Abstract: 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.
Abstract: 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:
Grant
Filed:
May 11, 1990
Date of Patent:
October 20, 1992
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
David J. Litman, Thomas M. Li, Laura L. Buelteman, Emmy T. Wong
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; 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.
Abstract: 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:
Grant
Filed:
October 12, 1989
Date of Patent:
October 6, 1992
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Richard A. Runkel, Stephen A. Berry, Mahmood M. Ghani
Abstract: 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:
Grant
Filed:
April 1, 1991
Date of Patent:
September 8, 1992
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Thomas L. Tarnowski, Mae W. L. Hu, Maureen Laney, John S. Pease, Vartan Ghazarossian
Abstract: Aryl- and heterocyclic-methanamines are prepared by reacting a hydroxy-aryl carbinol or a heterocyclic carbinol with a primary or a secondary amine in the presence of a cationic effect reagent.
Abstract: 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:
Grant
Filed:
July 31, 1989
Date of Patent:
August 11, 1992
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Edwin F. Ullman, Pyare Khanna, Rohan Peries
Abstract: 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:
Grant
Filed:
December 1, 1988
Date of Patent:
August 4, 1992
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Thomas L. Tarnowski, Cheng-I Lin, Edwin F. Ullman
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:
December 23, 1988
Date of Patent:
August 4, 1992
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Mae Wan Leng Hu, Cheng-I Lin, Chen-jung Hsu, James V. Freeman, Marcel Pirio, Edwin F. Ullman
Abstract: 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:
Grant
Filed:
November 27, 1989
Date of Patent:
August 4, 1992
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Rajesh D. Patel, Nurith Kurn, Martin Becker, Edwin F. Ullman
Abstract: 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:
Grant
Filed:
December 3, 1991
Date of Patent:
August 4, 1992
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Lawrence E. Fisher, Joseph M. Muchowski, Edvige Galeazzi, Roberto P. Rosenkranz, Deborah L. McClelland
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 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.
Abstract: 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.
Abstract: 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.
Abstract: 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.
Abstract: 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:
Grant
Filed:
July 25, 1988
Date of Patent:
May 26, 1992
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Arthur C. Switchenko, Nurith Kurn, Christian Neukom, Marcel Pirio, Donald E. Berger, Jr., Edwin F. Ullman
Abstract: Stable, clear, antimicrobially effective, ophthalmic formulations include an ophthalmologically effective amount of a drug, especially a --COOH group-containing drug or a NSAID, and a preservative system formed of a quaternary ammonium preservative and a nonionic surfactant, all in an aqueous vehicle. These formulations are useful for treating diseases that are either caused by, associated with or accompanied by inflammatory processes, including, among others, glaucoma, cystoid macular edema, uveitis, diabetic retinopathy and conjunctivitis, or any trauma caused by eye surgery or eye injury.
Type:
Grant
Filed:
December 7, 1990
Date of Patent:
May 5, 1992
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Roger F. Cherng-Chyi, Deborah M. Lidgate
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 where W 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.
Abstract: Disclosed are devices and methods for interrupting capillary flow of a liquid between two pieces of bibulous material which, prior to actuation, are in a capillary flow relationship to each other. In particular, the capillary flow relationship of two pieces of bibulous material is interrupted by utilizing a liquid expandable piece of bibulous material.
Type:
Grant
Filed:
November 27, 1989
Date of Patent:
April 14, 1992
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Nurith Kurn, Rajesh D. Patel, Martin Becker, Edwin F. Ullman
Abstract: Carbonyl derivatives of acetaminophen are provided for use in homogeneous enzyme immunoassays for acetaminophen. The derivatives are conjugated to antigenic substances for the preparation of antisera specific to acetaminophen, and to enzymes for the preparation of enzyme conjugates which compete with acetaminophen for antibody binding sites in a typical assay.