Abstract: This invention provides compounds of formula I where Ar1 is a 5- to 10-member mono- or bicyclic aromatic group, optionally substituted; where the —NR3R4 group is situated ortho to the NHC(?X) group; n=1 or 2; X?O or S; Y is O or S; and q=1 or 0. The invention also provides pharmaceutical compositions comprising compounds of formula I and/or salts, esters, and prodrugs thereof. These compounds modulate the activation and inactivation of potassium channels. The compounds are useful for the treatment and prevention of diseases and disorders—such as seizure disorders—which are affected by modulation of potassium ion channels.
Abstract: This invention provides compounds of formula I where the dashed line represents an optional double bond; where R1 is phenyl, naphthyl, pyridyl, pyrimidyl, pyrrolyl, imidazolyl, pyrazyl, furyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, or isothiazolyl, optionally substituted, and other substituents are defined herein. Such compounds are potassium channel modulators.
Type:
Application
Filed:
August 13, 2010
Publication date:
May 19, 2011
Applicant:
Valeant Pharmaceuticals International
Inventors:
Jean-Michel Vernier, Huanming Chen, Jianlan Song
Abstract: This invention provides a compound of formula IA where X=0 or S; Y is 0 or S; q=1 or 0; and other substituents are defined herein. Such compounds can affect the opening of, or otherwise modulate, voltage-gated potassium channels. Such compounds useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.
Type:
Application
Filed:
February 1, 2010
Publication date:
January 6, 2011
Applicant:
Valeant Pharmaceuticals International, Inc.
Inventors:
Jean-Michel Vernier, Martha Alicia De La Rosa, Huanming Chen, Jim Zhen Wu, Gary Lee Larson, Ian Wayne Cheney
Abstract: This invention provides compounds of formula I where the dashed line represents an optional double bond; where R1 is phenyl, naphthyl, pyridyl, pyrimidyl, pyrrolyl, imidazolyl, pyrazyl, furyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, or isothiazolyl, optionally substituted, and other substituents are defined herein. Such compounds are potassium channel modulators.
Type:
Grant
Filed:
August 11, 2008
Date of Patent:
August 31, 2010
Assignee:
Valeant Pharmaceuticals International
Inventors:
Jean-Michel Vernier, Huanming Chen, Jianlan Song
Abstract: A modified release pharmaceutical formulation includes about 30-70% N-(2-amino-4-(fluorobenzylamino)-phenyl)carbamic acid ethyl ester (retigabine), or a pharmaceutically acceptable salt, solvate or hydrate thereof, about 5-30% of a drug delivery matrix including hydroxypropylmethylcellulose (HPMC), about 1.0-10% of an anionic surfactant, and an enteric polymer. The pharmaceutical formulation produces a sustained plasma concentration of retigabine following administration to a subject for 4-20 hours longer than the time required for in vitro release of 80% of retigabine. A formulation includes about 30-70% N-(2-amino-4-(fluorobenzylamino)-phenyl)carbamic acid ethyl ester (retigabine), or a pharmaceutically acceptable salt, solvate or hydrate thereof, about 5-30% of a drug delivery matrix, and an agent for retarding release in the gastric environment. The plasma concentration vs. time profile of this formulation is substantially flat over an extended period lasting for about 4 hours to about 36 hours.
Abstract: The present invention relates to benzyloxyanilide derivatives having the following structural formula: The compounds of the present invention are useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.
Type:
Application
Filed:
June 24, 2009
Publication date:
December 31, 2009
Applicant:
VALEANT PHARMACEUTICALS INTERNATIONAL
Inventors:
Jim Zhen Wu, Jean-Michel Vernier, Huanming Chen, Jianlan Song
Abstract: This invention provided compounds of formula I where W and Z are, independently, CH or N, and where other substituents are defined herein. Such compounds are potassium channel modulators. The invention also provides a composition comprising a pharmaceutically acceptable carrier or excipient and at least one of the following: a pharmaceutically effective amount of a compound of formula I; a pharmaceutically acceptable salt of a compound of formula I; a pharmaceutically acceptable ester of a compound of formula I. The invention also provides a method of preventing or treating a disease or disorder which is affected by activities of potassium channels, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula I or a salt or ester or solvate thereof.
