Patents Assigned to Syntex (U.S.A.)
  • Patent number: 4739056
    Abstract: Compounds are disclosed according to the formula ##STR1## or an optical isomer thereof. The compounds of Formula I are cyclic AMP phosphodiesterase inhibitors useful as antithrombotic and inotropic agents and the like in mammals.
    Type: Grant
    Filed: November 26, 1986
    Date of Patent: April 19, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Michael C. Venuti
  • Patent number: 4737456
    Abstract: A method for assaying for a ligand analyte which is a member of a specific binding pair ("sbp member") consisting of ligand and its complementary receptor is disclosed. The ligand analyte has a binding site in common with an interfering substance present in a sample suspected of containing the analyte. The interfering substance has at least two binding sites. The method comprises combining in an assay medium without intervening separation (1) the sample, (2) a blocking receptor which does not bind to the ligand and does bind to the interfering substance, thereby blocking the binding of a common receptor to the interfering substance, and (3) a common receptor which binds to the common binding site. Any additional members of a signal producing system capable of producing a detectable signal in relation to the amount of analyte in the sample are added to the assay medium. Next, the assay medium is examined for the presence of a detectable signal.
    Type: Grant
    Filed: May 9, 1985
    Date of Patent: April 12, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Litai Weng, Iam Gibbons
  • Patent number: 4735966
    Abstract: Compounds useful in treating cardiovascular disorders such as thrombosis, hypertension and atherosclerosis are depicted in formulas (1), (2) and (3): ##STR1## wherein: A is --C.tbd.C--, trans --HC.dbd.CH--, --CH.sub.2 CH.sub.2 -- or --CH.dbd.CHCH.sub.2 --;X is lower alkoxy, hydroxy, or (2,2,2)-trifluoroethoxy;Y is hydrogen, exo-(lower alkyl) or endo-(lower alkyl);is an integer of 2-4;R.sub.1 is --CH.sub.2 OH, --CHO, --CO.sub.2 R or --CO.sub.2 H, and the olefin formed by the R.sub.1 (CH.sub.2).sub.n CH.dbd. moiety is either (E) or (Z);R.sub.2 is hydrogen or methyl, or optionally --CH.dbd.CH.sub.2 when A is --CH.dbd.CHCH.sub.2 --; andR.sub.3 is linear or branched alkyl, alkenyl or alkynyl having 5-10 carbon atoms, ##STR2## --(CH.sub.2).sub.m -phenyl or CH.sub.
    Type: Grant
    Filed: August 25, 1986
    Date of Patent: April 5, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Helen Y. Wu, Walter Kurz
  • Patent number: 4727022
    Abstract: Methods are provided for modulating Ligand-Receptor interactions by binding of molecules at two epitopes of a receptor, where the epitopes are in relatively close special relationship. By providing for inhibition of changes in conformation of the receptor, where the inhibition is due to steric interactions or molecular bridging between the two epitopic sites, Ligand-Receptor interactions may be modulated. The modulation of Ligand-Receptor interactions has application to diagnostic assays, modulation of cellular activity, and modulation of the physiological activity of macromolecular compounds.
    Type: Grant
    Filed: March 14, 1984
    Date of Patent: February 23, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Carl Skold, Dennis R. Gould, Edwin F. Ullman
  • Patent number: 4727069
    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: January 30, 1987
    Date of Patent: February 23, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Peter H. Nelson, Chee-Liang L. Gu, Anthony C. Allison, Elsie M. Eugui, William A. Lee
  • Patent number: 4725622
    Abstract: A method of treating rheumatoid arthritis which method comprises administering to a mammal in need of such treatment a therapeutically effective amount of a compound of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein:A is oxygen or sulfur;R.sup.1 is selected from the group consisting of H, ##STR2## in which Y is oxygen or sulfur:R.sup.2 is alkyl, haloalkyl or --NR.sup.4 R.sup.5, where R.sup.4 and R.sup.5 are independently H, alkyl, haloalkyl, cycloalkyl, phenyl optionally monosubstituted with halogen, hydroxy, carboxy, chlorocarbonyl, sulfonylamino, nitro, cyano, phenyl, alkyl, acyl, alkoxycarbonyl, acylamino, dialkylamino or dialkylaminoethoxycarbonyl, phenyl optionally disubstituted with hydroxy, carboxy, nitro or alkyl, or benzyl optionally substituted with dialkylamino;n is an integer from 0-6;R.sup.3 is H alkyl or a pharmaceutically acceptable cation;Q and R are independently H or --CO.sub.2 R.sup.
