Patents Assigned to Pfizer Inc.
  • Process for preparing azabicyclo[2.2.2]octan-3-imines
    Patent number: 5216163
    Abstract: Azabicyclo[2.2.2]octan-3-imines of the general formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined herein are prepared by reacting a compound of the formula ##STR2## ps with a compound of the formula wherein A is MgCl, MgBr or Li.
    Type: Grant
    Filed: April 1, 1992
    Date of Patent: June 1, 1993
    Assignee: Pfizer Inc
    Inventors: Dennis M. Godek, Charles W. Murtiashaw
  • Thiazolyl and oxazolyl[5,4-c]piperidyl-substituted quinolone-carboxylic acid and related analogs thereof having antibacterial properties are disclosed
    Patent number: 5214051
    Abstract: Thiazolyl and oxazolyl [5,4-c] piperidyl-substituted quinolone-carboxylic acids and related analogs thereof having antibacterial properties are disclosed.
    Type: Grant
    Filed: May 16, 1991
    Date of Patent: May 25, 1993
    Assignee: Pfizer Inc.
    Inventors: Katherine E. Brighty, John A. Lowe, III, Paul R. McGuirk
  • 1,4-dihydropyridines useful as pharmaceuticals
    Patent number: 5214044
    Abstract: The invention provides compounds of the formula: ##STR1## The variables are defined in the specification. The compounds are useful e.g. for the curative or prophylactic treatment of allergic conditions.
    Type: Grant
    Filed: September 18, 1991
    Date of Patent: May 25, 1993
    Assignee: Pfizer Inc.
    Inventors: Kelvin Cooper, Michael J. Fray
  • Process for 5-fluoro-6-chlorooxindole
    Patent number: 5210212
    Abstract: Process for the production of 5-fluoro-6-chloro- oxindole, (III), which is useful in the synthesis of certain analgesic and antiinflammatory agents, via two different synthetic pathways.Compounds of formula (I) and (II) shown below ##STR1## which are intermediates in the process of this invention.
    Type: Grant
    Filed: August 14, 1992
    Date of Patent: May 11, 1993
    Assignee: Pfizer Inc
    Inventor: Robert W. Dugger
  • Triazole antifungal agents
    Patent number: 5206364
    Abstract: The invention provides antifungal agents of the formula: ##STR1## and their pharmaceutically acceptable salts, wherein R is phenyl optionally substituted by 1 to 3 substituents each independently selected from halo and CF.sub.3 ;R.sup.1 is C.sub.1 -C.sub.4 alkyl;R.sup.2 is H or C.sub.1 -C.sub.4 alkyl; and"Het", which is attached to the adjacent carbon atom by a ring carbon atom, is selected from pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl and triazinyl, "Het" being optionally substituted by C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3, CN, NO.sub.2, NH.sub.2, --NH(C.sub.1 -C.sub.4 alkanoyl) or --NHCO.sub.2 (C.sub.1 -C.sub.4 alkyl).
    Type: Grant
    Filed: March 4, 1992
    Date of Patent: April 27, 1993
    Assignee: Pfizer Inc.
    Inventors: Roger P. Dickinson, Kenneth Richardson
  • Preparation of optically active spiro-hydantoins
    Patent number: 5206367
    Abstract: This invention relates to the preparation of preparing optically-active asymmetric spiro-hydantoin compounds, which are known to be of value in the medical control of certain chronic diabetic complications arising from diabetes mellitus. This invention also includes within its scope certain corresponding novel amino and hydantoic acid compounds and the cinchonine salt of optically active hydantoic acid, which are used as intermediates in the aforesaid process.
    Type: Grant
    Filed: February 18, 1992
    Date of Patent: April 27, 1993
    Assignee: Pfizer Inc.
    Inventor: Frank J. Urban
  • Acidic polycyclic ether useful as an anticoccidial agent and as a growth promotant
    Patent number: 5206263
    Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Streptomyces hygroscopicus ATCC 53626. This novel antibiotic is useful as an anticoccidial in chickens and as a growth promotant in cattle and swine.
    Type: Grant
    Filed: December 5, 1989
    Date of Patent: April 27, 1993
    Assignee: Pfizer Inc.
    Inventors: John P. Dirlam, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone
  • Process for preparing aryl piperazinyl-heterocyclic compounds
    Patent number: 5206366
    Abstract: A process for preparing a compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof, which comprises reacting a monosubstituted piperazine of the formula ##STR2## with an alkyl halide containing compound of the formula ##STR3## in water with a reagent to neutralize the hydrohalic acid and refluxing the mixture under conditions which are suitable to effect the coupling of said monosubstituted piperazines with said alkyl halide containing compound.
    Type: Grant
    Filed: August 26, 1992
    Date of Patent: April 27, 1993
    Assignee: Pfizer Inc.
