Patents Assigned to Pfizer Inc.
  • Patent number: 4863948
    Abstract: A series of novel alkanesulphonamidophenyl-N-alkyl-N-(heterocyclic-alkyl)alkylamine derivatives have been prepared, including their pharmaceutically acceptable salts, wherein the heterocyclic moiety is a 5- or 6-membered nitrogen-containing heterocyclic group which is attached to the adjacent carbon atom by a carbon or nitrogen atom and optionally contains a further heteroatom selected from oxygen and nitrogen, said nitrogen-containing heterocyclic group being either (i) substituted by a phenyl or benzyl group or (ii) fused at two adjacent carbon atoms to a benzene ring, with the resulting heterocyclic ring moiety also being optionally substituted. These particular compounds are useful in therapy as highly effective anti-arrhythmic agents and therefore, are of value in the treatment of various cardiac arrythmias. The most preferred member compound of the series is 2-hydroxy-2-(4-methanesulphonamidophenyl)-N-methyl-N-[2-(6-chloro-2H-isoin dolin-1-on-2-yl)ethyl]ethylamine.
    Type: Grant
    Filed: April 9, 1987
    Date of Patent: September 5, 1989
    Assignee: Pfizer, Inc.
    Inventors: John E. Arrowsmith, Peter E. Cross, Geoffrey N. Thomas
  • Patent number: 4864046
    Abstract: Intermediates and a stepwise process for the conversion of ethyl 4-chloro-3R-hydroxybutyrate to optically active compounds of the formula ##STR1## wherein R is (C.sub.1 -C.sub.3)alkyl, phenyl or tolyl. The later compounds are in turn useful as an intermediate in the preparation of penem antibiotic 5R,6S-6-(1R-hydroxyethyl)-2-(1R-oxo-3S-thiolanylthio)-2-penem-3-carboxylic acic and corresponding pharmaceutically acceptable salts and esters.
    Type: Grant
    Filed: February 9, 1989
    Date of Patent: September 5, 1989
    Assignee: Pfizer Inc.
    Inventor: Robert A. Volkmann
  • Patent number: 4863934
    Abstract: Bicyclic fused benzenoid compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, where M is O, CH.sub.2 or NR.sub.6 ; R.sub.6 is hydrogen, formyl, carbobenzyloxy or certain carboalkoxyalkyl, alkanoyl, alkyl, aralkyl or aralkylcarbonyl groups;A' is:(1) A where one of A and B is hydrogen such that when A is hydrogen, B is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 1 or 2; when B is hydrogen, A is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 0 or 1, when taken together A and OR.sub.1 form a lactone or certain derivatives thereof;(2) A' is ##STR2## (3) A' is Q.sub.3 ; Q is CO.sub.2 R.sub.7, COR.sub.8, C(OH)R.sub.8 R.sub.9, CN, CONR.sub.12 R.sub.13, CH.sub.2 NR.sub.12 R.sub.13, CH.sub.2 NHCOR.sub.14, CH.sub.2 NHSO.sub.2 R.sub.17 or 5-tetrazoyl;Q.sub.3 is ##STR3## 5-tetrazolyl, CH.sub.2 CONHCOR.sub.7, COOH or certain ester, amide, carboximido or sulfonimido derivatives thereof, CONHOH, CONHCONH.sub.2, or COCH.sub.2 Q.sub.4 where Q.sub.
    Type: Grant
    Filed: December 1, 1988
    Date of Patent: September 5, 1989
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4861596
    Abstract: A method for enhancing the unrolling of a rolled active agent-containing laminate device in an aqueous use environment which comprises coating one side of the device with an elastomer prior to constraining it in a rolled configuration; and the devices so treated.
    Type: Grant
    Filed: March 21, 1988
    Date of Patent: August 29, 1989
    Assignee: Pfizer Inc.
    Inventors: Alan C. Curtiss, Jeelin Lo
  • Patent number: 4861794
    Abstract: This invention relates to the use of certain 3-substituted-2-oxindole-1-carboxamides of the formula ##STR1## and the pharmaceutically-acceptable base salts thereof wherein X is H, Cl or F; Y is H or Cl; and R is benzyl or thienyl 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: April 13, 1988
    Date of Patent: August 29, 1989
    Assignee: Pfizer Inc.
