Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.
Type:
Grant
Filed:
May 10, 2005
Date of Patent:
December 11, 2007
Assignee:
Incyte Corporation
Inventors:
Chu-Biao Xue, Changsheng Zheng, Ganfeng Cao, Hao Feng, Michael Xia, Rajan Anand, Joseph Glenn, Brian W. Metcalf
Abstract: The present invention provides novel compounds, and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsey, irritable bowl syndrome, immune supression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula:
wherein R1, R3, R5, Q, Z, Y, V, X and X′ are as defined herein.
Type:
Grant
Filed:
March 17, 2003
Date of Patent:
November 16, 2004
Assignee:
Bristol-Myers Squibb Pharma
Inventors:
Robert John Chorvat, Parthasarathi Rajagopalan
Abstract: Methods of identifying ligand binding sites in a target molecule such as a polynucleotide or polypeptide, as well as methods for determining whether a particular site in a target molecule is at or near the ligand binding site, are provided. Ligand binding affinities corresponding to both the target molecule and a modified version thereof are compared, preferably using mass spectral analysis. The modified molecules, or test molecules, incorporate a modification capable of modulating ligand binding affinity when located at or near the ligand binding sites. Binding site information is derived from the known position of the modification.
Type:
Grant
Filed:
July 31, 2002
Date of Patent:
September 7, 2004
Assignee:
Isis Pharmaceuticals, Inc.
Inventors:
Richard H. Griffey, Steven A. Hofstadler, Eric E. Swayze
Abstract: The present invention provides monocyclic, bicyclic and oligomeric amine compounds with at least two sites of diversity. These compounds are formed from monocyclic scaffolds which can be cyclized to form bicyclic amine scaffolds. These can then be reacted with building blocks to form the amine compounds of the invention. This invention further provides libraries or monocyclic, bicyclic and oligomeric amine compounds. Also provided are methods for preparing monocyclic, bicyclic and oligomeric amine compounds and libraries thereof. The present invention also provides pharmaceutical compositions of the monocyclic, bicyclic and oligomeric amine compounds.
Type:
Grant
Filed:
September 5, 1997
Date of Patent:
June 15, 2004
Assignee:
ISIS Pharmaceuticals, Inc.
Inventors:
Eric Edward Swayze, Peter William Davis, Robert Jay Tinder, Kelly G. Sprankle
Abstract: Methods of identifying ligand binding sites in a target molecule such as a polynucleotide or polypeptide, as well as methods for determining whether a particular site in a target molecule is at or near the ligand binding site, are provided. Ligand binding affinities corresponding to both the target molecule and a modified version thereof are compared, preferably using mass spectral analysis. The modified molecules, or test molecules, incorporate a modification capable of modulating ligand binding affinity when located at or near the ligand binding sites. Binding site information is derived from the known position of the modification.
Type:
Grant
Filed:
July 31, 2002
Date of Patent:
May 4, 2004
Assignee:
ISIS Pharmaceuticals, Inc.
Inventors:
Richard H. Griffey, Steven A. Hofstadler, Eric E. Swayze
Abstract: Methods of identifying ligand binding sites in a target molecule such as a polynucleotide or polypeptide, as well as methods for determining whether a particular site in a target molecule is at or near the ligand binding site, are provided. Ligand binding affinities corresponding to both the target molecule and a modified version thereof are compared, preferably using mass spectral analysis. The modified molecules, or test molecules, incorporate a modification capable of modulating ligand binding affinity when located at or near the ligand binding sites. Binding site information is derived from the known position of the modification.
Type:
Grant
Filed:
July 31, 2002
Date of Patent:
May 4, 2004
Assignee:
ISIS Pharmaceuticals, Inc.
Inventors:
Richard H. Griffey, Steven A. Hofstadler, Eric E. Swayze
Abstract: This invention relates to a method of treating human immunodeficiency virus (HIV) infection in a mammal comprising administering to the mammal a therapeutically effective amount of a combination of: (i) at least one cytotoxic agent and (ii) at least one non-nucleoside reverse transcriptase HIV inhibitor (NNRTI). This invention also relates to a method of treating chronic viral infections comprising administering to the mammal a therapeutically effective amount of a combination of: (i) at least one cytotoxic agent and (ii) at least one antiviral agent.
Abstract: Corticotropin releasing factor (CRF) antagonists of Formula (I):
and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.
Type:
Grant
Filed:
February 21, 2001
Date of Patent:
February 25, 2003
Assignee:
Bristol-Myers Squibb Company
Inventors:
Argyrios G. Arvanitis, Paul J. Gilligan, James P. Beck, Rajagopal Bakthavatchalam
Abstract: The present invention describes novel imidazo-pyridines of formula I:
wherein D is aryl or heteroaryl or pharmaceutically acceptable salt forms thereof, which are useful as corticotropin releasing factor antagonists.
Type:
Grant
Filed:
July 25, 2000
Date of Patent:
February 18, 2003
Assignee:
Bristol-Myers Squibb Company
Inventors:
Paul Joseph Gilligan, Richard Eric Olson, William Eric Frietze
Abstract: Corticotropin releasing factor (CRF) antagonists of formula I:
and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.
Type:
Grant
Filed:
August 9, 2000
Date of Patent:
February 11, 2003
Assignee:
Bristol-Myers Squibb Company
Inventors:
Paul Joseph Gilligan, Rajagopal Bakthavatchalam
Abstract: The present invention describes novel pyrazolo[1,5-a]triazines of formula:
wherein R3 is an alkyl, alkenyl, alkynyl, or cycloalkyl group, or pharmaceutically acceptable salt forms thereof, which are useful as CRF antagonists.
Type:
Grant
Filed:
June 14, 1999
Date of Patent:
January 21, 2003
Assignee:
Bristol-Myers Squibb Company
Inventors:
Richard Eric Olson, William Eric Frietze