Abstract: Trovafloxacin acid salts are prepared via the hydrolysis of imine intermediates using mineral acid including, but not limited to, methanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid, nitric acid, sulfuric acid, phosphoric acid, hydrochloric acid, hydrobromic acid, tartaric acid, citric acid, acetic acid, and maleic acid. Trovafloxacin acid salts are useful as antibiotic agents.
Type:
Grant
Filed:
August 26, 1999
Date of Patent:
March 19, 2002
Assignee:
Pfizer Inc.
Inventors:
Timothy Norris, Keith M. DeVries, Peter R. Rose
Abstract: The invention relates to processes for preparing a compound of the formula
and the enantiomer of said compound, wherein the benzoic acid moiety is attached at position 6 or 7 of the chroman ring, and R1, R2, and R3 are as defined herein. The invention further relates to intermediates that are useful in the preparation of the compound of formula X above.
Type:
Grant
Filed:
March 21, 2001
Date of Patent:
March 12, 2002
Assignee:
Pfizer Inc.
Inventors:
Anthony Piscopio, Joel M. Hawkins, Stephanie Caron, Sarah E. Kelly, Jeffrey W. Raggon, Michael J. Castaldi, Robert W. Dugger, Sally G. Ruggeri
Abstract: NPY antagonists, methods of using such NPY antagonists and pharmaceutical compositions containing such NPY antagonists. The NPY antagonists are useful for the treatment of NPY mediated disease/conditions including obesity.
Type:
Grant
Filed:
March 31, 2000
Date of Patent:
March 12, 2002
Assignee:
Pfizer Inc.
Inventors:
Richard L. Elliott, Richard F. Hank, Marlys Hammond
Abstract: The present invention provides novel methods of inhibiting pathological conditions related to organ systems which respond to estrogen agonists comprising administering to a mammal in need of such treatment an effective amount of a compound of formula I
Abstract: Compounds of Formula (1.0.0):
are described wherein A is for example aryl, heteroaryl or heterocyclyl, Y is preferably —C(═O)—; B is independently selected from a group of moieties, the most preferred of which are those of partial Formulas (1.1.2) and (1.1.6):
and E is a single bond; oxygen; 1,1-cyclopropyl; C(CH3)2; CF2; or a bridging moiety of partial Formula (1.9.0):
where R1a is hydrogen when R1 has the meaning of a mono-valent substituent; and R1a is a single bond when R1 has the meaning of a di-valent substituent. Said compounds are useful in methods of treating or preventing an inflammatory, autoimmune or respiratory diseases by inhibiting cell adhesion and consequent or associated pathogenic processes subsequently mediated by VLA-4.
Type:
Grant
Filed:
October 26, 1999
Date of Patent:
March 12, 2002
Assignee:
Pfizer Inc
Inventors:
Allen Jacob Duplantier, Anthony John Milici, Louis Stanley Chupak
Abstract: This invention relates to methods for treating bone loss in a mammal by administering to the mammal a therapeutically effective amount of leptin or a leptin mimetic. This invention also relates to methods for treating bone fracture, enhancing bone healing following facial reconstruction, maxillary reconstruction or madibular reconstruction, enhancing long bone extension, enhancing the healing rate of a bone graft, enhancing prosthetic growth and inducing vertebral synostosis by administering a therapeutically effective amount of leptin or a leptin mimetic. This invention further relates to methods and compositions comprising leptin or a leptin mimetic and estrogen, a selective estrogen receptor modulator or a bisphonate for treating the above-recited diseases and conditions.
Type:
Grant
Filed:
February 19, 1999
Date of Patent:
March 5, 2002
Assignee:
Pfizer Inc.
Inventors:
HuaZhu Ke, Claire M. Steppan, Andrew Gordon Swick
Abstract: This invention relates to pharmaceutical combinations of amlodipine or a pharmaceutically acceptable acid addition salt thereof and statins or pharmaceutically acceptable salts thereof, kits containing such combinations and methods of using such combinations to treat subjects suffering from angina pectoris, atherosclerosis, combined hypertension and hyperlipidemia and to treat subjects presenting with symptoms of cardiac risk, including humans. This invention also relates to additive and synergistic combinations of amlodipine or a pharmaceutically acceptable acid addition salt thereof and statins or pharmaceutically acceptable salts thereof whereby those additive and synergistic combinations are useful in treating subjects suffering from angina pectoris, atherosclerosis, combined hypertension and hyperlipidemia and those subjects presenting with symptoms of cardiac risk, including humans.
Abstract: The invention relates anhydrous para-toluenesulphonic acid salts of 3-ethyl-5-[5-(4-ethylpiperazin-1-ylsulphonyl)-2-(2-methoxyethoxy) pyridin-3-yl]-2-(pyridin-2-yl)methyl-2,6-dihydro-7H-pyrazolo [4,3-d]pyrimidin-7-one having the formula (I):
a process for preparing compounds (I), pharmaceutical compositions containing (I) and use of (I) in medicine.
