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Attorney: Demeter; John C.


Number of patents: 77
Last date: May 08, 2012

1    
NumberTitleIssue Date
8173695Kappa selective opioid receptor antagonist
A selective kappa opioid receptor antagonist useful for treating ethanol use disorder withdrawal and anxiety, and/or depression, or schizophrenia as independent comorbid conditions. ...
05/08/2012
8153683Methods of treatment using a prodrug of an excitatory amino acid
This invention relates to synthetic excitatory amino acid prodrugs and processes for their preparation. The invention further relates to methods of using, and pharmaceutical compositions comprising, the compounds for the treatment of neurological disorders and psych...
04/10/2012
81016386-substituted nicotinamide derivatives as opioid receptor antagonists
A compound of the formula (I) or a pharmaceutically acceptable salt, enantiomer, racemate, diasteromers or mixtures thereof, or a solvate thereof, formulations and methods of use thereof, as opioid receptor antagonists are disclosed wherein the variables are as desc...
01/24/2012
8093302Substituted tetralins as selective estrogen receptor-β agonists
The present invention relates to novel tetralin ER-β agonist compounds, pharmaceutical compositions thereof, and use of these compounds to treat a ER-β mediated disease such as nocturia, obstructive uropathy, benign prostatic hypertrophy, obesity, dementia, hypert...
01/10/2012
80888004-(5-aminomethyl)-indole-1-ylmethyl)-benzamide derivatives and related compounds as opioid receptor antagonists for the treatment of obesity
The present invention relates to compounds of formulae (I) and (II) useful as opioid receptor antagonists for the treatment of obesity, wherein p is 0, 1, or 2; y is 0, 1, or 2; and z is 0, 1, or 2; X1 is CH2, CH, or N; to form a indolinyl, ind...
01/03/2012
8071776Thienopyridines as allosteric potentiators of the M4 muscarinic receptor
The present invention relates to selective allosteric potentiators of the Formula (I): or pharmaceutically acceptable salts thereof, for the treatment of disorders associated with M4 muscarinic receptors. ...
12/06/2011
8058425Purine derivatives as kinase inhibitors
The present invention provides kinase inhibitors of Formula I. ...
11/15/2011
8022065Purine derivatives as kinase inhibitors
The present invention provides kinase inhibitors of Formula I. ...
09/20/2011
7981892Disubstituted phthalazine hedgehog pathway antagonists
The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer. ...
07/19/2011
7964632Methods of treatment using a prodrug of an excitatory amino acid
This invention relates to synthetic excitatory amino acid prodrugs and processes for their preparation. The invention further relates to methods of using, and pharmaceutical compositions comprising, the compounds for the treatment of neurological disorders and psych...
06/21/2011
7943670Liquid formulations of ractopamine
Described is a soluble stable liquid formulation, process for preparing, and a method of using the soluble stable liquid formulation comprising ractopamine or a physiologically acceptable salt thereof, a liquid nonionic cosolvent, and water. ...
05/17/2011
7902372Opioid receptor antagonists
A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3′, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mi...
03/08/2011
7842822Substituted benzopyrans as selective estrogen receptor-beta agonists
The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof useful as Estrogen Receptor beta agonists for treating Estrogen Receptor beta mediated diseases such as benign prostatic hyperplasia. ...
11/30/2010
7834187Crystalline variable hydrate of (S)-6-(4-(2-((3-9H-carbazol-4-yloxy)-2-hydroxypropyl)amino)-2-methylpropyl)phenoxy)-3-pyridinecarbox amide hemisuccinate salt
The present invention relates to a crystalline variable hydrate of (S)-(3-pyridinecarboxamide,6-[4-[2-[[3-(9H-carbazol-4-yloxy)-2-hydroxypropyl]amino]-2-methylpropyl]phenoxy]) -hemi-succinate, a pharmaceutical formulation containing...
11/16/2010
7709522Kappa selective opioid receptor antagonist
A selective kappa opioid receptor antagonist, (S)-3-Fluoro-4-[4-[2-(3,5-dimethylphenyl)pyrrolidin-1-yl-methyl]phenoxy]benzamide or a pharmaceutically acceptable salt thereof, useful for treating ethanol use disorder withdrawal, and anxiety and/or depression, or schi...
05/04/2010
7709447Use of spinosyns for wound healing
A spinosyn or a physiologically acceptable derivative or salt thereof for promoting or accelerating wound healing in humans. ...
05/04/2010
7585985Substituted benzopyrans as selective estrogen receptor-beta agonists
The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof useful as Estrogen Receptor beta agonists for treating Estrogen Receptor beta mediated diseases such as benign prostatic hyperplasia. ...
09/08/2009
7560463Diaryl ethers as opioid receptor antagonists
Compound 5-(2-Methoxy-4-{[2-(tetrahydro-pyran-4-yl)-ethylamino]-methyl}-phenoxy)-pyrazine-2-carboxamide or a pharmaceutically acceptable salt thereof, useful for the treatment of irritable bowel syndrome. ...
