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).
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Functionalized heterocycles as modulators of chemokine receptor function and methods of use therefor
Patent number: 6951848Abstract: Disclosed are novel compounds having the formula or a physiologically acceptable salt, amide, ester or prodrug thereof. The compounds can be used to modulate (antagonize, agonize) chemokine receptor function. Also disclosed is a method for treating a patient having an inflammatory disease and/or viral infection comprising administering an effective amount of a compound of Formula I. In particular embodiments, the invention is a method for treating a patient infected with HIV.Type: GrantFiled: March 12, 2002Date of Patent: October 4, 2005Assignee: Millennium Pharmaceuticals, Inc.,Inventors: Geraldine C. B. Harriman, Kenneth G. Carson, Daniel L. Flynn, Michael E. Solomon, Yuntao Song, Bharat K. Trivedi, Bruce D. Roth, Christine N. Kolz, Ly Pham, Kuai-lin Sun -
Functionalized heterocycles as modulators of chemokine receptor function and methods of use therefor
Publication number: 20030064991Abstract: Disclosed are novel compounds having the formula 1Type: ApplicationFiled: March 12, 2002Publication date: April 3, 2003Applicant: Millennium Pharmaceuticals, Inc.Inventors: Geraldine C.B. Harriman, Kenneth G. Carson, Daniel L. Flynn, Michael E. Solomon, Yuntao Song, Bharat K. Trivedi, Bruce D. Roth, Christine N. Kolz, Ly Pham, Kuai-lin Sun -
Patent number: 5612002Abstract: A method for the multiple, simultaneous synthesis of compounds comprising the steps of: 1) providing an apparatus comprising a plurality of reaction tubes having filter members on their lower ends, a reservoir member for receiving the filter member, a holder member having a plurality of apertures for supporting the reaction tubes, and a manifold member adjacent to the holder member and enclosing the upper ends of the reaction tubes; 2) charging the apparatus with reactants required for synthesis; 3) synthesizing the compounds in solution; or optionally 4) cleaving the compounds from a solid support within the apparatus.Type: GrantFiled: April 28, 1995Date of Patent: March 18, 1997Assignee: Warner-Lambert CompanyInventors: Donna R. Cody, Sheila H. H. DeWitt, John C. Hodges, John S. Kiely, Walter H. Moos, Michael R. Pavia, Bruce D. Roth, Mel C. Schroeder, Charles J. Stankovic
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Patent number: 5593967Abstract: Novel cholecystokinin antagonists useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further, the compounds are antianxiety agents and antiulcer agents. They are agents useful for preventing the response to the withdrawal from chronic treatment with use of nicotine, diazepam, alcohol, cocaine, coffee, or opioids. The compounds of the invention are also useful in treating and/or preventing panic. Also disclosed are pharmaceutical compositions and methods of treatment using the antagonists as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds in diagnostic compositions.Type: GrantFiled: April 1, 1993Date of Patent: January 14, 1997Assignee: Warner-Lambert CompanyInventors: David C. Horwell, Edward Roberts, Ann Holmes, Janak K. Padia, William H. Roark, Bruce D. Roth, Bharat K. Trivedi, Jurgen Kleinschroth, David C. Rees, Reginald S. Richardson
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Patent number: 5489611Abstract: Retinoids are effective to lower plasma levels of Lp (a) in mammals.Type: GrantFiled: February 10, 1995Date of Patent: February 6, 1996Assignee: Warner-Lambert CompanyInventors: Helen T. Lee, Joseph A. Picard, Randy R. Ramharack, Bruce D. Roth, Drago R. Sliskovic
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Patent number: 5441975Abstract: Pharmaceutically useful compounds having ACAT inhibitory activity of the formula ##STR1## wherein n is 0, 1, or 2, for X other than tetrazole and n=2 then R.sub.2 =R.sub.3 =H; R.sub.1 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, a heteroaromatic group or a hydrocarbon group having from one to 18 carbon atoms; R.sub.2 and R.sub.3 are hydrogen, halo, hydroxy, alkyl, alkenyl, cycloalkyl, phenyl, substituted phenyl, a heteroaryl, or form a spiroalkyl group; X is a heteromonocyclic 5-membered ring containing one to four heteroatoms, said heteroatoms being nitrogen, oxygen or sulfur, and combination thereof; and R.sub.4 is a hydrocarbon group having from one to 20 carbon atoms are described as well as methods of their manufacture.Type: GrantFiled: July 12, 1994Date of Patent: August 15, 1995Assignee: Warner-Lambert CompanyInventors: Helen T. Lee, Patrick M. O'Brien, Joseph A. Picard, Claude F. Purchase, Jr., Bruce D. Roth, Drago R. Sliskovic, Andrew D. White
