Patents Assigned to Pfizer Inc.
  • Herbicidal compositions containing salinomycin
    Patent number: 4584009
    Abstract: Herbicidal compositions containing salinomycin for the control of weeds are disclosed.
    Type: Grant
    Filed: December 13, 1984
    Date of Patent: April 22, 1986
    Assignee: Pfizer Inc.
    Inventors: Meiro Adachi, Kenji Hamada
  • Antibacterial 2-amino-oxazolinones and process therefor
    Patent number: 4584385
    Abstract: A series of novel antibacterially active derivatives of indolmycin as well as some prodrug forms of indolmycin is disclosed. A novel process for the production of these compounds is also disclosed.
    Type: Grant
    Filed: February 4, 1985
    Date of Patent: April 22, 1986
    Assignee: Pfizer Inc.
    Inventor: John P. Dirlam
  • Erythromycin D and esters thereof by fermentation with Nocardia sp. ATCC 39043
    Patent number: 4582796
    Abstract: Fermentation of a culture of Nocardia sp. ATCC 39043 produces an antibiotic complex comprising erythromycin D, 3",4"-di-O-acetylerythromycin D, 3"-O-acetyl-4"-O-propionylerythromycin D and 4"-O-acetylerythromycin D. The components are separated and are each useful in vitro and in vivo as antibacterial agents. If erythromycin D is the desired product, the esters can be hydrolyzed prior to the separation of the erythromycin D.
    Type: Grant
    Filed: April 16, 1984
    Date of Patent: April 15, 1986
    Assignee: Pfizer, Inc.
    Inventors: Walter D. Celmer, Walter P. Cullen, Paul C. Watts, Riichiro Shibakawa, Junsuke Tone
  • Trimazosin as an anti-atherosclerosis agent
    Patent number: 4582832
    Abstract: The use of trimazosin or a pharmaceutically acceptable acid addition salt thereof as an agent for retarding the development of atherosclerosis in a mammal, especially for retarding and reducing the development of fibrous plaques associated with atherosclerosis.
    Type: Grant
    Filed: August 28, 1985
    Date of Patent: April 15, 1986
    Assignee: Pfizer Inc.
    Inventor: Archie C. Swindell
  • Antibacterial 6'-(2-amino-2-[4-acyloxyphenyl]acetamido)penicillanoyloxymethyl penicillanate 1,1-dioxide compounds
    Patent number: 4582829
    Abstract: 6-(2-Amino-2-[4-acyloxyphenyl]acetamido)penicillanoyloxymethyl esters of penicillanic acid 1,1-dioxide are useful as antibacterial agents. Derivatives of the aforesaid antibacterial agents which have an amino protecting group on the amino function in the 2-amino-2-(4-acyloxyphenyl)acetamido side chain are useful intermediates to the antibacterial agents themselves.
    Type: Grant
    Filed: May 15, 1985
    Date of Patent: April 15, 1986
    Assignee: Pfizer Inc.
    Inventor: Michael S. Kellogg
  • Anti-inflammatory polymorphic monoethanolamine salt of N-(2-pyridyl)-2-methyl-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide compound, composition, and method of use therefor
    Patent number: 4582831
    Abstract: A novel crystalline form of the monoethanolamine salt of N-(2-pyridyl)-2-methyl-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide has been prepared. This novel crystalline form is designated as polymorph I and is useful in therapy as a non-steroidal anti-arthritic agent. Methods for preparing this polymorph from readily available materials are provided.
    Type: Grant
    Filed: November 16, 1984
    Date of Patent: April 15, 1986
    Assignee: Pfizer Inc.
    Inventor: Robert L. Robertson
  • 2-(2-amino-2-thiazolin-4-yl)acetic acid
    Patent number: 4582907
    Abstract: 2-(2-Amino-2-thiazolin-4-yl)acetic acid or a pharmaceutically acceptable acid addition or cationic salt thereof useful in removal of excessive levels of certain metal ions from animals, including humans, and in protection of said animals from exposure to radioactivity.
