Patents Assigned to Syntex (U.S.A.)
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Patent number: 5164405Abstract: There is disclosed a stable pharmaceutical composition containing nicardipine hydrochloride, a non-chloride isotonicity agent, a buffering agent and a pharmaceutically acceptable aqueous vehicle for parenteral administration.Type: GrantFiled: October 22, 1990Date of Patent: November 17, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Calum B. McFarlane, Alistair B. Selkirk, Michael J. Dey
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Patent number: 5164294Abstract: 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: GrantFiled: July 7, 1989Date of Patent: November 17, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Carl N. Skold, Armen B. Shanafelt, Vartan Ghazarossian, Edwin F. Ullman
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Patent number: 5158936Abstract: Thiol protease inhibitors are disclosed having the formula: ##STR1## or an optical isomer thereof, or a pharmaceutically acceptable salt thereof, wherein:n is 0 or 1;m is 0, 1 or 2;X is H or an N-protecting group;each Y is independently an optionally protected .alpha.-amino acid residue;R is an optionally protected .alpha.-amino acid side chain that is H or CH.sub.3 or that is bonded to the .alpha.-carbon atom to which it is attached by a methylene, methine or phenyl radial; andR' is optionally substituted aryl.Type: GrantFiled: May 15, 1991Date of Patent: October 27, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Alexander Krantz, Heinz W. Pauls, Roger A. Smith, Robin W. Spencer
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Patent number: 5158949Abstract: Compounds of formula (I): ##STR1## wherein n is 2 or 3;p is 0, 1 or 2;q is 0, 1 or 2;X is oxygen or S(O).sub.t where t is 0, 1 or 2;each R.sup.1 is independently halo, lower alkyl, lower alkoxy, or trifluoromethyl;each R.sup.2 is independently halo or lower alkyl;R.sup.3 is nitro or --N(R.sup.5)R.sup.6 whereR.sup.5 is hydrogen or lower alkyl;R.sup.6 is hydrogen lower alkyl, lower alkylsulfonyl or --C(Y)R.sup.7 where Y is oxygen or sulfur and R.sup.7 is hydrogen, lower alkyl, lower alkoxy or --N(R.sup.8)R.sup.9 where R.sup.8 is hydrogen or lower alkyl and R.sup.9 is hydrogen, lower alkyl or lower alkoxycarbonyl; orR.sup.5 and R.sup.6 together with N is pyrrolidino, piperidino, morpholino, thiomorpholino or piperazino, wherein the piperazino is optionally substituted at the 4-position by --N(O)R.sup.10 where R.sup.10 is hydrogen, lower alkyl, lower alkoxy or amino; andR.sup.Type: GrantFiled: December 20, 1990Date of Patent: October 27, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Keith A. Walker, Pamela M. Burton, David C. Swinney
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Patent number: 5156952Abstract: A method for determining the presence of a predetermined minimum detectible amount of one or more analytes in a sample suspected of containing the analyte is disclosed. Each analyte is a member of a specific binding pair ("sbp member") consisting of ligand and its complementary receptor. The method comprises contacting with a test solution containing said sample and predetermined amounts of two or more of a plurality of first sbp members, each respectively analogous to one of said analytes, a contact portion of a piece of bibulous material capable of being traversed in a least one direction by the test solution by capillary migration. The bibulous material contains predetermined amounts of two or more of a plurality of second sbp members, each respectively capable of binding one of the analytes and corresponding first sbp member.Type: GrantFiled: May 11, 1990Date of Patent: October 20, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: David J. Litman, Thomas M. Li, Laura L. Buelteman, Emmy T. Wong
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Patent number: 5157120Abstract: Nucleoside analogues having a ring-open structure, of general formula: ##STR1## where R and R' may be hydrogen, silyl groups, substituted alkyl groups, benzyl groups and the like, and X is an optionally substituted base such as guanine or adenine, have been shown to exhibit anti-viral and other biological activities at non-toxic levels.Type: GrantFiled: September 16, 1981Date of Patent: October 20, 1992Assignee: Syntex (U.S.A.) Inc.Inventor: Kelvin K. Ogilvie
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Patent number: 5156953Abstract: An assay method and compositions are provided for determining the presence of an analyte in a sample. The analyte is a member of an immunological pair (mip) comprising ligand and receptor. By providing a first measurement surface capable of specifically binding a labelled reagent in an amount depending upon the presence of analyte in the sample and a second calibration surface capable of binding a second labelled reagent in a manner unaffected by the presence of analyte in the sample, calibration of individual tests can be accomplished simultaneously with the performance of the test itself. A signal producing system includes an enzyme, a catalyst usually bonded to a mip which defines the first labeled reagent for binding to the measurement surface and the same catalyst conjugated to a ligand capable of binding to the calibration surface. Preferably, both labeled reagents have the same composition and the calibration surface includes anti-(first catalyst).Type: GrantFiled: April 4, 1989Date of Patent: October 20, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: David J. Litman, Edwin F. Ullman
