced and non-human transgenic animals carrying a human MEKK1 transgene. The invention further provides human MEKK1 fusion proteins and anti-human MEKK1 antibodies. Methods of using the human MEKK1 proteins and nucleic acid molecules of the invention are also disclosed, including methods for detecting human MEKK1 activity in a biological sample, methods of modulating human MEKK1 activity in a cell, and methods for identifying agents that modulate the activity of human MEKK1.
Abstract: A method is disclosed for determining whether a compound binds to a lipoprotein such as LDL or VLDL in a manner which will lower plasma cholesterol. The method provided includes assessing the ability of the compound to form a complex with the lipoprotein, and then determining whether the newly formed complex causes a change in the structure of apoB-100 that results in increased binding affinity to an LDL receptor.
Abstract: It has been discovered that certain selected ethers of probucol, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may also improve HDL functionality by (a) increasing clearance of cholesteryl esters, (b) increasing HDL-particle affinity for hepatic cell surface receptors or (c) increasing the half life of apoAI-HDL.
Type:
Grant
Filed:
April 11, 2001
Date of Patent:
April 19, 2005
Assignee:
Atherogenics, Inc.
Inventors:
Jayraz Luchoomun, Charles Q. Meng, Uday Saxena, James A. Sikorski
Abstract: Thioketals and thioethers are provided that inhibit the expression of VCAM-1, and which can be used in the treatment of VCAM-1 mediated diseases including inflammatory disorders, cardiovascular diseases, occular diseases, autoimmune diseases, neurological disorders, and cancer. The compounds also can be used to treat hyperlipidemia and/or hypercholesterolemia.
Type:
Grant
Filed:
March 21, 2001
Date of Patent:
February 8, 2005
Assignee:
Atherogenics, Inc.
Inventors:
Charles Q. Meng, Lee K. Hoong, Patricia K. Somers