    Type: Grant
    Filed: April 8, 1985
    Date of Patent: April 15, 1986
    Assignee: Pfizer Inc.
    Inventor: Malcolm M. Campbell
  • Process for the preparation of biotin
    Patent number: 4581459
    Abstract: A novel process is described for preparation of biotin comprising preparation of substituted 3H, 5H-imidazo[1, 5c]tetrahydro thiazoles by contacting the boron trifluoride adduct of an appropriate thiazoline with the metallic derivative of an ester enolate, reducing the ester, hydrolyzing the thiazolidine moiety and hydrolyzing or oxidizing the resultant compound. Intermediates obtained in the preparation of biotin by the above process and alternate procedures for preparing said intermediates are also presented. A novel process for preparation of d-biotin is also given.
    Type: Grant
    Filed: May 17, 1984
    Date of Patent: April 8, 1986
    Assignee: Pfizer Inc.
    Inventor: Robert A. Volkmann
  • Antiinflammatory compositions and methods
    Patent number: 4579846
    Abstract: An improved antiinflammatory composition and method of treating inflammation which employs a combination of antiinflammatory piroxicam, or a pharmaceutically acceptable salt thereof, with analgesic acetaminophen, antidepressant doxepin, bronchodilator pirbuterol, minor tranquilizer diazepam, or antihypertensive trimazosin.
    Type: Grant
    Filed: January 28, 1985
    Date of Patent: April 1, 1986
    Assignee: Pfizer Inc.
    Inventors: Thomas C. Crawford, Stanley L. Keely, David L. Larson, Joseph G. Lombardino, James J. Maciejko
  • Immobilization of catalytically active microorganisms in agar gel fibers
    Patent number: 4578354
    Abstract: A process for immobilizing enzyme-containing microbial cells by contacting such cells with an aqueous agar solution containing from about 1.0 to 8.0% sulfate moiety on a weight/weight basis, contacting a solution of inorganic sodium salts with a stream of the cell mixture whereby agar fibers containing cells are formed; and recovering the cell-containing agar fibers produced.
    Type: Grant
    Filed: May 9, 1983
    Date of Patent: March 25, 1986
    Assignee: Pfizer Inc.
    Inventor: John J. Cannon
  • Substituted hexahydrobenzo[e]indene and octahydrophenanthrene CNS agents and pharmaceutical compositions thereof
    Patent number: 4576964
    Abstract: Tricyclic benzo fused compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, wherein n is zero, 1 or 2, and t is 1 or 2; M is CH or N, R.sub.1 is H or certain acyl groups; Q is CO.sub.2 R.sub.4, COR.sub.5, C(OR.sub.7)R.sub.5 R.sub.6, CN, CONR.sub.9 R.sub.10, CH.sub.2 NR.sub.9 R.sub.10, CH.sub.2 NHCOR.sub.11, CH.sub.2 NHSO.sub.2 R.sub.12, 5-tetrazolyl or when n is 1, Q and OR.sub.1 together form a lactone or certain reduced derivatives thereof; and Z is certain alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl groups, are valuable central nervous system active agents, methods for their use, pharmaceutical compositions containing them and certain intermediates therefor.
    Type: Grant
    Filed: June 7, 1984
    Date of Patent: March 18, 1986
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Spiro-imidazolidines as aldose reductase inhibitors and their pharmaceutical use
    Patent number: 4575507
    Abstract: Compounds related to 3',4'-dihydrospiro[imidazolidine-4,1'(2'H)-naphthalene]2,3',5-trione, spiro[chroman-4,4'-imidazolidine]2,2',5'-trione and 1',2'-dihydrospiro[imidazolidine-4,4'-(3'H)-quinoline 2,2'5-trione and reduced products thereof as aldose reductase inhibitors.
    Type: Grant
    Filed: May 29, 1985
    Date of Patent: March 11, 1986
    Assignee: Pfizer Inc.
