Patents by Inventor Bruce D. Roth

Bruce D. Roth 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).

  • Antihyperlipidemic and antiatherosclerotic urea and carbamate compounds
    Patent number: 5015644
    Abstract: Certain substituted urea, thiourea, carbamate, and thiocarbamate compounds are potent inhibitors of the enzyme acyl-CoA: cholesterol acyltransferase and are thus useful agents for inhibiting the intestinal absorption of cholesterol, and for lowering blood plasma cholesterol.
    Type: Grant
    Filed: June 1, 1989
    Date of Patent: May 14, 1991
    Assignee: Warner-Lambert Company
    Inventors: Bruce D. Roth, Bharat K. Trivedi
  • Process for trans-6-(2-(substituted-pyrrol-1-yl)alkyl)pryan-2-one inhibitors of cholesterol synthesis
    Patent number: 5003080
    Abstract: An improved process for the preparation of trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where 1,6-heptadien-4-ol is converted in eight operations to the desired products, as well as an improved process for the preparation of (2R-trans) and trans-(.+-.)-5-(4-fluorophenyl)-2-(1-methylethyl)-N-4-diphenyl-1-[2-tetrah ydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide by a novel synthesis where 4-methyl-3-oxo-N-phenylpentanamide is converted in eight operations to the desired product or alternatively 4-fluoro-.alpha.-[2-methyl-1-oxopropyl]-.gamma.-oxo-N,.beta.-diphenylbenze nebutaneamide is converted in one step to the desired product, and additionally, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahy dro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide from (R)-4-cyano-3-[[(1,1-dimethylethyl)dimethylsilyl]oxy]butanoic acid, as well as other valuable intermediates used in the processes.
    Type: Grant
    Filed: February 1, 1989
    Date of Patent: March 26, 1991
    Assignee: Warner-Lambert Company
    Inventors: Donald E. Butler, Carl F. Deering, Alan Millar, Thomas N. Nanninga, Bruce D. Roth
  • 6-(((substituted)pyridin-3-yl)alkyl)-and alkenyl)-tetrahydro-4-hydroxypyran-2-one inhibitors of cholesterol biosynthesis
    Patent number: 4997837
    Abstract: Certain trans-6-[[(substituted)pyridin-3-yl]-alkyl- and alkenyl]tetrahydro-4-hydroxypyran-2-ones and the corresponding ring-opened acids derived therefrom are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase) and are useful as hypocholesterolemic and hypolipidemic agents.
    Type: Grant
    Filed: October 6, 1989
    Date of Patent: March 5, 1991
    Assignee: Warner-Lambert Company
    Inventors: Alexander W. Chucholowski, Mark W. Creswell, Bruce D. Roth, Drago R. Sliskovic
  • Trans-6-(2-(N-heteroaryl-3,5-disubstituted)pyrazol-4-yl)-ethyl)-or ethenyl)tetrahydro-4-hydroxypyran-2-one inhibitors of cholesterol biosynthesis
    Patent number: 4957971
    Abstract: Certain trans-6-[2-(N-heteroaryl-3,5-disubstituted) pyrazol-4-yl)ethyl]- or ethenyl]tetrahydro-4-hydroxy-2H-pyran-2-ones and the corresponding ring-opened acids, esters and N-oxides derived therefrom which are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG CoA reductase) and are thus useful hypolipidemic or hypocholesterolemic agents. Pharmaceutical compositions containing such compounds, and a method of inhibiting the biosynthesis of cholesterol employing such pharmaceutical compositions are also disclosed.
    Type: Grant
    Filed: December 6, 1988
    Date of Patent: September 18, 1990
    Assignee: Warner-Lambert Company
    Inventors: Joseph A. Picard, Bruce D. Roth, Drago R. Sliskovic
  • Bicyclo heptane and bicyclo octane substituted inhibitors of cholesterol synthesis
    Patent number: 4957940
    Abstract: Certain bicyclo [2.2.1] heptane and bicyclo [2.2.2] octane substituted tetrahydro-2H-pyran-2-ones and the corresponding ring-opened acids derived therefrom are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase) and are useful as hypocholesterolemic and hypolipidemic agents.
