Patents by Inventor Edward J. J. Grabowski

Edward J. J. Grabowski 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).

  • Process for racemizing an enantiomer of 5,6-dihydro-4-alkylamino-4H-thieno(or furo) [2,3-B]-thiopyran-2-sulfonamide-7,7-dioxide
    Patent number: 5011942
    Abstract: Compounds classified as 5,6-dihydro-4-alkylamino-4H-thieno (or furo) [2,3-b]thiopyran-2-sulfonamide-7,7-dioxide are carbonic anhydrase inhibitors useful in the treatment of ocular hypertension, and most of the carbonic anhydrase inhibitory activity resides in only one of the enantiomers. The undesired enantiomer is utilized by racemization by thermolysis of an N-acyl derivative in a basic environment followed by removal of the acyl group. The racemate may then be resolved into the enantiomers.
    Type: Grant
    Filed: February 5, 1990
    Date of Patent: April 30, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Thomas J. Blacklock, Edward J. J. Grabowski, Paul Sohar
  • (S)-Alkyl 3-(thien-2-ylthio)butyrate and analogs and synthesis thereof
    Patent number: 4968814
    Abstract: (S)-Alkyl 3-(thien-2-ylthio)butyrate and analogs are intermediates in the synthesis of the chiral (S,S)-5,6-dihydro-4-ethylamino-6-methyl-4H-thieno[2,3-b]thiopyran-2-sulfon amide-7,7-dioxide and analogs thereof, topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma.
    Type: Grant
    Filed: April 18, 1990
    Date of Patent: November 6, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Thomas J. Blacklock, Edward J. J. Grabowski, Paul Sohar
  • Resolution of a carboxylic acid
    Patent number: 4940813
    Abstract: A process is described for the preparation of an optically active carboxylic acid or ester derivative thereof from a ketene and an optically active .alpha.-hydroxyester or an .alpha.-hydroxy amide.
    Type: Grant
    Filed: March 31, 1989
    Date of Patent: July 10, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Edward G. Corley, Robert D. Larsen, Edward J. J. Grabowski, Paul Reider
  • Crystalline salts of L or (S)-3-(3,4-dihydroxyphenyl)-2-methylalanine esters and process
    Patent number: 4914222
    Abstract: Crystalline salts of (R,S)-pivaloyloxyethyl esters of (S)-3-(3,4-dihydroxyphenyl)-2-methylalanine, processes for their preparation and pharmaceutical composition are disclosed.
    Type: Grant
    Filed: September 30, 1986
    Date of Patent: April 3, 1990
    Assignee: Merck & Co., Inc.
    Inventors: John Budavari, Robert F. Czaja, Edward J. J. Grabowski, William F. Shukis, Arthur J. Zambito
  • Process for 2-(aminoalkylthio) carbapenems
    Patent number: 4894450
    Abstract: This invention relates to a process for preparing 2-(aminoalkylthio)carbapenems. In particular, this invention relates to a process in which a bis(substituted phenyl) phosphorohalidate is used to form an enol phosphate intermediate that can be converted to 2-(aminoalkylthio)carbapenems by reaction with suitable thioalkylamines.
    Type: Grant
    Filed: May 11, 1987
    Date of Patent: January 16, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. J. Grabowski, David L. Hughes
  • Process for resolution and racemization of amines with acidic .alpha.-hydrogens
    Patent number: 4859771
    Abstract: An economical, one-pot process for resolution-racemization of primary amines with .alpha.-hydrogens via selective crystallization of diastereomeric chiral sulfonic acid salts and the subsequent in situ racemization of the other enantiomer by the catalytic addition of aromatic aldehydes, and a key process intermediate thereof.
    Type: Grant
    Filed: January 19, 1989
    Date of Patent: August 22, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Paul J. Reider, Edward J. J. Grabowski
  • Process for crystalline salts of L or (S)-3-(3,4-dihydroxyphenyl)-2-methylalanine esters
    Patent number: 4670578
    Abstract: Crystalline salts of (R,S)-pivaloyloxyethyl esters of (S)-3-(3,4-dihydroxyphenyl)-2-methylalanine and processes for their preparation are disclosed.
    Type: Grant
    Filed: August 29, 1983
    Date of Patent: June 2, 1987
    Assignee: Merck & Co., Inc.
    Inventors: John Budavari, Edward J. J. Grabowski
  • Preparation of 2-Deutero-D-serine
    Patent number: 4582931
    Abstract: A process for the preparation of 2-Deutero-D-serine and its fluorination is disclosed.
    Type: Grant
    Filed: December 24, 1984
    Date of Patent: April 15, 1986
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. J. Grabowski, Paul J. Reider
  • Process for preparing a manipulated enantiomer mixture by asymmetric chiral phase transfer catalysis
    Patent number: 4578509
    Abstract: A process is disclosed for obtaining manipulated proportions of the (+) and (-) enantiomers of [(6,7-dichloro-2,3-dihydro-2-methyl-1-oxo-2-phenyl-1H-inden-5-yl)oxy]aceti c acid by asymmetric chiral phase transfer catalysis.
