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Attorney: Stemerick; David M.


Number of patents: 44
Last date: May 15, 2012

1    
NumberTitleIssue Date
8178534cMET inhibitors
Compounds of the following formula are provided for use with cMET: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; meth...
05/15/2012
8163755Hexahydrooxazinopterine compounds
The present invention provides mTOR inhibitors of the formula wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods o...
04/24/2012
8088783MAPK/ERK kinase inhibitors
Compounds of the substituted 1,3-dialkyl-2,4-dioxo-6-(pyrimidinylamino)-1,2,3,4-tetrahydropyrimidine-5-hydroxamic acids, show below: wherein the variables are as defined herein, and pharmaceutical compositions thereof, are ...
01/03/2012
8071766HSP90 inhibitors
The invention relates to HSP90 inhibiting compounds consisting of the formula: wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture compris...
12/06/2011
8063066MAPK/ERK kinase inhibitors
Compounds are provided for use with MEK that comprise: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and inte...
11/22/2011
8030317MAPK/ERK kinase inhibitors
Compounds of the following formula are provided for use with MEK: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; metho...
10/04/2011
8026234Polo-like kinase inhibitors
Compounds of the following formula are provided for use with kinases: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; m...
09/27/2011
8022057MAPK/ERK kinase inhibitors
Compounds of the following formula are provided for use with MEK: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; metho...
09/20/2011
8003785Halo-substituted pyrimidodiazepines
The present invention provides PLK1 inhibitor compounds of formula I: useful in the treatment or control of cell proliferative disorders, particularly oncological disorders. These compounds and formulations containing such ...
08/23/2011
7943659MAPK/ERK kinase inhibitors
Compounds, pharmaceutical compositions, kits and methods are provided for use with MEK that comprise a compound selected from the group consisting of: wherein the variables are as defined herein. ...
05/17/2011
7943626Substituted 1,3-dialkyl-2,4-dioxo-6-(pyridylamino)-1,2,3,4-tetrahydropyrimidine-5-hydroxamic acid inhibitors of MAPK/ERK kinase
Compounds of the substituted 1,3-dialkyl-2,4-dioxo-6-(arylamino)-1,2,3,4-tetrahydropyrimidine-5-hydroxamic acids, show below: wherein the variables are as defined herein, and pharmaceutical compositions thereof, are provide...
05/17/2011
78680141-(hetero)aryl-3-amino-pyrrolidine derivatives for use as mGluR3 antagonists
The present invention relates to compounds of the Formula (I) which are useful for treating conditions associated with mGluR3 receptors, such as depression, schizophrenia and migraine, pharmaceutical compositions thereof, and methods of using the same.
01/11/2011
7384983Inhibitor of monoamine uptake
The present invention provides compounds and methods for the inhibition of monoamine uptake in mammals. ...
06/10/2008
65591717-oxo-2-azabicyclo[2.2.1]heptanes as selective muscarinic receptor antagonist
The present invention relates to muscarinic receptor modulators, specifically, 7-oxo-2-azabicyclo[2.2.1]heptanes of formula (I) which are useful for the treatment of various diseases and conditions, for example, Alzheimer's disease, glaucoma, psychosis, p...
05/06/2003
6187776Heterocyclic compounds and their use
The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nerv...
02/13/2001
6034108Method for treating mental retardation
The present invention is directed to a method for using 3-(4-hexyloxy-1,2,5-thiadiazol-3yl)-1,2,5,6-tetrahydro-1-methylpyridine, i.e., xanomeline, for the treatment of autism and mental retardation....
03/07/2000
6008412Process to make chiral compounds
The present invention relates to processes for resolving N-methyl-3(R,S)-hydroxy-3-phenylpropylamine and N,N-dimethyl-3 (R,S) -hydroxy-3-phenylpropylamine with the isomers of mandelic acid and the resulting salts....
12/28/1999
5977139Carboxysubstituted cyclic carboxamide derivatives
The present invention relates to novel carboxy substituted cyclic carboxamide derivatives of formula (1), ##STR1## and stereoisomers and pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are ...
11/02/1999
5872251Process for preparing intermediates of inhibitors of enkephalinase and angiotensin converting enzyme and intermediates thereof
The present invention relates to novel processes for preparing intermediates of the formula I ##STR1## and to novel intermediates thereof which are useful in the preparation of inhibitors of enkephalinase and angiotensin converting enzyme....
02/16/1999
5864045Heterocyclic substituted piperazinone derivatives
The present invention relates to substituted piperazinone derivatives of formula (1) or stereoisomers, or pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment of tachykini...
01/26/1999
5861417Heterocyclic substituted pyrrolidine amide derivatives
The present invention relates to novel heterocyclic substituted pyrrolidine amide derivatives of formula (1), ##STR1## and stereoisomers and pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists ...
01/19/1999
5861416Substituted pyrrolidin-3-yl-alkyl-piperidines
The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their ...
