Abstract: The present invention provides genetically engineered type I/type II hybrid BVDV viruses. The hybrid viruses, as well as the hybrid viral genome, can be used in immunogenic compositions and vaccines for protecting cattle from BVDV infection.
Abstract: Compounds of formulae (IA) and (IB):
wherein R1, R2, R3, Ar1 and X are as defined above, are endothelin antagonists. The compounds are therefore useful in the treatment of a variety of conditions mediated by endothelin, such as restenosis, renal failure and systemic and pulmonary hypertension.
Type:
Grant
Filed:
August 21, 2001
Date of Patent:
June 3, 2003
Assignee:
Pfizer Inc.
Inventors:
Bernard Joseph Banks, Nathan Anthony Logan Chubb, James John Eshelby, Darren John Schulz
Abstract: This invention relates to methods for preparing anhydrous CETP inhibitor, (2R,4S)-4-[(3,5-bis-trifluoromethyl-benzyl)-methoxycarbonyl-amino]-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester.
Abstract: The invention provides a process for the production of a compound of formula (A), or a pharmaceutically acceptable salt or solvate thereof, 1
Type:
Application
Filed:
July 19, 2002
Publication date:
May 29, 2003
Applicant:
Pfizer Inc.
Inventors:
Lee Terence Boulton, Robert James Crook, Alan John Pettman, Robert Walton
Abstract: The invention relates to the field of bioinformatics. More particularly, the invention relates to methods of identifying sequence motifs characteristic of G-protein-coupled receptor (GPCR) subfamilies and using these motifs, for example, to classify “orphan GPCRs.” The invention provides methods of classifying “orphan GPCRs” that focus on amino acid residue similarities for ligand-binding positions. The methods use optimized sequence alignments and avoid mechanical calculation of scores and cutoffs. In particular, a sequence motif characteristic of a GPCR subfamily that binds a certain ligand type is determined, and “orphan GPCRs” having the sequence motif are assigned to the subfamily.
Abstract: The present invention is directed to a novel process for the preparation of the mesylate trihydrate of the compound of formula (I), (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propanol:
The present invention is further directed to a process for the preparation of a (2S)-(+)-compound of formula (II):
wherein R1 is a protecting group. In addition, the present invention relates to intermediates useful in said processes.
Type:
Grant
Filed:
April 23, 2001
Date of Patent:
May 27, 2003
Assignee:
Pfizer Inc
Inventors:
Stanley Walter Walinsky, Terry Gene Sinay, Jr., Joseph Philip Rainville
Abstract: The present invention relates to method for the preparation of dialkylpyridylboranes by reacting a pyridine Grignard reagent with an alkoxydialkylborane or a trialkylborane. The reaction can be conducted at a temperature ranging from about 0° C. to about 40° C. The pyridine Grignard reagent is preferably prepared in situ by the reaction of a Grignard reagent (RMgX) and a halopyridine in a suitable solvent, such as tetrahydrofuran, followed by the addition of an alkoxydialkylborane or a trialkylborane to form a dialkylpyridylborane.
Abstract: This invention relates to [4-oxo-(5-trifluoromethyl-benzothiazol-2-ylmethyl)-3,4-dihydro-phthalazin-1-yl]-acetic acid ethanolamine salt, pharmaceutical compositions thereof and methods of treating diabetic complications in mammals comprising administering to said mammals said salt and said compositions. This invention is also directed to combinations of said diethylamine salt with NHE-1 inhibitors, selective serotonin retuptake inhibitors (SSRIs), glycogen phosphorylase inhibitors (GPIs), sorbitol dehydrogenase inhibitors (SDIs) and antihypertensive agents. Said combinations are useful in treating diabetic complications in mammals.
Abstract: The invention features a method of screening for an agent that inhibits intracellular phosphodiesterase 10A activity, comprising administering an agent to striatal medium spiny neurons and submaximally activating adenylate cyclase, administering an agent to striatal medium spiny neurons and submaximally activating guanylate cyclase, measuring cAMP generation and cGMP generation in the cells, and calculating the cAMP EC200 and the cGMP EC200, wherein the agent is identified as a PDE10A inhibitor if the ratio of cAMP EC200/cGMP EC200 is comparable to the ratio produced by administration of papaverine under the same assay conditions. Also featured are rat PDE10A polynucleotide and polypeptide sequences.
Type:
Application
Filed:
July 24, 2002
Publication date:
May 22, 2003
Applicant:
Pfizer Inc.
Inventors:
Larry C. James, Lorraine A. Lebel, Frank S. Menniti, Christine A. Strick
Abstract: The invention provides a process for the optical resolution of a racemic mixture, or an optically enriched mixture, of trans-7-(hydroxymethyl)octa-hydro-2H-pyrido-1,2a)pyrazine, a key intermediate for preparing pharmacologically active 2,7-substituted octahydro-1H-pyrido[1,2-a]pyrazine derivatives useful in the treatment of disorders of the dopamine system. The process of the invention involves use of D-(−) or L-(+)naproxen as a resolving agent.
Abstract: The present invention provides compositions and methods for the use of antigenic peptides derived from the Fc portion of the epsilon heavy chain of IgE molecules from two unrelated species as vaccines for the treatment and prevention of IgE-mediated allergic disorders. In particular, the invention provides compositions for the treatment and prevention of IgE-mediated allergic disorders comprising an immunogenic amount of one or more antigenic peptides.
Abstract: The invention is directed to two forms of isolated or purified human NHE2 polypeptide sequences, NHE2-LF and NHE2-SF, as well as the polynucleotide coding sequences that encode the human NHE2-LF and NHE2-SF polypeptides. Also featured are NHE2-LF- and NHE2-SF-related hosts, cell membrane preparations, vectors, and antibodies, as well as methods of using cells recombinantly expressing the human NHE2-LF or NHE2-SF, to identify agents that modulate human NHE activity.
Abstract: Substituted spiro[isobenzofuran-1,4′-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4′-piperidines capable of modulating NPY5 receptor activity are provided. Such compounds may be used to modulate ligand binding to NPY5 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders (e.g., eating disorders such as obesity or bulimia, psychiatric disorders, diabetes and cardiovascular disorders such as hypertension) in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such compounds for detecting NPY5 receptors.
Type:
Grant
Filed:
December 11, 2001
Date of Patent:
May 20, 2003
Assignees:
Pfizer Inc., Neurogen Corporation
Inventors:
Rajagopal Bakthavatchalam, Charles A. Blum, Harry L. Brielmann, James William Darrow, Stéphane De Lombaert, Alan Hutchison, Jennifer Tran, Xiaozhang Zheng, Richard Louis Elliott, Marlys Hammond
Abstract: Cyclic amino acids, such as gabapentin and pregabalin, are used for treating physiological conditions associated with the use, or sequelae of use, of cocaine or other psychomotor stimulants and other addictive drugs/substances. Physiological conditions include stimulant-induced toxicities.
Type:
Grant
Filed:
August 29, 2000
Date of Patent:
May 20, 2003
Assignee:
Pfizer Inc.
Inventors:
Hyacinth Chi Akunne, Ann Elizabeth Corbin, David James Dooley, Alysia Latrese Green, Thomas Gary Heffner
Abstract: This invention relates to a series of substituted aromatic ethers of the formula I
wherein ring A and X and Y are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.