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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
6239152 Oxazolidinone combinatorial libraries, compositions and methods of preparation May 29, 2001
Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable composi
6239142 4-oxo-4,7-dihydro-thieno[2,3-b]pyridine-5carboxamides as antiviral agents May 29, 2001
The invention provides a compound of formula I: ##STR1##wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 have any of the values defined in the specification, or a pharmaceutically acceptable salt thereof, as well as processes and intermediates useful for preparing such compounds or sal
6235928 .beta.-sulfonyl hydroxamic acids May 22, 2001
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof. Such compounds may be incorporated into pharmaceutical compositions which can inhibit various enzymes from the matrix metalloproteinase family. ##STR1##
6235907 Intermediates useful in making mappicine and related compounds May 22, 2001
This invention discloses and claims novel intermediates and procedures for the synthesis of camptothecin derivatives, such as irinotecan, and other compounds related to the synthesis of CPT-11. Related procedures and compounds are also disclosed, such as a novel method of making mappicin
6231887 Pharmaceutical composition for acidic lipophilic compounds in a form of a self-emulsifying formu May 15, 2001
The present invention provides a novel pharmaceutical composition based on the use of a particular amount of basic amine which comprises a pyranone compound as a pharmaceutically active agent, a basic amine in an amount of from about 0.1% to about 10% by weight of the total composition,
6228397 Pharmaceutical composition having two coating layers May 8, 2001
The present invention provides a pharmaceutical composition which is substantially free of unpleasant tastes and orally administrable which comprises:(a) an active medicament,(b) an inner coating layer comprising an oil substance having a melting point at a range of from about 50.degree.
6224864 Antibiotic 10381A, and process for the preparation of anitbiotics 10381B May 1, 2001
Antibiotic 10381a.sub.1, wherein R is hydrogen, is a cytosine-containing antibiotic producible by culturing the novel microorganism Streptomyces arginensis in an aqueous medium and isolation thereof. Derivatives wherein R is a C.sub.1 to C.sub.3 alkyl ester of antibiotic 10381a.sub.1, ar
6218413 Oxazolidinone antibacterial agents having a thiocarbonyl functionality April 17, 2001
The present invention provides compounds of Formula 1 ##STR1##or pharmaceutical acceptable salts thereof wherein A, G and R.sub.1 are as defined in the claims which are antibacterial agents.
6211386 Process for asymmetric hydrogenation April 3, 2001
The present invention is a process for the preparation of a compound of the formula: ##STR1##where R.sub.3, R4 and n are defined in the specification which comprises hydrogenating a compound of the formula: ##STR2##the E-geometrical isomer thereof or a mixture of the Z- and E-isomers
6203994 Fluorescence-based high throughput sereening assays for protein kinases and phosphatases March 20, 2001
The invention relates to novel fluorescence-based assays for protein kinases and phosphatases which can be used in high throughput screening. The methods of the invention utilize a competitive immunoassay to determine the amount of substrate that is phosphorylated or dephosphorylated
6200746 Methods of identifying anti-viral agents March 13, 2001
The invention provides methods to identify specific inhibitors of HPV E7 binding to CDK2 and methods to identify specific inhibitors of E7-induced CDK2 kinase activity. Specific inhibitors identified by the methods, compositions comprising the specific inhibitors, and methods of treatmen
6197339 Sustained release tablet formulation to treat Parkinson's disease March 6, 2001
The sustained release tablet of (R)-5,6-dihydro-5-(methylamino)-4H-imidazo[4,5-ij]-quinolin-2(1H)-one (Z)-2-butenedioate (1:1) which is disclosed permits twice daily administration of (R)-5,6-dihydro-5-(methylamino)-4H-imidazo[4,5-ij]-quinolin-2(1H)-one (Z)-2-butenedioate (1:1) t
6194445 Use of pramipexole in the treatment of restless legs syndrome February 27, 2001
The present invention provides the use of pramipexole in the treatment of restless legs syndrome.
6191143 Topical administration of antimicrobial agents for the treatment of systemic bacterial diseases February 20, 2001
The present invention provides a method of topically administering antimicrobial agents such as premafloxacin, premafloxacin-like compound, premafloxacin ester, ciprofloxacin, enrofloxacin, cefquinome, cefpodoxime, gentamicin or erythromycin for the treatment of systemic bacterial di
6191124 Methanol derivatives for treatment of retroviral infections especially HIV infections February 20, 2001
The present invention relates to compounds of formula (I) which are imidazo[2,1-b]benzothiazole-3-methanol and imidazo[2,1-b]thiazole-5-methanol derivatives useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus, wherein R.sub.1 is --H or --CH.sub.3 ; wh
6187818 Prostaglandins formulation and process February 13, 2001
This invention comprises new formulations and methods of preparing a new formulations of prostaglandins and in particular dinoprost tromethamine, where the pH of the formulation is adjusted to between about 5.5-7.5 and where the the concentration of benzyl alcohol is between about 1.2 to
6187552 Method for identifying inhibitors of JAK2/cytokine receptor binding February 13, 2001
The invention provides a method of identifying a therapeutic useful for treating or preventing asthma, which method includes the steps of contacting a identify compounds that inhibit the binding of human JAK2 protein to the .beta..sub.c first molecule comprising at least the N termin
6184216 Aminoguanidine carboxylate lactams for the treatment of non-insulin-dependent diabetes mellitus February 6, 2001
Compounds selected from the group consisting of formulae III, IV, VI and VIII ##STR1##wherein R is H is NH.sub.2, or a pharmacologically acceptable salt thereof, are suitable for use in methods for treating non-insulin-dependent diabetes mellitus (NIDDM) or obesity in a patient susce
6177573 Process to prepare taxol January 23, 2001
The invention is an oxazolidine ester of silylated baccatin III of formula (VII) ##STR1##which is a useful intermediate to produce pharmaceutically useful anti-cancer compounds.
