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Pharmacia & Upjohn Company Patents
Assignee:
Pharmacia & Upjohn Company
Address:
Kalamazoo, MI
No. of patents:
471
Patents:


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Patent Number Title Of Patent Date Issued
6861521 Stereoselective transacetalization of steroidal C-22 acetonide March 1, 2005
The present invention is a process for the preparation of rofleponide of formula (II) ##STR1##where the 22R/22S ratio is 90/10 or greater which comprises contacting an acetonide of formula (I) ##STR2##with CH.sub.3 --CH.sub.2 --CH.sub.2 --CHO (III) in the presence of perchloric a
6861433 Oxazolidinone photoaffinity probes March 1, 2005
The present invention provides compounds of the formula: ##STR1##compositions comprising such compounds, and methods for using the same.
6861420 N-substituted 1,2,4,5-tetrahydro-1H-benzo[d]azepine compounds March 1, 2005
The present invention provides compounds of Formula I: ##STR1##wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therape
6858635 Oxazolidinone photoaffinity probes February 22, 2005
Disclosed are novel compounds that are useful and effective as photoaffinity probes and methods of using oxazolidinone photoaffinity probes.
6858385 Pseudorabies virus protein February 22, 2005
The present invention provides recombinant DNA molecules comprising a sequence encoding a pseudorabies virus (PRV) glycoprotein selected from the group consisting of gI, gp50, and gp63, host cells transformed by the recombinant DNA molecule sequences, the gI, gp50 and gp63 polypeptides.
6855709 Pyridyl sulfone derivatives February 15, 2005
The invention provides compounds of the formula ##STR1##and methods of using those compounds for treating a disease or condition in a mammal wherein a 5-HT receptor, such as a 5-HT.sub.6 receptor, is implicated and modulation of a 5-HT function is desired, wherein A, G and W.sub.1 -W
6849640 Therapeutic 1H-pyrido [4,3-b] indoles February 1, 2005
The present invention provides 2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indoles and 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles. These compounds are 5-HT ligands that are useful for treating diseases wherein modulation of 5-HT activity is desired.
6846813 Compounds to treat alzheimer's disease January 25, 2005
The present invention is disubstituted amines of formula (I) ##STR1##and disubstituted amines of formula (II) ##STR2##useful in treating Alzheimer's disease and other similar diseases.
6846640 Time-resolved fluorescence assay for the detection of multimeric forms of A-beta 1-40 January 25, 2005
The present invention provides for a polypeptide aggregation screening assay for the purpose of detecting modulators of polypeptide aggregation, which can provide for new therapies in pathologic states associated with polypeptide aggregation, especially considered is Alzheimer's Disease.
6844148 Alzheimer's disease secretase, APP substrates therefor, and uses therefor January 18, 2005
The present invention provides the enzyme and enzymatic procedures for cleaving the .beta. secretase cleavage site of the APP protein and associated nucleic acids, peptides, vectors, cells and cell isolates and assays. An enzyme that cleaves the .alpha.-secretase site of APP also is
6835565 Alzheimer's disease secretase December 28, 2004
The present invention provides the enzyme and enzymatic procedures for cleaving the .beta. secretase cleavage site of the APP protein and associated nucleic acids, peptides, vectors, cells and cell isolates and assays.
