Patents Represented by Attorney Albert E. Frost

Find this attorney in the Justia Lawyer Directory

  • 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
  • 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
  • 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-(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
  • Antiinflammatory salts of piroxicam
    Patent number: 4567179
    Abstract: Improved antiinflammatory salts of piroxicam with antidepressant doxepin, with bronchodilator pirbuterol or isoproterenol, with H.sub.2 -antagonist inhibitor 2-guanidino-4-(2-methyl-4-imidazolyl)thiazole, with pyridoxine, a member of the vitamin B.sub.6 complex, or with antihypertensive trimazosin.
    Type: Grant
    Filed: October 11, 1984
    Date of Patent: January 28, 1986
    Assignee: Pfizer, Inc.
    Inventor: Joseph G. Lombardino
  • Acyltripeptide immunostimulants
    Patent number: 4565653
    Abstract: Acyltripeptides having the formula below, pharmaceutically acceptable salts thereof and intermediates therefor; processes for their preparation and use as immunostimulant and antibacterial agents. ##STR1## wherein R.degree. is C.sub.1-6 alkyl; x is an integer and is 1 to 4.
    Type: Grant
    Filed: March 30, 1984
    Date of Patent: January 21, 1986
    Assignee: Pfizer Inc.
    Inventors: Jeffrey L. Ives, Frank C. Sciavolino
  • Hypoglycemic 5-pyrrolyl, indolyl and quinolyl substituted oxazolidine-2,4-diones and their use
    Patent number: 4565820
    Abstract: Hypoglycemic 5-chromanyl, 2,3-dihydro-5-benzo[b]-furanyl, 5-pyridyl, 5-quinolyl, 5-pyrrolyl, 5-indolyl, 5-thiazolyl, 5-oxazolyl, 5-isothiazolyl and 5-isoxazolyl oxazolidine-2,4-diones and the pharmaceutically-acceptable salts thereof; certain 3-acylated derivatives thereof; a method of treating hyperglycemic animals therewith; and intermediates useful in the preparation of said compounds.
    Type: Grant
    Filed: January 26, 1984
    Date of Patent: January 21, 1986
    Assignee: Pfizer Inc.
    Inventor: Rodney C. Schnur
  • Antiinflammatory methods
    Patent number: 4564614
    Abstract: An improved antiinflammatory composition and method of treating inflammation which employs a combination of a non-steroidal antiinflammatory agent such as piroxicam, or a pharmaceutically acceptable salt thereof, with pyridoxine.
    Type: Grant
    Filed: January 28, 1985
    Date of Patent: January 14, 1986
    Assignee: Pfizer Inc.
    Inventors: Thomas C. Crawford, Stanley L. Keely, David L. Larson, Joseph G. Lombardino, James J. Maciejko
  • Intermediates of hypoglycemic 5-substituted oxazolidine-2,4-diones
    Patent number: 4562267
    Abstract: Variously substituted alkyl 2-(furyl or thienyl)-2-hydroxyacetates and 2-(furyl or thienyl)-2-hydroxyacetamides are useful as intermediates for hypoglycemic oxazolidine-2,4-diones.
    Type: Grant
    Filed: October 14, 1983
    Date of Patent: December 31, 1985
    Assignee: Pfizer Inc.
    Inventor: Rodney C. Schnur
  • 1,3-Bis-(1H-1,2,4-triazol-1-yl)-2-perfluoro-alkylpropan-2-ol antifungal agents
    Patent number: 4560697
    Abstract: Compounds of the formula ##STR1## or a pharmaceutically or agriculturally acceptable acid addition salt thereof wherein R is (C.sub.1 -C.sub.5) perfluoroalkyl and R.sup.1 is H or CH.sub.3, method for their use in combatting fungal infections in plants, seeds and animals, including humans; and as antileishmanial agents, and pharmaceutical and agricultural compositions containing them.
    Type: Grant
    Filed: January 16, 1984
    Date of Patent: December 24, 1985
    Assignee: Pfizer Inc.
    Inventors: Kenneth Richardson, Peter J. Whittle
  • 2-(N-substituted guanidino)-4-hetero-arylthiazole antiulcer agents
    Patent number: 4560690
    Abstract: 2,4-Disubstituted thiazole compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof wherein X is NH and Y is CH or N, orX is S and Y is CH;R.sup.1 is certain straight or branched chain alkyl groups, (R.sup.3).sub.2 C.sub.6 H.sub.3, or (R.sup.3).sub.2 Ar(CH.sub.2).sub.n where n is an integer from 1 to 4, R.sup.3 is H or certain substituent groups and Ar is phenylene, naphthalene or the residue of certain heteroaromatic groups;R.sup.2 is H or (C.sub.1 -C.sub.4)alkyl; orR.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached form certain heterocyclic groups; andR.sup.4 is H, (C.sub.1 -C.sub.5)alkyl, NH.sub.2 or CH.sub.2 OH; a method for their use in treatment of gastric ulcers in mammals and pharmaceutical compositions containing said compounds.
    Type: Grant
    Filed: April 30, 1984
    Date of Patent: December 24, 1985
    Assignee: Pfizer Inc.
