Patents by Inventor Lawrence I. Kruse

Lawrence I. Kruse has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • 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
  • Dopamine-.beta.-hydroxylase inhibitors
    Patent number: 4761415
    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: August 28, 1986
    Date of Patent: August 2, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: Joseph A. Finkelstein, Lawrence I. Kruse, Thomas B. Leonard
  • Irreversible dopamine-.beta.-hydroxylase inhibitors
    Patent number: 4760089
    Abstract: Potent, irreversible dopamine-.beta.-hydroxylase inhibitors having the Formula: ##STR1## which are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmaceutical compositions including these inhibitors or 2-cyano-2-phenethylamine, and methods of using these inhibitors or 2-cyano-2-phenethylamine to inhibit dopamine-.beta.-hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.
    Type: Grant
    Filed: September 9, 1985
    Date of Patent: July 26, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: Pamela A. Chambers, James S. Frazee, Carl Kaiser, Lawrence I. Kruse
  • Dopamine-beta-hydroxylase inhibitors
    Patent number: 4749717
    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: January 8, 1987
    Date of Patent: June 7, 1988
    Assignee: SmithKline Beckman Corporation
    Inventor: Lawrence I. Kruse
  • Ester prodrugs of dopamine-.beta.-hydroxylase, inhibitors, composition containing them, and method of using them to inhibit dopamine-.beta.-hydroxylase activity
    Patent number: 4743613
    Abstract: Compounds having the formula: ##STR1## which are ester prodrugs of potent dopamine-.beta.-hydroxylase inhibitors and thus are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmeceutical compositions including these compounds, and methods of using these compounds to inhibit dopamine-.beta.-hydroxylase activity in mammals.
    Type: Grant
    Filed: April 8, 1986
    Date of Patent: May 10, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: James S. Frazee, Carl Kaiser, Lawrence I. Kruse, Stephen T. Ross
  • 1-substituted-2-mercapto benzimidazole compounds and intermediates
    Patent number: 4728741
    Abstract: 1-substituted-2-mercapto(or aminomethyl)benzimidazole compounds of the formula ##STR1## inhibit dopamine-.beta.-hydroxylase activity. Intermediates are also disclosed.
    Type: Grant
    Filed: January 8, 1985
    Date of Patent: March 1, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: Carl Kaiser, Lawrence I. Kruse
  • Imidazolethiol dopamine-beta-hydroxylase inhibitors
    Patent number: 4719223
    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 31, 1985
    Date of Patent: January 12, 1988
    Assignee: SmithKline Beckman Corporation
    Inventors: Carl Kaiser, Lawrence I. Kruse, Stephen T. Ross
  • Substituted te[1]trahydroisoquinoline derivatives having .beta.-adrenergic receptor activity
    Patent number: 4707485
    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: June 24, 1986
    Date of Patent: November 17, 1987
    Assignee: Smithkline Beckman Corporation
    Inventors: Carl Kaiser, Lawrence I. Kruse
  • Dopamine-.beta.-hydroxylase inhibitors and use thereof
    Patent number: 4707488
    Abstract: The compounds of this invention are 1-phenylalkyl-2-mercaptotetrazole compounds which are dopamine-.beta.-hydroxylase inhibitors.
    Type: Grant
    Filed: February 11, 1985
    Date of Patent: November 17, 1987
    Assignee: Smithkline Beckman Corporation
    Inventors: Carl Kaiser, Lawrence I. Kruse
  • Pyridylalkyl imidazole-2-thiols
    Patent number: 4634711
    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: August 2, 1985
    Date of Patent: January 6, 1987
    Assignee: Smithkline Beckman Corporation
    Inventors: Carl Kaiser, Lawrence I. Kruse, Stephen T. Ross
  • Dopamine-.beta.-hydroxylase inhibitors
    Patent number: 4628059
    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: October 31, 1985
    Date of Patent: December 9, 1986
    Assignee: SmithKlein Beckman Corporation
    Inventors: Joseph A. Finkelstein, Carl Kaiser, Lawrence I. Kruse
  • 1-Benzyl-2-aminomethyl imidazole derivatives
    Patent number: 4532331
    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 12, 1983
    Date of Patent: July 30, 1985
    Assignee: Smithkline Beckman Corporation
    Inventors: James S. Frazee, Carl Kaiser, Lawrence I. Kruse
  • Semicarbazide intermediates for preparing 4-substituted indoles
    Patent number: 4454337
    Abstract: A new chemical sequence for preparing certain indoles is disclosed which employes certain 2-substituted-6-nitrophenylacetaldehyde semicarbazones claimed here. Said semicarbazones are cyclized to the indoles by low pressure hydrogenation.
    Type: Grant
    Filed: March 2, 1983
    Date of Patent: June 12, 1984
    Assignee: SmithKline Beckman Corporation
    Inventor: Lawrence I. Kruse
  • Processes for preparing 4-substituted indoles
    Patent number: 4394514
    Abstract: A new chemical sequence for preparing indoles is disclosed whose key reactions are reaction of a o-nitrotoluene with tris(dimethylamino)methane to give a .beta.-dimethylamino-o-nitrostyrene which is converted into a semicarbazone and cyclized.
    Type: Grant
    Filed: June 29, 1981
    Date of Patent: July 19, 1983
    Assignee: SmithKline Beckman Corporation
    Inventor: Lawrence I. Kruse