    Type: Grant
    Filed: January 23, 1986
    Date of Patent: February 16, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Peter H. Nelson, Anthony C. Allison, Elsie M. Eugui, Joseph M. Muchowski
  • Patent number: 4723033
    Abstract: This invention concerns a new process of preparing optically active .alpha.-arylalkanoic acids and their precursors. These .alpha.-arylalkanoic acids, esters, amides, nitriles, oxazolines and metal salts are stereoselectively prepared by forming the metal or metal halide of the corresponding acid, ester, amide, oxazoline, nitrile, or metal salt and treating the compound so prepared with an aryl halide in the presence of a chiral (optically active) transition metal catalyst of the formula (LL*)QZT wherein Q is a transition metal selected from palladium and nickel; Z and T are independently halogen; and LL* is a chiral tertiary diphosphine compound capable of acting as a bidentate ligand with Q to form a 5-membered ring, optionally in the presence of a dipolar aprotic solvent or mixtures thereof, for a time sufficient to form the corresponding optically active .alpha.
    Type: Grant
    Filed: March 7, 1986
    Date of Patent: February 2, 1988
    Assignee: Syntex Pharmaceuticals International Ltd.
    Inventor: Gary W. Erickson
  • Patent number: 4713382
    Abstract: Compounds having the formula ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the definitions given herein, are useful as antiarrhythmic agents.
    Type: Grant
    Filed: May 30, 1985
    Date of Patent: December 15, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Jean-Claude Pascal
  • Patent number: 4713348
    Abstract: Methods are provided for rapidly determining a number of parameters in a few determinations. Particularly, the method is applicable to blood typing, determining the blood type as to the ABO and Rh type, as well as the determination of isoantibodies to the antigens. The method employs fluorescent particles having a plurality of fluorescers, where the presence or absence of light emission of a particular wavelength can be determined.
    Type: Grant
    Filed: October 22, 1985
    Date of Patent: December 15, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Edwin F. Ullman
  • Patent number: 4707473
    Abstract: 4-Monosubstitued and 4,6-disubstituted phenoxazines, methods of preparing them and pharmaceutical compositions containing them. These compounds are useful as anti-inflammatories.
    Type: Grant
    Filed: May 30, 1986
    Date of Patent: November 17, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Joseph M. Muchowski, Robert J. Greenhouse, Angel Guzman
  • Patent number: 4704392
    Abstract: Compounds useful as antiviral agents are depicted in the formula: ##STR1## wherein: X is oxygen or NH, Y is hydrogen, iodo, fluoro, methyl or trifluoromethyl, Z is hydrogen or fluoro and Z' is fluoro; and the wavy line indicates that the group may be above or below the plane of the ring; and the pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: April 14, 1986
    Date of Patent: November 3, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Julien P. H. Verheyden, John C. Martin, G. V. Bindu Madhavan, Daniel P. C. McGee, Ernest J. Prisbe
  • Patent number: 4698442
    Abstract: .alpha.-amino acids having a substituted .omega.-guanidino group are disclosed herein.