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Patent number: 5155132Abstract: 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; and R.sup.6 and R.sup.7 are independently hydrogen, lower alkyl, cycloalkyl or optionally substituted phenyl.The compounds of this invention are also useful for the treatment of disease-states caused by lipoxygenase activity in mammals, particularly 5-lipoxygenase activity, when administered systemically.Type: GrantFiled: March 21, 1988Date of Patent: October 13, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Michael C. Venuti, John M. Young
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Patent number: 5152995Abstract: Acid-sensitive antibiotic esters for oral administration to livestock are stabilized by incorporation in premix formulations comprising a carrier, a base, a protective coating, and optionally a sealant film.Type: GrantFiled: October 12, 1989Date of Patent: October 6, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Richard A. Runkel, Stephen A. Berry, Mahmood M. Ghani
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Patent number: 5145774Abstract: The present invention describes a class of dyes for use in staining cell samples and methods of making such dyes. A preferred class of dyes known as detergent dyes which possess the ability to stain cells in whole blood and are only slowly leached or lost from the stained cells over time are described. The present invention has application, for example, to blood typing for the determination of the presence of blood group antigens A, B, AB, O, and D (Rh.sub.o) and antibodies to such antigens.Type: GrantFiled: April 1, 1991Date of Patent: September 8, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Thomas L. Tarnowski, Mae W. L. Hu, Maureen Laney, John S. Pease, Vartan Ghazarossian
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Patent number: 5137808Abstract: A device is disclosed for conducting an assay method. The device comprises a housing, means enclosed in the housing for capturing a member of a specific binding pair in a zone and for allowing liquid to be transported by capillary action away from the zone, one or more self-contained liquid reagents enclosed in the housing for conducting an assay method for the determination of an analyte in the sample, and means in the housing for introducing the sample into the device. Preferably, the self-contained reagents are liquid reagents which are contained in a breakable container. The device of the invention finds use in assay methods for the determination of an analyte in a sample suspected of containing the analyte. Kits for conducting an assay method are also disclosed.Type: GrantFiled: July 31, 1989Date of Patent: August 11, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Edwin F. Ullman, Pyare Khanna, Rohan Peries
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Patent number: 5136095Abstract: Compounds and methods are disclosed for reversibly aggregating particles suspended in a liquid medium. The method comprises combining the liquid medium containing the particles with a polyionic polymer capable of aggregating the particles under conditions suitable for such aggregation. Thereafter, the particles are contacted with a chemical reagent capable of cleaving the polyionic polymer under conditions sufficient to reverse the aggregation. Optionally, magnetic particles are added to the liquid medium in the present method under conditions for non-specific binding and the medium including the aggregates is subjected to a magnetic field gradient to separate the aggregates from the medium. The compounds of the present invention are polyions. The aggregation of the particles is reversible upon contact with chemical agents which cleave at least some of the bonds within the polyionic polymer.Type: GrantFiled: December 1, 1988Date of Patent: August 4, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Thomas L. Tarnowski, Cheng-I Lin, Edwin F. Ullman
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Patent number: 5135873Abstract: Disclosed are methods and devices for permitting capillary flow of liquid between two or more pieces of bibulous material which, prior to actuation, are in a non-capillary flow relationship. In particular, the device is actuated and a capillary flow relationship is initiated between the two or more pieces of bibulous material in non-capillary flow relationship by utilizing a liquid expandable piece of bibulous material.Type: GrantFiled: November 27, 1989Date of Patent: August 4, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Rajesh D. Patel, Nurith Kurn, Martin Becker, Edwin F. Ullman