    Inventor: Lawrence A. Reiter
  • Antiinflammatory compositions and methods
    Patent number: 4559326
    Abstract: An improved antiinflammatory composition and method of treating inflammation which employs a combination of a non-steroidal antiinflammatory agent such as prioxicam, or a pharmaceutically acceptable salt thereof, with inositol.
    Type: Grant
    Filed: January 31, 1985
    Date of Patent: December 17, 1985
    Assignee: Pfizer Inc.
    Inventors: Thomas C. Crawford, Stanley L. Keely, David L. Larson, Joseph G. Lombardino, James J. Maciejko
  • N-Benzyl-imidazoles as selective inhibitors of the thromboxane synthetase enzyme
    Patent number: 4555516
    Abstract: The N-(substituted benzyl) imidazoles are selective enzyme inhibitors and thus are useful in the treatment of heart disease, circulatory and vascular problems.
    Type: Grant
    Filed: January 9, 1980
    Date of Patent: November 26, 1985
    Assignee: Pfizer Inc.
    Inventors: Peter E. Cross, Roger P. Dickinson
  • Antifungal 1-triazolyl-2-aryl-3-(5-trifluoromethylimidazol-1-yl)propan-2-ol derivatives
    Patent number: 4554286
    Abstract: 1-Triazolyl-2-aryl-3-(5-trifluoromethylimidazol-1-yl)propan-2-ol derivatives useful in the treatment of fungal infections in humans, animals and plants, and their preparation.
    Type: Grant
    Filed: May 3, 1984
    Date of Patent: November 19, 1985
    Assignee: Pfizer Inc.
    Inventors: Kenneth Richardson, Peter J. Whittle
  • Process for producing an acidic polycyclic ether antibiotic by cultivation of a novel strain of Streptomyces endus subspecies aureus
    Patent number: 4552843
    Abstract: A new acidic polycyclic ether antibiotic, CP-63,517, having the formula: ##STR1## and cationic salts thereof produced by submerged aerobic propagation of Streptomyces endus subsp. aureus, ATCC-39574, a new strain of microorganism isolated from a soil sample in Japan, a process for producing this antibiotic and methods for its use to improve feed utilization, promote growth of cattle and swine and to control coccidiosis.
    Type: Grant
    Filed: February 17, 1984
    Date of Patent: November 12, 1985
    Assignee: Pfizer Inc.
    Inventors: Walter D. Celmer, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone
  • Regeneration of 6-fluoro-4-chromanone from 6-fluoro-4-ureidochroman-4-carboxylic acid
    Patent number: 4551542
    Abstract: 6-Fluoro-4-chromanone can be regenerated from (R)-6-fluoro-4-ureidochroman-4-carboxylic acid, or from mixtures of (R)-6-fluoro-4-ureidochroman-4-carboxylic acid and its racemic modification, by oxidation with a permanganate, especially potassium permanganate. 6-Fluoro-4-chromanone is a chemical intermediate useful for preparing sorbinil, an aldose reductase inhibitor which can be used in clinical medicine for the control of the chronic complications of diabetes. (R)-6-Fluoro-4-ureidochroman-4-carboxylic acid and its racemic modification are by-products from the production of sorbinil from 6-fluoro-4-chromanone.
    Type: Grant
    Filed: September 26, 1984
    Date of Patent: November 5, 1985
    Assignee: Pfizer Inc.
    Inventor: Bernard S. Moore
  • Heterocyclic thromboxane synthetase inhibitors and pharmaceutical compositions containing them
    Patent number: 4551468
    Abstract: Heterocyclic thromboxane synthetase inhibitors of the formula ##STR1## wherein R.sup.1, which is attached to the 2-, 3- or 4-position, is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, hydroxy or C.sub.1 -C.sub.4 alkoxy;Y, which is attached to the 2- or 3-position, is --COOH, --COO(C.sub.1 -C.sub.4 alkyl) or --CONH.sub.2 ;X is O, S, NH, N(C.sub.1 -C.sub.4 alkyl) or N(benzyl); andR, which is attached to the 5-, 6- or 7-position, is a group of the formula ##STR2## or (3- or 4-pyridyl)--Z.sup.2 -- wherein Z.sup.1 is --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 O-- and Z.sup.2 is --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 O-- or --OCH.sub.2 --;and their pharmaceutically acceptable salts; processes for their preparation, and pharmaceutical compositions containing them which are useful, for example, in the treatment of thrombosis.
    Type: Grant
    Filed: August 22, 1983
    Date of Patent: November 5, 1985
    Assignee: Pfizer Inc.
    Inventors: Peter E. Cross, Roger P. Dickinson, Geoffrey N. Thomas
  • Anti-inflammatory 2-methyl-2H-1,2-benzo-(or -thieno-)thiazine-3-carboxamide 1,1-dioxide derivatives, compositions, and method of use therefor
    Patent number: 4551452
    Abstract: Certain enol ether derivatives of oxicams (1,1-dioxides of N-heteroaryl-4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxamides and N-heteroaryl-4-hydroxy-2-methyl-2H-thieno[2,3-e]-1,2-thiazine-3-carboxamid es) are useful as prodrugs of these antiinflammatory compounds.
    Type: Grant
    Filed: May 2, 1984
    Date of Patent: November 5, 1985
    Assignee: Pfizer Inc.
    Inventor: Anthony Marfat