Patents Represented by Attorney Alan D. Lourie

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  • Process for preparing beta-methyl-gamma-oxo-4-(4-oxo-1(4H)-pyridinyl) derivative of benzene butanoic acid
    Patent number: 4782159
    Abstract: A process for the prepartion of 3-[4-(4-oxo-1,4-dihydropyridin-1-yl)benzoyl]butanoic acid which comprises the reaction of 3-(4-fluorobenzoyl)butanoic acid with 4-hydroxypyridine under aqueous conditions in the presence of a base.
    Type: Grant
    Filed: January 29, 1988
    Date of Patent: November 1, 1988
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Michael B. Mitchell, Kiritkant D. Pancholi
  • Inhibition of interleukin-1 by monocytes and/or macrophages
    Patent number: 4780470
    Abstract: A method of inhibiting the production of interleukin-1 by monocytes in a human in need thereof which comprises administering to such human an effective interleukin-1 production inhibiting amount of a 4,5-diaryl-2(substituted)imidazole.
    Type: Grant
    Filed: August 19, 1986
    Date of Patent: October 25, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: Paul E. Bender, Don E. Griswold, Nabil Hanna, John C. Lee
  • Inhibition of interleukin-1 production by monocytes and/or macrophages
    Patent number: 4778806
    Abstract: A method of inhibiting the production of interleukin-1 by monocytes and/or macrophages in a human in need thereof which comprises administering to such human an effective interleukin-1 production inhibiting amount of a 2-2'-[1,3-propan-2-onediyl-bis(thio)]bis-1H-imidazole or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 19, 1986
    Date of Patent: October 18, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: Paul E. Bender, Don E. Griswold, Nabil Hanna, John C. Lee
  • Affinity chromatography sorbent
    Patent number: 4778846
    Abstract: A novel process for the isolation and purification of vancomycin class antibiotics which utilized affinity chromatography by the formation of a sorption complex between the antibiotic and an immobilizing ligand selected from -D-alanyl-D-alanine or -X-D-alanyl-D-alanine, wherein X is an amino acid radical and the novel affinity chromatography sorbent employed therein are disclosed.
    Type: Grant
    Filed: February 4, 1987
    Date of Patent: October 18, 1988
    Assignee: Smithkline Beckman Corporation
    Inventors: Robert D. Sitrin, Kenneth M. Snader, Gail F. Wasserman
  • Pyrimidylalkylthio benzimidale compounds, pharmaceutical compositions and use
    Patent number: 4777172
    Abstract: This invention relates to 2- and 4-pyrimidinylmethylsulphinyl(and thio)benzimidazoles in which the pyrimidyl group is substituted by an optionally substituted amino group. These compounds inhibit exogenously and endogenously stimulated gastric acid secretion.
    Type: Grant
    Filed: February 14, 1986
    Date of Patent: October 11, 1988
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Robert J. Ife, Thomas H. Brown
  • Leukotriene antagonists
    Patent number: 4775662
    Abstract: The compounds represented by the formula (I) ##STR1## wherein n is 1 or 2; m is 0, 1 or 2; p is 9, 10, 11, 12 or 13; X is hydrogen or hydroxyl; R is hydroxyl or amino; R.sub.1 is hydrogen, amino or ##STR2## and R.sub.2 is hydroxyl, amino, ##STR3## with the proviso that when m is 0, R.sub.1 is hydrogen or pharmaceutically acceptable salts thereof have been found to be leukotriene antagonists and useful in the treatment of diseases in which leukotrienes are a factor, such as asthma.
    Type: Grant
    Filed: October 29, 1987
    Date of Patent: October 4, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: John G. Gleason, Thomas W. Ku
  • Dopamine .beta.-hydroxylase inhibitors
    Patent number: 4772723
    Abstract: Potent DBH Inhibitors having the formula: ##STR1## wherein R is --CO.sub.2 H or --CH.sub.2 NHR.sup.1 can be used to inhibit DBH activity in mammals.
    Type: Grant
    Filed: April 16, 1985
    Date of Patent: September 20, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: James S. Frazee, Carl Kaiser, Lawrence I. Kruse
  • 3,4-diamino-1,2,5-thiadiazole-1-oxides having histamine H.sub.1 -antagonist activity
    Patent number: 4771058
    Abstract: The invention relates to a class of 3,4-diamino-1,2,5-thiadiazole-1-oxides which have histamine H.sub.1 -antagonist activity. A preferred compound of the invention is 3-[3-(5-bromo-3-methylpyrid-2-ylamino)-propylamino]-4-amino-1,2,5-thiadiaz ole-1-oxide.
    Type: Grant
    Filed: June 11, 1986
    Date of Patent: September 13, 1988
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: David G. Cooper, George S. Sach
  • 2,3,4,8,9,9A-Hexahydro-4-aryl-1H-indeno(1,7-CD)azepines
    Patent number: 4769368
    Abstract: 2,3,4,8,9,9a-Hexahydro-4-aryl-1H-indeno[1,7-cd;]-azepines are selective dopamine receptor site binding agents.
    Type: Grant
    Filed: February 10, 1986
    Date of Patent: September 6, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: Carl Kaiser, Hye-Ja Oh, Joseph Weinstock
  • Substituted tetrahydro isoquinoline intermediates
    Patent number: 4767862
    Abstract: Compounds having the formula ##STR1## are .beta.-adrenergic receptor antagonists. Also disclosed are pharmaceutical compositions and methods for producing .beta.-adrenergic receptor antagonistic activity in animals including man.
