Patents by Inventor Carl Kaiser

Carl Kaiser 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).

  • 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
  • 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
  • N,N-Di-(n-Propyl)dopamine derivatives
    Patent number: 4529604
    Abstract: N,N-Di-(n-propyl)dopamine derivatives having peripheral dopamine receptor agonist activity prepared by synthetic routes known for phenethylamines. The renal vasodilator effect of 3,4-dihydroxy-N,N-di(n-propyl)-phenethylamine is potentiated by the concomitant administration of the .beta.-blocker propranolol.
    Type: Grant
    Filed: March 28, 1977
    Date of Patent: July 16, 1985
    Assignee: SmithKline Beckman Corporation
    Inventors: Carl Kaiser, Alfonso J. Tobia
  • 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
  • Process useful for preparing 7,8-acetamido, hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines
    Patent number: 4382029
    Abstract: A chemical process is described for preparing 7,8-acetamido, hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines which involves reacting a 7,8-quinone derivative of a 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine with a benzyl or benzhydrylamine followed by hydrolysis of the resulting imine and reaction with acetic anhydride or acetyl chloride.
    Type: Grant
    Filed: August 14, 1981
    Date of Patent: May 3, 1983
    Assignee: SmithKline Beckman Corporation
    Inventors: Kenneth G. Holden, Carl Kaiser, Joseph Weinstock
  • Intermediates for preparing 7,8-amino, hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines
    Patent number: 4327023
    Abstract: A group of new chemical compounds are described which are intermediates for preparing 7,8-amino, hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines. The intermediates are distinguished in structure by a benzyloxy substituent at either the 7 or 8-position.
    Type: Grant
    Filed: August 7, 1980
    Date of Patent: April 27, 1982
    Assignee: SmithKline Corporation
    Inventors: Kenneth G. Holden, Carl Kaiser, Joseph Weinstock
  • 7,8-Amino, hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines
    Patent number: 4284556
    Abstract: A group of 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines whose structures have amino, hydroxy substituents at the 7,8-positions of the benzazepine nucleus is disclosed. Novel intermediates and routes of synthesis used for preparing them are also described. The end products have pharmacodynamic activity.
    Type: Grant
    Filed: January 31, 1980
    Date of Patent: August 18, 1981
    Assignee: SmithKline Corporation
    Inventors: Kenneth G. Holden, Carl Kaiser, Joseph Weinstock
  • 6-Phenyl thio- and 6-cyclohexyl thio-2,3,4,5-tetrahydro-1H-3-benzazepines
    Patent number: 4265890
    Abstract: Mercapto substituted-2,3,4,5-tetrahydro-1H-3-benzazepines having dopamine receptor blocking activity are prepared from o-quinones or via standard preparative procedures.
    Type: Grant
    Filed: May 17, 1979
    Date of Patent: May 5, 1981
    Assignee: SmithKline Corporation
    Inventors: Kenneth G. Holden, Carl Kaiser
  • Antipsychotically useful quinolizidylidene derivatives of xanthenes, thioxanthenes and dibenzoxepins
    Patent number: 4089961
    Abstract: Tricyclic quinolizidine derivatives administered internally to an animal host, in therapeutically effective amounts, produce antipsychotic activity essentially free of extrapyramidal symptoms.
    Type: Grant
    Filed: November 8, 1976
    Date of Patent: May 16, 1978
    Assignee: SmithKline Corporation
    Inventors: Carl Kaiser, John Joseph Lafferty
  • Piperidylidene derivatives of benzo-fused xanthenes, thioxanthenes and dibenzoxepins and antipsychotic use thereof
    Patent number: 4073912
    Abstract: Novel piperidylidene derivatives of benzo-fused xanthenes, thioxanthenes and dibenzoxepins administered internally to an animal host, in therapeutically effective amounts, produce antipsychotic activity essentially free of extrapyramidal symptoms.
    Type: Grant
    Filed: October 12, 1976
    Date of Patent: February 14, 1978
    Assignee: SmithKline Corporation
    Inventors: Carl Kaiser, John J. Lafferty
  • Pharmaceutical compositions and methods of inhibiting phenylethanolamine N-methyltransferase
    Patent number: 4062961
    Abstract: Pharmaceutical compositions and methods of inhibiting phenylethanolamine N-methyltransferase using 7 and/or 8 substituted 1,2,3,4-tetrahydroisoquinoline compounds.
    Type: Grant
    Filed: August 5, 1976
    Date of Patent: December 13, 1977
    Assignee: SmithKline Corporation
    Inventors: Carl Kaiser, Robert G. Pendleton
  • Pharmaceutical compositions and method of producing anti-Parkinsonism activity
    Patent number: 4052506
    Abstract: Pharmaceutical compositions and method of producing anti-Parkinsonism activity by administering internally a nontoxic effective quantity of a benzazepine derivative to an animal.
    Type: Grant
    Filed: August 5, 1975
    Date of Patent: October 4, 1977
    Assignee: SmithKline Corporation
    Inventors: Carl Kaiser, Robert G. Pendleton, Paulette E. Setler
  • .alpha.-AMINOMETHYL-4-HYDROXY-3-METHYLSULFONYL BENZYL ALCOHOLS
    Patent number: 4048229
    Abstract: .alpha.-Aminomethyl-4-hydroxy-3-methylsulfonyl benzyl alcohols having .beta.-adrenergic antagonist activity are prepared generally from 4-benzyloxy-3-methylsulfonylacetophenone by, for example, bromination and treatment of the resulting .alpha.-bromo derivative with an N-benzyl secondary amine, followed by catalytic hydrogenation to remove protective benzyl groups and reduce the ketone moiety.
    Type: Grant
    Filed: January 8, 1975
    Date of Patent: September 13, 1977
    Assignee: SmithKline Corporation
    Inventors: Donald F. Colella, Carl Kaiser