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Patent number: 5385929Abstract: 2-(4-Fluorophenyl)-.beta.,.delta.-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[( hydroxyphenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid, and their lactone forms, and salts and solyates thereof, inhibit cholesterol biosynthesis, and thus are useful in treating hypercholesterolemia.Type: GrantFiled: May 4, 1994Date of Patent: January 31, 1995Assignee: Warner-Lambert CompanyInventors: Susan M. Bjorge, Ann E. Black, Bruce D. Roth, Thomas Woolf
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Patent number: 5366987Abstract: Pharmaceutically useful compounds having ACAT inhibitory activity of the formula ##STR1## wherein n is 0, 1, or 2, for X other than tetrazole and n=2 then R.sub.2 =R.sub.3 =H; R.sub.1 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, a heteroaromatic group or a hydrocarbon group having from one to 18 carbon atoms; R.sub.2 and R.sub.3 are hydrogen, halo, hydroxy, alkyl, alkenyl, cycloalkyl, phenyl, substituted phenyl, a heteroaryl, or form a spiroalkyl group; X is a heteromonocyclic 5-membered ring containing one to four heteroatoms, said heteroatoms being nitrogen, oxygen or sulfur, and combination thereof; and R.sub.4 is a hydrocarbon group having from one to 20 carbon atoms are described as well as methods of their manufacture.Type: GrantFiled: February 18, 1993Date of Patent: November 22, 1994Assignee: Warner-Lambert CompanyInventors: Helen T. Lee, Patrick M. O'Brien, Joseph A. Picard, Claude F. Purchase, Jr., Bruce D. Roth, Drago R. Sliskovic, Andrew D. White
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Patent number: 5331006Abstract: Novel unnatural dipeptoids useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further, the compounds are antianxiety agents and antiulcer agents. The compounds are agents useful for preventing the response to withdrawal from chronic treatment or use of nicotine, diazepam, alcohol, cocaine, caffeine, and opioids. The compounds are also useful in treating and/or preventing panic attacks. Also disclosed are pharmaceutical compositions and methods of treatment using the dipeptoids as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds to prepare diagnostic compositions.Type: GrantFiled: July 12, 1991Date of Patent: July 19, 1994Assignee: Warner-Lambert CompanyInventors: David C. Horwell, Julian Aranda, Corinne Augelli-Szafran, Hans-Jurgen Betche, Ann Holmes, Michael D. Mullican, Martyn C. Pritchard, Reginald S. Richardson, Edward Roberts, Bruce D. Roth, Bradley D. Tait, Bharat K. Trivedi, Uwe Trostmann, Paul C. Unangst
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Patent number: 5324483Abstract: An apparatus and method which provides a suitable location for multiple, simultaneous synthesis of compounds. The apparatus consists of: a reservoir block having a plurality of wells; a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends; a holder block, having a plurality of apertures; and a manifold, which may have ports to allow introduction/maintenance of a controlled environment. The manifold top wall has apertures and a detachable plate with identical apertures. The apparatus is constructed from materials which will accommodate heating, cooling, agitation, or corrosive reagents. Gaskets are placed between the components. Rods or clamps are provided for fastening the components together. Apparatus operation involves placing the filters on the lower ends of the reaction tubes in the reservoir block wells, and the upper ends passing through the holder block apertures and into the manifold.Type: GrantFiled: February 2, 1993Date of Patent: June 28, 1994Assignee: Warner-Lambert CompanyInventors: Donna R. Cody, Sheila H. H. DeWitt, John C. Hodges, John S. Kiely, Walter H. Moos, Michael R. Pavia, Bruce D. Roth, Mel C. Schroeder, Charles J. Stankovic
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Patent number: 5280126Abstract: 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-(tetra hydro-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]-Y-oxo-N,.beta.-diphenylbenzenebuta neamide 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: GrantFiled: May 6, 1993Date of Patent: January 18, 1994Assignee: Warner-Lambert CompanyInventors: Donald E. Butler, Carl F. Deering, Alan Millar, Thomas N. Nanninga, Bruce D. Roth
