Patents by Inventor David G. Melillo

David G. Melillo 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).

  • Radioligand and binding assay
    Patent number: 6838291
    Abstract: The present invention is directed to the radioligand compound, [35S]-radiolabeled (+)-N-[1?-(6-cyano-1,2,3,4-tetrahydro-2(R)-naphthalenyl)-3,4-dihydro-4(R)-hydoxyspiro[2H-1-benzopyran-2,4?-piperidin]-6-yl]methanesulfonamide. Also within the scope of this invention is a method for identifying compounds that bind to the IKr channel, and may have antiarrhythmic activity.
    Type: Grant
    Filed: July 12, 2001
    Date of Patent: January 4, 2005
    Assignee: Merck & Co., Inc.
    Inventors: John W. Butcher, David A. Claremon, Thomas M. Connolly, Jerzy Karczewski, Kenneth S. Koblan, Matthew J. Kostura, Nigel J. Liverton, Dennis C. Dean, David G. Melillo
  • Radioligand and binding assay
    Publication number: 20020034730
    Abstract: The present invention is directed to the radioligand compound, [35S]-radiolabeled (+)-N-[1′-(6-cyano-1,2,3,4-tetrahydro-2(R)-naphthalenyl)-3,4-dihydro-4(R)-hydoxyspiro[2H-1-benzopyran-2,4′-piperidin]-6-yl]methanesulfonamide. Also within the scope of this invention is a method for identifying compounds that bind to the IKr channel, and may have antiarrhythmic activity.
    Type: Application
    Filed: July 12, 2001
    Publication date: March 21, 2002
    Inventors: John W. Butcher, David A. Claremon, Thomas M. Connolly, Jerzy Karczewski, Kenneth S. Koblan, Matthew J. Kostura, Nigel J. Liverton, Dennis C. Dean, David G. Melillo
  • Radiolabeled growth hormone secretagogue
    Patent number: 5830433
    Abstract: The present invention is directed to ?.sup.35 S!-N-?1(R)-?(1,2-dihydro-1-methanesulfonylspiro?3H-indole-3,4'-piperidin!- 1'-yl)carbonyl!-2-(phenylmethyloxy)ethyl!-2-amino-2-methylpropanamide, and pharmaceutically acceptable salts thereof. This ?.sup.35 S! radioligand is useful in identifying and characterizing cellular receptors which play a role in the activity of growth hormone secretatogogues. In addition, this ?.sup.35 S! radioligand is useful in assays which test compounds for growth hormone secretagogue activity.
    Type: Grant
    Filed: December 17, 1996
    Date of Patent: November 3, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Dennis C. Dean, David G. Melillo, Ravi Nargund, Leonardus Van Der Ploeg, Sheng-Shung Pong, James M. Schaeffer, Roy G. Smith
  • Process for preparing 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid or salts thereof
    Patent number: 4922007
    Abstract: A process for the preparation of 4-amino-1-hydroxybutylidene-1, 1-bisphosphonic acid or salts thereof which comprises:(a) reacting 4-aminobutyric acid with a mixture of phosphorous acid and PC1.sub.3 in the presence of methanesulfonic acid; and(b) recovering said 4-amino-1-hydroxybutylidene-1, 1-bisphosphonic acid or salts thereof.
    Type: Grant
    Filed: June 9, 1989
    Date of Patent: May 1, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Gerard R. Kieczykowski, David G. Melillo, Ronald B. Jobson
  • Chiral synthesis of (+)-trans-1a,2,3,4a,5,6-hexahydro-9-hydroxy-4-propyl-4H-naphth[1,2-b]-1, 4-oxazine
    Patent number: 4758661
    Abstract: (+)-trans-1a,2,3,4a,5,6-Hexahydro-9-hydroxy-4-propyl-4H-naphth[1,2-b]-1,4-o xazine is elaborated by a series of process steps that retain the enantiomeric purity of the starting material, D-aspartic acid. The product is a direct acting dopaminergic agent, useful in the treatment of Parkinson's disease.
    Type: Grant
    Filed: June 24, 1986
    Date of Patent: July 19, 1988
    Assignee: Merck & Co., Inc.
    Inventors: David G. Melillo, David J. Mathre, Robert D. Larsen
  • Trans-3-carboxymethylene-4-carboxy-5-methyl-delta2-isoxazoline as intermediate
    Patent number: 4499278
    Abstract: Disclosed is a process for the stereocontrolled total synthesis of thienamycin, which synthesis proceeds via intermediate II: ##STR1## wherein R.sup.5 and R.sup.6 are removable protecting groups.
