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Assignee: Pharmacia & Upjohn Company


Location: Kalamazoo, MI
No. of patents: 450

1                      
NumberTitleIssue Date
7851433Method of purifying TFPI and TFPI analogs
Highly purified preparations of TFPI or TFPI analogs can be prepared using a method that generally involves the following steps: (1) expression of TFPI or TFPI analog in E. coli, (2) isolation of refractile bodies, (3) dissolution of the refractile bodies and...
12/14/2010
7659061Pharmaceutical compositions having a modified vehicle
A composition comprising: (a) one to three bioactive agents; and (b) a vehicle comprising; (i) a modified liquid carrier, and (ii) an unmodified liquid carrier ...
02/09/2010
75827563-(4-amidopyrrol-2-ylmethylidene)-2-indolinone derivatives as protein kinase inhibitors
The present invention provides a method to make a pyrrole substituted 2-indolinone compound of the formula ...
09/01/2009
7476391Anti-bacterial vaccine compositions
Gram negative bacterial virulence genes are identified, thereby allowing the identification of novel anti-bacterial agents that target these virulence genes and their products, and the provision of novel gram negative bacterial mutants useful in vaccines. ...
01/13/2009
7456269Alzheimer's disease secretase, APP substrates thereof, and uses thereof
The present invention provides the enzyme and enzymatic procedures for cleaving the β secretase cleavage site of the APP protein and associated nucleic acids, peptides, vectors, cells and cell isolates and assays. An enzyme that cleaves the α-secretase site of APP...
11/25/2008
7452913Polymorphs of pyrrole substituted 2-indolinone protein kinase inhibitors
The present invention relates to polymorphs of the 3-pyrrole substituted 2-indolinone compound 5-(5-fluoro-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-pyrrolidin-1-yl-ethyl)-amide. ...
11/18/2008
7442691Macrocycles useful in the treatment of alzheimer's disease
The present invention are macrocycles of the formula (IX): for treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alz...
10/28/2008
7435832Crystals including a malic acid salt of a 3-pyrrole substituted 2-indolinone, and compositions thereof
The present invention provides crystals, and compositions thereof, wherein the crystals include a malic acid salt of N-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide. Methods of preparing such ...
10/14/2008
7377894Methods for creating a compound library and identifying lead chemical templates and ligands for target molecules
A method for developing a library of compounds, the compound library, a method for identifying ligands for target molecules, and a method for identifying lead chemical templates, which, for example, can be used in drug discovery and design are provided. Certain embo...
05/27/2008
7378511Alzheimer's disease secretase, APP substrates therefor, and uses therefor
The present invention provides the enzyme and enzymatic procedures for cleaving the β secretase cleavage site of the APP protein and associated nucleic acids, peptides, vectors, cells and cell isolates and assays. The invention further provides a modified APP prote...
05/27/2008
7375187Alzheimer's disease secretase, APP substrates therefor, and uses therefor
The present invention provides the enzyme and enzymatic procedures for cleaving the β secretase cleavage site of the APP protein and associated nucleic acids, peptides, vectors, cells and cell isolates and assays. The invention further provides a modified APP prote...
05/20/2008
7368536Alzheimer's disease secretase, APP substrates therefor, and uses therefor
The present invention provides the enzyme and enzymatic procedures for cleaving the β secretase cleavage site of the APP protein and associated nucleic acids, peptides, vectors, cells and cell isolates and assays. The invention further provides a modified APP prote...
05/06/2008
7364866G protein coupled receptors, nucleic acids, and methods related to the same
The present invention provides Drosophila melanogaster GPCR (DmGPCR) polypeptides and polynucleotides which identify and encode such a DmGPCR. In addition, the invention provides expression vectors, host cells, and methods for its production. The invention al...
04/29/2008
RE40278Heterocyclic amines having central nervous system activity
Tricyclic nitrogen containing compounds, having anxiolytic and anti-depressant activity and central nervous system activity of the following structural formula: and pharmaceutically acceptable salts thereof wherein R1 ...
04/29/2008
7358264Statine derivatives for the treatment of Alzheimer's disease
The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment ...
04/15/2008
7354724Drosophila G protein coupled receptors, nucleic acids, and methods related to the same
The present invention provides a Drosophila melanogaster GPCR (DmGPCR) polypeptides and polynucleotides which identify and encode such a DmGPCR. In addition, the invention provides expression vectors, host cells and methods for its production. The invention a...
04/08/2008
7351738Substituted ureas and carbamates
The invention provides compounds of formula I: useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer...
04/01/2008
7338953Method of treating chronic fatigue syndrome
Disclosed herein are methods of treating an individual suffering from, chronic fatigue syndrome. The methods generally include administration of a therapeutic amount of racemic reboxetine, or a pharmaceutically acceptable salt thereof, to the individual. ...
03/04/2008
73389653,4-disubstituted, 3,5-disubstituted and 3,4,5-substituted piperidines
The invention relates to substituted piperidine, piperazine, morpholine and thiomorpholine compounds useful in the treatment of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precu...