    Inventor: Christopher A. Lipinski
  • Dihydropyridines
    Patent number: 4572908
    Abstract: Dihydropyridine anti-ischaemic agents of the formula: ##STR1## and their salts where R is aryl or heteroaryl, R.sup.1 and R.sup.2 are each C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl, Y is --(CH.sub.2).sub.n -- where n is 2, 3, or 4 and is optionally substituted by 1 or 2 CH.sub.3 groups, and R.sup.3 is an optionally substituted 5- or 6-membered heterocyclic group attached to the adjacent N atom by a C atom, said group R.sup.3 being optionally fused to a further heterocyclic group or to a benzene ring.
    Type: Grant
    Filed: December 16, 1983
    Date of Patent: February 25, 1986
    Assignee: Pfizer Inc.
    Inventors: Simon F. Campbell, Peter E. Cross, John K. Stubbs, John E. Arrowsmith
  • 2-(Secondary aminoalkoxymethyl) dihydropyridine derivatives as anti-ischaemic and antihypertensive agents
    Patent number: 4572909
    Abstract: A dihydropyridine compound of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof, whereinY is --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 --, --CH.sub.2 CH(CH.sub.3)-- or --CH.sub.2 C(CH.sub.3).sub.2 --;R is aryl or heteroaryl;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl; andR.sup.3 is hydrogen, C.sub.1 -C.sub.4 alkyl, 2-(C.sub.1 -C.sub.4 alkoxy)ethyl, cyclopropylmethyl, benzyl, or --(CH.sub.2).sub.m COR.sup.4 where m is 1, 2 or 3 andR.sup.4 is hydroxy, C.sub.1 -C.sub.4 alkoxy or --NR.sup.5 R.sup.6 where R.sup.5 and R.sup.6 are each independently hydrogen or C.sub.1 -C.sub.4 alkylcan be employed for treating or preventing a heart condition or hypertension.
    Type: Grant
    Filed: February 3, 1984
    Date of Patent: February 25, 1986
    Assignee: Pfizer Inc.
    Inventors: Simon F. Campbell, Peter E. Cross, John K. Stubbs
  • N,3-Disubstituted 2-oxindole-1-carboxamides as analgesic and antiinflammatory agents
    Patent number: 4569942
    Abstract: Certain 2-oxindole-1-carboxamide compounds having an acyl substituent at the 3-position, and also further substituted on the carboxamide nitrogen by an alkyl, cycloalkyl, phenyl or substituted phenyl group, are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic and antiinflammatory agents in mammalian subjects. These 2-oxindole-1-carboxamide compounds are of particular value for ameliorating pain in human patients recovering from surgery or trauma, and alleviating the symptoms of chronic diseases, such as rheumatoid arthritis and osteoarthritis, in human subjects.Certain 2-oxindole-1-carboxamide compounds unsubstituted at C-3, but having a substituent on the carboxamide nitrogen, are useful as intermediates to the analgesic and antiinflammatory agents of the invention.
    Type: Grant
    Filed: March 22, 1985
    Date of Patent: February 11, 1986
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin
  • Certain 5-aryl-2-[(4-aryl)-4-hydroxybutyn-2-yl]-1,2,3,4-.gamma.-carbolines
    Patent number: 4568749
    Abstract: A novel process for preparing various 2-substituted-5-aryl-1,2,3,4-tetrahydro-.gamma.-carboline derivatives is provided, which involves (1) condensing a corresponding 2-unsubstituted compound with formaldehyde and an appropriate acetylenic derivative in the presence of cuprous chloride or cuprous bromide, followed by (2) reduction of the corresponding unsaturated intermediate to yield the desired final product. The latter compounds are known to be useful as tranquilizing agents, with 2-[4-(p-fluorophenyl)-4-hydroxybutyl]-5-(p-fluorophenyl)-8-fluoro-1,2,3,4- tetrahydro-.gamma.-carboline representing a preferred final product. The aforesaid unsaturated intermediates are all novel compounds.