    Inventor: Ivan G. Otterness
  • Patent number: 4861880
    Abstract: Certain substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones are highly potent gabaergic agents, valuable in the treatment of individuals suffering from schizophrenia or reversing the side effects of a previously or concurrently administered neuroleptic agent; or in the treatment of epilepsy. A wider class of substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones, together with 1-phenyl-3-(2-pyrrolidinylidene)-2(1H,3H)-indolones, and homologs thereof, are valuable in the treatment of anxiety.
    Type: Grant
    Filed: August 15, 1984
    Date of Patent: August 29, 1989
    Assignee: Pfizer Inc.
    Inventors: Harry R. Howard, Jr., Reinhard Sarges
  • Patent number: 4861891
    Abstract: Certain N-substituted nicotinamide compounds having formula (I) below ##STR1## and pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is 1-piperidyl, 1-(3-indolyl)ethyl, C.sub.1-4 alkyl, phenyl, 1-(1-phenylethyl), benzyl or mono-substituted benzyl wherein the substituent is methyl, methoxy, chloro or fluoro; and R.sup.2 is bicyclo[2.2.1]hept-2-yl or ##STR2## wherein Y is hydrogen, fluoro or chloro; and X is hydrogen, fluoro, chloro, methoxy, trifluoromethyl, cyano, carboxy, carbo (C.sub.1-4 alkoxy), methylcarbamoyl or dimethylcarbamoyl function as selective inhibitors of calcium-independent phosphodiesterase and are useful as antidepressants.
    Type: Grant
    Filed: August 31, 1988
    Date of Patent: August 29, 1989
    Assignee: Pfizer Inc.
    Inventors: Nicholas A. Saccomano, Fredric J. Vinick
  • Patent number: 4861779
    Abstract: Antibacterial compounds have the formula ##STR1## wherein R.sup.1 is hydrogen, a pharmaceutically acceptable cation, or alkyl; A is CH, CF, CCl or N; Y is alkyl, haloalkyl, cyclopropyl, vinyl, methoxy, N-methylamino, p-fluorophenyl, p-hydroxyphenyl or p-aminophenyl; or A is carbon and is taken together with Y and the carbon and nitrogen to which A and Y are attached to form a five to seven membered ring which is optionally substituted; and R.sup.2 is a bridged-diazabicycloalkyl group.
    Type: Grant
    Filed: August 19, 1986
    Date of Patent: August 29, 1989
    Assignee: Pfizer Inc.
    Inventors: Martin R. Jefson, Paul R. Mc Guirk
  • Patent number: 4859686
    Abstract: 4-Aryl-3-alkoxycarbonyl-6-methyl-5-carbamyl-2-triazolylalkoxymethyl-1,4-dih yd ropyridines as anti-allergic and anti-inflammatory agents.
    Type: Grant
    Filed: January 6, 1989
    Date of Patent: August 22, 1989
    Assignee: Pfizer Inc.
    Inventors: Kelvin Cooper, John Steele, Kenneth Richardson
  • Patent number: 4859679
    Abstract: Quaternary 8-(alkyldithio)-1-(2-pyrimidyl)-quinolinium salts, inhibitors of the H.sup.30 /K.sup.+ ATPase enzyme, are useful in the treatment of ulcers.
    Type: Grant
    Filed: July 19, 1988
    Date of Patent: August 22, 1989
    Assignee: Pfizer Inc.
    Inventor: Conrad Santini
  • Patent number: 4859654
    Abstract: Polypeptides and derivatives thereof containing homocyclostatine and cyclostatine are useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin.
    Type: Grant
    Filed: June 1, 1988
    Date of Patent: August 22, 1989
    Assignee: Pfizer Inc.
    Inventors: Dennis J. Hoover, Robert L. Rosati
  • Patent number: 4857641
    Abstract: Antibacterial 12,12'-anhydro-9R-hydroxy-9-deoxoerythromycin A derivatives, intermediate therefor and process of 12,12'-dehydration.
    Type: Grant
    Filed: August 14, 1987
    Date of Patent: August 15, 1989
    Assignee: Pfizer Inc.