01/19/1999
5859252Processes for preparing intermediates of inhibitors of enkephalinase and angiotensin converting enzyme and intermediates thereof
The present invention relates to novel processes for preparing intermediates of the formula I ##STR1## and to novel intermediates thereof which are useful in the preparation of inhibitors of enkephalinase and angiotensin converting enzyme....
01/12/1999
5849908Processes for preparing intermediates of inhibitors of enkephalinase and angiotensin converting enzyme and intermediates thereof
The present invention relates to novel processes for preparing intermediates of the formula I ##STR1## and to novel intermediates thereof which are useful in the preparation of inhibitors of enkephalinase and angiotensin converting enzyme....
12/15/1998
5840726Heterocyclic substituted piperazinone derivatives
The present invention relates to substituted piperazinone derivatives (compounds of formula (1)) or stereoisomers, or pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment ...
11/24/1998
5824690Substituted pyrrolidin-3-yl-alkyl-piperidines
The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their ...
10/20/1998
5756739Process for preparing polyamine derivative and intermediates thereof
The present invention provides a novel process for preparing polyamine derivatives and pharmaceutically acceptable salts thereof, which are useful as antineoplastic agents and to novel intermediates thereof....
05/26/1998
5756762(S)-4-amino-hepta-5,6-dienoic acid and intermediates therof
The present invention relates to a novel enantiospecific processes for preparing (S)-4-amino-hepta-5,6-dienoic acid and pharmaceutically acceptable salts thereof, which is useful as an irreversible inhibitor of GABA-T, to novel intermediates thereof, and ...
05/26/1998
5750521Mercaptoacetylamide disulfide derivatives useful as inhibitors of enkephalinase and ACE
The present invention relates to certain mercaptoacetylamide disulfide derivatives of Formula (I) ##STR1## useful as inhibitors of enkephalinase and ACE....
05/12/1998
5734049Processes for preparing intermediates of inhibitors of enkephalinase and angiotensin converting enzyme and intermediates thereof
The present invention relates to novel processes for preparing intermediates of the formula I ##STR1## and to novel intermediates thereof which are useful in the preparation of inhibitors of enkephalinase and angiotensin converting enzyme....
03/31/1998
5693674Method of using triaryl-ethylene derivatives in the treatment and prevention of osteoporosis
The present invention relates to a method of using triaryl-ethylene derivatives in the treatment or prevention bone tissue loss or osteoporosis....
12/02/1997
5691384Method of using triaryl-ethylene derivatives in the treatment and prevention of osteoporosis
The present invention relates to a method of using triaryl-ethylene derivatives in the treatment or prevention bone tissue loss or osteoporosis....
11/25/1997
5684004Triaryl-ethylene derivatives
The present invention relates to novel triaryl-ethylene derivatives that are useful as anti-neoplastic agents, antiatherosclerotic agents, and hypocholesterolemic agents....
11/04/1997
5679854Process for the preparation of (epsilon)-1-amino-2-(fluoromethylene)-4-(p-fluorophenyl)butane and novel intermediate thereof
The present invention relates to a novel process for preparing (E)-1-amino-2-(fluoromethylene)-4-(p-fluorophenyl)butane, also known in the art as (E)-(p-fluorophenethyl)-3-fluoroallylamine, novel intermediates thereof, a novel process for the preparing ...
10/21/1997
5654477Processes for preparing (S)-4-amino-hepta-5,6-dienoic acid and intemediates thereof
The present invention relates to a novel enantiospecific processes for preparing (S)-4-amino-hepta-5,6-dienoic acid and pharmaceutically acceptable salts thereof, which is useful as an irreversible inhibitor of GABA-T, to novel intermediates thereof, and ...
08/05/1997
5641880Processes for preparing intermediates of inhibitors of enkephalinase and angiotensin converting enzyme and intermediates thereof
The present invention relates to novel processes for preparing intermediates of the formula I ##STR1## and to novel intermediates thereof which are useful in the preparation of inhibitors of enkephalinase and angiotensin converting enzyme....
06/24/1997
5635510Substituted pyrrolidin-3-yl-alkyl-piperidines
The present invention relates to substituted pyrrolidinyl-3-yl-alkyl-piperidines, their stereoisomers, and pharmaceutically acceptable salts thereof and processes for preparation of the same. The compounds of the present invention are useful in their ...
06/03/1997
56293092-substituted indane-2-mercaptoacetylamide disulfide derivatives useful as inhibitors of enkephalinase and ACE
The present invention relates to certain novel 2-substituted indane-2-mercaptoacetylamide disulfide derivatives useful as inhibitors of enkephalinase and of ACE....
05/13/1997
5604221Indane-2-mercaptoacetylamide disulfide derivatives useful as inhibitors of enkephalinase
The present invention relates to certain novel indane-2-mercaptoacetylamide disulfide derivatives of the formula ##STR1## useful as inhibitors of enkephalinase....
02/18/1997
5599986Process for the preparation of alkali metal salts of diformylamide
The present invention relates to a novel process for preparing alkali metal salts of diformylamide and a novel crystalline form of sodium diformylamide....
02/04/1997
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