Patents Represented by Attorney William H. Edgerton

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  • Antihypertensive 7-[2-(dialkylamino)ethyl]-4-hydroxy-1,3-benzimidazol-2-ones
    Patent number: 4554287
    Abstract: 7-[2-Dialkylamino)ethyl]-4-hydroxy-1,3-benzimidazol-2-ones are prepared by oxidative cyclization of a urea, followed by removal of protective groups. The compounds are D.sub.2 -agonists and, thereby, have anti-hypertensive activity. A species of the group is 7[2-N,N-di-n-propylamino)ethyl]-4-hydroxyl-1,3-benzimidazol-2-one.
    Type: Grant
    Filed: September 12, 1984
    Date of Patent: November 19, 1985
    Assignee: Smithkline Beckman Corporation
    Inventors: Orum D. Stringer, Joseph Weinstock
  • Basic heptapeptide vasopressin antagonists
    Patent number: 4543349
    Abstract: Certain cyclic vasopressin-like peptides, which have an .omega.-amino- or guanidinoalkyl substituent attached to the cysteine in the 6-position of the ring, have vasopressin antagonist activity. A species of this series of new compounds is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl-D-tyrosine)-4-valine-8-(1,5-diaminopentane)-8-desarginine -9-desglycinamide]-vasopressin.
    Type: Grant
    Filed: August 28, 1984
    Date of Patent: September 24, 1985
    Assignee: SmithKline Beckman Corporation
    Inventors: James F. Callahan, Michael L. Moore, Nelson C. Yim
  • Octapeptide vasopressin antagonists
    Patent number: 4542124
    Abstract: Certain octapeptides, which have structures characterized by being a six unit cyclic peptide ring with a dipeptide tail which lacks a glycine unit at position 9, have potent vasopressin antagonist activity. The compounds here claimed are in general characterized by having an amino acid unit at position 4 which is other than valine. An important species of the group is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl-D-tyrosine)-4-.alpha.-aminobutyric acid-8-arginine-9-desglycine]vasopressin.
    Type: Grant
    Filed: June 26, 1984
    Date of Patent: September 17, 1985
    Assignee: Smithkline Beckman Corporation
    Inventors: William F. Huffman, Michael L. Moore
  • Process for preparing secondary amines
    Patent number: 4540819
    Abstract: New intermediates and processes for preparing 6-halo-7,8-dihydroxy-1-(p-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepi nes involve the reaction of a p-methoxyphenylglyoxal, lower alkyl hemimercaptal with a 2-chloro-3,4-dimethoxyphenethylamine, followed by a borohydride reduction.
    Type: Grant
    Filed: April 28, 1983
    Date of Patent: September 10, 1985
    Assignee: SmithKline Beckman Corporation
    Inventors: Kathleen L. Wert, Alan W. Tremper
  • Anti-hypertensive use of 1-(4'-branched alkylsulfonylphenyl)-6-chloro-7,8-dihydroxy-2,3,4,5-tetrahydro-1H-3-benz azepines
    Patent number: 4514394
    Abstract: 6-Chloro-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines whose structures have an isopropylsulfonyl, isopropylthio, isobutylsulfonyl or isobutylthio group substituted at the 4-position of the 1-phenyl substituent have potent renal dopaminergic and anti-hypertensive activity.
    Type: Grant
    Filed: May 25, 1983
    Date of Patent: April 30, 1985
    Assignee: Smithkline Beckman Corporation
    Inventors: Pamela A. Chambers, Joseph Weinstock
  • Dopaminergic agonist N,N-di-n-propyl-4-hydroxy-3-methanesulfonamidophenethylamine
    Patent number: 4507320
    Abstract: N,N-Di-n-propyl-4-hydroxy-3-methanesulfonamidophenethylamine is a potent, selective presynaptic dopaminergic agonist. The compound is prepared by N-sulfonylation of an optionally O-protected derivative of 3-amino-4-hydroxy-N,N-di-n-propylphenethylamine, followed by removal of the protecting group.