    Type: Grant
    Filed: June 13, 1986
    Date of Patent: October 6, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John J. Nestor, Brian H. Vickery
  • Patent number: 4690925
    Abstract: Compounds according to the formula ##STR1## , its optical isomers, or a pharmaceutically acceptable salt thereof wherein:m and n are integers of 1 to 6;R.sub.1 is hydrogen or alkyl of 1 to 4 carbons;R.sub.2 is hydrogen or R.sub.1 and R.sub.2 are combined to form an oxo group;R.sub.3 is hydrogen, alkyl of 1 to 6 carbons, phenyl, benzyl, hydroxy lower alkyl and its aliphatic acylates of 1 to 6 carbon atoms or aryl acylates of 7 to 12 carbon atoms, carbamoyl alkyl, carboxyalkyl, alkoxycarbonylalkyl or .alpha.-amino acid side chains;R.sub.4 is hydrogen, alkyl of 1 to 6 carbons, benzyl, or hydroxy lower alkyl;R.sub.5 is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms or cycloalkyl lower alkyl of 4 to 12 carbon atoms wherein the cycloalkyl ring is unsubstituted or substituted with a lower alkyl, lower alkoxy, --OH, --OCOR.sub.6, halo, --NH.sub.2, --N(R.sub.6).sub.2, --NHCOR.sub.6, --COOH, or --COO(R.sub.6) group wherein R.sub.
    Type: Grant
    Filed: May 15, 1985
    Date of Patent: September 1, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John H. Fried, Michael C. Venuti
  • Patent number: 4690916
    Abstract: Synthetic nonapeptide and decapeptide LHRH antagonist analogues having a halo lower alkyl guanadino-substituted amino acyl residue at position six are disclosed herein.
    Type: Grant
    Filed: November 13, 1984
    Date of Patent: September 1, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John J. Nestor, Jr., Brian Vickery
  • Patent number: 4687735
    Abstract: Improved sensitive immunoassays are provided involving channeling involving one, usually two enzymes, where the enzymes are related by the product of one enzyme being the substrate of the other enzyme. A dispersed aggregation is formed in the assay medium of (1) the analyte, (2) one of the enzymes bound to a second binding member ("SBM") (enzyme - SBM conjugate) which conjugate is non-covalently bound to a first binding member ("FBM"), and (3) a multiplied amount of the other enzyme bound in the complex. The large amount of enzyme or reactant in the complex is achieved by having a multiplicity of linkages binding the enzyme or reactant directly or indirectly to FBMs. The enzyme channeling provides for a detectable signal which can be related to the amount of analyte in the medium.
    Type: Grant
    Filed: March 14, 1983
    Date of Patent: August 18, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robert K. DiNello, Ian Gibbons, Edwin F. Ullman
  • Patent number: 4686234
    Abstract: Compounds useful for treating inflammatory diseases, in particular rheumatoid arthritis, represented by the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein:R.sub.1 is H or lower alkyl having 1 to 6 carbon atoms;R.sub.2 is H, lower alkyl having 1 to 6 carbon atoms or ##STR2## in which R.sub.3 is H, lower alkyl having 1 to 6 carbon atoms or a pharmaceutically acceptable cation;R.sub.4 and R.sub.5 are each independently H or lower alkyl having 1 to 6 carbon atoms;X and Y are each independently O or S; andn is an integer of 1-6.
    Type: Grant
    Filed: November 27, 1985
    Date of Patent: August 11, 1987
    Assignee: Syntex (U.S.A) Inc.
    Inventors: Peter H. Nelson, Anthony C. Allison, Elsie M. Eugui
  • Patent number: 4686002
    Abstract: Solutions of choline base, (2-hydroxyethyl)trimethylammonium hydroxide, in water and/or lower alkanols may be stabilized by the addition of a stabilizing concentration of formaldehyde or paraformaldehyde. The stabilized solutions may be used as cleaning solutions, etchants for semiconductors and metal layers, and developers and strippers for positive working photoresists, and for other uses where a metal ion-free base is desired.
    Type: Grant
    Filed: July 18, 1986
    Date of Patent: August 11, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Carl J. Tasset
  • Patent number: 4686283
    Abstract: Polypeptides analogs of fragments of TGF.alpha. and EGF are useful as therapeutic and diagnostic agents.
    Type: Grant
    Filed: April 16, 1985
    Date of Patent: August 11, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John J. Nestor, Jr., Alain B. Schreiber
  • Patent number: D291185
    Type: Grant
    Filed: November 15, 1984
    Date of Patent: August 4, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: S. Nicholas Stiso, Robert F. Zuk
  • Patent number: D294807
    Type: Grant
    Filed: May 2, 1985
    Date of Patent: March 22, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: S. Nicholas Stiso, Robert F. Zuk