Patents Assigned to Syntex (U.S.A.)
  • Patent number: 5366737
    Abstract: This invention relates to compounds of the formulaor an optical isomer thereof wherein R.sup.1 and R.sup.2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms; R.sup.3, R.sup.4 and R.sup.5 are the same or different and are alkyl of 1 to 8 carbon atoms, aryl, aralkyl of 7 to 11 carbon atoms, or when two or three of R.sup.3, R.sup.4, and R.sup.5 are taken together to form quinuclidino, piperidino, pyrrolidino, or morpholino; n is 1 to 8; and X is a pharmaceutically acceptable anion.
    Type: Grant
    Filed: February 10, 1993
    Date of Patent: November 22, 1994
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Deborah A. Eppstein, Philip L. Felgner, Thomas R. Gadek, Gordon H. Jones, Richard B. Roman
  • Patent number: 5358717
    Abstract: The present invention relates to directly-compressible naproxen or naproxen sodium compositions comprising spray-dried naproxen or naproxen sodium. The present invention further relates the processes for preparing the directly-compressible naproxen or naproxen sodium compositions, to aqueous mixtures containing naproxen or sodium naproxen suitable for spray-drying and useful in the processes for preparing the directly-compressible compositions, to naproxen or naproxen sodium tablets prepared from the directly-compressible compositions, and to the processes for preparing the naproxen or naproxen sodium tablets.
    Type: Grant
    Filed: May 4, 1992
    Date of Patent: October 25, 1994
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Roy Kuramoto, Zakauddin T. Chowhan, Randal O. Pendleton, Hafez Hafezzadeh
  • Patent number: 5344782
    Abstract: Assay methods are provided for determining the presence of lithium in high sodium content liquids such as serum, plasma, urine or other sample without deproteinization. The novel compounds are water soluble derivatives of TMC-crownformazans and provide signal enhancement by increased absorbance of the dye-lithium complex over the dye anion.
    Type: Grant
    Filed: March 4, 1993
    Date of Patent: September 6, 1994
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Cheng-I Lin, Marcel Pirio
  • Patent number: 5342953
    Abstract: Compounds of the formula: ##STR1## wherein: A is oxo or dioxo;R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen or lower alkyl of one to six carbon atoms;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are independently hydrogen, lower alkyl of one to six carbon atoms, alkoxy, acyl or halo;are advantageously converted to thieno[3,2-c]pyridine derivatives and the pharmaceutically acceptable salts thereof, particularly ticlopidine hydrochloride.
    Type: Grant
    Filed: January 31, 1991
    Date of Patent: August 30, 1994
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Gary F. Cooper, Keith E. McCarthy
  • Patent number: 5334513
    Abstract: Methods are disclosed for conducting assays. One such method comprises providing in combination a first bibulous member zone ("first zone") and a liquid medium containing a component. The first zone has non-diffusively bound thereto a reagent interreactive with the component. Conditions are selected wherein the liquid medium and at least a portion of the component contained therein traverse all of the first zone and migrate by capillary migration into a second bibulous member zone ("second zone"). The second zone is of a different composition than the first zone and is incapable of specifically binding the component except when an analyte is to be detected and the method further includes causing a reagent to become bound to the first bibulous member zone in relation to the amount of analyte present.
    Type: Grant
    Filed: September 3, 1992
    Date of Patent: August 2, 1994
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Carl N. Skold, Armen B. Shanafelt, Vartan Ghazarossian, Edwin F. Ullman
  • Patent number: 5332662
    Abstract: Methods and compositions are disclosed for determining a peroxidatively active substance (PAS). The methods comprise the step of detecting a fluorescent signal produced upon cleavage of a compound of the formula F-L-Q, wherein F is a fluorester capable of producing the signal, Q is a quencher capable of quenching the signal when linked to F, and L is a bond, or a linking group having a bond, wherein the bond is capable of being cleaved by a reaction of the PAS with a substrate of the PAS and a hydrogen donor wherein the cleavage of the bond substantially reduces the quenching. The methods have application in a wide variety of systems including assays and improved assays for analytes. Also disclosed are kits for conducting the methods and improvements in accordance with the present invention.
