Abstract: The present invention relates to compounds of the Formula: wherein R1 to R6, X, Z and A are as defined. These compounds have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods for treating diseases, for example, neurodegenerative diseases, e.g., Alzheimer's disease, in a mammal comprising compounds of the present Formula.
Abstract: The present invention provides compounds of formula (I) wherein R1 and R2 are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.
Abstract: The use of a compound of formula I: an isomer thereof, a prodrug of said compound or isomer, or a pharmaceutically acceptable salt of said compound, isomer or prodrug, in the manufacture of a medicament for the palliative, prophylactic or curative treatment of negative energy balance in ruminants. The use of a compound of formula 1, in the manufacture of a medicament for the palliative, prophylactic or curative treatment of ruminant disease associated with negative energy balance in ruminants, wherein, preferably, the ruminant disease associated with negative energy balance in ruminants is selected from fatty liver syndrome, dystocia, immune dysfunction, impaired immune function, toxification, primary ketosis, secondary ketosis, downer cow syndrome, indigestion, inappetence, retained placenta, displaced abomasum, mastitis, (endo-)-metritis, infertility, low fertility, and lameness.
Abstract: Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable compositions comprising compounds of formula I. Compounds of formula I as disclosed herein can be used in a variety of applications, including using the invention compounds to treat bacterial infections.
Type:
Grant
Filed:
September 1, 2004
Date of Patent:
December 4, 2007
Assignee:
Pfizer Inc.
Inventors:
Susan Hagen, Vara Prasad Venkata Nagendra Josyula
Abstract: A process and intermediates for producing 3-amino nitrites. The process involves resolving an enantiomeric mixture of chiral 3-amino nitrites in the presence of a chiral acid in a solvent system to produce a chiral 3-amino nitrile salt. The process may further comprise a recrystalizing step, wherein an enantiomerically enriched 3-amino nitrile salt is produced. The process may further comprise a salt exchanging step, wherein another acid is added to the chiral 3-amino nitrile salt or the enantiomerically enriched 3-amino nitrile salt to produce another 3-amino nitrile salt.
Type:
Grant
Filed:
September 21, 2004
Date of Patent:
November 27, 2007
Assignee:
Pfizer Inc.
Inventors:
David Robert Allen, Crystal A Achenbach-McCarthy
Abstract: The present invention provides compounds of formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs, wherein R1, R2 and R3 are as defined herein; pharmaceutical formulations thereof; and use thereof in the treatment of, inter alia, conditions, diseases, and symptoms such as bipolar disorder, diabetes, dementia, Alzheimer's Disease, stroke, schizophrenia, depression, hair loss, and cancer.
Abstract: The invention provides compounds of formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs, wherein R1, R2, and R3 are as defined herein; pharmaceutical compositions thereof; and use thereof in the treatment of, inter alia, conditions, diseases, and symptoms such as diabetes, dementia, Alzheimer's Disease, stroke, schizophrenia, depression, hair loss, and cancer.
Abstract: A method for resolving enantiomers of a compound containing the structure of the forula: wherein R4 or R5 may contan one or more asymmetric centers, by mixing a racemic mixture of enantiomers of a compound, containing the structure of said formula; in a solvent, with a resolving compound having a defined sterospecificity, to form a solution and with said resolving agent being capable of binding with at least one but not all of said enantiomers to form a precipitate, containing said at least one of said enantiomers in sterospecific form and collecting either the precipitate and purifying it or collecting the solution with contained other of said enantiomers and recrystallizing the enantiomer contained in said solution.
Abstract: This invention relates to a novel crystalline diphosphate salt of (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-13-[[2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(propylamino)methyl]-?-L-ribo-hexopryanosyl]oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-?-D-xylo-hexopyranosyl]oxy]-1-oxa-6-azacyclopentadecan-15-one that is useful as an antibacterial and antiprotozoal agent in mammals. This invention also relates to pharmaceutical compositions containing the free base of the diphosphate salt and the methods of treating bacterial and protozoal infections in mammals by administering the free base of the diphosphate to mammals requiring such treatment. The free base of the diphosphate salt of the present invention possesses potent activity against various bacterial and protozoal infections when given by parenteral application to mammals.