    Type: Grant
    Filed: February 17, 1984
    Date of Patent: March 25, 1986
    Assignee: Merck & Co., Inc.
    Inventors: Ulf H. Dolling, Seemon H. Pines, Edward J. J. Grabowski
  • Process for preparing indenyl acetic acids
    Patent number: 4233457
    Abstract: This invention relates to an improved process for preparing 5-fluoro-2-methyl-1-(p-methylsulfinylbenzylidene)-3-indenyl acetic acid.
    Type: Grant
    Filed: May 17, 1979
    Date of Patent: November 11, 1980
    Assignee: Merck & Co., Inc.
    Inventors: Robert F. Czaja, Edward J. J. Grabowski
  • Synthesis of racemic 3-fluoro-alanine and its salts
    Patent number: 4149012
    Abstract: The racemate of 3-fluoro-alanine, and salts thereof, are prepared by reductive amination of 3-fluoro-pyruvic acid, its hydrate, or salts thereof, via the intermediate 2-imino-3-fluoro propionic acid salt, using alkali metal borohydrides as reducing agents. The racemates thus obtained are valuable in the production of 3-fluoro-D-alanine and its pharmacologically acceptable salts, and derivatives thereof, which are potent antibacterial agents.
    Type: Grant
    Filed: October 7, 1977
    Date of Patent: April 10, 1979
    Assignee: Merck & Co., Inc.
    Inventors: Ulf-H. Dolling, Edward J. J. Grabowski, Erwin F. Schoenewaldt, Meyer Sletzinger
  • 7-(Amidinothio)acetamido-7-methoxy cephalosporins
    Patent number: 4121041
    Abstract: New 7-(Amidinothio)acetamido-7-methoxy-3-carbamoyloxymethyl-3-cephem-4-carboxy lic acid compounds are prepared which are useful as antibacterial agents, especially Pseudomonas.
    Type: Grant
    Filed: February 4, 1977
    Date of Patent: October 17, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Robert F. Czaja, Edward J. J. Grabowski
  • Process for preparing 5,11-diazatetracyclododecanes
    Patent number: 4070359
    Abstract: A new heterocycle, 5,11-diazatetracyclo]6.2.2.0.sup.2,7.0.sup.4,9 ]dodecane, is prepared by heating an endo-diazatricyclo[6.2.2.0.sup.2,7 ]dodec-11-ene substituted in the 7 and 11 positions with electron withdrawing groups. 2,9-Bis-phenylacetyl derivatives of the new heterocycle and closely related derivatives are potent analgesic agents.
    Type: Grant
    Filed: March 24, 1977
    Date of Patent: January 24, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Jan ten Broeke, Edward J. J. Grabowski, Lars M. Flataker, Michael H. Fisher, Arthur A. Patchett
  • 4,9-Diazatricyclo[6.2.2.0.sup.2,7 ]dodec-11-enes
    Patent number: 4070360
    Abstract: A new heterocycle, 5,11-diazatetracyclo-[6.2.2.0.sup.2,7.0.sup.4,9 ]dodecane, is prepared by heating an endo-diazatricyclo[6.2.2.0.sup.2,7 ]dodec-11-ene substituted in the 7 and 11 positions with electron withdrawing groups. 2,9-Bis-phenylacetyl derivatives of the new heterocycle and closely related derivatives are potent analgesic agents.
    Type: Grant
    Filed: March 24, 1977
    Date of Patent: January 24, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Jan ten Broeke, Edward J. J. Grabowski, Lars M. Flataker, Michael H. Fisher, Arthur A. Patchett
  • Diazatetracyclododecanes
    Patent number: 4033968
    Abstract: A new heterocycle, 5,11-diazatetracyclo[6.2.2.0.sup.2,7.0.sup.4.9 ]dodecane, is prepared by heating an endo-diazatricyclo[6.2.2.0.sup.2,7 ]dodec-11-ene substituted in the 7 and 11 positions with electron withdrawing groups. 2,9-Bis-phenylacetyl derivatives of the new heterocycle and closely related derivatives are potent analgesic agents.
    Type: Grant
    Filed: April 14, 1976
    Date of Patent: July 5, 1977
    Assignee: Merck & Co., Inc.
    Inventors: Jan ten Broeke, Edward J. J. Grabowski, Lars M. Flataker, Michael H. Fisher, Arthur A. Patchett
  • Synthesis of racemic 2-deutero-3-fluoro-alanine and its salts
    Patent number: 3972921
    Abstract: The racemates of 2-deutero-3-fluoro-alanine and its salts are prepared by reductive amination of 3-fluoro-pyruvic acid, its hydrate or salts thereof, via the intermediate 2-imino-3-fluoro propionic acid salt, using alkali metal borodeuterides as reducing agents. The racemates thus obtained are valuable in the production of the corresponding 2-deutero-3-fluoro-D-alanine, and its pharmacologically acceptable salts, and derivatives thereof, which are potent antibacterial agents.
    Type: Grant
    Filed: November 8, 1974
    Date of Patent: August 3, 1976
    Assignee: Merck & Co., Inc.
    Inventors: Ulf-H. Dolling, Edward J. J. Grabowski, Erwin F. Schoenewaldt, Meyer Sletzinger