    Type: Grant
    Filed: July 31, 1992
    Date of Patent: July 26, 1994
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Edwin F. Ullman
  • Patent number: 5328828
    Abstract: The instant invention is directed toward an immunoassay which can determine the presence of amphetamines in a sample suspected of containing amphetamine and/or methamphetamine by employing at least two conjugates, each comprised of a functionally similar label bound to an amphetamine analog and a methamphetamine analog respectively and an antibody to amphetamine and an antibody to methamphetamine wherein at least one of the antibodies is a monoclonal antibody.
    Type: Grant
    Filed: July 20, 1992
    Date of Patent: July 12, 1994
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Mae W. Hu, Cheng-I Lin, Chen-jung Hsu, James V. Freeman, Marcel Pirio, Edwin F. Ullman
  • Patent number: 5329019
    Abstract: Novel squaraine dyes and compositions of matter containing such dyes are disclosed . The novel squaraine dyes have an absorption maximum greater than 600 nanometers and are particularly useful in conjunction with a helium/neon (He/Ne) laser. Some of the squaraine dyes are hydrophilic and are therefore water soluble or water compatible and others of the squaraine dyes are lipophilic.
    Type: Grant
    Filed: April 27, 1992
    Date of Patent: July 12, 1994
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John Pease, Thomas L. Tarnowski, Donald Berger, Chiu C. Chang, Chun-Hua Chuang
  • Patent number: 5328907
    Abstract: This invention is directed to compounds of the formula (I): ##STR1## wherein R.sup.1 is --OR.sup.4 (where R.sup.4 is hydrogen, lower alkyl, lower hydroxyalkyl, phenyl, phenyl-lower-alkyl, or --(CH.sub.2).sub.n Y where n is an integer from 1 to 4 and Y is morpholino, --SR.sup.5, --C(O)OR.sup.5, --C(O)N(R.sup.6).sub.2, --N(R.sup.6).sub.2, or --N.sup.+ (R.sup.6).sub.3 X.sup.-, in which R.sup.5 is lower alkyl, each R.sup.6 is independently selected from hydrogen or lower alkyl, and X is halogen)or --SR.sup.7 (where R.sup.7 is lower alkyl, phenyl-lower-alkyl, or --(CH.sub.2).sub.n W whereW is --N(R.sup.6).sub.2 or --N.sup.+ (R.sup.6).sub.3 X.sup.-, and n, R.sup.6 and X are as previously defined);R.sup.2 is lower alkyl, phenyl or phenyl-lower-alkyl;R.sup.3 is halo, hydroxy, lower alkyl, lower alkoxy, lower haloalkyl, lower haloalkoxy, or --C(O)OR.sup.5 where R.sup.5 is as previously defined; andZ is a bond, 2,5-thienyl or 2,5-furanyl;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 8, 1992
    Date of Patent: July 12, 1994
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John W. Patterson, Bruce H. Devens
  • Patent number: 5310922
    Abstract: Novel squaraine dyes and compositions of matter containing such dyes are disclosed. The novel squaraine dyes have an absorption maximum greater than 600 nanometers and are particularly useful in conjunction with a helium/neon (He/Ne) laser. Some of the squaraine dyes are hydrophilic and are therefore water soluble or water compatible and others of the squaraine dyes are lipophilic.
    Type: Grant
    Filed: June 13, 1991
    Date of Patent: May 10, 1994
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John Pease, Thomas L. Tarnowski, Donald Berger, Chiu C. Chang, Chun-Hua Chuang
  • Patent number: 5296609
    Abstract: The invention provides a new and efficient process for preparing 2,4(5)-substituted or 1,2,4-substituted imidazole derivatives.The invention also provides a process for preparing substituted aminoalkylimidazole derivatives, useful for the treatment of mammals having a variety of disease states, including stroke, epilepsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism, and the like.The invention also relates to novel aminoalkylimidazole compounds.
    Type: Grant
    Filed: April 9, 1993
    Date of Patent: March 22, 1994
    Assignee: Syntex Pharmaceuticals, Ltd.
    Inventors: Gary McCort, Jean-Claude Pascal
  • Patent number: 5289930
    Abstract: An evaporation closure is disclosed. One embodiment of the closure includes a cap, made of pliable material, which in turn includes a top wall having an opening, a skirt downwardly depending from the top wall and having a threadless internal wall adapted to slip on and sealingly engage a container, and biasing means integral with the skirt; and an elongated arm, which in turn includes a means for sealing the opening, pivotally attached to the cap for movement between a first position wherein the sealing means seals the opening and a second position wherein the sealing means does not seal the opening, the arm being biased toward the first position by the biasing means. Such a closure is useful for minimizing evaporation from containers, particularly automated clinical analyzer reagent bottles.A kit including in packaged combination component parts of the evaporation closure is also disclosed. Such a kit is useful for conveniently assembling the evaporation closures of the present invention.
