Patents Represented by Attorney Gerard A. Blaufarb
  • Patent number: 3997587
    Abstract: d1- and 8R-9-fluoro-11,15.alpha.-dihydroxyprosta-5-cis,13-trans-dienoic acid, d1- and 8R-9-fluoro-11,15.alpha.-dihydroxy-15.beta.-methyl-prosta-5-cis,13-trans-d ienoic acid and d1- and 8R-9-fluoro-11,15.beta.-dihydroxy-15.alpha.-methylprosta-5-cis,13-trans-di enoic acid, the pharmaceutically acceptable, nontoxic lower alkyl esters and salts thereof and process for the production of such compounds. 8R-9.beta.-fluoro-11.alpha.,15.alpha.-dihydroxyprosta-5-cis,13-trans-dieno ic acid is a representative compound of the class. These compounds possess prostaglandin-like activities and thus are useful in the treatment of mammals where prostaglandins are indicated. They are particularly useful as luteolytic agents in female mammals and as bronchodilators.
    Type: Grant
    Filed: June 26, 1975
    Date of Patent: December 14, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph M. Muchowski, Esperanza V. Velarde
  • Patent number: 3989720
    Abstract: Compositions containing and methods employing, as the essential ingredient, novel disubstituted xanthone carboxylic acid compounds which are useful in the treatment of allergic conditions. Methods for preparing these compounds and compositions and intermediates therein are also disclosed. 5-Methylsulfinyl-7-isopropoxyxanthone-2-carboxylic acid and 5,7-di(methylsulfinyl)xanthone-2-carboxylic acid are illustrated as representative compounds.
    Type: Grant
    Filed: December 4, 1975
    Date of Patent: November 2, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jurg R. Pfister, Ian T. Harrison, John H. Fried
  • Patent number: 3989839
    Abstract: This invention relates to novel 6,11-dihydrodibenzo-[b.e.]-thiepin-11-ones, methods of preparation, compositions and uses thereof.
    Type: Grant
    Filed: August 13, 1975
    Date of Patent: November 2, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Jack Ackrell
  • Patent number: 3989721
    Abstract: Compositions containing and methods employing, as the essential ingredient, novel disubstituted xanthone carboxylic acid compounds which are useful in the treatment of allergic conditions. Methods for preparing these compounds and compositions and intermediates therein are also disclosed. 5-Methylsulfinyl-7-isopropoxyxanthone-2-carboxylic acid and 5,7-di(methylsulfinyl)xanthone-2-carboxylic acid are illustrated as representative compounds.
    Type: Grant
    Filed: December 4, 1975
    Date of Patent: November 2, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jurg R. Pfister, Ian T. Harrison, John H. Fried
  • Patent number: 3988352
    Abstract: Compositions containing and methods employing, as the essential ingredient, novel disubstituted xanthone carboxylic acid compounds which are useful in the treatment of allergic conditions. Methods for preparing these compounds and compositions and intermediates therein are also disclosed. 5-Methylsulfinyl-7-isopropoxyxanthone-2-carboxylic acid and 5,7-di(methylsulfinyl)xanthone-2-carboxylic acid are illustrated as representative compounds.
    Type: Grant
    Filed: December 4, 1975
    Date of Patent: October 26, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jurg R. Pfister, Ian T. Harrison, John H. Fried
  • Patent number: 3985791
    Abstract: Novel racemic and 8R-antimeric 16-phenoxy- and 16-(o, m or p)-substituted phenoxy derivatives of 9.alpha., 11.alpha.,15-trihydroxy-17,18,19,20-tetranorprosta-4,5,13-trans-trienoic acids, which may be further substituted at C-15 by a methyl or ethyl group, the pharmaceutically acceptable, non-toxic lower alkyl esters and salts thereof and processes for the production of such compounds. dl 9.alpha.,11.alpha.,15.alpha.-trihydroxy-16-m-trifluoromethylphenoxy-17,18, 19,20-tetranorprosta-4,5,13-trans-trienoic acid and dl 9.alpha.,11.alpha.,15 -trihydroxy-15 -methyl-16-m-trifluoromethylphenoxy-17,18,19,20-tetranorprosta-4,5,13-tran s-trienoic acid are representative compounds of the class. These compounds possess prostaglandin-like activities and thus are useful in the treatment of mammals where prostaglandins are indicated. They are particularly useful as luteolytic agents in female mammals.
    Type: Grant
    Filed: December 22, 1975
    Date of Patent: October 12, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph M. Muchowski, John H. Fried
  • Patent number: 3979414
    Abstract: Compositions containing and methods employing, as the essential ingredient, novel disubstituted xanthone carboxylic acid compounds which are useful in the treatment of allergic conditions. Methods for preparing these compounds and compositions and intermediates therein are also disclosed. 5-Isopropyl-7-acetylxanthone-2-carboxylic acid is illustrated as a representative compound.