6835546 Drosophila G protein coupled receptors, nucleic acids, and methods related to the same December 28, 2004
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 also provides methods for the
6833453 Methods of producing oxazolidinone compounds December 21, 2004
Methods of synthesizing pharmacologically useful oxazolidinones are disclosed, and, in particular, a method of manufacturing a 5-(tert-butylcarbamoyl)-aminomethyl-oxazolidinone by condensing a carbamate with a tert-butylcarbamoyl protected derivative of glycidylamine or 3-amino-1-hal
6833248 Human caspase-12 materials and methods December 21, 2004
The present invention provides novel human caspase-12 polynucleotides and polypeptides; constructs and recombinant host cells incorporating the polynucleotides; the human caspase-12 polypeptides encoded by the polynucleotides; antibodies to the polypeptides; and methods of making and
6828330 Quinuclidine-substituted hetero-bicyclic aromatic compounds for the treatment of disease December 7, 2004
The invention provides compounds of Formula I: ##STR1##wherein W.sup.0 is a bicyclic moiety and is ##STR2##These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful to treat diseases or conditions
6828317 Antimicrobial thiadiazinone derivatives and their application for treatment of bacterial infecti December 7, 2004
The present invention provides certain thiadiazinone derivatives of oxazolidinones of the following formula I: ##STR1##or pharmaceutically acceptable salts thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for prepa
6828117 Alzheimer's disease secretase, APP substrates therefor, and uses therefor December 7, 2004
The present invention provides the enzyme and enzymatic procedures for cleaving the .beta. 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 protein and associa
6825225 Bicyclic isoxazolinones as antibacterial agents November 30, 2004
The present invention provides compounds of formula I useful as anti microbial agents ##STR1##wherein X, Y, R.sup.1, and n are as defined in thereof.
6825023 Alzheimer's disease secretase, APP substrates therefor, and uses therefor November 30, 2004
The present invention provides the enzyme and enzymatic procedures for cleaving the .beta. 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 protein and associa
6821970 Oxazinocarbazoles for the treatment of CNS diseases November 23, 2004
The present invention provides oxazinocarbazole derivatives having a ring connecting position 8 (C-8) and position 9 (N-9), and more specifically, provides compounds of formula (I) wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are described herein. ##STR1##These compounds are 5-HT li
6821969 Thioxazinoquinolones as antiviral agents November 23, 2004
The present invention provides a compound of formula I ##STR1##These compounds are useful as antiviral agents, in particular, as agents against viruses of the herpes family.
6814319 Laboratory scale milling process November 9, 2004
There is provided a process for reducing particle size of a drug, the process comprising (a) a step of dispersing about 10 g or less of the drug in a suitable volume of a liquid dispersion medium to form a suspension; (b) a step of bringing together in a vessel grinding media, magnetical
6809112 Method of treating sexual disturbances October 26, 2004
The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) ##STR1##in a dosage range where the sexually therapeutic amount is from about 0.2 thru 8 mg/person/dose and where the sexually matin
6797834 Phosphoric acid isomerization of A 5 (10), 9 (11)--diene steroid to the corresponding 4, 9-diene September 28, 2004
The invention is a process for the preparation of a .DELTA..sup.4,9 -steroid of formula (II) ##STR1##which comprises contacting a .DELTA..sup.5(10),9(11) -steroid of formula (I) ##STR2##with a phosphorous containing acid.
6797003 Aspheric soft lens September 28, 2004
An aspheric soft intraocular lens, having an optical power surface, which may have multiple radii portions or aspherical portions, as well as spherical portions, intended to replace the crystalline lens of a patient's eye, in particular after a cataract extraction. Such an aspheric s
6796975 Container for linezolid intravenous solution September 28, 2004
The present invention is a container for an IV aqueous solution of a Gram-positive oxazolidinone agent, such as linezolid a the compound of formula: ##STR1##which comprises having the container-solution contact surface material be a polyolefin.
6790950 Anti-bacterial vaccine compositions September 14, 2004
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.