    Inventor: Paul Bowles
  • Certain 9-amino-2-(or 4)-oxa 1,2,3,4-tetrahydro- or 1,2,3,4,5,6,7,8-octahydro-acridines
    Patent number: 5202440
    Abstract: Compounds selected from the group consisting of 9-amino-4-oxa-1,2,3,4-tetrahydro-acridine, 9-amino-2-oxa-1,2,3,4-tetrahydro-acridine, 9-amino-8-fluoro-4-oxa-1,2,3,4-tetrahydro-acridine, 9-amino-4-oxa-1,2,3,4,5,6,7,8-octahydro-acridine or a pharmaceutical acceptable salt thereof are useful treating Alzheimer's disease.
    Type: Grant
    Filed: April 27, 1990
    Date of Patent: April 13, 1993
    Assignee: Pfizer Inc.
    Inventor: Manoj C. Desai
  • Preparation of diazabicyclic Intermediates
    Patent number: 5196548
    Abstract: Diazabicyclo[2.2.1]heptane intermediates are prepared from 4-hydroxy-L-proline in a five step procedure, or from allo-4-hydroxy-D-proline, through a novel 2-(C.sub.1 -C.sub.6)alkyl-5-substituted-2,5-diazabicyclo[2.2.1]heptane intermediate. The diazabicycloheptanes are of use in the preparation of antibiotic quinolones.
    Type: Grant
    Filed: July 2, 1992
    Date of Patent: March 23, 1993
    Assignee: Pfizer Inc.
    Inventors: Tamim F. Braish, Darrell E. Fox
  • Transdermal flux enhancing compositions
    Patent number: 5196410
    Abstract: A transdermal flux enhancing pharmaceutical composition for transdermal administration to a human or lower animal subject comprising a safe and effective amount of pharmacologically active compound or a prodrug thereof, an aqueous solvent system comprising from about 15 to 75% by volume of one or more water miscible solvents, and a penetration enhancer selected from certain 1-alkylazacycloheptan-2-ones and cis-olefin compounds of the formulaCH.sub.3 (CH.sub.2).sub.x CH.dbd.CH(CH.sub.2).sub.y R.sup.3where R.sup.3 is CH.sub.2 OH, CH.sub.2 NH.sub.2 or COR.sup.4 and R.sup.4 is OH or (C.sub.1 -C.sub.4)alkoxy, x and y are each an integer from 3 to 13 and the sum of x and y is from 10 to 16; methods for their use in treating various illnesses in a human or lower animal by transdermal administration of said composition.
    Type: Grant
    Filed: September 11, 1991
    Date of Patent: March 23, 1993
    Assignee: Pfizer Inc.
    Inventors: Michael L. Francoeur, Russell O. Potts
  • Process for preparing ketone enantiomer
    Patent number: 5196607
    Abstract: A novel multi-step process for preparing the (4S)-enantiomer of 4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenone in a highly-optically pure form is disclosed. The process involves (1) first reacting 3,4-dichlorocinnamyl chloride with L-(-)-ephedrine in a chlorinated lower hydrocarbon solvent to form the corresponding chiral N-methyl-N-(.beta.-hydroxy-.beta.-phenylisopropyl)-3-(3,4-dichlorophenyl)p ropenoamide; (2) then subjecting the chiral .alpha.,.beta.-unsaturated amide formed in the first step to a Grignard reaction with phenyl magnesium chloride or bromide, followed by hydrolysis, to effect a conjugate addition of the phenyl group and the hydrogen element to the aforesaid .alpha.,.beta.-unsaturated propenoamide and so selectively form the corresponding chiral N-methyl-N-(.beta.-hydroxy-.beta.
    Type: Grant
    Filed: February 14, 1992
    Date of Patent: March 23, 1993
    Assignee: Pfizer Inc.
    Inventor: George J. Quallich
  • Calcium independent C amp phosphodiesterase inhibitor antidepressant
    Patent number: 5196426
    Abstract: Antidepressant agents having the formula ##STR1## wherein R.sup.1 is a polycycloalkyl group; R.sup.2 is methyl or ethyl, X is O or NH; and Y comprises a 5- or 6-membered heterocyclic ring having one or two nitrogens; or fused bicyclic heterocyclic rings having a total of three nitrogen atoms, one in each ring and one angular nitrogen.
    Type: Grant
    Filed: March 19, 1992
    Date of Patent: March 23, 1993
    Assignee: Pfizer Inc.
    Inventors: Nicholas A. Saccomano, Fredric J. Vinick
  • Certain amines which are muscarinic receptor antagonists
    Patent number: 5192765
    Abstract: Amines of the following formula: ##STR1## where the variables are defined in the specification are useful in the treatment of diseases associated with altered motility and/or tone of smooth muscle.
