Patents Assigned to Pfizer
  • Benzopyran and related LTB.sub.4 antagonists
    Patent number: 5550152
    Abstract: The invention relates to benzopyran leukotriene B.sub.4 (LTB.sub.4) antagonists and pharmaceutical compositions containing the compounds. The compounds inhibit the action of LTB.sub.4 and are therefore useful in the treatment of LTB.sub.4 induced illnesses such as inflammatory disorders.
    Type: Grant
    Filed: September 30, 1994
    Date of Patent: August 27, 1996
    Assignee: Pfizer Inc.
    Inventors: Kevin Koch, Lawrence S. Melvin, Jr., Lawrence A. Reiter, Sally G. Ruggeri
  • Derivatives of 16-membered ring antibiotic macrolides
    Patent number: 5545624
    Abstract: The present invention relates to derivatives of 16-membered ring macrolide antibiotics rosaramicin, repromicin, 5-mycaminosyltylonide, desmycosin, lactenocin, O-demethyllactenocin, cirramycin A1, and 23-deoxymycaminosyltylonide, which are useful against bacterial and mycoplasmic pathogens in animals. Also claimed are a pharmaceutical composition of such derivatives and their use in treating bacterial and mycoplasmic infections in animals.
    Type: Grant
    Filed: January 11, 1995
    Date of Patent: August 13, 1996
    Assignee: Pfizer Inc.
    Inventors: Scott J. Hecker, Martin R. Jefson, James W. McFarland
  • Indole derivatives
    Patent number: 5545644
    Abstract: Compounds of the formula ##STR1## wherein n is 0, 1, or 2; X is hydrogen, chlorine, bromine or iodine; R.sub.1 is hydrogen; R.sub.3 is selected from hydrogen and C.sub.1 to C.sub.6 linear or branched alkyl; and R.sub.2 is as defined in the specification and the pharmaceutically acceptable salts thereof are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of a dihalogenated intermediate is also disclosed.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 13, 1996
    Assignee: Pfizer Inc.
    Inventors: John E. Macor, Martin J. Wythes
  • 2-Oxidole-1-carboxamide pharmaceutical agents for the treatment of alzheimer's disease
    Patent number: 5545656
    Abstract: This invention relates to the use of certain 3-substituted 2-oxindole-1-carboxamides and their pharmaceutically acceptable base salts for the treatment or prevention of Alzheimer's disease in mammals, including humans.
    Type: Grant
    Filed: April 5, 1995
    Date of Patent: August 13, 1996
    Assignee: Pfizer Inc.
    Inventors: Leland D. Loose, Joseph G. Lombardino, Ethan S. Weiner
  • Quinuclidine esters process and intermediate for their preparation and pharmaceutical compositions containing them
    Patent number: 5543419
    Abstract: Compounds of formula (I) wherein X is either (a) a phenyl group optionally substituted by 1 or 2 substituents each independently selected from halo, CF.sub.3, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and hydroxy or (b) a thienyl group; and Y is of formula (Ya) or (Yb) where A and B are 0, 1 or 2, D and E are 0 or 1, F is 0-3 and D+E+F=1-3, Z is 0, 1 or 2, R.sub.1 and R.sub.2 are H or alkyl or form a ring, and R.sub.3 is C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.6 cycloalkyl or optionally substituted phenyl or benzyl, are antimuscarinic bronchodilators useful for treating chronic obstructive airways disease or asthma.
    Type: Grant
    Filed: July 5, 1994
    Date of Patent: August 6, 1996
    Assignee: Pfizer Inc
    Inventors: Peter E. Cross, Alan Stobie
  • Hydroxylated metabolites and derivatives of doxazosin as anti-atherosclerosis agents
    Patent number: 5543411
    Abstract: This invention relates to the use of certain hydroxylated metabolites and derivatives of doxazosin and their pharmaceutically acceptable acid addition salts for retarding the development of atherosclerosis in a mammal. Such compounds are useful for reducing atherosclerotic plaque involvement and for retarding and reducing both lipid deposition fibrosis in the development of atherosclerotic plaques.
    Type: Grant
    Filed: May 8, 1995
    Date of Patent: August 6, 1996
    Assignee: Pfizer Inc.