    Type: Grant
    Filed: November 19, 1991
    Date of Patent: March 1, 1994
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Kenneth K. Inouye
  • Patent number: 5284971
    Abstract: Compounds of general formula (I) ##STR1## wherein R.sup.1 is (CH.sub.2).sub.n ((CHNR.sup.7 R.sup.8).sub.m C(O)R.sup.9 ; n=1-3; and m=0 or 1;R.sup.3 and R.sup.5 are independently Cl, Br, I, or CH.sub.3 ;R.sup.7 and R.sup.8 are independently H or (C.sub.1 -C.sub.4)alkyl;R.sup.9 is OH, (C.sub.1 -C.sub.4)alkoxy, or NR.sup.7 R.sup.8 ;R.sup.31 is H, Cl, Br, I, (C.sub.1 -C.sub.4)alkyl, (C.sub.4 -C.sub.6)cycloalkyl, (C.sub.1 -C.sub.4)haloalkyl, (C.sub.4 -C.sub.6)halocycloalkyl, or --CH(R.sup.10)Ar where Ar is selected from 5-hydroxypyrid-2-yl, 6-hydroxypyrid-3-yl, 6-hydroxypyridazin-3-yl, 6-methoxypyridazin-3-yl, 6-hydroxypyridazin-3-yl N-oxide, and 6-methoxypyridazin-3-yl N-oxide and R.sup.10 is H or (C.sub.1 -C.sub.4)alkyl;R.sup.41 is OH or a bioprecursor thereof; and the pharmaceutically acceptable salts thereof; are structural analogs of the thyroid hormones T.sub.3 and T.sub.4 and exhibit selective thyromimetic activity.
    Type: Grant
    Filed: July 16, 1992
    Date of Patent: February 8, 1994
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Keith A. Walker, Sharada S. Labadie, Denis J. Kertesz, Craig W. Laughton
  • Patent number: 5279936
    Abstract: Methods are disclosed for separating a component of interest from a mixture containing the component of interest and other components. The method comprises contacting a first liquid medium containing the component of interest and other components with a second liquid medium that is of different density than and/or of different viscosity than the first liquid medium. The contact is carried out in such a way that mixing of the media is minimized or avoided. The component of interest is bound to magnetic particles. The contacted first liquid medium and second liquid medium are subjected to a magnetic field gradient to allow the magnetic particles to migrate into the second liquid medium and separation of the component of interest from other components is realized. Also disclosed are assays employing the present method. Kits for carrying out the present method and assays are also disclosed.
    Type: Grant
    Filed: December 22, 1989
    Date of Patent: January 18, 1994
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: John Vorpahl
  • Patent number: 5276034
    Abstract: Substituted imidazolyl-alkyl-piperazine and diazepine derivatives and the pharmaceutically acceptable salts thereof are useful for treating mammals having any of a variety of disease states. These disease states include: 1) diseases treated by direct neuronal protection, including focal and global ischemia, spinal injuries, and head trauma, and neurological diseases including Alzheimer's and Huntington's chorea; 2) uraemic and hyponatraemic encephalopathy; 3) diseases treated by diuresis; 4) diseases treated by calcium channel antagonism, including cardiovascular diseases (i.e. hypertension, angina, stable and unstable angina, Prinzmetal angina, arrhythmia, thrombosis, embolism, and congestive heart failure including chronic or acute cardiac failure), diseases characterized by ischemia of lower legs due to peripheral vascular disease (e.g., intermittent claudication), diseases characterized by spasms of smooth muscle (i.e.
    Type: Grant
    Filed: April 19, 1991
    Date of Patent: January 4, 1994
    Assignee: Syntex Pharmaceutical Ltd.