    Type: Grant
    Filed: November 22, 1982
    Date of Patent: February 12, 1985
    Assignee: Merck & Co., Inc.
    Inventors: David G. Melillo, Kenneth M. Ryan
  • Synthesis of thienamycin via (3SR, 4RS)-3-[1 (SR)-hydroxyethyl]-2-oxo-4-azetidineacetic acid
    Patent number: 4473502
    Abstract: Disclosed is a process for the stereocontrolled total synthesis of thienamycin via intermediates II and IIa: wherein R is a readily removable carboxyl protecting group.
    Type: Grant
    Filed: June 7, 1982
    Date of Patent: September 25, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Thomas M. H. Liu, David G. Melillo, Kenneth M. Ryan, Ichiro Shinkai, Meyer Sletzinger
  • 1-Hydroxyethyl-2-amino pentanedioic acid derivatives
    Patent number: 4467107
    Abstract: Disclosed is a process for the stereocontrolled total synthesis of thienamycin via intermediates II and IIa: ##STR1## wherein R is a readily removable carboxyl protecting group.
    Type: Grant
    Filed: June 7, 1982
    Date of Patent: August 21, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Thomas M. H. Liu, David G. Melillo, Kenneth M. Ryan, Ichiro Shinkai, Meyer Sletzinger
  • Hydroxy amino dicarboxylic acids and esters
    Patent number: 4454332
    Abstract: Disclosed is a process for the stereocontrolled total synthesis of thienamycin from acetone dicarboxylate via intermediate II: ##STR1## wherein R is a readily removable carboxyl protecting group.
    Type: Grant
    Filed: June 7, 1982
    Date of Patent: June 12, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Thomas M. H. Liu, David G. Melillo, Kenneth M. Ryan, Meyer Sletzinger, Ichiro Shinkai
  • Synthesis of thienamycin via esters of (3SR, 4RS)-3-[(SR)-1-hydroxyethyl]-.beta.,2-dioxo-4-azetidinebutanoic acid
    Patent number: 4414155
    Abstract: Disclosed is a process for the stereocontrolled total synthesis of thienamycin, which synthesis proceeds via intermediate II: ##STR1## wherein R.sup.3 is a readily removable carboxyl protecting group.
    Type: Grant
    Filed: March 29, 1982
    Date of Patent: November 8, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Thomas M. H. Liu, David G. Melillo, Kenneth M. Ryan, Ichiro Shinkai, Meyer Sletzinger
  • Process for the preparation of 6-hydroxymethyl-2-(.beta.-aminoethylthio)-1-carbadethiapen-2-em-3-carbox ylic acid
    Patent number: 4375433
    Abstract: Disclosed is a process for preparing the antibiotic 6-hydroxymethyl-2-(.beta.-aminoethylthio)-1-carbadethiapen-2-em-3-carboxyl ic acid (I) ##STR1## and its pharmaceutically acceptable salt and ester derivatives. An intermediate for the production of these compounds are compounds of the formula ##STR2## wherein R.sup.5 and R are readily removable protecting groups.
    Type: Grant
    Filed: September 12, 1980
    Date of Patent: March 1, 1983
    Assignee: Merck & Co., Inc.
    Inventors: David G. Melillo, Kenneth M. Ryan
  • Process for the preparation of (2S)-tetrahydro-2.alpha.-methyl-6-oxo-4.beta..alpha.-carboxylic acid
    Patent number: 4360684
    Abstract: Disclosed is a process for preparing (2S)-tetrahydro-2.alpha.-methyl-6-oxo-4.beta.-amino-2H-pyran-3.alpha.-carb oxylic acid (I) which is useful in the synthesis of thienamycin. The process proceeds via a stereospecific reduction of the 2-acetyl-3-(R)-.alpha.-methylbenzylamino-2-pentenedioic acid diester (II). ##STR1## wherein R is, .alpha.-methylbenzyl, and R.sup.1 is lower alkyl having 1-6 carbon atoms or arylalkyl such as benzyl.
    Type: Grant
    Filed: April 8, 1981
    Date of Patent: November 23, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Raymond J. Cvetovich, David G. Melillo, Kenneth M. Ryan, Meyer Sletzinger
  • Intermediate for synthesis of thienamycin via (3SR, 4RS)-3-[1 (SR)-hydroxyethyl]-2-oxo-4-azetidineacetic acid
    Patent number: 4349687
    Abstract: Disclosed is a process for the stereocontrolled total synthesis of thienamycin via intermediates II and IIa: ##STR1## wherein R is a readily removable carboxyl protecting group.