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Patent number: 5135863Abstract: 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: GrantFiled: December 23, 1988Date of Patent: August 4, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Mae Wan Leng Hu, Cheng-I Lin, Chen-jung Hsu, James V. Freeman, Marcel Pirio, Edwin F. Ullman
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Patent number: 5135944Abstract: Compounds of Formula I ##STR1## in which: R.sub.1 is hydrogen, lower alkyl, --C(O)R.sub.3, or --C(O)NR.sub.3 R.sub.4, where R.sub.3 and R.sub.4 are independently lower alkyl, phenyl, or phenyl lower alkyl;R.sub.2 is hydrogen or lower alkyl; andX is --(CH.sub.2).sub.m -- where m is an integer of 1 to 10, or --(CH.sub.2).sub.n Y(CH.sub.2).sub.n -- where n is an integer of 1 to 3 and Y is oxygen or sulfur,their individual R,R-; R,S-; and S,S-stereoisomers, and racemic or non-racemic mixtures of stereoisomers, and their pharmaceutically acceptable salts are dopamine agonist compounds useful in the treatment of hypertension and congestive heart failure in mammals.Type: GrantFiled: December 3, 1991Date of Patent: August 4, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Lawrence E. Fisher, Joseph M. Muchowski, Edvige Galeazzi, Roberto P. Rosenkranz, Deborah L. McClelland
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Patent number: 5134161Abstract: 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 the same as R.sup.1, or 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;both X groups are the same and X is either --C(O)OR.sup.4 or --C(O)NR.sup.5 R.sup.6, whereinR.sup.4 is alkyl, phenyl or benzyl optionally substituted with one or two lower alkyl groups, lower alkoxy groups or halo; andR.sup.5 and R.sup.6 are independently hydrogen, lower alkyl, cycloalkyl or phenyl optionally substituted with one or two lower alkyl groups, lower alkoxy groups or halo.Type: GrantFiled: April 15, 1988Date of Patent: July 28, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Michael C. Venuti, John M. Young
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Patent number: 5130432Abstract: A process for preparing a cyclic amine of Formula I ##STR1## in which R.sup.1 is phenyl, optionally substituted by 1 to 3 lower alkoxy groups;R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen or lower alkyl; andn is 1 or 2,comprises(1) converting an aminoalcohol of Formula III ##STR2## to a dioxooxathiazolidine of Formula II ##STR3## in which R.sup.2, R.sup.3, R.sup.4 and n are as defined above; and (2) reacting the dioxooxathiazolidine of Formula II with an organometallic nucleophile, R.sup.1 M*, wherein R.sup.1 is as defined above, and hydrolyzing the resulting sulfamate salt.Type: GrantFiled: December 21, 1990Date of Patent: July 14, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Gary F. Cooper, Michael G. Martin
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Patent number: 5120135Abstract: The methods and apparatus disclosed herein allow for the controlling of the suspension of particles in a liquid medium. The method comprises intermittently magnetically causing at least a portion of a device immersed in the fluid medium (i) to rotate from a rest position about an approximately horizontal axis to a second position at an angle not greater than about 135 degrees from the rest position and (ii) to return to a rest position. The frequency of movement of the device is sufficient to control the suspension of particles in the medium. The method is particularly applicable to controlling a suspension of cells, for example, erythrocytes, in a liquid medium with a minimization of lysis.Type: GrantFiled: December 13, 1989Date of Patent: June 9, 1992Assignee: Syntex (U.S.A.) Inc.Inventor: Edwin F. Ullman
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Patent number: 5116817Abstract: The present invention relates to a novel nasal composition comprising a nona- or decapeptide having LHRH agonist or antagonist activity and a surfactant which is a bile acid or a pharmaceutically acceptable salt thereof in a buffered aqueous solution.Type: GrantFiled: September 20, 1990Date of Patent: May 26, 1992Assignee: Syntex (U.S.A.) Inc.Inventor: Shabbir T. Anik
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Patent number: 5116726Abstract: Compounds having detergent properties are disclosed. When a modifying reagent is brought into contact with these compounds, the detergent properties are decreased. These compounds are useful, for example, as solubilizing agents for microbial antigens and/or antibodies and for reversibly wetting hydrophobic surfaces. Accordingly, methods are disclosed for increasing the hydrophilic properties of a material, such as a microbial antigen and/or antibody, the methods generally comprising the steps of contacting the material with the compound having detergent properties and a modifiable group, and modifying the compound with a modifying reagent. Kits are also disclosed for use in accordance with this methodology.Type: GrantFiled: July 25, 1988Date of Patent: May 26, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Arthur C. Switchenko, Nurith Kurn, Christian Neukom, Marcel Pirio, Donald E. Berger, Jr., Edwin F. Ullman