    Inventors: Jean C. Pascal, Chi-Ho Lee, Brian J. Alps, Henri Pinhas, Roger L. Whiting, Calum B. MacFarlane, Serge Beranger, Robert J. Dow
  • Patent number: 5273879
    Abstract: A Kit is disclosed for a method for producing multiple copies of a primary polynucleotide sequence located at the 3' terminus of a polynucleotide. The method comprises (a) forming in the presence of nucleoside triphosphates and template-dependent polynucleotide polymerase an extension of a primary polynucleotide sequence hybridized with a template sequence of a single stranded pattern polynucleotide comprising two or more template sequences each containing one or more site specific cleavage sequences, (b) cleaving into fragments said extension at cleavable polynucleotide sequences in the presence of means for specifically cleaving said cleavable polynucleotide sequences when said extension is hybridized with said site specific cleavage sequences, (c) dissociating said fragments, (d) hybridizing said fragments with single stranded pattern polynucleotide, and repeating steps (a)-(d). Steps (a)-(d) may be conducted simultaneously or wholly or partially sequentially.
    Type: Grant
    Filed: November 13, 1990
    Date of Patent: December 28, 1993
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Thomas C. Goodman, Martin Becker, Edwin F. Ullman, Samuel Rose
  • Patent number: 5273885
    Abstract: Methods employing thyroid analog conjugates to enzymes and to immunogenic carriers are provided, which find use in the determination of thyroid compounds normally in physiological fluids, such as serum. The immunogenic carrier conjugates are used to raise antibodies specific to thyroid compounds. The antibodies and enzyme conjugates are used in assays for thyroid compounds. The thyroid analogs are characterized by the presence of only one phenyl ring that contains a hydroxyl substituent and one or two substituents in an ortho relationship to the hydroxyl substituent on the phenyl ring wherein the phenyl ring is conjugated to an enzyme or an immunogenic carrier by a bond or a linking group. Kits for conducting the methods of the present invention are also disclosed.
    Type: Grant
    Filed: July 31, 1992
    Date of Patent: December 28, 1993
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jill M. Visor, Anthony Delizza, Edwin F. Ullman
  • Patent number: 5274108
    Abstract: This invention provides an improved process for the preparation of compounds of formula (I): ##STR1## wherein: n is 0, 1 or 2;each R.sup.1 is independently halo or lower alkyl;R.sup.2 is nitro or --N(R.sup.3)R.sup.4 whereR.sup.3 is hydrogen or lower alkyl;R.sup.4 is hydrogen, lower alkyl, lower alkylsulfonyl or --C(Y)R.sup.5 where Y is oxygen or sulfur and R.sup.5 is hydrogen, lower alkyl, lower alkoxy or --N(R.sup.6)R.sup.7 where R.sup.6 is hydrogen or lower alkyl and R.sup.7 is hydrogen, lower alkyl or lower alkoxycarbonyl; orR.sup.3 and R.sup.4 together with N is pyrrolidino, piperidino, morpholino, thiomorpholino or piperazino, wherein the piperazino is optionally substituted at the 4-position by --C(O)R.sup.8 where R.sup.8 is hydrogen, lower alkyl, lower alkoxy or amino;or pharmaceutically acceptable salts thereof. These compounds are useful in treating disease-states characterized by hypercholesterolemia.
    Type: Grant
    Filed: December 21, 1992
    Date of Patent: December 28, 1993
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Norman H. Dyson, John O. Gardner, Anthony Prince, Denis J. Kertesz
  • Patent number: 5272063
    Abstract: A method for the construction of recombinant DNA molecules capable of producing biologically active human nerve growth factor (hNGF) in insect cells is disclosed. Expression of the mature protein is achieved using the baculovirus expression system. The biologically active hNGF so produced is potentially of value in the treatment of patients suffering from Alzheimer's Disease and other neurological disorders.
    Type: Grant
    Filed: July 20, 1989
    Date of Patent: December 21, 1993
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Hardy W. Chan, Jim W. Barnett, Preston A. Baecker, Hela Bursztyn-Pettegrew, Binh T. Nguyen, Carol Ward
  • Patent number: 5272054
    Abstract: A method of assay for isotopically exchangeable analytes is disclosed. Analytes are labeled by enzymatic exchange of a hydrogen atom of the analyte and a deuterium or tritium atom. Preferably, analytes are labeled by reaction with an oxidant, a reducing agent which contains a deuterium or tritium atom, and an enzyme capable of catalyzing the reversible exchange of a hydrogen atom between the analyte, the oxidant, and the reducing agent. Kits for conveniently performing the assay methods are also disclosed.
    Type: Grant
    Filed: March 26, 1992
    Date of Patent: December 21, 1993
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Arthur C. Switchenko, Edwin F. Ullman