Patents Assigned to Syntex (U.S.A.)
  • Processes and intermediates for making 16-phenoxy and 16-substituted phenoxy-prostatrienoic acid derivatives and their stereoisomers
    Patent number: 4780562
    Abstract: This invention relates to a process for making a compound of formula I ##STR1## in the form of a stereoisomer or mixture thereof, wherein R is hydrogen, lower alkyl; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta., or a pharmaceutically acceptable, non-toxic salt of the compound wherein R is hydrogen; novel intermediates useful for preparing these compounds; processes for making the intermediates; and a stereoisomer of the compound of formula I wherein R is methyl and X is hydrogen and a process for making same.
    Type: Grant
    Filed: September 13, 1985
    Date of Patent: October 25, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Gary F. Cooper, Douglas L. Wren, Albert R. Van Horn, Tsung-Tee Li, Colin C. Beard
  • Aroyl benzofuran and benzothiophene acetic and propionic acids
    Patent number: 4780480
    Abstract: Novel aroyl-substituted benzofuran and benzothiophene acetic and proprionic acids are disclosed herein. These compounds are useful as analgesic, anti-inflammatory, and antipyretic agents.
    Type: Grant
    Filed: April 20, 1987
    Date of Patent: October 25, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: James P. Dunn
  • Intermediates for making 16-phenoxy- and 16-(substituted phenoxy)-prostatrienoic acid derivatives
    Patent number: 4778904
    Abstract: Compounds of the formula ##STR1## where R.sup.1 and R.sup.2 are hydrogen or an ether-forming group and X is hydrogen, halo, trifluoromethyl, lower alkyl, or lower alkoxy, are useful intermediates for making PGE and PGF derivatives having an allenic function.
    Type: Grant
    Filed: January 9, 1987
    Date of Patent: October 18, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Gary F. Cooper
  • Method and compositions for protecting anerobic microorganisms
    Patent number: 4775626
    Abstract: A method is disclosed for reducing the oxygen content of a medium in which are present cells, usually anaerobic microorganisms, to extend the time during which the cells remain viable. The method comprises having in fluid contact with the aqueous medium an effective amount of an oxidase and substrate for the oxidase. The oxidase and substrate for the oxidase in an aqueous medium can be in fluid, e.g., air, contact with a separately contained aqueous medium in which the cells are present. Alternatively, the cells can be present in the same aqueous medium as the oxidase and substrate for the oxidase. The aqueous medium containing the oxidase and the substrate for the oxidase can further contain a hydrogen peroxide scavenger in an effective amount.
    Type: Grant
    Filed: May 23, 1986
    Date of Patent: October 4, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Richard Armenta, Ian Gibbons, Edwin F. Ullman
  • Fluorescent conjugates bound to a support
    Patent number: 4774191
    Abstract: Fluorescent antigen conjugates are provided comprising antigens covalently bonded to at least one 2,7-dialiphatic substituted-9-phenyl-6-hydroxy-3H-xanthen-3-one, wherein the 1- and 8-positions are unsubstituted. Also provided are novel fluorescent compounds absorbing at wavelengths in excess of 500 nm, having active functionalities for linking to the antigen. Finally, methods are provided for analyzing antigens in serum, whereby serum interference is avoided.
    Type: Grant
    Filed: February 5, 1986
    Date of Patent: September 27, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Pyare Khanna, Edwin F. Ullman
  • Tricylic antidepressant conjugates to antigens and enzymes
    Patent number: 4772697
    Abstract: Tricyclic antidepressant functionalized compounds are provided for conjugation through a side chain to antigenic compounds, particularly poly(amino acids), and enzymes. The antigenic conjugates are employed for the production of antibodies and together with the enzyme conjugates find particular use in immunoassays for the determination or detection of the total amount of tricyclic antidepressants present in a sample.
    Type: Grant
    Filed: August 21, 1986
    Date of Patent: September 20, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Christine G. Collins, Marcel R. Pirio, Prithipal Singh
  • Vaccines comprising polyoxypropylene-polyoxyethylene block polymer based adjuvants
    Patent number: 4772466
    Abstract: A vaccine contains an immunologically effective amount of an antigen, a polyoxypropylene-polyoxyethylene block polymer, a glycol ether-based surfactant, an immunopotentiating amount of an immunostimulating glycopeptide, and, optionally, a metabolizable non-toxic oil.