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Patent number: 5278326Abstract: Novel pharmaceutically useful compounds which lower blood cholesterol levels and are beta-ketoamides, oximes, amines, and hydroxyl derivatives thereof.Type: GrantFiled: March 18, 1991Date of Patent: January 11, 1994Assignee: Warner-Lambert CompanyInventors: Corinne E. Augelli-Szafran, Bruce D. Roth
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Patent number: 5273995Abstract: [R-(R*,R*)]-2-(4-fluorophenyl)-.beta.,.delta.-dihydroxy-5-((1-methylethyl)- 3-phenyl-4-[(phenylamino)-carbonyl]-1H-pyrrole-1-heptanoic acid or (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl-N,4-diphenyl-1-[2-(tetrahyd ro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide; and pharmaceutically acceptable salts thereof.Type: GrantFiled: February 26, 1991Date of Patent: December 28, 1993Assignee: Warner-Lambert CompanyInventor: Bruce D. Roth
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Patent number: 5254589Abstract: A pharmaceutically useful compound which lowers blood cholesterol levels having the formula ##STR1## wherein X is oxygen or --NH--; Ar is phenyl, substituted phenyl, naphthyl or substituted naphthyl; R.sub.1 is hydrogen, lower alkyl or benzyl; and R.sub.2 is a straight or branched alkyl group having from 5 to 17 carbon atoms which may be substituted on the 1-carbon position with methyl, ethyl, phenyl, or substituted phenyl, or a cycloalkyl group having from 3 to 8 carbon atoms.Type: GrantFiled: October 15, 1991Date of Patent: October 19, 1993Assignee: Warner-Lambert CompanyInventors: Joseph A. Picard, William H. Roark, Bruce D. Roth
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Patent number: 5245047Abstract: 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-(tetra hydro-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-2 H-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: GrantFiled: February 16, 1993Date of Patent: September 14, 1993Assignee: Warner-Lambert CompanyInventors: Donald E. Butler, Carl F. Deering, Alan Millar, Thomas N. Nanninga, Bruce D. Roth
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Patent number: 5216174Abstract: 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-heptadien4-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-(tetra hydro4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3carboxamide by a novel synthesis where 4-methyl-3-oxoN-phenylpentanamide is converted in eight operations to the desired product or alternatively 4-fluoro-.alpha.-[2methyl-1-oxopropyl]-.gamma.-oxo-N,.beta.-diphenylbenzen ebutaneamide 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]-1Hpyrrole-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: GrantFiled: June 1, 1992Date of Patent: June 1, 1993Assignee: Warner-Lambert Co.Inventors: Donald E. Butler, Carl F. Deering, Alan Millar, Thomas N. Nanninga, Bruce D. Roth
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Patent number: 5149837Abstract: 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-fluoro-phenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetr ahydro-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: GrantFiled: February 12, 1992Date of Patent: September 22, 1992Assignee: Warner-Lambert CompanyInventors: Donald E. Butler, Carl F. Deering, Alan Millar, Thomas N. Nanninga, Bruce D. Roth
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Process for trans-6-(2-substituted-pyrrol-1-yl)alkyl)pyran-2-one inhibitors of cholesterol synthesis
Patent number: 5124482Abstract: 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: GrantFiled: November 14, 1991Date of Patent: June 23, 1992Assignee: Warner-Lambert CompanyInventors: Donald E. Butler, Carl F. Deering, Alan Millar, Thomas N. Nanninga, Bruce D. Roth -
Patent number: 5102893Abstract: 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 hydrolipidemic 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: GrantFiled: June 19, 1990Date of Patent: April 7, 1992Assignee: Warner-Lambert CompanyInventors: Joseph A. Picard, Bruce D. Roth, Drago R. Sliskovic
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Patent number: 5097045Abstract: 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-(tetra hydro-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: GrantFiled: October 9, 1990Date of Patent: March 17, 1992Assignee: Warner-Lambert CompanyInventors: Donald E. Butler, Carl F. Deering, Alan Millar, Thomas N. Nanninga, Bruce D. Roth