    Type: Grant
    Filed: December 7, 1983
    Date of Patent: March 26, 1985
    Assignee: Smithkline Beckman Corporation
    Inventors: Robert M. DeMarinis, J. Paul Hieble, Carl Kaiser, James W. Wilson
  • .beta.-Glycerophosphate salts of antimalarial phenanthrenemethanol compounds
    Patent number: 4507288
    Abstract: The compounds of formula (I) ##STR1## wherein R.sub.1 is hydrogen or an alkyl radical containing one to six carbon atoms and R.sub.2 is an alkyl radical containing one to six carbon atoms possess markedly increased activity against malaria-causing parasites. Pharmaceutical compositions and method of treatment of subjects with malaria are also disclosed.
    Type: Grant
    Filed: September 16, 1983
    Date of Patent: March 26, 1985
    Assignee: Smithkline Beckman Corporation
    Inventor: Jean F. Rossignol
  • Feed compositions containing a (1-oxo-2-pyridyl) disulfide
    Patent number: 4505917
    Abstract: Selected (1-oxo-2-pyridyl) disulfides are used as active ingredients in animal feed compositions and in methods for increasing the growth and feed efficiency of monogastric animals. A useful new compound of this invention is 2-carboxyphenyl (1-oxo-2-pyridyl) disulfide.
    Type: Grant
    Filed: September 21, 1982
    Date of Patent: March 19, 1985
    Assignee: SmithKline Beckman Corporation
    Inventors: Govind K. Menon, Winfred J. Sanders
  • 1-Acylamino-1-cyclopentanecarboxylic acids
    Patent number: 4482572
    Abstract: 1-Acylamino-1-cyclopentanecarboxylic acids have been prepared by acylation of certain 1-amino-1-cyclopentanecarboxylic acids and found to have renal vasodilating and diuretic properties.
    Type: Grant
    Filed: May 5, 1983
    Date of Patent: November 13, 1984
    Assignee: SmithKline Beckman Corporation
    Inventors: David L. Ladd, Joseph Weinstock
  • Des-proline vasopressin antagonists
    Patent number: 4481193
    Abstract: Certain octapeptides, which have structures characterized by being a six unit cyclic peptide ring with a dipeptide tail with no proline unit, have vasopressin antagonist activity. An important species of the group is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl-D-tyrosine)-4-valine]-7-desproline-8-arginine-vasopressin .
    Type: Grant
    Filed: March 7, 1984
    Date of Patent: November 6, 1984
    Assignee: SmithKline Beckman Corporation
    Inventors: Fadia E. Ali, William F. Huffman
  • Des-proline-des-glycine vasopressin antagonists
    Patent number: 4481194
    Abstract: Certain heptapeptides which have structures characterized by being a six unit cyclic peptide ring with an arginine or lysine tail have vasopressin antagonist activity. An important species of the group is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl-D-tyrosine)-4-valine-7-desproline-8-arginine-9-desglycine ]-vasopressin.
    Type: Grant
    Filed: March 7, 1984
    Date of Patent: November 6, 1984
    Assignee: SmithKline Beckman Corporation
    Inventors: Fadia E. Ali, William F. Huffman
  • Oligopeptide prodrugs
    Patent number: 4479898
    Abstract: Prodrugs are described whose structures have a oligopeptide chain which is substituted by a nucleophilic chemotherapeutic residue at the .alpha.-position. The products have increased cell membrane permeability and beneficial physico-chemical properties.
    Type: Grant
    Filed: February 29, 1984
    Date of Patent: October 30, 1984
    Assignee: SmithKline Beckman Corporation
    Inventors: Charles Gilvarg, William D. Kingsbury
  • Synthesis of benzhydrylamine resins
    Patent number: 4478984
    Abstract: N-(.alpha.-Chlorobenzyl)-phthalimide is condensed with a styrene resin in the presence of stannic chloride to give, after splitting the protective imide, benzhydrylamine resin for use in solid phase peptide synthesis.
    Type: Grant
    Filed: September 23, 1983
    Date of Patent: October 23, 1984
    Assignee: SmithKline Beckman Corporation
    Inventor: William M. Bryan
  • Kaliuretic compositions containing TMPPT
    Patent number: 4477455
    Abstract: 1,3,7,9-Tetramethylpyrimido[5,4-g]pteridine-2,4,6,8-(1H,3H,7H,9H)-tetraone is an active ingredient in pharmaceutical compositions useful for inducing kaliuresis. It, also, can be used in combination with a distal tubule acting diuretic to give an improved diuretic effect.
