Abstract: 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.
Abstract: The present invention provides the enzyme and enzymatic procedures for cleaving the &bgr; 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 associated nucleic acids, peptides, vectors, cells, and cell isolates, and assays that are particularly useful for identifying candidate therapeutics for treatment or prevention of Alzheimer's disease.
Type:
Grant
Filed:
April 12, 2000
Date of Patent:
May 18, 2004
Assignee:
Pharmacia & Upjohn Company
Inventors:
Mark E. Gurney, Michael J. Bienkowski, Robert L. Heinrikson, Luis A. Parodi, Riqiang Yan
Abstract: The invention relates to a method for determining an analyte by means of binding reactions, which method comprises: i) applying the sample to an application zone for sample (ASZ) on a flow matrix in which transport of components present in the sample can take place (transport flow), the flow matrix further exhibiting: a) optionally an application zone (AR*Z) for a binding reactant (Reactant*=R*) which is analytically detectable; b) a detection zone (DZ), which is located downstream of ASZ and exhibits an additional binding reactant (Capturer) firmly anchored to the matrix, and in which a complex (signal complex) containing the Capturer and the analyte and/or Reactant* is formed during the reaction, and ii) detecting the signal complex in the detection zone, the measured signal being used for determining the analyte.
Abstract: The present invention provides genes encoding heretofore unknown G protein-coupled receptors, constructs and recombinant host cells incorporating the genes; the GPCR polypeptides encoded by the genes; antibodies to the polypeptides; and methods of making and using all of the foregoing.
Type:
Application
Filed:
October 24, 2003
Publication date:
May 13, 2004
Applicant:
PHARMACIA & UPJOHN COMPANY
Inventors:
Gabriel Vogeli, Linda S. Wood, Kalpana Merchant
Abstract: 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.
Abstract: 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.
Type:
Grant
Filed:
March 8, 2001
Date of Patent:
May 11, 2004
Assignee:
Pharmacia & Upjohn Company
Inventors:
Michael Dalton Ennis, Robert Louis Hoffman, Nabil B. Ghazal, Rebecca M. Olson
Abstract: 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 methods include the use of NMR spectroscopy.
Type:
Application
Filed:
October 27, 2003
Publication date:
May 6, 2004
Applicant:
PHARMACIA & UPJOHN COMPANY
Inventors:
Brian J. Stockman, Kathleen A. Farley, Claudio Dalvit
Abstract: The present invention provides a compound of formula I
which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
Type:
Grant
Filed:
June 22, 2001
Date of Patent:
May 4, 2004
Assignee:
Pharmacia & Upjohn Company
Inventors:
Mark E. Schnute, Valerie A. Vaillancourt
Abstract: The present invention provides isolated nucleic acid molecules comprising a polynucleotide encoding either of two alternative splice variants of human sel-10, one of which is expressed in hippocampal cells, and one of which is expressed in mammary cells. The invention also provides isolated sel-10 polypeptides and cell lines which express them in which A&bgr; processing is altered.
Type:
Grant
Filed:
June 9, 1999
Date of Patent:
May 4, 2004
Assignee:
Pharmacia and Upjohn Company
Inventors:
Mark E. Gurney, Adele M. Pauley, Jinhe Li
Abstract: The invention provides compounds of formula I for use in treating conditions in which 5-HT6 receptors are involved such as in anxiety, depression, schizophrenia, Alzheimer's disease, stress-related disease, panic, a phobia, obsessive compulsive disorder, obesity, post-traumatic stress syndrome, epilepsy, and other CNS disorders.
Abstract: The present invention provides the enzyme and enzymatic procedures for cleaving the &bgr; 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 associated nucleic acids, peptides, vectors, cells, and cell isolates, and assays that are particularly useful for identifying candidate therapeutics for treatment or prevention of Alzheimer's disease.
Type:
Grant
Filed:
February 27, 2001
Date of Patent:
April 27, 2004
Assignee:
Pharmacia & Upjohn Company
Inventors:
Mark E. Gurney, Michael J. Bienkowski, Robert L. Heinrikson, Luis A. Parodi, Riqiang Yan
Abstract: 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.