    Inventors: Archie C. Swindell, Samuel S. Wong
  • Triazole antifungal agents
    Patent number: 5541203
    Abstract: The invention provides antifungal compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein R is phenyl substituted by up to 3 substituents each independently selected from halo and trifluoromethyl;R.sup.1 is C.sub.1 -C.sub.4 alkyl;R.sup.2 is ##STR2## R.sup.3 is --S(O).sub.m R.sup.4 ; R.sup.4 is C.sub.1 -C.sub.4 alkyl; andm is 0, 1 or 2, together with pharmaceutical compositions containing, and processes and intermediates for preparing, said compounds.
    Type: Grant
    Filed: April 8, 1994
    Date of Patent: July 30, 1996
    Assignee: Pfizer Inc.
    Inventors: Andrew S. Bell, Kenneth Richardson, Peter J. Whittle
  • Indolinyl N-hydroxyurea and N-hydroxamic acid derivatives as lipoxygenase inhibitors
    Patent number: 5541218
    Abstract: Certain indoline derivatives of the formula I: ##STR1## wherein the variables Y, A, R.sub.1, R.sub.4 and n have the definitions set forth in the disclosure, have the ability to inhibit the 5-lipoxygenase enzyme. These compounds are useful in the treatment or alleviation of inflammatory diseases, allergic conditions and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.
    Type: Grant
    Filed: March 24, 1995
    Date of Patent: July 30, 1996
    Assignee: Pfizer Inc.
    Inventors: Takafumi Ikeda, Rodney W. Stevens
  • Processes and intermediates for preparing cis(+)3-[4,6-dihydroxy chroman-3-ylmethyl]-4-methoxyaniline
    Patent number: 5539128
    Abstract: Processes, and intermediates, for use in preparing the compound of the formula ##STR1## The compounds of formula II are useful in the preparation of cis (+) N-trifluoromethylsulfonyl-3-[4-hydroxy-6-ArO-chroman-3-ylmethyl]-4-methoxy aniline compounds wherein Ar is defined below. The cis (+) N-trifluoromethylsulfonyl-3-[4-hydroxy-6-ArO-chroman-3-ylmethyl]-4-methoxy aniline compounds are useful for inhibiting the production of leukotrienes and/or blocking leukotriene receptors and in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction and related disease states in mammals.
    Type: Grant
    Filed: November 30, 1994
    Date of Patent: July 23, 1996
    Assignee: Pfizer Inc.
    Inventor: George J. Quallich
  • Methods of using piperidyl-benzisoxazole and benisothiazole derivatives as cholinesterase inhibitors
    Patent number: 5538984
    Abstract: Disclosed herein are compounds of the formula ##STR1## wherein R.sup.1 R.sup.2, R.sup.7, R.sup.8, X, Y, M and L are defined as below The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer's disease.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: July 23, 1996
    Assignee: Pfizer Inc.
    Inventors: Anabella Villalobos, Arthur A. Nagel, Yuhpyng L. Chen
  • Benzimidazole anthelmintics
    Patent number: 5538990
    Abstract: This invention is directed to anthelmintic benzimidazole compounds of the formula (I), ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.6 alkylthio; R.sup.2 is C.sub.1 -C.sub.4 alkyl; and R.sup.3 is C.sub.1 -C.sub.4 alkyl.
    Type: Grant
    Filed: January 14, 1994
    Date of Patent: July 23, 1996
    Assignee: Pfizer Inc.
    Inventors: Bernard J. Banks, Christopher J. Dutton, Alexander C. Goudie
  • Pasteurella multocida toxoid vaccines
    Patent number: 5536496
    Abstract: This invention provides vaccine compositions, methods of producing same and methods for protecting porcine animals against disease associated with infection by toxigenic Pasteurella multocida. The vaccines of this invention contain effective amounts of a free, soluble P. multocida toxoid and/or a P. multocida bacterin with a cell-bound toxoid.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: July 16, 1996
    Assignee: Pfizer Inc.
    Inventors: Joseph C. Frantz, David S. Roberts, Leroy A. Swearingin, Richard J. Kemmy
  • Triazine derivatives for enhancing antitumor activity
    Patent number: 5536722
    Abstract: 2,4,6-Triaminotriazine derivatives as potentiators of chemotherapeutic agents in the treatment of cancer.
    Type: Grant
    Filed: May 11, 1994
    Date of Patent: July 16, 1996
    Assignee: Pfizer Inc.