07/14/2009
7531557Diaryl ethers as opioid receptor antagonists
Compound 6-(2-fluoro-4-[[2-(tetrahydro-pyran-4-yl)-ethylamino]-methyl]-phenoxy)-nicotinamide, or a pharmaceutically acceptable salt thereof, is useful for the treatment of alcoholism. ...
05/12/2009
7462647Pentalfluoroalkanesulfinyl naphthalenes and related estrogen receptor modulators
The present invention provides a compound of the formula (I) wherein R is —H, or —C1-C4 alkyl; R1 is —H, —OH, —O(C1-C4 alkyl), —SO2(C1-C4 alkyl), or halo; X is —Oâ€...
12/09/2008
7442812Substituted benzopyrans as selective estrogen receptor-beta agonists
The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof useful as Estrogen Receptor β agonists for treating Estrogen Receptor β mediated diseases such as benign prostatic hyperplasia. ...
10/28/2008
7414132Opioid receptor antagonists
A compound of the formula (I); wherein the variables X1 to X10, R1 to R7 including R3′, E, W, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereom...
08/19/2008
73997746-substituted nicotinamide derivatives as opioid receptor antagonists
A compound of the formula (I) or a pharmaceutically acceptable salt, enantiomer, racemate, diastereomers or mixtures thereof, or a solvate thereof, formulations and methods of use thereof, as opioid receptor antagonists are disclosed wherein the variables are as des...
07/15/2008
7396943Opioid receptor antagonists
A compound of the formula I: (I) wherein the variables are as described herein, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixture thereof, formulations and methods of use thereof are disclosed.
07/08/2008
7381750Amino-phenoxymethyl-benzamide opioid receptor antagonists
A compound of the formula (I) wherein the variables X1, X2, R1 to R7 including R3′, j, k, p, y, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful fo...
06/03/2008
7381719Diaryl ethers as opioid receptor antagonist
A compound of the formula (I) wherein the variables X1 to X10, R1 to R7 including R3′, E, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer o...
06/03/2008
7378448Diphenylether amide derivatives as opioid receptor antagonists
A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3′, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mi...
05/27/2008
7375229Dihydro-dibenzo[B,E]oxepine based selective estrogen receptor modulators, compositions and methods
The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6
05/20/2008
7354951Substituted benzopyrans as selective estrogen receptor-beta agonists
The present invention relates to novel benzopyran ER-β agonist compounds, pharmaceutical compositions thereof, and use of these compounds to treat a ER-β mediated disease such as nocturia, obstructive uropathy, benign prostatic hypertrophy, obesity, dementia, hype...
04/08/2008
7288543Opioid receptor antagonists
A compound of the formula (I) (I) wherein the variables X1 to X6, Ra, Rb, R1 to R7 including R3′, E, p, j, y, z, A, B and C are as described or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the trea...
10/30/2007
7279499Substituted benzopyrans as selective estrogen receptor-beta agonists
The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof and processes for the preparation of the same. The compounds of the present invention are useful as Estrogen Receptor ? agonists. Such ago...
10/09/2007
7271264Pentacyclic oxepines and derivatives thereof, compositions and methods
The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6
09/18/2007
7265127βadrenergic agonists
The present invention relates to 2-imidazo[1,2-a]pyridine group containing β3 adrenergic receptor agonists or pharmaceutical salts thereof. ...
09/04/2007
7253181βadrenergic agonists
The present invention relates to pyrrolopyridine-3-yl group containing β3 adrenergic receptor agonists or pharmaceutical salts thereof. ...
08/07/2007
7241772βadrenergic agonists
The present invention relates to 2-imidazo[1,5-a]pyridine containing β3 adrenergic receptor agonists or pharmaceutical salts thereof. ...
07/10/2007
7217734Substituted benzopyrans as selective estrogen receptor-beta agonists
The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof and processes for the preparation of the same. The compounds of the present invention are useful as Estrogen Receptor β agonists. Such ag...
05/15/2007
72146972-Oxo-benzimidazolyl substituted ethanolamine derivatives and their use as βagonists
The present invention relates to a β3 adrenergic receptor agonist of formula (I), wherein R is C3–C8 alkyl or (C3–C7 cycloalkyl)C1–C5 alk-di-yl: R1 is H, CN, halo; C1...
05/08/2007
7208505β3 adrenergic agonists
The present invention relates to a β3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful, e.g., for treating Type 2 diabetes and/or obesity...
04/24/2007
72054073-Substituted oxindole β3 agonists
The present invention relates to a β3 adrenergic receptor agonist of Formula (I) or a pharmaceutical salt thereof; useful for treating Type II diabetes and/or obesity ...
04/17/2007
7196100Opioid receptor antagonists
A compound of the formula (I) wherein the variables X1 to X5, R1 to R7 including R3′, E, q, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer...
03/27/2007
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