    Type: Grant
    Filed: February 21, 1985
    Date of Patent: September 20, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Anthony C. Allison, Noelene E. Byars
  • Polyoxypropylene-polyoxyethylene block polymer based adjuvants
    Patent number: 4770874
    Abstract: An adjuvant composition contains an immunopotentiating amount of an immunostimulating glycopeptide, a polyoxypropylene-polyoxyethylene block polymer, a glycol ether-based surfactant, and, optionally, a metabolizable non-toxic oil.
    Type: Grant
    Filed: May 5, 1986
    Date of Patent: September 13, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Anthony C. Allison, Noelene E. Byars
  • 2-(3-pyridylmethyl)naphthalene-6-carboxylic acid as a thromboxane synthetase inhibitor
    Patent number: 4766127
    Abstract: The invention concerns a method of inhibiting thromboxane synthetase with a compound of the formula: ##STR1## or a pharmaceutically acceptable salt or ester thereof, in a mammal having a disease characterized by elevated thromboxane levels or an imbalance of prostacyclinthromboxane levels.
    Type: Grant
    Filed: February 10, 1987
    Date of Patent: August 23, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Gregory R. Martinez, John J. Bruno
  • N',N"-dialkylguanidino dipeptides
    Patent number: 4762821
    Abstract: N',N"-dialkylguanidino dipeptides with angiotension converting enzyme (ACE) inhibiting activity are useful as antihypertensives. Proline and proline analogs are components of the dipeptides.
    Type: Grant
    Filed: September 10, 1986
    Date of Patent: August 9, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: John J. Nestor
  • N-N-disubstituted-.omega.-[2-amino-3-(carbonylmethyl)-3, 4-dihydroquinazolinyl]oxyalkylamides and related compounds
    Patent number: 4761416
    Abstract: Pharmaceutical compositions comprising, or compositions consisting essentially of, compounds according to the formula ##STR1## or an optical isomer thereof are disclosed, wherein the substituents A, Z and R.sup.1 are defined herein. The invention is also directed to certain compounds of the above class. The compounds of Formula I are cyclic AMP phosphodiesterase inhibitors useful as antithrombotic and inotropic agents and the like in mammals.
    Type: Grant
    Filed: July 25, 1986
    Date of Patent: August 2, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John H. Fried, Michael C. Venuti
  • Quantitative opaque particle agglutination assay
    Patent number: 4760030
    Abstract: A method is disclosed for determining the presence of a member of a specific binding pair ("sbp member") consisting of ligand and its homologous receptor in a sample suspected of containing the sbp member. The method comprises combining in an assay medium the sample and an opaque particle capable of agglutinating in the presence of the sbp member. The opaque particle has a particle size of from about 0.2 to 5.0 microns. Next, the assay medium is irradiated with light having a wavelength of from about 350 to 2000 nm, and the optical density of the assay medium is measured. A change in optical density indicates the presence of the sbp member in the sample. The method has particular application in the determination of an antibody in a sample, particularly an autoantibody, such as, for example, rheumatoid factor.
    Type: Grant
    Filed: September 10, 1984
    Date of Patent: July 26, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Paulette Peterson, Martin Becker
  • Naphthalene anti-psoriatic agents
    Patent number: 4758587
    Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is lower alkoxy or optionally substituted phenoxy;R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl;R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halo, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl or optionally substituted phenyl-lower-alkoxy, and m is 1 or 2;X and Y are different and are either R.sup.4 or --C(O)W whereinR.sup.4 is lower alkyl or optionally substituted phenyl-lower-alkyl;W is --OR.sup.5 or --NR.sup.6 R.sup.7,whereinR.sup.5 is alkyl, optionally substituted phenyl or optionally substituted benzyl; andR.sup.6 and R.sup.7 are independently hydrogen, lower alkyl, cycloalkyl or optionally substituted phenyl.
    Type: Grant
    Filed: March 9, 1987
    Date of Patent: July 19, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Michael C. Venuti
  • Chromatographic devices having modified edges
    Patent number: 4757004
    Abstract: A device is disclosed for use in a chromatographic system wherein a component of a mixture is paritioned between a liquid phase and an immobile phase. The device is comprised of a chromatographic material. In the chromatographic system the component traverses at least a portion of the chromatographic material. The device generally has at least one longitudinal edge substantially corresponding to the direction of traverse of the component. The longitudinal edge includes means for controlling the shape of the front of the traversing component.