    Type: Grant
    Filed: February 11, 1985
    Date of Patent: February 4, 1986
    Assignee: Pfizer Inc.
    Inventor: Willard M. Welch, Jr.
  • 2-Carbobenzoxy-8-fluoro-5-(p-fluorophenyl-2,3,4,5-tetrahydr o-1H-pyrido[4,3-b]indole
    Patent number: 4568748
    Abstract: 1,1-Di(p-fluorophenyl)urea, 2-carbobenzoxy-8-fluoro-5-(p-fluorophenyl)-2,3,4,5-tetrahydro-1H-pyrido[4, 3-b]indole, an efficient process for converting the former to the latter, further comprising conversion of the latter to 8-fluoro-5-(p-fluorophenyl)-2-[4-(p-fluorophenyl)-4-hydroxybutyl)-]2,3,4,5 -tetrahydro-1H-pyrido[4,3-b]indole (flutroline) or to 8-fluoro-5-(p-fluorophenyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole (an alternative flutroline intermediate).
    Type: Grant
    Filed: August 16, 1984
    Date of Patent: February 4, 1986
    Assignee: Pfizer Inc.
    Inventor: Stephen S. Massett
  • 2-(4-Pyrimidone alkoxyalkyl) dihydropyridine anti-ischaemic and antihypertensive agents
    Patent number: 4568677
    Abstract: 1,4-Dihydropyridine derivatives of the formula: ##STR1## wherein R is aryl or heteroaryl; R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl; X is a 5 or 6 membered nitrogen-containing heterocyclic ring which is substituted with one or more hydroxyl or oxo groups and which may optionally be fused to a further 5 or 6 membered nitrogen-containing heterocyclic ring, and which may optionally be further substituted in the heterocyclic ring or further fused heterocyclic ring; Y is --(CH.sub.2).sub.n --, --CH.sub.2 CH(CH.sub.3)-- or --CH.sub.2 C(CH.sub.3).sub.2 --; and n is 1 to 3 when X is linked to Y by a ring carbon atom, or 2 or 3 when X is linked to Y by a ring nitrogen atom; and their pharmaceutically acceptable salts, and pharmacuetical preparation containing such compounds, have utility as anti-ischaemic and antihypertensive agents.
    Type: Grant
    Filed: June 21, 1984
    Date of Patent: February 4, 1986
    Assignee: Pfizer Inc.
    Inventors: David Alker, Peter E. Cross, Simon F. Campbell
  • High temperature drilling fluids
    Patent number: 4566978
    Abstract: An aqueous drilling fluid suitable for high-temperature use comprising a water base, clay suspended in said base and from about 0.01-25 pounds per barrel total composition of a hydrolyzed terpolymer of maleic anhydride, styrene and a third monomer selected from acrylamide, methacrylamide, acrylic acid or methacrylic acid, the molar ratio of maleic anhydride to styrene to said third monomer being from about 30:10:60 to 50:40:10, and the alkali metal, ammonium and lower aliphatic amine salts thereof, the weight-average molecular weight of said hydrolyzed terpolymer being from about 500-10,000. An improved drilling process wherein such fluids remain flowable at elevated temperatures is also disclosed.
    Type: Grant
    Filed: May 21, 1984
    Date of Patent: January 28, 1986
    Assignee: Pfizer Inc.
    Inventors: Randel E. Stong, Stanley W. Walinsky
  • Indigoid dyes
    Patent number: 4567048
    Abstract: A series of novel water-soluble sulfonated indoxyl derivatives have been prepared, including their base salts with pharmacologically acceptable cations. These particular compounds are useful as food dyes or as cosmetic colorants. 2,2'-(1,4-phenylenedimethylidyne)-bis(2,3-dihydro-3-oxo-1H-indole-5-sulfon ic acid) represents a typical and preferred member compound. Methods for preparing these compounds are provided.
    Type: Grant
    Filed: April 30, 1984
    Date of Patent: January 28, 1986
    Assignee: Pfizer Inc.
    Inventor: Gordon D. Gruetzmacher