Type:
Grant
Filed:
May 6, 2004
Date of Patent:
November 20, 2007
Assignees:
Pfizer Inc., Pfizer Products Inc.
Inventors:
Robert J. Rafka, Colman B. Ragan, Douglas J. M. Allen
Abstract: Novel 3,3-diphenylpropylamines of the formula and stereoisomers and physiologically acceptable acid addition salt thereof; wherein R1, R2, R3, R4, R5, and R6 are as defined herein; methods of use thereof; and pharmaceutical compositions thereof.
Type:
Grant
Filed:
August 24, 2006
Date of Patent:
November 6, 2007
Assignee:
Pfizer Inc.
Inventors:
John Gregory Slatter, Raymond Charles Grabiak, Robert John Kaufman
Abstract: The invention provides compounds of formula (I), prodrugs and stereoisomers thereof, and the pharmaceutically acceptable salts of the compounds, prodrugs, and stereoisomers, wherein R1, R2, R3, HET, n, Q, X, Y, and Z are as described herein; compositions thereof; and uses thereof in treating diabetic complications including diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, and the like.
Abstract: The present invention relates to a class of substituted 1,2,4-triazoles of formula (I) with activity as oxytocin antagonists, uses thereof, processes for the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction, particularly premature ejaculation (P.E.
Type:
Grant
Filed:
September 20, 2004
Date of Patent:
November 6, 2007
Assignee:
Pfizer Inc.
Inventors:
Alan Daniel Brown, David Ellis, Christopher Ronald Smith
Abstract: The present invention provides an improved process for the preparation of the anti-migraine drug, (R)-5-(2-benzenesulphonylethyl)-3-N-methylpyrrolidin-2-ylmethyl)-1H-indole (eletriptan), available commercially as the hydrobromide salt, and an intermediate and dimer-free products obtained from such process.
Abstract: The present invention relates to antibodies and antigen-binding portions thereof that specifically bind to CD40, preferably human CD40, and that function as CD40 agonists. The invention also relates to human anti-CD40 antibodies and antigen-binding portions thereof. The invention also relates to antibodies that are chimeric, bispecific, derivatized, single chain antibodies or portions of fusion proteins. The invention also relates to isolated heavy and light chain immunoglobulins derived from human anti-CD40 antibodies and nucleic acid molecules encoding such immunoglobulins. The present invention also relates to methods of making human anti-CD40 antibodies, compositions comprising these antibodies and methods of using the antibodies and compositions for diagnosis and treatment. The invention also provides gene therapy methods using nucleic acid molecules encoding the heavy and/or light immunoglobulin molecules that comprise the human anti-CD40 antibodies.
Type:
Grant
Filed:
November 8, 2002
Date of Patent:
October 30, 2007
Assignees:
Abgenix, Inc., Pfizer Inc.
Inventors:
Vahe Bedian, Ronald P. Gladue, Jose Corvalan, Xiao-Chi Jia, Xiao Feng
Abstract: An improved process for the preparation of 1,3 substituted indenes which are useful intermediates in the synthesis of aryl fused azapolycyclic compounds as agents for the treatment of neurological and psychological disorders.
Type:
Grant
Filed:
November 17, 2003
Date of Patent:
October 23, 2007
Assignee:
Pfizer Inc
Inventors:
Robert Eugene Handfield, Jr., Timothy J. N. Watson, Phillip James Johnson, Peter Robert Rose
Abstract: This invention provides the compounds of formula (I): or a pharmaceutically acceptable ester of such compound, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 independently represent a hydrogen atom or the like; R3 represents an aryl group having from 6 to 10 ring atoms or the like; X represents an oxygen atom, or the like; Y represents an oxygen atom or the like; and n represents an integer 0, 1 or 2. These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.
Abstract: The present invention provides certain [3.1.0] bicyclic oxazolidinone derivatives of formula I or pharmaceutically acceptable salts or prodrugs thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
Type:
Grant
Filed:
April 1, 2004
Date of Patent:
October 9, 2007
Assignee:
Pfizer Inc.
Inventors:
Adam Renslo, Mikhail Fedor Gordeev, Dinesh Vinoobhai Patel, Hongwu Gao, Vara Prasad Venkata Nagendra Josyula