03/04/2008
7322965Infection-resistant medical devices
A method for preventing medical device-associated microorganism infection includes the steps of providing a medical device and incorporating an effective amount of an oxazolidinone compound, such as linezolid, into the medical device. ...
01/29/2008
7312360Substituted hydroxyethylamines
Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein the variables G, L, A, W, E, R2, R3, R4, R5, RN, and Rc are defined herein. These compounds i...
12/25/2007
7309811Transgenic mice knockouts of BACE-1
The invention provides transgenic animals that are heterozygous or homozygous for a nonfunctional allele of BACE-1. These animals show normal development indicating that BACE-1 is not necessary for development and hence is an appropriate therapeutic target. The tran...
12/18/2007
7291738Therapeutic compounds
The present invention provides compounds, for example, of formula (I): wherein R1, R2, and R3 have any of the values defined in the specification, as well as pharmaceutical compos...
11/06/2007
7276503Method of treating chronic fatigue syndrome
Disclosed herein are methods of treating an individual suffering from, chronic fatigue syndrome. The methods generally include administration of a therapeutic amount of optically pure (S,S) reboxetine, or a pharmaceutically acceptable salt thereof, to the individual...
10/02/2007
7262208Hydroxypropyl amides for the treatment of Alzheimer's disease
The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the...
08/28/2007
72561893-(4-amidopyrrol-2-ylmethylidene)-2-indolinone der derivatives as protein kinase inhibitors
The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related c...
08/14/2007
7247706Double mutant alpha-7 nicotinic acetylcholine receptors
The invention relates ton novel methods for measuring ion channel transmission and methods and compositions useful in the indentification of ligand gated channel agonists and modulators. ...
07/24/2007
7247627Salts and polymorphs of a pyrrole-substituted indolinone compound
The invention relates to non-hygroscopic salts of 5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, such as maleate salts, and to crystalline polymorphs of these salts. The ...
07/24/2007
7244755Hydroxypropylamines
Disclosed are compounds of formula I: and the pharmaceutically acceptable salts thereof wherein the variables RN, R1, R2, R3, RP and RC are define...
07/17/2007
7244725Acetyl 2-hydroxy-1, 3-diaminoalkanes
Disclosed are compounds of the formula: where variables Z, X, R15, R2, R3, and RC are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase en...
07/17/2007
7241762Method of treating peripheral neuropathy
Disclosed herein are methods of treating an individual suffering from peripheral neuropathy. The methods generally include administration of a therapeutic amount of racemic reboxetine, or a pharmaceutically acceptable salt thereof, to the individual. ...
07/10/2007
7235655Processes to prepare eplerenone
The present invention involves intermediates, including a 7α-substituted steroid (II), and processes which are used to prepare eplerenone, a useful pharmaceutical agent. ...
06/26/2007
7232930Compounds and methods for preparing methanesulfonamides
A process for preparing (S)-(−)-N-[4-[4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxy]phenyl]methanesulfonamide hemifumarate salt, which comprises reacting N-[4-[(2S)-tetrahydro-5-hydroxy-2-furanyl]phenyl]methanesulfonamide(IIa) with fluoroamine (III) in the pre...
06/19/2007
7208591G protein-coupled receptor-like receptors and modulators thereof
The invention provides neuropeptide ligands, G protein-coupled receptors and methods of screening for modulators of receptor activity. Identified modulators, including neuropeptide ligand mimetics, are useful as biostatic and biocidal agents of varying scope, rangin...
04/24/2007
7208490Tricyclic tetrahydroquinoline antibacterial agents
The invention includes tetrahydroquinoline and related compounds of formula I, and pharmaceutical compositions thereof, that exhibit useful antibacterial activity against a wide range of human and veterinary pathogens ...
04/24/2007
7205120Substrates and assays for β-secretase activity
The present invention is directed to novel substrates for Hu-Asp. More particularly, the invention provides peptide substrates and fusion polypeptide substrates comprising a β-secretase cleavage site. Methods and compositions for making and using the peptides are d...
04/17/2007
7186539Method for refolding enzymes
The invention provides methods for efficient recombinant expression, refolding, and purification of Beta-site APP cleaving enzyme (BACE) polypeptides. In various aspects, the method includes the steps of expressing a recombinant construct in bacteria, dissolving inc...
03/06/2007
7176242N,N′-substituted-1,3-diamino-2-hydroxypropane derivatives
Disclosed are compounds of the formula wherein the variables RN, RC, R1, R25, R2, and R3 are as defined herein. These compounds have activity as i...
02/13/2007
7160544Method of vaccinating vertebrates
The invention provides a vaccine composition and a method of preparation including the steps of: forming a water-in-oil emulsion including an alginate in water, an oil, an antigen, and either (a) a cellulose ether and at least one nonionic surfactant or (b) a PEO-PP...
01/09/2007
7151109Pyrazolo[1,5-a]pyridine derivatives and their use as neurotransmitter modulators
The present invention relates to novel pyrazolo[1,5-a]pyridine derivatives of general formula I: that bind with high affifnity to CRF1 receptors, including human CRF1 receptors. This inventi...
12/19/2006
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