6790610 Alzheimer's disease, secretase, APP substrates therefor, and uses therefor September 14, 2004
The present invention provides the enzyme and enzymatic procedures for cleaving the .beta. 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 protein and associa
6774231 Method for the preparation of oxazolidinones August 10, 2004
The present invention relates to a process for making a compound of structure 4 ##STR1##which comprises reacting a compound of structure 1 with vinyl sulfone in the presence of a Lewis-acid at a temperature in a range of from 40.degree. C. to 170.degree. C., wherein each R.sup.1 is i
6764858 Methods for creating a compound library July 20, 2004
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 embodiments of these m
6764823 Antimicrobial methods and materials July 20, 2004
The present invention provides methods of identifying antimicrobial agents that target genes essential for the survival of Staphylococcus bacteria, including antimicrobial agents that interfere with the expression of essential coding sequence products and antimicrobial agents that interf
6762191 Therapeutic compounds July 13, 2004
The present invention provides compounds of formula (I): ##STR1##wherein: R.sub.1, R.sub.2, R.sub.3 R.sub.4, R.sub.5, R.sub.6, X, - - - , m, and n have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds or salts thereof. The
6757618 Chemical structure identification June 29, 2004
A method for generating a numeric or alpha-numeric identifier representative of a chemical structure having at least two atoms connected by a bond includes the step of assigning a numerical value to each atom and a numerical bond value to each bond. The method updates the numerical v
6753163 Alzheimer's disease secretase, APP substrates therefor, and uses therefor June 22, 2004
The present invention provides the enzyme and enzymatic procedures for cleaving the .beta. 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 protein and associa
6743811 Oxazalidinone compounds and methods of preparation and use thereof June 1, 2004
Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. Oxazolidinones as disclosed herein can be readily synthesized and used
6740754 Process to produce oxazolidinones May 25, 2004
The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)and processes for production of pharmacologically useful oxazolidinones.
6740652 Oxazolidinones to treat eye infections May 25, 2004
The present invention involves a method of treating an ophthalmic infection in a useful warm blooded mammal who is in need of such treatment which comprises topical administration of an ophthalmologically effective amount of an OXAZOLIDINONE.
6737510 Alzheimer's disease secretase, APP substrates therefor, and uses thereof May 18, 2004
The present invention provides the enzyme and enzymatic procedures for cleaving the .beta. 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 protein and associa
6734301 2,3,4,5-Tetrahydro-1H-[1,4]diazepino[1,7-a]indole compounds May 11, 2004
Certain 2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,7-a]indoles are 5-HT ligands and are useful for treating diseases wherein modulation of 5-HT activity is desired.
6734005 Matrix metalloproteinases May 11, 2004
The present invention provides genes encoding novel matrix metalloproteinases termed MMP; constructs and recombinant host cells incorporating the genes; the MMP polypeptides encoded by the genes; antibodies to the MMP polypeptides; and methods of making and using all of the foregoing
6730682 Heterocycle carboxamides as antiviral agents May 4, 2004
The present invention provides a compound of formula I ##STR1##which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
6727274 Arylsulphonyl substituted-tetrahydro- and hexahydro-carbazoles April 27, 2004
The invention provides compounds of formula I for use in treating conditions in which 5-HT.sub.6 receptors are involved such as in anxiety, depression, schizophrenia, Alzheimer's disease, stress-related disease, panic, a phobia, obsessive compulsive disorder, obesity, post-traumatic
6727248 Substituted quinolinecarboxamides as antiviral agents April 27, 2004
The present invention discloses disubstiuted 4-oxo-1,4-dihydro-3-quinolinecarboxamide derivatives. The compounds are useful as antiviral agents, in particular, as agents against viruses of the herpes family.
6727074 Alzheimer's disease secretase, APP substrates therefor, and uses therefor April 27, 2004
The present invention provides the enzyme and enzymatic procedures for cleaving the .beta. 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 protein and associa
6720316 Therapeutic 5-HT ligand compounds April 13, 2004
The present invention provides compounds of Formula (I) ##STR1##wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and Z have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention als
6716980 Process to produce oxazolidinones April 6, 2004
The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)and processes for production of pharmacologically useful oxazolidinones.
6716870 Prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives April 6, 2004
The present invention is directed to prodrugs of certain 3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that modulate the activity of protein kinases ("PKs"). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity ut
6713260 Methods of identifying compounds that bind to target species under isothermal denaturing conditi March 30, 2004
The present invention provides a method for identifying a test compound that binds to a target species. The method includes: incubating at least one test mixture under isothermal denaturing conditions, each test mixture comprising at least one test compound, and at least one target speci
6710067 Mannich base prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives March 23, 2004
The present invention is directed to Mannich base prodrugs of certain 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases ("PKs"). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK
6706485 Method of identifying agents that inhibit APP processing activity March 16, 2004
The present invention provides methods of identifying agents that inhibit the amyloid precursor protein (APP) processing activity of Asp2 polypeptide.
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