Patents by Inventor Haydn W. R. Williams

Haydn W. R. Williams 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: 5118858
    Abstract: Disclosed herein are /.sup.35 S/-labelled compound of the formula (I):(C.sub.6 H.sub.5).sub.3 C.sup.35 SHand processes therefor. This Compound (I) is useful as an intermediate for the introduction of sulfur isotope into a variety of compounds. For example, it is useful in the introduction of sulfur isotope into important compounds such as 6-mercaptopurine, 5-[3-(2-(7-chloroquinolin-2-yl)ethenyl)phenyl]-8-dimethylcarbamyl-4,6-dith ioactanoic acid, a potent antagonist of leukotriene D.sub.4 ; thiophosphoric acid derivatives, photo-affinity reagents and the like.
    Type: Grant
    Filed: October 19, 1990
    Date of Patent: June 2, 1992
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Haydn W. R. Williams, Robert N. Young, Robert J. Zamboni
  • Patent number: 4962203
    Abstract: Compounds having the formula: ##STR1## are selective antagonists of leukotrienes of D.sub.4. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents.
    Type: Grant
    Filed: August 14, 1989
    Date of Patent: October 9, 1990
    Assignee: Merck Frost Canada, Inc.
    Inventors: Robert N. Young, Haydn W. R. Williams, Serge Leger, Richard Frenette, Robert Zamboni
  • Patent number: 4906658
    Abstract: Compounds of Formula I ##STR1## the pharmaceutically acceptable salts, and the gamma-lactone form thereof are described. They are antagonists of leukotrienes and SRS-A.
    Type: Grant
    Filed: April 21, 1987
    Date of Patent: March 6, 1990
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Haydn W. R. Williams, Robert N. Young
  • Patent number: 4537902
    Abstract: Novel 4-substituted-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate renal lithiasis.
    Type: Grant
    Filed: June 11, 1979
    Date of Patent: August 27, 1985
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme (I.A.) Corp.
    Inventors: Edward J. Cragoe, Jr., Clarence S. Rooney, Haydn W. R. Williams
  • Patent number: 4453005
    Abstract: Substituted phenylalkenoic acids and esters of the formula: ##STR1## having useful pharmaceutical activity and processes for their preparation are disclosed.
    Type: Grant
    Filed: December 6, 1982
    Date of Patent: June 5, 1984
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Patrice C. Belanger, Claude Dufresne, John W. Gillard, Haydn W. R. Williams
  • Patent number: 4448786
    Abstract: Novel 4-substituted-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate kidney stone formation. A novel process for their preparation is also disclosed.
    Type: Grant
    Filed: June 25, 1982
    Date of Patent: May 15, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Clarence S. Rooney, Haydn W. R. Williams
  • Patent number: 4435579
    Abstract: The present invention is concerned with an improved process for the production of highly active optical isomers of (-) 7 or 8 fluorodibenzo[b,f]thiepin-3-carboxylic acid-5-oxide having the structural formula ##STR1## in which the fluoro substituent replaces a hydrogen in the 7 or 8 position. The two active isomers represented by formula II are S(-)7-fluorodibenzo[b,f]thiepin-3-carboxylic acid-5-oxide and R(-)8-fluorodibenzo[b,f]thiepin-3-carboxylic acid-5-oxide. It is especially concerned with the resolution of the racemic 7 or 8 fluorodibenzo[b,f]thiepin-3-carboxylic acid-5-oxide by first forming and separating diastereomers of said racemic carboxylic acids by salt formation with ephedrine followed by crystallization and regeneration of the desired (-) isomers and recycling of the (+) isomer by racemization of the regenerated isomer. The compounds obtained in high yield by this process are highly active prostaglandin antagonists which are useful in treating a variety of conditions such as allergic asthma.