Type:
Application
Filed:
July 28, 2008
Publication date:
July 2, 2009
Applicant:
VALEANT PHARMACEUTICALS INTERNATIONAL, INC.
Abstract: This invention provides compounds of formula I where the dashed line represents an optional double bond; where R1 is phenyl, naphthyl, pyridyl, pyrimidyl, pyrrolyl, imidazolyl, pyrazyl, furyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, or isothiazolyl, optionally substituted, and other substituents are defined herein. Such compounds are potassium channel modulators.
Type:
Application
Filed:
August 11, 2008
Publication date:
May 28, 2009
Applicant:
Valeant Pharmaceuticals International, Inc.
Inventors:
Jean-Michel Vernier, Huanming Chen, Jianlan Song
Abstract: This invention provides potassium channel modulators which are compounds of formula I where at least one of W and Z is N; where the moiety is one of Groups A or B below A where Ar is a 1,2-fused, six membered ring aromatic group, bearing substituents R1 and R2 as defined below, and containing zero or one ring nitrogen atom; and where other substituents are defined herein. The invention also provides a composition comprising a pharmaceutically acceptable carrier and at least one of the following: i) a pharmaceutically effective amount of a compound of formula I and ii) a pharmaceutically acceptable salt, ester, or prodrug thereof. The invention also provides a method of preventing or treating a disease or disorder which is affected by activities of potassium channels, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula I or a salt, ester, or prodrug thereof.
Type:
Application
Filed:
June 12, 2008
Publication date:
December 25, 2008
Applicant:
VALEANT PHARMACEUTICALS INTERNATIONAL
Inventors:
Jean-Michel VERNIER, Samedy OUK, Martha A. DE LA ROSA
Abstract: This invention is directed to compounds of formula I, where G is —O—, —S—, —C(g1)(g2)-, or —NH—, and n=1, 2, or 3. Such compounds modulate potassium channels. The compounds are useful for the treatment and prevention of diseases and disorders which are affected by modulation of potassium ion channels. One such condition is seizure disorders.
Type:
Application
Filed:
November 28, 2007
Publication date:
September 25, 2008
Applicant:
VALEANT PHARMACEUTICALS INTERNATIONAL
Inventors:
Huanming CHEN, Jianlan SONG, Jean-Michel VERNIER, Jim Zhen WU
Abstract: The present invention provides methods for treating individuals having a hepatitis C virus (HCV) infection, which individuals have failed to respond to therapy with an IFN-? other than consensus interferon (CIFN), or who, following cessation of therapy with an IFN-? other than CIFN, have suffered relaspe. The methods generally involve a treatment regimen comprising administering a first dosing regimen of CIFN, followed by a second dosing regimen of CIFN. Ribavirin is administered with at least the second dosing regimen.
Type:
Application
Filed:
February 20, 2008
Publication date:
September 4, 2008
Applicant:
VALEANT PHARMACEUTICALS INTERNATIONAL, INC.
Abstract: Novel heterocyclic aromatic compounds are disclosed. The novel compounds or pharmaceutically acceptable esters or salts thereof may be used in pharmaceutical compositions, and such compositions may be used to treat an infection, an infestation, a neoplasm, or an autoimmune disease. The novel compounds may also be used to modulate aspects of the immune system, including modulation of Type 1 and Type 2 activity.
Abstract: A number of modified nucleosides are disclosed composed of modified sugar moieties which contain substituents at C1 and C4 positions, or branched substituents at C3 and C5 positions of deoxyribose or ribose. Each nucleoside is converted to or properly protected and then converted to the corresponding phosphoramidites. These phosphoramidites are used to assemble oligonucleotides in which there is at least one of the forenoted nucleosides. These sugar modified oligonucleotides have the potential to be used as antisense therapies since they are expected to enhance nuclease resistance and cellular uptake while they maintain sequence-specificity and affinity to nucleic acid targets in vitro or in vivo.