    Type: Grant
    Filed: February 4, 1983
    Date of Patent: October 16, 1984
    Assignee: SmithKline Beckman Corporation
    Inventors: Joseph Weinstock, Virgil D. Wiebelhaus
  • Method for producing diuresis using m-amino-.alpha.-methylphenethylamine
    Patent number: 4477470
    Abstract: m-Amino-.alpha.-methylphenethylamine, when administered internally, induces water diuresis in patients having edema.
    Type: Grant
    Filed: October 20, 1983
    Date of Patent: October 16, 1984
    Assignee: SmithKline Beckman Corporation
    Inventors: Francis T. Brennan, Genevieve F. Sosnowski, Joseph Weinstock
  • Intermediates for preparing substituted pyrimidinones
    Patent number: 4477663
    Abstract: A series of chemical reactions starting from the condensation of uracil with an acid stable heterocyclic aldehyde in an acid medium produces biologically active end products which are 2-heterocyclylmethylthioethylamino-5-heterocyclylmethyl-4-pyrimidinones. The new reactions and intermediates of this invention are particularly useful for preparing 2[2-(5-dimethylaminomethyl-2-furylmethylthio)-ethylamino]-5-(6-methyl-3-py ridylmethyl)-4-pyrimidinone and its salts. This compound is a potent H.sub.2 -antagonist with a long duration of activity.
    Type: Grant
    Filed: April 7, 1982
    Date of Patent: October 16, 1984
    Assignee: SmithKline Beckman Corporation
    Inventors: Bing L. Lam, Lendon N. Pridgen
  • Allyloxy- and allylthio-2,3,4,5-tetrahydro-1H-3-benzazepines
    Patent number: 4469634
    Abstract: A series of allyloxy- and allylthio-2,3,4,5-tetrahydro-1H-3-benzazepines has been prepared and found to have utility as .alpha..sub.2 -antagonists and as intermediates for preparing .alpha..sub.2 -adrenergic affinity resins.
    Type: Grant
    Filed: July 29, 1982
    Date of Patent: September 4, 1984
    Assignee: SmithKline Beckman Corporation
    Inventor: Robert M. DeMarinis
  • Synergistic compositions of renal dopaminergic agent and .beta.-blocker
    Patent number: 4469690
    Abstract: Compositions useful for improving kidney function and treating hypertension are comprised of a 6-chloro, 6-fluoro or 6-methyl-7,8-dihydroxy-1-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzaze pine combined with a .beta.-adrenergic blocking agent known to the art, especially, propranolol. The compositions are administered, most readily, orally.
    Type: Grant
    Filed: November 16, 1982
    Date of Patent: September 4, 1984
    Assignee: SmithKline Beckman Corporation
    Inventors: Dennis M. Ackerman, Barry A. Berkowitz, Virgil D. Wiebelhaus
  • Iodinated vasopressin antagonists
    Patent number: 4469680
    Abstract: A series of vasopressin antagonists which have a 3'-iodo-tyrosine unit at position 2 are prepared by iodination of the tyrosine congeners. The compounds have antagonist activity manifested by an aquaretic effect and, also, are useful in studying various biological reactions.
    Type: Grant
    Filed: July 6, 1983
    Date of Patent: September 4, 1984
    Assignee: SmithKline Beckman Corporation
    Inventors: William F. Huffman, Michael L. Moore
  • Octapeptide vasopressin antagonists
    Patent number: 4469679
    Abstract: Certain octapeptides which have structures characterized by being a six unit cyclic peptide ring with a dipeptide tail have vasopressin antagonist activity. An important species of the group is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl-D-tyrosine)-4-valine-8-arginine-9-desglycine]vasopressin.
    Type: Grant
    Filed: February 16, 1983
    Date of Patent: September 4, 1984
    Assignee: SmithKline Beckman Corporation
    Inventors: William F. Huffman, Michael L. Moore