    Type: Grant
    Filed: March 16, 1984
    Date of Patent: July 12, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Thomas M. Houts, Edwin F. Ullman
  • Chromatographic strip having non-compressed edges
    Patent number: 4756828
    Abstract: A device is disclosed for use in a chromatographic system wherein a component of a mixture is partitioned between a liquid phase and an immobile phase. The device comprises at least one strip of a bibulous material. In the chromatographic system the component traverses at least a portion of the strip. The strip generally has a longitudinal edge substantially corresponding to the direction of traverse of the component. The longitudinal edge has the characteristic of substantially the same rate of traversal by the component along this edge when compared to the rate of traversal of the component along the body of the strip. The strips are prepared from a sheet of a bibulous material by non-deformative or non-compressive cutting of the sheet. The preferred cutting means is a laser beam.
    Type: Grant
    Filed: April 12, 1984
    Date of Patent: July 12, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: David Litman, Robert Zuk, Gerald Rowley
  • Thiol esters of 4,5-allenyl prostaglandins and use thereof as antigastric secretion agents
    Patent number: 4755531
    Abstract: Thiol esters of 4,5-allenyl prostaglandins, methods of making them, and pharmaceutical compositions containing them. These compounds are useful as gastric acid secretion inhibitors.
    Type: Grant
    Filed: August 11, 1986
    Date of Patent: July 5, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph M. Muchowski, Angel Guzman
  • Morpholinoethylesters of mycophenolic acid and pharmaceutical compositions
    Patent number: 4753935
    Abstract: The compounds and pharmaceutical compositions of Formula A, wherein Z is hydrogen or --C(O)R, where R is lower alkyl or aryl, and the pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, anti-inflammatory agents, anti-tumor agents, anti-viral agents, and anti-psoriatic agents.
    Type: Grant
    Filed: January 30, 1987
    Date of Patent: June 28, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Peter H. Nelson, Chee-Liang L. Gu, Anthony C. Allison, Elsie M. Eugui, William A. Lee
  • Arylalkyl amines useful for lowering intraocular pressure
    Patent number: 4752621
    Abstract: Intraocular hypertensive diseases such as glaucoma are treated with compounds represented by formula I ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sub.1 is alkyl of two to four carbon atoms;R.sub.2 is --(CH.sub.2).sub.n --C.sub.6 H.sub.4 --R.sub.5 ; wheren is an integer from 1 to 4; andR.sub.5 is --H, --OH, halo, lower alkyl, lower alkoxy, ureido, lower alkyl-ureido, lower alkyl-amido, or formamido;R.sub.3 is hydro or hydroxy; andR.sub.4 is hydro, lower alkyl, amino, or lower alkylamino.
    Type: Grant
    Filed: August 25, 1986
    Date of Patent: June 21, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robin D. Clark, L. David Waterbury
  • Preparation of stereoisomers of ketals
    Patent number: 4749804
    Abstract: Pharmaceutically useful optically active .alpha.-arylalkanoic acids or esters, ortho esters, or amides thereof are stereoselectively prepared by contacting an aryl magnesium Grignard reagent with an optically active .alpha.-substituted acyl halide to form the optically active aryl .alpha.-substituted alkyl ketone, which is ketalized and rearranged to the desired optically active .alpha.-arylalkanoic acid or the corresponding ester, ortho ester or amide. In an alternate embodiment, the aryl .alpha.-substituted alkyl ketone is reduced to the corresponding alkanol, which is rearranged to the .alpha.-arylalkanal. The alkanal so produced is converted to the desired optically active .alpha.-arylalkanoic acid by conventional methods.
    Type: Grant
    Filed: June 10, 1986
    Date of Patent: June 7, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: George C. Schloemer
  • Heterocyclic aminoalkyl esters of mycophenolic acid and derivatives thereof and pharmaceutical compositions
    Patent number: 4748173
    Abstract: Heterocyclic aminoalkyl esters of mycophenolic acid, and the derivatives and pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, anti-inflammatory agents, anti-tumor agents, anti-viral agents, and anti-psoriatic agents.
    Type: Grant
    Filed: September 23, 1987
    Date of Patent: May 31, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Peter H. Nelson, Chee-Liang L. Gu, Anthony C. Allison, Elsie M. Eugui, William A. Lee