    Inventors: Jotham W. Coe, Anton F. J. Fliri, Takushi Kaneko, Eric R. Larson
  • Combinations of anthelmintically active agents
    Patent number: 5536715
    Abstract: Pharmaceutical compositions comprising a compound of formula (I) and at least one other anthelmintically active compound, being an avermectin or a milbemycin, are useful in the treatment of helminthiasis. In formula (I): R is optionally substituted phenyl, C.sub.3-8 cycloalkyl, C.sub.5-8 cycloalkenyl, C.sub.1-8 straight or branched chain alkyl, C.sub.2-8 straight or branched alkenyl, a 5- or 6-membered heterocyclyl, or optionally substituted phenyl C.sub.1-4 alkyl; each of Y and Z, which may be the same or different, is oxygen or sulfur; and X is a bond, a methylene group (--CH.sub.2 --), or oxygen.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: July 16, 1996
    Assignee: Pfizer Inc.
    Inventor: John D. Hood
  • 1-arylethyl-3-substituted piperidines
    Patent number: 5534626
    Abstract: Synthetic intermediates of 1-arylethyl-3-substituted piperidines.
    Type: Grant
    Filed: January 4, 1995
    Date of Patent: July 9, 1996
    Assignee: Pfizer Inc.
    Inventors: David Alker, Peter E. Cross, Robert M. Wallis
  • Method of producing porous delivery devices
    Patent number: 5529789
    Abstract: An efficient method for making high strength, highly porous, fast dissolving delivery devices. The method comprises mixing a formulation comprising menthol, a water-soluble, menthol-soluble polymer, and an active agent at a temperature such that the menthol is substantially molten. The formulation is disposed in a mold, solidified and the menthol is sublimed from the solidified molded formulation. Preferably, the solidification occurs at a temperature sufficient to provide a substantially amorphous menthol structure.
    Type: Grant
    Filed: September 15, 1994
    Date of Patent: June 25, 1996
    Assignee: Pfizer, Inc.
    Inventor: Julian B. Lo
  • Method for making steroidal peracyl glycosides
    Patent number: 5530107
    Abstract: Processes for the synthesis of tigogenin beta-O-cellobioside heptaalkanoate which is an intermediate for the known hypocholesterolemic agent tigogenin beta-cellobioside. The process comprises reacting .alpha.-cellobiosyl bromide heptaalkanoate and .beta.-tigogenin in the presence of zinc fluoride or zinc cyanide under conditions capable of forming said tigogenyl .beta.-O-cellobioside heptaalkanoate. The analogous preparations of hecogenin .beta.-O-cellobioside heptaalkanoate, 11-ketotigogenin .beta.-O-cellobioside heptaalkanoate, and diosgenin .beta.-O-cellobioside heptaalkanoate are also disclosed. The process provides both high .beta.-anomeric selectivity and high yields.
    Type: Grant
    Filed: May 23, 1994
    Date of Patent: June 25, 1996
    Assignee: Pfizer Inc.
    Inventors: Douglas J. M. Allan, Frank R. Busch, John F. Lambert, Russell J. Shine, Stanley W. Walinsky
  • Intermediates for 2-piperidino-1-alkanol derivatives
    Patent number: 5527912
    Abstract: 2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula ##STR1## wherein Q is S or CH.dbd.CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y.sup.1 are taken together and are arylmethylene or aralkylmethylene (or a corresponding epoxy derivative) or Y and Y.sup.1 are taken separately and Y is hydrogen or OH, and Y.sup.1 is aryl, aralkyl, arylthio, or aryloxy; and structurally related 2-(piperidino) alkanols; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.
    Type: Grant
    Filed: March 27, 1995
    Date of Patent: June 18, 1996
    Assignee: Pfizer Inc.
    Inventor: Bertrand L. Chenard
  • Fused tricyclic nitrogen containing heterocycles
    Patent number: 5527808
    Abstract: The present invention relates to novel fused tricycylic nitrogen containing heterocyclic compounds, and specifically, to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined below. These novel compounds are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.
    Type: Grant
    Filed: September 15, 1994
    Date of Patent: June 18, 1996
    Assignee: Pfizer Inc.
    Inventor: John A. Lowe, III
  • Process for production of avermectins and cultures therefor
    Patent number: 5525506
    Abstract: Streptomyces avermitilis lacking branched-chain amino acid transaminase activity and/or branched-chain 2-oxo acid dehydrogenase activity, methods for preparation thereof, and use thereof to produce natural and non-natural avermectins useful as parasiticides.
    Type: Grant
    Filed: October 14, 1994
    Date of Patent: June 11, 1996
    Assignee: Pfizer Inc.
    Inventors: Edmund W. Hafner, Kelvin S. Holdom, S. Edward Lee