Patents by Inventor John H. Dygos

John H. Dygos 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).

  • Patent number: 5432284
    Abstract: The present invention relates to a novel process for the preparation of heterocyclic alkylamide derivatives having the following formula: ##STR1## and the pharmaceutically acceptable acid addition salt thereof wherein X represents halo, alkyl having 1 to 6 carbon atoms, hydrido, trifluoromethyl, phenyl, or lower alkoxy having 1 to 6 carbon atoms; Y represents the group --CN or --CONH.sub.2 ; R.sub.2 represents alkyl having 1 to 6 carbon atoms; R.sub.
    Type: Grant
    Filed: September 8, 1993
    Date of Patent: July 11, 1995
    Assignee: G. D. Searle & Co.
    Inventors: John H. Dygos, Thomas R. Kowar, Kathleen T. McLaughlin, Gatis Plume, Michael L. Prunier, Richard J. Salzmann, Mike G. Scaros, Joseph J. Wieczorek
  • Patent number: 5252763
    Abstract: A process for preparing higher order cuprate complexes by reacting an alkyne with zirconocene chloride hydride to produce a zirconium intermediate which is reacted with an alkyllithium and a first copper reagent selected from R.sup.2 Cu(CN)Li or the mixture CuCN and R.sup.2 Li to produce a higher order cuprate complex.
    Type: Grant
    Filed: July 8, 1992
    Date of Patent: October 12, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Kevin A. Babiak, James R. Behling, John H. Dygos, John S. Ng
  • Patent number: 5220019
    Abstract: Disclosed is a process for the preparation of 3-aryl-3-aminoalkyl-2,6-dioxohexahydropridines and particularly the compound 3-[3-(dimethylamino)propyl]3-(3 methoxyphenyl)-4, 4-dimethyl-2,6-piperidinedione, monohydrochloride, which is useful as an antidepressant.The process of the present invention comprises the condensation of a sterically hindered nitrile with a sterically hindered .alpha.,.beta.-unsaturated diester to produce a nitrile diester. These compounds can then undergo acid catalyzed cyclization and decarboalkoxylation in a one step process to provide the desired 3-aryl-3-aminoalkyl-2,6 -dioxohexahydropyridine.
    Type: Grant
    Filed: March 27, 1992
    Date of Patent: June 15, 1993
    Assignee: G. D. Searle & Co.
    Inventors: John H. Dygos, Kathleen T. McLaughlin, John S. Ng, Kalidas Paul
  • Patent number: 5106750
    Abstract: A process for irreversible regio- and stereoselective enzyme catalyzed acylation of alcohols using enol esters as acylating reagents is disclosed. The present invention permits the selective modification of hydroxyl group(s) of chiral and meso alcohols, including sugars, organometallics, and glycosides. The enol freed upon transesterification rapidly tautomerizes to the corresponding volatile aldehyde or ketone thereby preventing the reverse reaction from occurring.
    Type: Grant
    Filed: August 24, 1989
    Date of Patent: April 21, 1992
    Assignee: G. D. Searle & Co.
    Inventors: Chi-Huey Wong, Yi-Fong Wang, William J. Hennen, Kevin A. Babiak, John H. Dygos, John S. Ng
  • Patent number: 5104990
    Abstract: Disclosed is a process for the preparation of 3-aryl-3-aminoalkyl-2,6-dioxohexahydropridines and particularly the compounds 3-[3-(dimethylamino)propyl]-3-(3-methoxyphenyl)-4, 4-dimethyl-2,6-piperidinedione, monohydrochloride, which is useful as an antidepressant.the process of the present invention comprises the condensation of a sterically hindered nitrile with a sterically hindered .alpha., .beta.-unsaturated diester to produce a nitrile diester. These compounds can then undergo acid catalyzed cyclization and decarboalkoxylation in a one step process to provide the desired 3-aryl-3-aminoalkyl-2,6-dioxohexahydropyridine.
    Type: Grant
    Filed: February 27, 1990
    Date of Patent: April 14, 1992
    Assignee: G. D. Searle & Co.
    Inventors: John H. Dygos, Kathleen T. McLaughlin, John S. Ng, Kalidas Paul
  • Patent number: 5055604
    Abstract: A process for preparing a prostaglandin derivative by reacting an alkyne with zirconocene chloride hydride to produce a zirconium intermediate which is reacted with an alkyllithium and a first copper reagent selected from R.sup.2 Cu(CN)Li or the mixture CuCN and R.sup.2 Li to produce a higher order cuprate complex intermediate and reacting the higher order cuprate complex intermediate with a cyclopentenone to produce the prostaglandin derivative.
    Type: Grant
    Filed: April 17, 1990
    Date of Patent: October 8, 1991
    Assignee: G. D. Searle & Co.
    Inventors: Kevin A. Babiak, James R. Behling, John H. Dygos, John S. Ng
  • Patent number: 4125544
    Abstract: Preparation and the antimicrobial and antihypercholesterolemic utility of 20/22/23/24-oxa-7-oxocholesterols and esters thereof are disclosed.
    Type: Grant
    Filed: June 9, 1977
    Date of Patent: November 14, 1978
    Assignee: G. D. Searle
    Inventor: John H. Dygos
  • Patent number: 4008257
    Abstract: Preparation and the antihypercholesterolemic activity of 2,2-dimethyl-2-[(7,15,16,17-tetrahydro-17,17-dimethyl-6H-cyclopenta[a]phen anthren-3-yl)oxy]ethyl alkanedioates and intermediates thereto are disclosed.
    Type: Grant
    Filed: March 10, 1976
    Date of Patent: February 15, 1977
    Assignee: G. D. Searle & Co.
    Inventors: John H. Dygos, Karlene W. Salamon
  • Patent number: 3970686
    Abstract: Preparation and the antihypercholesterolemic activity of 5-(1,2,3,4-tetrahydro-6-methoxy-2-napthyl)-2-hydroxy-1-methylcyclopentanee thanols and esters thereof are disclosed.
    Type: Grant
    Filed: March 31, 1975
    Date of Patent: July 20, 1976
    Assignee: G. D. Searle & Co.
    Inventor: John H. Dygos