Patents Represented by Attorney Charles J. Knuth

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  • 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
  • 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
  • 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
  • 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
  • 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
  • Bone prosthesis
    Patent number: 4578081
    Abstract: A bone prosthesis comprising at least one joint component replacing a natural joint half, which is provided with a shank adapted to be connected to the bone, wherein a set of joint components is provided, and the shank is designed as a bone replacement member, with a connection portion provided adapted to be connected to the bone at one end and at the other end to the shank.
    Type: Grant
    Filed: May 24, 1982
    Date of Patent: March 25, 1986
    Assignee: Howmedica International, Inc.
    Inventors: Hans E. Harder, Klaus Behrens, Rainer Kotz
  • 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
  • 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
  • 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
  • Arched bridge staple
    Patent number: 4570623
    Abstract: A bone staple for attaching tubular shaped soft tissue to bone, in which the transverse bridge of the staple has teeth on its underside to grip the tissue and is arch shaped so that the center of the bridge is above the bone surface when the staple legs are driven fully into a bone.
    Type: Grant
    Filed: June 2, 1983
    Date of Patent: February 18, 1986
    Assignee: Pfizer Hospital Products Group Inc.
    Inventors: Arthur E. Ellison, Rocco R. Borzone
  • 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
  • 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
  • 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.
  • Blood defoamer with improved liquid seal
    Patent number: 4568367
    Abstract: A blood defoamer for use in surgical procedures is disclosed comprising a porous defoaming element, a non-porous end piece in contact with a surface of the defoaming element, and a layer of fabric affixed to the end piece adjacent to said surface. Bypass of blood flow around the layer of fabric, which is situated downstream of the defoaming element, and accumulation of bubbles in the defoamed blood reservoir are prevented by bonding a suitably configured retaining ring to the end piece with a portion of the layer of fabric held in a fluid-tight seal between the end piece and the retaining ring.
    Type: Grant
    Filed: November 15, 1982
    Date of Patent: February 4, 1986
    Assignee: Shiley Incorporated
    Inventors: Robert F. Gremel, Kenneth M. Galt
  • 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
  • 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