    Type: Grant
    Filed: April 8, 1981
    Date of Patent: September 14, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Thomas M. H. Liu, David G. Melillo, Kenneth M. Ryan, Ichiro Shinkai, Meyer Sletzinger
  • Intermediate for the preparation of thienamycin
    Patent number: 4344885
    Abstract: Disclosed is a process for the stereocontrolled total synthesis of thienamycin from acetone dicarboxylate via intermediate II: ##STR1## wherein R is a readily removable carboxyl protecting group.
    Type: Grant
    Filed: April 17, 1981
    Date of Patent: August 17, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Thomas M. H. Liu, David G. Melillo, Kenneth M. Ryan, Ichiro Shinkai, Meyer Sletzinger
  • Synthesis of thienamycin via (3SR, 4RS)-3-((RS)-1-acyloxyethyl)-2-oxo-4-azetidineacetate
    Patent number: 4287123
    Abstract: Disclosed is a process for the stereocontrolled total synthesis of thienamycin, which synthesis proceeds via intermediate II: ##STR1## wherein R is a readily removable carboxyl protecting group; and ##STR2## is a readily removable acyl group.
    Type: Grant
    Filed: January 14, 1980
    Date of Patent: September 1, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Thomas M. H. Liu, David G. Melillo, Kenneth M. Ryan, Ichiro Shinkai, Meyer Sletzinger
  • Synthesis of thienamycin via esters of (3SR, 4RS)-3-[(SR)-1-hydroxyethyl]-.beta.,2-dioxo-4-azetidinebutanoic acid
    Patent number: 4282148
    Abstract: Disclosed is a process for the stereocontrolled total synthesis of thienamycin, which synthesis proceeds via intermediate II: ##STR1## wherein R.sup.3 is a readily removable carboxyl protecting group.
    Type: Grant
    Filed: January 14, 1980
    Date of Patent: August 4, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Thomas M. H. Liu, David G. Melillo, Kenneth M. Ryan, Ichiro Shinkai, Meyer Sletzinger
  • Synthesis of thienamycin via trans-3-carboxymethylene-4-carboxy-5-methyl-.DELTA..sup.2 -isoxazoline
    Patent number: 4269772
    Abstract: Disclosed is a process for the stereocontrolled total synthesis of thienamycin, which synthesis proceeds via intermediate II: ##STR1## wherein R.sup.5 and R.sup.6 are removable protecting groups.
    Type: Grant
    Filed: January 14, 1980
    Date of Patent: May 26, 1981
    Assignee: Merck & Co., Inc.
    Inventors: David G. Melillo, Kenneth M. Ryan
  • Process for the preparation of 6-hydroxymethyl-2-(.beta.-aminoethylthio)-1-carbadethiapen-2-em-3-carbox ylic acid
    Patent number: 4252722
    Abstract: Diclosed is a process for preparing the antibiotic 6-hydroxymethyl-2-(.beta.-aminoethylthio)-1-carbadethiapen-2-em-3-carboxyl ic acid (I) ##STR1## and its pharmaceutically acceptable salt and ester derivatives.
    Type: Grant
    Filed: August 8, 1979
    Date of Patent: February 24, 1981
    Assignee: Merck & Co., Inc.
    Inventors: David G. Melillo, Kenneth M. Ryan
  • 5-Fluoro-2-methyl-ind-1-ene-3-acetic acid
    Patent number: 4167640
    Abstract: Invention relates to improved processes for preparing 5-fluoro-2-methyl-1-(p-methylsulfinylbenzylidene)-indenyl-3-acetic acid, to intermediates thereof, and to the preparation of said intermediates.
    Type: Grant
    Filed: July 17, 1978
    Date of Patent: September 11, 1979
    Assignee: Merck & Co., Inc.
    Inventors: Roger J. Tull, David G. Melillo
  • 2-Methyl-5-fluoro-indanol-3-acetic acid
    Patent number: 4123457
    Abstract: Invention relates to improved processes for preparing 5-fluoro-2-methyl-1-(p-methylsulfinylbenzylidene)-indenyl-3-acetic acid, to intermediates thereof, and to the preparation of said intermediates.
    Type: Grant
    Filed: September 22, 1976
    Date of Patent: October 31, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Roger J. Tull, David G. Melillo