    Type: Grant
    Filed: December 4, 1975
    Date of Patent: September 7, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jurg R. Pfister, Ian T. Harrison, John H. Fried
  • Patent number: 3979404
    Abstract: Novel 2-substituted-1,2,4-thiadiazolo-[2,3-a]-imidazoles of the formula ##SPC1##And the pharmaceutically acceptable salts thereof; and process for their preparation. These 2-substituted-1,2,4-thiadiazolo-[2,3-a]-imidazoles are useful as fungistatic and fungicidal agents.
    Type: Grant
    Filed: January 10, 1975
    Date of Patent: September 7, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Colin C. Beard
  • Patent number: 3976654
    Abstract: Novel 2-substituted-1,2,4-thiadiazolo-[2,3-a]-benzimidazoles of the formula ##SPC1##And the pharmaceutically acceptable salts thereof; and process for their preparation. These 2-substituted-1,2,4-thiadiazolo-[2,3-a]-benzimidazoles are useful as fungistatic and fungicidal agents.
    Type: Grant
    Filed: October 16, 1975
    Date of Patent: August 24, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Colin C. Beard
  • Patent number: 3975427
    Abstract: (d1)-13-Substituted sulfinyl-prostaglandin-like [(d1)-2.alpha.-substituted-3.beta.-(1.alpha.-substituted sulfinyl-trans-2-alkenyl)-1-oxygenated cyclopentane and (d1)-2.alpha.-substituted-3.beta.-(1.alpha.-substituted sulfinyl-trans-2-alkenyl-4.alpha.-hydroxy-1-oxygenated cyclopentane]compounds exhibiting prostaglandin-like biological properties are prepared from known prostaglandins and prostaglandin-like compounds.
    Type: Grant
    Filed: June 5, 1974
    Date of Patent: August 17, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Karl G. Untch
  • Patent number: 3970685
    Abstract: (dl)-13-Substituted sulfinyl-prostaglandin-like [(dl)-2.alpha.-substituted-3.beta.-(1.alpha.-substituted sulfinyl-trans-2-alkenyl)-1-oxygenated cyclopentane and (dl)-2.alpha.-substituted -3.beta.-(1.alpha.-substituted sulfinyl-trans-2-alkenyl)-4-oxygenated-1-oxygenated cyclopentane] compounds exhibit prostaglandin-like biological properties and are also useful intermediates in the preparation of known prostaglandins.
    Type: Grant
    Filed: June 5, 1974
    Date of Patent: July 20, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Karl G. Untch, Gilbert J. Stork
  • Patent number: 3970684
    Abstract: Novel prostaglandin dehydro analogs of the PGA and PGB series and the 9-hydroxy-derivatives thereof, which possess a diethylenic unsaturation in the carboxylic acid chain and may be additionally substituted at C-4, C-6, C-9 and/or C-15 by a methyl, ethyl or propyl group, as well as the C-20-nor, bisnor or C-20 alkyl derivatives thereof, the alkyl group being of a straight chain and containing from 1 to 5 carbon atoms inclusive,, and processes for making same. 9-keto-15.alpha.-hydroxyprosta-4,5,10,13-trans-tetraenoic acid and 9-keto-15.alpha.-hydroxyprosta-4,5,8(12),13-trans-tetraenoic acid are representative of the class. Also included are the pharmaceutically acceptable, non toxic esters and salts of the carboxylic acid function and the pharmaceutically acceptable, non toxic esters and/or ethers of the secondary hydroxyl groups. These compounds possess prostaglandin-like activities and thus are useful in the treatment of mammals, where prostaglandins are indicated.
    Type: Grant
    Filed: July 15, 1974
    Date of Patent: July 20, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Pierre Crabbe, John H. Fried, Angel Guzman
  • Patent number: 3965115
    Abstract: Compositions containing and methods employing, as the essential ingredient, novel disubstituted xanthone carboxylic acid compounds which are useful in the treatment of allergic conditions. Methods for preparing these compounds and compositions and intermediates therein are also disclosed. 5-Methyl-sulfinyl-7-isopropoxyxanthone-2-carboxylic acid and 5,7-di(methylsulfinyl)xanthone-2-carboxylic acid are illustrated as representative compounds.