    Type: Grant
    Filed: August 24, 1987
    Date of Patent: August 30, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: Carl Kaiser, Lawrence I. Kruse
  • Antitumor pharmaceutical compositions and methods for treating tumors employing .alpha.,.omega.-bis(disubstitutedphosphino)hydrocarbon derivatives or [.alpha., .omega.-bis(disubstitutedphosphino)hydrocarbon] d i
    Patent number: 4766226
    Abstract: Antitumor pharmaceutical compositions and methods for treating tumors employing .alpha.,.omega.-bis(disubstitutedphosphino)hydrocarbon derivatives or [.alpha.,.omega.-bis(disubstituted phosphino)hydrocarbon] digold(I), digold(III), disilver(I), and dicopper(I) derivatives are disclosed.
    Type: Grant
    Filed: April 2, 1985
    Date of Patent: August 23, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: David T. Hill, Randall K. Johnson, Christopher K. Mirabelli
  • Tyr-Arg-vasopressin antagonists
    Patent number: 4766108
    Abstract: Vasopressin antagonists which have a dipeptide tail composed of a neutral and basic amino acid unit demonstrate potent V.sub.1 and V.sub.2 -antagonist activity. Two species of this invention, which are prepared by solid phase peptide synthesis, are [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylene propionic acid)-2-(O-ethyl)-D-tyrosine-4-valine-7-tyrosine-8-arginine-9-desglycine]- vasopressin and [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl)-D-tyrosine-4-valine-7-arginine-8-tyrosine-9-desglycine]- vasopressin.
    Type: Grant
    Filed: December 4, 1986
    Date of Patent: August 23, 1988
    Assignee: Smith Kline Beckman Corporation
    Inventor: Fadia E. Ali
  • Methylamidine compounds
    Patent number: 4766123
    Abstract: The invention relates to cyanoalkanimidamido derivatives that have utility as cardiac stimulants. A compound of the invention is 6-[4-(N.sup.2 -cyanoethanimidamido)phenyl]-5-methyl-4,5-dihydro-3(2H)-pyridazinone.
    Type: Grant
    Filed: February 10, 1987
    Date of Patent: August 23, 1988
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: William J. Coates
  • Pyridyl and pyridazinyl substituted thyronine compounds having selective thyromimetic activity
    Patent number: 4766121
    Abstract: This invention relates to chemical compounds which have selective thyromimetic activity. A compound of this invention is 3,5-dibromo-3'-[6-oxo-3(1H)-pyridazinylmethyl]-thyronine.
    Type: Grant
    Filed: January 14, 1986
    Date of Patent: August 23, 1988
    Assignee: Smith Kline & French Laboratories Ltd.
    Inventors: David Ellis, John C. Emmett, Anthony H. Underwood, Paul D. Leeson
  • Cyanoamidine compounds and derivatives thereof
    Patent number: 4766122
    Abstract: The invention relates to cyanoalkanimidamido derivatives that have utility as cardiac stimulants. A compound of the invention is 6-[4-(N.sup.2 -cyanopropanimidamido)phenyl]-5-methyl-4,5-dihydro-3(2H)-pyridazinone.
    Type: Grant
    Filed: March 26, 1986
    Date of Patent: August 23, 1988
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: William J. Coates
  • 3-hydroxypyridines
    Patent number: 4764519
    Abstract: The disclosure relates to a class of 2-(pyridylalkylamino)-3-hydroxypyridines which are active as histamine H.sub.1 -antagonists.
    Type: Grant
    Filed: May 1, 1987
    Date of Patent: August 16, 1988
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: David G. Cooper, Peter D. Miles, Rodney C. Young
  • Pharmaceutical compositions containing di-gold phosphine
    Patent number: 4764509
    Abstract: Pharmaceutical compositions containing an effective, tumor cell growth-inhibiting amount of such a compound, and a method for treating tumor cells sensitive to such a di-gold phosphine compound which comprises administering a tumor cell growth-inhibiting amount of such a compound to an animal afflicted by said tumor cells.
    Type: Grant
    Filed: August 17, 1987
    Date of Patent: August 16, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: David T. Hill, Randall K. Johnson
  • In vivo cellular tracking
    Patent number: 4762701
    Abstract: Methods of tracking cells in vivo and for determining in vivo cell lifetimes. Cells are labelled with cyanine dyes and detection is by measuring fluorescence, absorbance, or by detecting nuclear magnetic resonance probes included in the cyanine dyes. Using the invented methods, for example, red blood cell and platelet lifetimes are determined. Also, cells are tracked to determine sites of primary or metastatic tumors, or sites of occult infection. Further, rates at which cells pass through vessels is used to determine blood vessel patency and platelet aggregation.
    Type: Grant
    Filed: October 31, 1986
    Date of Patent: August 9, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: Paul K. Horan, Sue E. Slezak
  • Dopamine-beta-hydroxylase inhibitors
    Patent number: 4762850
    Abstract: Potent dopamine-.beta.-hydroxylase inhibitors having the Formula ##STR1## that are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmaceutical compositions including these inhibitors, and methods of using these inhibitors to inhibit dopamine-.beta.-hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.
    Type: Grant
    Filed: March 24, 1987
    Date of Patent: August 9, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: Joseph A. Finkelstein, Lawrence I. Kruse, Thomas B. Leonard
  • P-toluene-sulfonyl-oxy substituted pyridines
    Patent number: 4761480
    Abstract: Potent dopamine-.beta.-hydroxylase inhibitors having the Formula: ##STR1## which are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmaceutical compositions including these inhibitors, and methods of using these inhibitors to inhibit dopamine-.beta.-hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.
    Type: Grant
    Filed: October 7, 1986
    Date of Patent: August 2, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: Carl Kaiser, Lawrence I. Kruse, Stephen T. Ross