    Type: Grant
    Filed: November 21, 1989
    Date of Patent: September 18, 1990
    Assignee: Warner-Lambert Company
    Inventor: Bruce D. Roth
  • 5-pyrimidinyl-3,5-dihydroxy-6-heptenoic acid compounds useful as inhibitors of cholesterol biosynthesis
    Patent number: 4929620
    Abstract: Certain trans-6-[[(substituted)pyrimidin-5-yl]-ethyl]- and ethenyl]tetrahydro-4-hydroxypyran-2-ones and the corresponding dihydroxy ring-opened acids derived therefrom are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase) and are useful as hypocholesterolemic and hypolipidemic agents.
    Type: Grant
    Filed: June 1, 1989
    Date of Patent: May 29, 1990
    Assignee: Warner-Lambert Company
    Inventors: Alexander W. Chucholowski, Bruce D. Roth, Drago R. Sliskovic
  • Bicyclo heptane and bicyclo octane substituted inhibitors of cholesterol synthesis
    Patent number: 4906657
    Abstract: Certain bicyclo [2.2.1] heptane and bicyclo [2.2.2] octane substituted tetrahydro-2H-pyran-2-ones and the corresponding ring-opened acids derived therefrom are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase) and are useful as hypocholesterolemic and hypolipidemic agents.
    Type: Grant
    Filed: December 21, 1988
    Date of Patent: March 6, 1990
    Assignee: Warner-Lambert Company
    Inventor: Bruce D. Roth
  • 6-(((Substituted)pyridin-3-yl)alkyl)-and alkenyl)-tetrahydro-4-hydroxypyran-2-one inhibitors of cholesterol biosynthesis
    Patent number: 4906624
    Abstract: Certain trans-6-[[(substituted)pyridin-3-yl]-alkyl- and alkenyl]tetrahydro-4-hydroxypyran-2-ones and the corresponding ring-opened acids derived therefrom are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase) and are useful as hypocholesterolemic and hypolipidemic agents.
    Type: Grant
    Filed: August 2, 1988
    Date of Patent: March 6, 1990
    Assignee: Warner-Lambert Company
    Inventors: Alexander W. Chucholowski, Mark W. Creswell, Bruce D. Roth, Drago R. Sliskovic
  • 6-[[Substituted)pyrimidinyl)ethyl]- and ethenyl]tetrahydro-4-hydroxypyran-2-one inhibitors of cholesterol biosynthesis
    Patent number: 4868185
    Abstract: Certain trans-6-[[(substituted)pyrimidin-5-yl]ethyl]- and ethenyl]tetrahydro-4-hydroxypyran-2-ones and the corresponding dihydroxy ring-opened acids derived therefrom are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase) and are useful as hypocholesterolemic and hypolipidemic agents.
    Type: Grant
    Filed: December 10, 1987
    Date of Patent: September 19, 1989
    Assignee: Warner-Lambert Company
    Inventors: Alexander W. Chucholowski, Bruce D. Roth, Drago R. Sliskovic
  • Trans-6-[2-(N-heteroaryl-3,5-disubstituted)pyrazol-4-yl)-ethyl]- or ethenyl]tetrahydro-4-hydroxypyran-2-one inhibitors of cholesterol biosynthesis
    Patent number: 4808621
    Abstract: Certain trans-6-[2-(N-heteroaryl-3,5-disubstituted)pyrazol-4-yl)ethyl]- or ethenyl]tetrahydro-4-hydroxy-2H-pyran-2-ones and the corresponding ring-opened acids derived therefrom which are potent inhibitors of the enzyme 3-hydroxy-3-methylglutarylcoenzyme A reductase (HMG CoA reductase) and are thus useful hypolipidemic or hypocholesterolemic agents. Pharmaceutical compositions containing such compounds, and a method of inhibiting the biosynthesis of cholesterol employing such pharmaceutical compositions are also disclosed.
    Type: Grant
    Filed: May 18, 1987
    Date of Patent: February 28, 1989
    Assignee: Warner-Lambert Company
    Inventors: Bruce D. Roth, Drago R. Sliskovic
  • 6-(((substituted)quinolinyl)ethyl)-and ethenyl)tetrahydro-4-hydroxypyran-2-one inhibitors of cholesterol biosynthesis
    Patent number: 4761419
    Abstract: Certain trans-6-[[(substituted)quinolinyl]ethyl]-and ethenyl]tetrahydro-4-hydroxypyran-2-ones and the corresponding dihydroxy ring-opened acids derived therefrom are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase) and are useful as hypocholesterolemic and hypolipidemic agents.