    Type: Grant
    Filed: July 12, 1982
    Date of Patent: March 6, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Patrice C. Belanger, Haydn W. R. Williams, Joshua Rokach
  • Patent number: 4432992
    Abstract: Novel 4-[5(and 4)-substituted-2-thienyl]-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate kidney stone formation. A novel process for their preparation is also disclosed.
    Type: Grant
    Filed: November 5, 1979
    Date of Patent: February 21, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Clarence S. Rooney, Haydn W. R. Williams
  • Patent number: 4431660
    Abstract: Novel 4-substituted-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate renal lithiasis.
    Type: Grant
    Filed: October 17, 1980
    Date of Patent: February 14, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Clarence S. Rooney, Haydn W. R. Williams
  • Patent number: 4431652
    Abstract: 4-Hydroxy-5-substituted-3(2H)-isothiazolone-1,1-dioxide derivatives of the formula: ##STR1## where X and Y are independently selected from the group consisting of hydrogen, halogen, and C.sub.1-6 alkyl; provided that positions 2 and 6 of the substituted phenyl moiety may not be substituted by C.sub.3-6 alkyl; or a pharmaceutically acceptable salt thereof;useful in treating urinary tract, especially renal calcium oxalate lithiasis.
    Type: Grant
    Filed: December 29, 1980
    Date of Patent: February 14, 1984
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme (I.A.) Corp.
    Inventors: Edward J. Cragoe, Jr., Clarence S. Rooney, Haydn W. R. Williams
  • Patent number: 4428956
    Abstract: 4-Hydroxy-5-substituted-3(2H)-isothiazolone-1,1-dioxide derivatives of the formula: ##STR1## where X and Y are independently selected from the group consisting of hydrogen, halogen, and C.sub.1-6 alkyl; provided that positions 2 and 6 of the substituted phenyl moiety may not be substituted; and n is 0 or 1;or a pharmaceutically acceptable salt thereof; useful in treating urinary tract, especially renal calcium oxalate lithiasis.
    Type: Grant
    Filed: December 29, 1980
    Date of Patent: January 31, 1984
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme (I.A.) Corp.
    Inventors: Edward J. Cragoe, Jr., Clarence S. Rooney, Haydn W. R. Williams
  • Patent number: 4424355
    Abstract: The present invention is concerned with an improved process for the production of highly active optical isomers of (-) 7 or 8 fluorodibenzo?b,f!thiepin-3-carboxylic acid-5-oxide having the structural formula ##STR1## in which the fluoro substituent replaces a hydrogen in the 7 or 8 position. The two active isomers represented by formula II are S(-)7-fluorodibenzo?b,f!thiepin-3-carboxylic acid-5-oxide and R(-)8-fluorodibenzo?b,f!thiepin-3-carboxylic acid-5-oxide. It is especially concerned with the resolution of the racemic 7 or 8 fluorodibenzo?b,f!thiepin-3-carboxylic acid-5-oxide by first forming and separating diastereomers of said racemic carboxylic acids by salt formation with brucine or ephedrine followed by crystallization and regeneration of the desired (-) isomers and recycling of the (+) isomer by racemization of the regenerated isomer.
    Type: Grant
    Filed: February 24, 1982
    Date of Patent: January 3, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Patrice C. Belanger, Haydn W. R. Williams, Joshua Rokach
  • Patent number: 4423063
    Abstract: 2,4-Dioxo-4-substituted-1-butanoic acid derivatives of the formula: ##STR1## where R is hydrogen or C.sub.1-4 alkyl; andL is a lipophilic group consisting essentially of ##STR2## where R' is (a) hydrogen; (b) C.sub.1-3 alkyl; (c) benzyl; (d) pyridyl C.sub.1-3 alkyl or (e) (3,4-dihydro-3-hydroxy-2H-1,5-benzodioxepin-3-yl) methyl; provided that positions 2 and 6 of the substituted phenyl moiety may not be substituted; or ##STR3## where R' has the same meaning as above; or a pharmaceutically acceptable salt thereof; useful in treating urinary tract, especially renal calcium oxalate lithiasis.