6177453 Aminoguanidine carboxylate lactams for the treatment of non-insulin-dependent diabetes mellitus January 23, 2001
The present invention provides for the treatment of non-insulin dependent diabetes mellitus or obesity comprising the systemic administration of a compound having the formula ##STR1##or a pharmacologically acceptable salt thereof, wherein each R is H or NH.sub.2, and with the proviso
6177101 Delavirdine high strength tablet formulation January 23, 2001
Disclosed is a non-sustained release pharmaceutical tablet composition which comprises a rapidly precipitating drug in an amount from about 5 to about 60% and at least one member selected from the group consisting of a binder in an amount of from about 2 to about 25% and a superdisintegr
6172186 Pseudorabies virus protein January 9, 2001
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 said recombinant DNA molecule sequences, the gI, gp50 and gp63 polypeptides.
6169181 Compounds useful to treat retroviral infections January 2, 2001
The present invention relates to compounds of formula I and II which are pyran-2-ones, 5,6-dihydro-pyran-2-ones, 4-hydroxy-benzopyran-2-ones, 4-hydroxy-cycloalkyl[b]pyran-2-ones, and derivatives thereof, useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus
6156777 Use of pramipexole as a neuroprotective agent December 5, 2000
The present invention provides the use of pramipexole as a neuroprotective agent.
6150385 1,3,4-thiadiazoles useful for the treatment of CMV infections November 21, 2000
The present invention presents novel 1,3,4-thiadiazole derivatives of formula I ##STR1## which have useful antiviral activity against herpes virus, cytomegalovirus (CMV).
6150330 Aqueous prolonged release formulation November 21, 2000
Prolonged parenteral release into the circulatory system of a cow of a bioactive growth hormone releasing factor at desirably effective levels can be achieved using novel compositions in which the growth hormone releasing factor is present in an aqueous liquid at a dose of at least a
6147116 Polyaromatic antiviral compositions November 14, 2000
The present invention relates to polyaromatic compounds having useful antiviral activity against viruses of the herpes family, to a composition containing them, and to a method of using them for the treatment of herpes viruses infections.
6147095 Method for improving the pharmacokinetics of tipranavir November 14, 2000
The present invention relates to a novel method for improving the pharmacokinetics of tipranavir, comprising administering to a human in need of such treatment a combination of a therapeutically effective amount of tipranavir or a pharmaceutically acceptable salt thereof, and a thera
6140510 Optically active 3-(1-(carbamoyl))alkyl-2-oxo-pyrrolidines and optically active 3-(1-(alkylamido October 31, 2000
This invention relates to processes for the synthesis of various optically active amino pyrrolidinyl stereoisomers, or enantiomers, that may be attached to quinolonecarboxylic acids or naphthyridones. Processes and essential intermediates are disclosed and claimed for the synthesis of
6133446 Heterocyclic compounds for the treatment of CNS and cardiovascular disorders October 17, 2000
Novel aromatic bicyclic amines of formula (I) ##STR1## are useful in treating central nervous system disorders and cardiac arrhythmias and cardiac fibrillation.
6127400 Salts of diamine pyrrolidine October 3, 2000
This invention provides a novel and useful purification step in the manufacture of a diamine pyrrolidine side chain intermediate for a quinolone antibiotic that allows production of the antibiotic in significantly greater yields and at lower costs than was previously possible. Salts,
6124334 Hetero-aromatic ring substituted phenyloxazolidinone antimicrobials September 26, 2000
A hetero-aromatic (Q) substituted phenyloxazolidinone antimicrobial of Formula I ##STR1## wherein Q is a 5-member hetero-aromatic having from one to four nitrogen atoms or alternatively a benzoannulated 5-member hetero-aromatic having from one to four nitrogen atoms where R.sup.1
6124306 Thioalkyl alpha substituted pyrimidine compounds September 26, 2000
The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula I ##STR1## and pyrimidine-thioalkyl and alkylethers of Formula I, where R.sub.4 is selected from the group consisting of --H or --NR.sub.15 R.sub.16 where R.sub.15 is --H and R.sub.16 is --H
6121451 Intermediates and process for the manufacture of camptothecin derivatives (CPT-11) and related c September 19, 2000
This invention relates to intermediates and processes for the synthesis of camtothecin derivatives, such as irinotecan. Related procedures and compounds are disclosed, such as a method of making mappicine.