    Type: Grant
    Filed: December 7, 1987
    Date of Patent: August 2, 1988
    Assignee: Warner-Lambert Company
    Inventors: Joseph A. Picard, Bruce D. Roth, Drago R. Sliskovic
  • Treating fungal infections with substituted-(6-(tetrahydro-4-hydroxy-2-oxo-2H-pyran-2-yl)ethyl)- or ethenyl)pyrazoles
    Patent number: 4751229
    Abstract: A method of treating fungal infections in mammals employing 1,3,5-trisubstituted-4- (4-hydroxy-2-oxo-pyran-6-yl)pyrazoles is disclosed.
    Type: Grant
    Filed: July 9, 1987
    Date of Patent: June 14, 1988
    Assignee: Warner-Lambert Company
    Inventors: Carl L. Heifetz, Milton L. Hoefle, Bruce D. Roth, Drago R. Sliskovic, Michael W. Wilson
  • Saturated fatty acid amides as inhibitors of acyl-coa:cholesterol acyltransferase
    Patent number: 4743605
    Abstract: Certain substituted amides of saturated fatty acids are potent inhibitors of the enzyme acyl-CoA:cholesterol acyltransferase and are thus useful agents for inhibiting the intestinal absorption of cholesterol.
    Type: Grant
    Filed: October 1, 1987
    Date of Patent: May 10, 1988
    Assignee: Warner-Lambert Company
    Inventors: Milton L. Hoefle, Ann Holmes, Bruce D. Roth
  • Trans-6-[2-[2-(substituted-phenyl)-3- (or 4-) heteroaryl-5-substituted-1H-pyrrol-1-yl]-ethyl]tetrahydro-4-hydroxy-2H-p yran-2-one inhibitors of cholesterol biosynthesis
    Patent number: 4735958
    Abstract: Certain trans-6-[2-[2-(substituted-phenyl)-3- (or 4-)heteroaryl-5-substituted-1H-pyrrol-1-yl]ethyl]tetrahydro-4-hydroxy-2H-p yran-2-ones and the corresponding lactone-ring-opened acids are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG CoA reductase) and are thus useful hypolipidemic or hypocholesterolemic agents. Pharmaceutical compositions containing such compounds, and a method of inhibiting the biosynthesis of cholesterol employing such pharmaceutical compositions are also disclosed.
    Type: Grant
    Filed: December 22, 1986
    Date of Patent: April 5, 1988
    Assignee: Warner-Lambert Company
    Inventors: Bruce D. Roth, Drago R. Sliskovic
  • Saturated fatty acid amides as inhibitors of acyl-CoA:cholesterol acyltransferase
    Patent number: 4716175
    Abstract: Certain substituted amides of saturated fatty acids are potent inhibitors of the enzyme acyl-CoA:cholesterol acyltransferase and are thus useful agents for inhibiting the intestinal absorption of cholesterol.
    Type: Grant
    Filed: February 24, 1987
    Date of Patent: December 29, 1987
    Assignee: Warner-Lambert Company
    Inventors: Milton L. Hoefle, Ann Holmes, Bruce D. Roth
  • Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis
    Patent number: 4681893
    Abstract: Certain trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-ones and the corresponding ring-opened acids derived therefrom which are potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG CoA reductase and are thus useful hypolipidemic or hypocholesterolemic agents. Pharmaceutical compositions containing such compounds, and a method of inhibiting the biosynthesis of cholesterol employing such pharmaceutical compositions are also disclosed.
    Type: Grant
    Filed: May 30, 1986
    Date of Patent: July 21, 1987
    Assignee: Warner-Lambert Company
    Inventor: Bruce D. Roth
  • Trans-6-[2-(substitutedpyrrol-1-yl)alkyl]-pyran-2-one inhibitors of cholesterol synthesis
    Patent number: 4647576
    Abstract: 6-[2-(Substituted-pyrrol-1-yl)alkyl]pyran-2-ones and the corresponding ring-opened hydroxy-acids derived therefrom are potent inhibitors of the enzyme 3-hydroxy-3-methylglutarylcoenzyme A reductase (HMG-CoA reductase), and are thus useful hypolipidemic and hypocholesterolemic agents. Pharmaceutical compositions containing such compounds, and a method of treatment employing such pharmaceutical compositions are also disclosed.
    Type: Grant
    Filed: December 10, 1984
    Date of Patent: March 3, 1987
    Assignee: Warner-Lambert Company
    Inventors: Milton L. Hoefle, Bruce D. Roth, Charlotte D. Stratton