Abstract: Compounds of formula (I):
or pharmaceutically acceptable salts thereof, or solvates of either entity, wherein the substituents have the values described herein, are useful as matrix metalloprotease (MMP) inhibitors
Type:
Grant
Filed:
April 11, 2000
Date of Patent:
February 26, 2002
Assignee:
Pfizer Inc
Inventors:
Michael Jonathan Fray, Roger Peter Dickinson, Kevin Neil Dack
Abstract: The present invention relates to compounds of the formula
and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as adenosine A2a receptor agonists.
Abstract: A novel process intermediate, tetrahydro-4-[3-(4-fluorophenyl)thio]phenyl-2H-pyran-4-carboxamide, of the formula:
is described, as well as its use in a process of preparing 5-lipoxygenase inhibitors of the formula:
which comprises establishing a reaction mixture consisting of:
and
an electron deficient monocyclic or benzo-fused bicyclic N-heterocycle containing two nitrogen atoms of the formula:
in an aprotic solvent; in the presence of a carbonate of the formula: (M)2-CO3, where M is an alkali metal, Group 1/Ia element, selected from the group consisting of lithium, Li; sodium,Na; potassium, K; rubidium, Rb; and cesium, Cs; followed by heating of said reaction mixture under a nitrogen atmosphere; whereby there is produced the desired compound of the above-recited formula.
Type:
Grant
Filed:
June 29, 2000
Date of Patent:
February 12, 2002
Assignee:
Pfizer Inc
Inventors:
Timothy Norris, Megan E. Hnatow, John F. Lambert
Abstract: The invention relates to pharmaceutical compositions and methods useful in the treatment of obesity which methods comprise administering to animal, including a human or companion animal, in need of such treatment an effective amount of a compound of the structural formula
or a pharmaceutically acceptable salt, racemate or enantiomer thereof, wherein
R is hydroxy, esterified hydroxy or etherified hydroxy;
R1 and R2 are, independently, halogen, trifluoromethyl or lower alkyl;
R3 is halogen, trifluoromethyl, lower alkyl, aryl, aryl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl, carbocyclic arylmethyl, carbocyclic aroyl, carbocyclic arylhydroxymethyl; or
R3 is the radical
wherein
R8 is hydrogen, lower alkyl, aryl, cycloalkyl, aryl-lower alkyl or cycloalkyl-lower alkyl;
R6 is hydroxy or acyloxy; R10 is hydrogen or lower alkyl; or R9 and R10, taken together with the carbon atom to which they are attached, form a carbonyl group;
R4 is hydrogen, halogen, trifluoromethyl
Type:
Grant
Filed:
January 20, 2000
Date of Patent:
February 5, 2002
Assignee:
Pfizer Inc.
Inventors:
Peter Cornelius, Diane M. Hargrove, Bradley P. Morgan, Andrew G. Swick
Abstract: A compound of the formula
wherein R1, R2 and Q is as defined above, are useful in the treatment of a arthritis (including osteoarthritis and rheumatoid arthritis), cancer (such as solid tumor cancer including colon cancer, breast cancer, lung cancer and prostrate cancer and hematopoietic malignancies including leukemias and lymphomas), and other disorders. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S) and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.
Abstract: A compound of the formula
wherein R1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R2 is hydrogen or methyl; and R3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.
Type:
Grant
Filed:
February 4, 1999
Date of Patent:
January 29, 2002
Assignees:
Northwestern University, Pfizer, Inc.
Inventors:
Richard B. Silverman, Ryszard Andruszkiewicz, Po-Wai Yuen, Denis Martin Sobieray, Lloyd Charles Franklin, Mark Alan Schwindt
Abstract: This invention relates to compounds of the formula
and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1 and R2 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1.
Abstract: A compound of the formula:
or a pharmaceutically acceptable salt thereof, wherein
R1 and R2 are independently selected from hydrogen, halo, hydroxy, (C1-C4)alkyl, halo (C1-C4)alkyl and the like; R3 and R4 are independently selected from hydrogen, halo(C1-C10)alkyl, optionally substituted (C1-C6)alkyl and the like, or R3 and R4, together with the nitrogen atom to which they are attached, form an optionally substituted fully saturated, partially saturated or fully unsaturated heterocyclic ring; and R5 is (C4-C11)cycloalkyl and the like, has ORL1-receptor agonist activity, and are useful as analgesics or the like in mammalian subjects.
Abstract: Compounds of the structures
are useful for treating conditions related to an excess of neuropeptide Y including obesity and circulatory disorders.
Abstract: The present invention relates to compounds of the formula (I)
and to pharmaceutically acceptable salts thereof, wherein R1-R4 and Z are as defined herein. The compounds of formula (I) are useful as antiproliferative agents. The invention further relates to pharmaceutical compositions and methods of treating hyperproliferative disorders such as cancer, using such compounds.