    Type: Grant
    Filed: June 6, 1991
    Date of Patent: March 9, 1993
    Assignee: Pfizer Inc.
    Inventors: David Alker, Robert J. Bass, Peter E. Cross
  • Glutaramide diuretic agents
    Patent number: 5192800
    Abstract: A series of novel spiro-substituted glutaramide derivatives have been prepared, including the pharmaceutically acceptable salts thereof and bioprecursors therefor, wherein the spiro-substituent completes a 5- or 6- membered carbocyclic ring and is located at the carbon atom adjacent to the carbamoyl group. These particular compounds are inhibitors of the neutral endopeptidase E.C.3,4.24.11 enzyme and are therefore useful in therapy as diuretic agents for the treatment of hypertension, heart failure, renal insufficiency and other disorders. Methods for preparing these compounds from known starting materials are provided.
    Type: Grant
    Filed: May 30, 1991
    Date of Patent: March 9, 1993
    Assignee: Pfizer Inc.
    Inventors: Ian T. Barnish, John C. Danilewicz, Keith James, Gillian M. B. Samuels, Nicholas K. Terrett, Michael T. Williams, Martin J. Wythes
  • 3-substituted-2-oxindole derivatives as inhibitors of interleukin-1 biosynthesis
    Patent number: 5192790
    Abstract: This invention relates to the use of certain 3-substituted-2-oxindole derivatives to inhibit interleukin-1 biosynthesis in a mammal. This invention also relates to the use of such compounds for treating interleukin-1 mediated disorders and dysfunctions such as bone and connective tissue metabolism disorders and immune dysfunction in a mammal. The methods of this invention comprise administering an interleukin-1 biosynthesis inhibiting amount of the compounds and salts of this invention to such a mammal.
    Type: Grant
    Filed: December 17, 1991
    Date of Patent: March 9, 1993
    Assignee: Pfizer Inc.
    Inventors: Carl J. Goddard, Douglas C. Hanson, Gary R. Schulte
  • Diastereomeric 5R,6S-6-(1R-hydroxyethyl)-2-(cis-1-oxo-3-thiolanylthio)-2-penem-3-carbox ylic acids
    Patent number: 5191077
    Abstract: Diastereomeric 5R,6S-6-(1R-hydroxyethyl)-2-(1S-oxo-3R-thiolanylthio)-2-penem-3-carboxylic acid and 5R,6S-6-(1R-hydroxyethyl)-2-(1R-oxo-3S-thiolanylthio)-2-penem-3-carboxylic acid, and pharmaceutically-acceptable salts and in vivo hydrolyzable esters thereof, useful as systemic antibacterial agents; and intermediates and processes which are useful in the said synthesis of said diastereoisomers.
    Type: Grant
    Filed: January 28, 1991
    Date of Patent: March 2, 1993
    Assignee: Pfizer Inc.
    Inventor: Robert A. Volkmann
  • Process for the preparation of penems
    Patent number: 5191075
    Abstract: An efficient, multistep process for the synthesis of certain 6-(1-hydroxyethyl) 2-substituted penem antibiotics from 2-[4R-(triphenylmethylthio)-3S-(1R-(dimethyl-t-butylsilyloxy)ethyl)-2-azet idon-1-yl]acetic acid esters.
    Type: Grant
    Filed: March 17, 1992
    Date of Patent: March 2, 1993
    Assignee: Pfizer Inc
    Inventors: Brian T. O'Neill, Douglas Phillips
  • Synergistic combinations in the treatment of anxiety
    Patent number: 5189037
    Abstract: Combinations having synergistic anxiolytic activity which comprise a first component selected from the group consisting of 8-hydroxy-2-(dipropylamino)-1,2,3,4-tetrahydronaphthalene, gepirone, ipsapirone, tandospirone, (7S,9S)-2-(2-pyrimidyl)-7-(succinimidomethyl)-perhydro-1H-pyrido[1,2-a]pyr azine, or chlordiazepoxide; and a second component selected from the group consisting of 1-(2-pyrimidyl)pyrazine and idazoxan.
    Type: Grant
    Filed: April 2, 1992
    Date of Patent: February 23, 1993
    Assignee: Pfizer Inc
    Inventor: Patricia A. Seymour
  • Bail applicator and method
    Patent number: 5185986
    Abstract: An apparatus and method for applying a cap member to a receptacle or container. The apparatus and method are particularly suitable for use in placing the cap member, including a bail, snugly onto the end of a receptacle adapted to contain a pharmaceutical agent.
    Type: Grant
    Filed: February 11, 1992
    Date of Patent: February 16, 1993
    Assignee: Pfizer, Inc.
    Inventors: John J. Connolly, John T. Kawochka