    Inventor: James R. Hauske
  • Patent number: 4855454
    Abstract: Amides of L-aspartyl-D-amino acid dipeptides of the formula ##STR1## and physiologically acceptable cationic and acid addition salts thereof wherein R.sup.a is methyl, ethyl, n-propyl or isopropyl; R is a branched member selected from the group consisting of fenchyl, diisopropylcarbinyl, d-methyl-t-butylcarbinyl, d-ethyl-t-butylcarbinyl, di-t-butylcarbinyl, 2-methylthio-2,4-dimethylpentan-3-yl, ##STR2## where at least one of R.sup.3, R.sup.4, R.sup.5, R.sup.6 is alkyl having from one to four carbon atoms and the remainder are hydrogen or alkyl having from one to four carbon atoms, X is O, S, SO, SO.sub.2, C.dbd.O or CHOH; m is zero or 1-4, n and p are each zero, 1, 2 or 3 where the sum of n+p is not greater than 3 and the sum of the carbon atoms in R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is not greater than six, and when both of R.sup.3 and R.sup.4 or R.sup.5 and R.sup.6 are alkyl they are methyl or ethyl, ##STR3## where one of R.sup.7, R.sup.8, R.sup.
    Type: Grant
    Filed: July 13, 1988
    Date of Patent: August 8, 1989
    Assignee: Pfizer Inc.
    Inventors: Thomas M. Brennan, Michael E. Hendrick
  • Patent number: 4855303
    Abstract: Polypeptides containing fluorinated cyclostatine derivatives as antihypertensive agents.
    Type: Grant
    Filed: June 10, 1988
    Date of Patent: August 8, 1989
    Assignee: Pfizer Inc.
    Inventor: Dennis J. Hoover
  • Patent number: 4855500
    Abstract: An improved condensation process for preparing N-[4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenylidene]methanamine from 4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenone and methylamine is disclosed. The process involves the use of a hydratable molecular sieve having a pore size that is at least about three Angstrom units in diameter as the dehydrating agent (catalyst) in a reaction-inert aprotic organic solvent. The ketimine final product so produced is known to be useful as an intermediate leading to cis-(1S)(4S)-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthal enamine (sertraline), which is an anti-depressant agent.
    Type: Grant
    Filed: May 4, 1988
    Date of Patent: August 8, 1989
    Assignee: Pfizer Inc.
    Inventor: James C. Spavins
  • Patent number: 4853409
    Abstract: This invention relates to the use of certain 3-substituted-2-oxindole-1-carboxamides of the formula ##STR1## and the pharmaceutically-acceptable base salts thereof wherein X is H, Cl or F; Y is H or Cl; and R is benzyl or thienyl to suppress T-cell function in a mammal. This invention also relates to the use of such compounds for treating T-cell mediated autoimmune disorders of the systemic or organ specific type. The methods of this invention comprise administering a T-cell function suppressing amount of the compounds and salts of this invention to such a mammal.
    Type: Grant
    Filed: April 13, 1988
    Date of Patent: August 1, 1989
    Assignee: Pfizer Inc.
    Inventor: Henry J. Showell
  • Patent number: 4853410
    Abstract: Racemic and chiral (2R,4R)-4-c-hydroxy-2-4-(substituted)chroman(and thiochroman)-4-acetic acids and their pharmaceutically acceptable salts, their use in the treatment of diabetic complications and intermediates therefor.
    Type: Grant
    Filed: October 9, 1987
    Date of Patent: August 1, 1989
    Assignee: Pfizer Inc.
    Inventor: Christopher A. Lipinski
  • Patent number: 4853392
    Abstract: Compounds of the formula ##STR1## where R.sup.1 is lower alkyl, R.sup.2 is chlorophenyl, Y is alkylene, X is heterocyclic and Z is a fused ring are useful as antiinflammatory and antiallergy agents.
    Type: Grant
    Filed: July 11, 1988
    Date of Patent: August 1, 1989
    Assignee: Pfizer Inc.
    Inventors: Kelvin Cooper, Peter E. Cross, Michael J. Fray, Kenneth Richardson
  • Patent number: 4851130
    Abstract: When an aqueous system containing dissolved oxygen and erythorbate or ascorbate is passed through an activated carbon bed, the oxygen is removed at ambient temperatures. This method of oxygen removal finds practical application in the removal of oxygen from boiler condensate, low temperature boiler feedwater and oil well injection water or brine.
    Type: Grant
    Filed: November 30, 1988
    Date of Patent: July 25, 1989
    Assignee: Pfizer Inc.
    Inventor: Ralph D. May
  • Patent number: 4851388
    Abstract: Peptides useful as antiinfective agents, immunomodulators for stimulation of host defenses in patients with an increased risk of bacterial infections, intermediates and process therefor.
    Type: Grant
    Filed: August 17, 1987
    Date of Patent: July 25, 1989
    Assignee: Pfizer Inc.
    Inventor: Gene M. Bright