6121313 Pharmaceutical composition in a form of self-emulsifying formulation for lipophilic compounds September 19, 2000
The present invention provides a novel pharmaceutical composition based on the use of a particular oil phase which comprises a pyranone compound as a pharmaceutically active agent, a mixture of diglyceride and monoglyceride in a ratio of from about 9:1 to about 6:4 (diglyceride:monoglyce
6114326 Use of cabergoline in the treatment of restless legs syndrome September 5, 2000
The present invention provides for the use of cabergoline and other agents for the treatment of restless legs syndrome (RLS).
6107519 Process to produce oxazolidinones August 22, 2000
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.
6107285 Injectable ready-to-use solutions containing an antitumor anthracycline glycoside August 22, 2000
According to the invention there is provided a sterile, pyrogen-free, ready-to-use solution of an anthracycline glycoside, especially doxorubicin, which consists essentially of a physiologically acceptable salt of an anthracycline glycoside dissolved in a physiologically acceptable s
6103766 Phenylsulfonamide-phenylethylamines useful as dopamine receptors August 15, 2000
Compounds of Formula I and their pharmaceutically acceptable salts having selective dopamine D3 receptor activity suitable for treating central nervous system disorders. Formula I: ##STR1## R.sub.1 is independently H or a C.sub.1 -C.sub.8 alkyl including isomeric forms thereof;R.
6096512 Cloned DNA encoding a UDP-GalNAc: Polypeptide, N-acetylgalactosaminyltransferase August 1, 2000
The present invention relates to a method for the isolation and expression of a glycosyltransferase enzyme for use in the synthesis of oligosaccharide or polysaccharide structures on glycoproteins, glycolipids, or as free molecules. The gene coding for the enzyme N-acetylgalactosamin
6093732 4-hydroxyquinoline-3-carboxamides and hydrazides as antiviral agents July 25, 2000
The present invention provides 4-hydroxyquinoline-3-carboxamide and hydrazide compounds of formula I ##STR1## These compounds are useful to treat or prevent the herpesviral infections, particularly, human cytomegaloviral infection.
6090820 Spirocyclic and bicyclic diazinyl and carbazinyl oxazolidinones July 18, 2000
A compound of structural Formula I or II which is useful for treating microbial infections in humans or other warm-blooded animals, or pharmaceultically acceptable salts thereof as defined herein. ##STR1##
6087377 Tamoxifen as a therapy to reduce irinotecan hydrochloride-induced diarrhea July 11, 2000
The present invention provides a method for preventing or decreasing diarrhea associated with irinotecan administration comprising the administration of tamoxifen at least two cell cycles prior to irinotecan administration.
6084130 Aryl substituted bicyclic amines as selective dopamine D3 ligands July 4, 2000
Compounds and their pharmaceutically acceptable salts suitable for treating central nervous system disorders associated with the dopamine D3 receptor activity of structural Formula I: ##STR1##
6083967 S-oxide and S,S-dioxide tetrahydrothiopyran phenyloxazolidinones July 4, 2000
The present invention provides compounds of formula I and formula II useful as antimicrobial agents wherein R.sub.1 is methyl, ethyl, cyclopropyl, or dichloromethyl; R.sub.2 and R.sub.3 are independently hydrogen or fluoro; R.sub.4 is ethyl or dichloromethyl. The invention also relates t
6077963 Process to produce a protease inhibitor June 20, 2000
Disclosed is a novel process and novel intermediates to prepare [R-(R*,R*)]-N-[3-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propy l-2H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide (XIX) ##STR1## which is a protease inhibitor useful in treating human
6077700 Fusion proteins of mutants of cycline E and their complexes with cycline dependent protein kinas June 20, 2000
A polypeptide of the amino acid sequence of SEQ ID NO: 2, and a composition including the polypeptide of SEQ ID NO: 2 bound to cyclin-dependent kinase 2 (Cdk2).
6074851 Catalytic macro molecules having cdc25B like activity June 13, 2000
This invention discloses novel forms of catalytic macro molecules that are related to cdc25B, a cell cycle specific phosphatase. These special domains of cdc25B, special fusions with GST, and unique peptides and proteins, their utility, and the method of making them are all described.
6069141 Substituted aminophenyl isoxazoline derivatives useful as antimicrobials May 30, 2000
The present invention provides novel substituted amionphenyl isoxazoline derivatives of formula I ##STR1## wherein R.sub.1 is H, alkyl, cycloalkyl, alkoxy, amino, or alkylamino; X and Y are the same and different and are H, F, or CH.sub.3 ; W is O, or S;Q is a 4-, 5-, 6-, 7-, or 9-me
6060600 Substituted tetronic acids useful for treating HIV and other retroviruses May 9, 2000
This application discloses novel tetronic acids for the treatment of AIDS and other diseases caused by retroviruses.
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