Abstract: A sealed glass container containing therein a stable, injectable, sterile, pyrogen-free doxorubicin anti-tumor composition in a solution which consists essentially of a physiologically acceptable salt of doxorubicin dissolved in a physiologically acceptable solvent therefor, wherein said solution has not been reconstituted from a lyophilizate, and wherein said solution has a pH of from 2.5-3.5 and a concentration of said doxorubicin of from 0.1 to 100 mg/ml.
Type:
Application
Filed:
November 24, 2003
Publication date:
April 22, 2004
Applicant:
Pharmacia & Upjohn Company
Inventors:
Gaetano Gatti, Diego Oldani, Giuseppe Bottoni, Carlo Confalonieri, Luciano Gambini, Roberto De Ponti
Abstract: 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 solvent therefor, which has not been reconstituted from a lyophilizate and which has a pH of from 2.5 to 6.5. The solution of the invention is particularly advantageous for the administration by injection of the anthracycline glycoside drugs. e.g. doxorubicin, in the treatment of both human and animal tumors.
Type:
Application
Filed:
June 4, 2003
Publication date:
April 22, 2004
Applicant:
Pharmacia & Upjohn Company
Inventors:
Gaetano Gatti, Diego Oldani, Giuseppe Bottoni, Carlo Confalonieri, Luciano Gambini, Roberto De Ponti
Abstract: Novel compounds are provided having the formula
and salt thereof, where R1 is hydrogen, an alkyl, aralkyl, hydroxymethyl, carboxymethyl acyloxymethyl or trialkylsilyl group, or a group —CH2NR3R4 where N is a linking nitrogen atom and where (a) R3 and R4 are independently selected from hydrogen and alkyl, alkenyl, hydroxyalkyl and alkoxyalkyl groups; (b) R3 is hydrogen or an alkyl, alkenyl, hydroxyalkyl or alkoxyalkyl group, and R4 is —COR5 where R5 is hydrogen or an alkyl, alkenyl, hydroxyalkyl or alkoxyalkyl group; or (c) R3 and R4 taken together with the linking nitrogen atom form a saturated 3- to 7-member heterocyclic group. These compounds are useful intermediates in a process to prepare camptothecin derivatives including the anti-cancer drug irinotecan.
Abstract: 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-PPO-PEO triblock copolymer surfactant and at least one nonionic surfactant; followed by crosslinking the alginate in the emulsion with at least two cations selected from the group consisting of aluminum, barium, calcium, lithium, manganese, strontium, and zinc, to form antigen-containing, crosslinked alginate microparticles; and harvesting the microparticles. Another aspect of the invention is a method of vaccinating a vertebrate species including the step of administering to the species a vaccine composition prepared according to the method of the invention.
Type:
Application
Filed:
November 10, 2003
Publication date:
April 15, 2004
Applicant:
Pharmacia & Upjohn Company
Inventors:
Terry L. Bowersock, Paul Guimond, Tzu-Chi R. Ju, Argaw Kidane
Abstract: A method of identifying a ligand to a target molecule that includes: providing a reference compound that interacts with the target molecule; collecting a WaterLOGSY nuclear magnetic resonance spectrum of the reference compound in the presence of the target molecule; providing a test sample comprising at least one test compound; collecting a WaterLOGSY nuclear magnetic resonance spectrum of the reference compound in the presence of the test sample and the target molecule; and comparing the WaterLOGSY spectra to determine if at least one test compound interacts with the target molecule with a binding affinity tighter than that of the reference compound.
Abstract: A method of identifying a ligand to a target molecule that includes: providing a reference compound that interacts with the target molecule; collecting a 1 D 1H nuclear magnetic resonance spectrum of the reference compound in the presence of the target molecule; providing a plurality of test samples, each test sample including at least one test compound; collecting a 1 D 1H nuclear magnetic resonance spectrum of the reference compound in the presence of each test sample and the target molecule; comparing the spectrum of the reference compound in the presence of the target molecule to the spectrum of the reference compound in the presence of each test sample and the target molecule to determine a change in one or more of the reference compound resonances; and identifying at least one test compound that interacts with the target molecule, wherein the test compound displaces the reference compound.
Abstract: The present invention provides compounds of Formula (I)
wherein R1, R2, R3, R4, R5, R6, R7, R8 and Z have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands, and are useful for treating diseases whereas modulation of 5-HT activity is desired.
Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)
X2—CH2—C•H(OH)—CH2—NH—CO—RN (VIIIA)
and processes for production of pharmacologically useful oxazolidinones.