    Type: Grant
    Filed: March 13, 1975
    Date of Patent: June 22, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jurg R. Pfister, Ian T. Harrison, John H. Fried
  • Patent number: 3963752
    Abstract: Compositions containing and methods employing, as the essential ingredient, novel disubstituted xanthone carboxylic acid compounds which are useful in the treatment of allergic conditions. Methods for preparing these compounds and compositions and intermediates therein are also disclosed. 5-Methylsulfinyl-7-isopropoxyxanthone-2-carboxylic acid and 5,7-di(methylsulfinyl)xanthone-2-carboxylic acid are illustrated as representative compounds.
    Type: Grant
    Filed: March 13, 1975
    Date of Patent: June 15, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jurg R. Pfister, Ian T. Harrison, John H. Fried
  • Patent number: 3963753
    Abstract: Compositions containing and methods employing, as the essential ingredient, novel disubstituted xanthone carboxylic acid compounds which are useful in the treatment of allergic conditions. Methods for preparing these compounds and compositions and intermediates therein are also disclosed. 5-Methyl-sulfinyl-7-isopropoxyxanthone-2-carboxylic acid and 5,7-di(methylsulfinyl)xanthone-2-carboxylic acid are illustrated as representative compounds.
    Type: Grant
    Filed: March 13, 1975
    Date of Patent: June 15, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jurg R. Pfister, Ian T. Harrison, John H. Fried
  • Patent number: 3962422
    Abstract: Method for immunizing nursing piglets against transmissible gastroenteritis (TGE) virus by administering to the pregnant sow an effective amount of a vaccine containing attenuated TGE virus and permitting the nursing piglets to suckle the sow. The vaccine is administered twice, (a) intramuscularly at from about 63 days to about 21 days pre-farrowing and (b) intranasally at from about 21 days to about 7 days pre-farrowing, with the proviso that at least 14 days and not more than 42 days elapse between the intranasal and intramuscular inoculations.
    Type: Grant
    Filed: February 18, 1975
    Date of Patent: June 8, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: John B. Parks
  • Patent number: 3953470
    Abstract: Prostaglandin analogs of the PGF.sub.2.sub..alpha., PGE.sub.2, PGF.sub.1.sub..alpha. and PGE.sub.1 series substituted at C-10.alpha. by a hydroxyl group, the derivatives of the PGF.sub.1.sub..alpha. and PGE.sub.1 series further substituted at C-5,6 by a methylene or dihalomethylene group, and the 10,11-ketals thereof and methods of preparing such compounds. 9.alpha.,15.alpha.-Dihydroxy-10.alpha.,11.alpha.-isopropylidenedioxyprosta -5,13-dienoic acid, 9-keto-10.alpha.,11.alpha.-isopropylidenedioxy-15.alpha.-hydroxyprosta-5,1 3-dienoic acid and 5,6-methylene-9.alpha.,15.alpha.-dihydroxy-10.alpha.,11.alpha.-isopropylid enedioxyprost-13-enoic acid are representative of the class. Also included are the corresponding esters, ethers, pharmaceutically acceptable salts and amides. These compounds possess prostaglandin-like activity and thus are useful in the treatment of mammals, where prostaglandins are indicated.
    Type: Grant
    Filed: July 11, 1974
    Date of Patent: April 27, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Pierre Crabbe, Angel Guzman
  • Patent number: 3951618
    Abstract: Compositions containing and methods employing, as the essential ingredient, novel disubstituted xanthone carboxylic acid compounds which are useful in the treatment of allergic conditions. Methods for preparing these compounds and compositions and intermediates therein are also disclosed. 5-Methylthio-7-isopropoxyxanthone-2-carboxylic acid and 5,7-di-(methylthio)xanthone-2-carboxylic acid are illustrated as representative compounds.
    Type: Grant
    Filed: January 20, 1975
    Date of Patent: April 20, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jurg R. Pfister, Ian T. Harrison, John H. Fried
  • Patent number: 3949084
    Abstract: Compositions containing and methods employing, as the essential ingredient, novel substituted xanthone carboxylic acid compounds which are useful in the treatment of allergic conditions. Methods for preparing these compounds and compositions and intermediates therein are also disclosed. 6-Acetylxanthone-2-carboxylic acid is illustrated as a representative compound.
    Type: Grant
    Filed: January 23, 1975
    Date of Patent: April 6, 1976
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jurg R. Pfister, Ian T. Harrison, John H. Fried
  • Patent number: 3946031
    Abstract: Novel 2-substituted-1,2,4-thiadiazolo-[ 2,3-a]-benzimidazoles of the formula ##SPC1##And the pharmaceutically acceptable salts thereof; and process for their preparation. These 2-substituted-1,2,4-thiadiazole-[2,3-a]-benzimidazoles are useful as fungistatic and fungicidal agents.
    Type: Grant
    Filed: November 14, 1974
    Date of Patent: March 23, 1976
    Assignee: Syntex Inc.
    Inventor: Colin C. Beard