    Type: Grant
    Filed: March 5, 1982
    Date of Patent: December 27, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Clarence S. Rooney, Haydn W. R. Williams, Edward J. Gragoe, Jr., Arthur A. Patchett
  • Patent number: 4379791
    Abstract: 4-(Substituted thiazolyl)-3-hydroxy-3-pyrroline-2,5-diones of the formula: ##STR1## are inhibitors of glycolic acid oxidase useful in treating or preventing calcium oxalate kidney or bladder stones.
    Type: Grant
    Filed: June 1, 1981
    Date of Patent: April 12, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Clarence S. Rooney, Haydn W. R. Williams
  • Patent number: 4377588
    Abstract: Novel 4-(substituted thiazolyl)-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate renal lithiasis.
    Type: Grant
    Filed: September 11, 1979
    Date of Patent: March 22, 1983
    Assignees: Merck Sharp & Dohme (I.A.) Corp., Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Clarence S. Rooney, Haydn W. R. Williams
  • Patent number: 4349561
    Abstract: Novel 4-substituted-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate kidney stone formation. A novel process for their preparation is also disclosed.
    Type: Grant
    Filed: November 5, 1979
    Date of Patent: September 14, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Clarence S. Rooney, Haydn W. R. Williams
  • Patent number: 4342776
    Abstract: Novel 4-substituted-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate kidney stone formation. A novel process for their preparation is also disclosed.
    Type: Grant
    Filed: November 5, 1979
    Date of Patent: August 3, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Clarence S. Rooney, Haydn W. R. Williams
  • Patent number: 4337258
    Abstract: 2,4-Dioxo-4-substituted-1-butanoic acid derivatives of the formula: ##STR1## where R is hydrogen or C.sub.1-4 alkyl; andL is a lipophilic group consisting essentially of(1) ##STR2## where R' is (a) hydrogen; (b) C.sub.1-3 alkyl; (c) benzyl; (d) pyridyl C.sub.1-3 alkyl; or (e) (3,4-dihydro-3-hydroxy-2H-1,5-benzodioxepin-3-yl) methyl; provided that positions 2 and 6 of the substituted phenyl moiety may not be substituted; or(2) ##STR3## where R' has the same meaning as above; or a pharmaceutically acceptable salt thereof; useful in treating urinary tract, especially renal calcium oxalate lithiasis.
    Type: Grant
    Filed: December 29, 1980
    Date of Patent: June 29, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Clarence S. Rooney, Haydn W. R. Williams, Edward J. Cragoe, Jr., Arthur A. Patchett
  • Patent number: 4336397
    Abstract: 2,4-Dioxo-4-substituted-1-butanoic acid derivatives of the formula: ##STR1## where R is hydrogen or C.sub.1-4 alkyl; andL is a lipophilic group consisting essentially of: ##STR2## where R.sup.1 and R.sup.2 are each independently selected from the group consisting of (a) hydrogen; (b) C.sub.4-12 straight or branched chain alkyl; (c) C.sub.4-7 cycloalkyl; and (d) tetrahydronaphthyl; provided that R.sup.1 and R.sup.2 may not both be hydrogen; and when one of R.sup.1 or R.sup.2 is tetrahydronaphthyl, the other must be some other substituent; and that positions 2 and 6 of the substituted phenyl moiety may not be substituted; and ##STR3## where R.sup.1, and R.sup.2 have the same meaning as above except tetrahydronaphthyl;R.sup.3 is bromine, chlorine, or fluorine;m is 0 to 3;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 29, 1980
    Date of Patent: June 22, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Arthur A. Patchett, Clarence S. Rooney, Haydn W. R. Williams
  • Patent number: 4298743
    Abstract: Novel 4-(substituted thiazolyl)-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate renal lithiasis.
    Type: Grant
    Filed: September 11, 1979
    Date of Patent: November 3, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Clarence S. Rooney, Haydn W. R. Williams