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.
Abstract: Compound 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 21, 1990
Date of Patent:
March 31, 1992
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Lawrence E. Fisher, Joseph M. Muchowski, Edvige Galeazzi, Roberto P. Rosenkranz, Deborah L. McClelland
Abstract: Disclosed is a novel microscope slide. The slide of this invention is a plastic microscope slide which is optically opaque and substantially non-fluorescent. The slide of this invention has particular utility in epi-fluorescent microscopy.
Abstract: Dopamine agonist compounds disclosed are useful in treating hypertension and congestive heart failure in mammals. The compounds have the following general formula (I) ##STR1## wherein: X is nitrogen or CH;R is hydrogen or lower alkyl;R.sub.1, R'.sub.1, R.sub.2, R'.sub.2, R.sub.3, R'.sub.3, R.sub.4, R'.sub.4, R.sub.5 and R'.sub.5 are each independently hydrogen, ##STR2## respectively represent --(CH.sub.2).sub.n -- and (CH.sub.2).sub.m wherein n and m are each independently an integer of from 1 to 10 and pharmaceutically acceptable salts, S stereoisomers and racemic and non-racemic mixtures thereof.
Type:
Grant
Filed:
June 24, 1991
Date of Patent:
March 3, 1992
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Lawrence E. Fisher, Joan M. Caroon, Joseph M. Muchowski, 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 alkoxy, alkylthio, optionally substituted phenoxy or optionally substituted phenylthio;R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl;R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2, or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(0).sub.
Type:
Grant
Filed:
March 6, 1987
Date of Patent:
February 25, 1992
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Gordon H. Jones, Michael C. Venuti, John M. Young
Abstract: A dispensing unit for a ketorolac topical gel formulation is disclosed, wherein the dispensing unit comprises a ketorolac topical gel formulation and a gas-impermeable multi-layered container wherein the container is comprised of a polyolefin inner layer and a metal foil outer layer.
Type:
Grant
Filed:
July 23, 1990
Date of Patent:
February 25, 1992
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
John T. H. Ong, Jean S. Fujiki, Wei-Cheng Liaw
Abstract: Methods and compositions are provided for assays involving members of a specific binding pair ("sbp members") and members of a signal producing system ("sps members"). The signal producing system is capable of producing a detectible signal in relation to the presence or amount of an analyte in a sample suspected of containing the analyte. Exemplary of sps members are enzymes and enzyme substrates, which react with each other to produce a signal. The improvement of the present invention comprises temporarily delaying the production of the signal without subsequent reagent addition. The delay can be achieved by employing an inhibitor which can be an alternate substrate for the enzyme or a compound which reacts with the product of the enzyme and its substrate in an effective amount.
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 phenyl-lower-alkyl;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 selected from the group consisting of hydrogen, R.sup.4 and -C(O)W, whereinW is alkyl of one to seven carbon atoms, optionally substituted phenyl or optionally substituted benzyl; andR.sup.4 is lower alkyl or optionally substituted phenyl-lower-alkyl.
Abstract: Conjugates of salicylic acid and certain poly(amino acids), which are either antigenic or enzymes, are provided. Antibodies raised against the antigenic poly(amino acids) and the enzyme conjugates are used as reagents in immunoassays.
Abstract: 2-methyl-4-hexene- and 3-methyl-5-heptene-1,2-diol derivatives are disclosed together with methods for preparing such derivatives. Where the derivative is a 2-methyl-4-hexene- or 3-methyl-5-heptene-1,2-diol conjugated to a label, the conjugates are useful in immunoassays. Where the 2-methyl-4-hexene or 3-methyl-5-heptene-1,2-diol is conjugated to an immunogenic carrier, the conjugates may be employed as an immunogen for use in the preparation of antibodies. The label conjugate and the antibodies can be utilized in an immunoassay for the determination or detection of cyclosporin in a sample suspected of containing cyclosporin.
Type:
Grant
Filed:
September 4, 1987
Date of Patent:
February 18, 1992
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Dariush Davalian, Cheng-I Lin, Edwin F. Ullman
Abstract: A method and device for determining the presence of an analyte in a sample suspected of containing the analyte are disclosed. The method involves contracting a test solution containing the sample, an antibody for the analyte, and a conjugate of the analyte and a label with a contact portion of a strip of bibulous material capable of being traversed by the test solution through capillary action. The strip contains a first receptor capable of binding to the conjugate. The first receptor is non-diffusively bound to a situs on the strip separate from the contact portion of the strip. The strip further contains a second receptor capable of binding the antibody to the analyte between the situs and the contact portion. The second receptor is non-diffusively bound to the strip. At least a portion of the test solution is allowed to traverse the strip by capillary action and thereby contact the situs.
Abstract: A method and device for determining the presence of an analyte in a sample suspected of containing the analyte is disclosed. The method involves contacting a test solution containing the sample, an antibody for the analyte, and a conjugate of the analyte and a label with a contact portion of a piece of bibulous material capable of being traversed in at least one direction by the test solution through capillary action. The bibulous material contains a first receptor capable of binding to said conjugate. The first receptor is non-diffusively bound to a situs on the bibulous material separate from the contact portion. The bibulous material further contains a second receptor capable of binding the antibody to the analyte between the situs and the contact portion. The second receptor is non-diffusively bound to the bibulous material. At least a portion of the test solution is allowed to traverse the bibulous material by capillary action and thereby contact the situs.
Abstract: Carbostyril derivatives of Formula I: ##STR1## wherein: m is 0, 1, or 2;n is 0, 1, or 2;R.sup.1 is hydrogen or lower alkyl;R.sup.2 is hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy, aralkoxy, or acyloxy;R.sup.3 is hydrogen, halogen, lower alkyl, or lower alkoxy;R.sup.4 is hydrogen, hydroxy, lower alkyl, acyloxy, provided that when R.sup.4 is hydroxy or acyloxy, m and n are both 1;R.sup.5 is hydrogen or lower alkyl; andR.sup.6 is alkyl, hydroxyalkyl, alkoxyalkyl, or (dialkylamino)alkyl;and the pharmaceutically acceptable acid addition salts and N-oxides (at the carbostyril nitrogen) thereof, and compositions containing them, are useful in treating cardiovascular diseases, particularly arrhythmias. Methods of preparing intermediates, the compounds, their formulations and methods of treatment therewith are also disclosed.
Type:
Grant
Filed:
July 18, 1990
Date of Patent:
January 21, 1992
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Jean-Claude Pascal, Leslie Patmore, Jurg Pfister, Dominique Blondet, John M. Armstrong
Abstract: 5-Aroyl-2,3-dihydro-1H-pyrrolizine-1,1-dicarboxylates of the formula ##STR1## are prepared from 2-aroylpyrroles. Hydrolysis and mono-decarboxylation of these compounds affords ketorolac and related compounds.
Abstract: 5-Aroyl-2,3-dihydro-1H-pyrrolizine-1,1-dicarboxylates of the formula ##STR1## are prepared from 2-aroylpyrroles. Hydrolysis and mono-decarboxylation of these compounds affords ketorolac and related compounds.
Abstract: A method is disclosed for separating a substance from a liquid medium. The method comprises combining the liquid medium containing the substance with magnetic particles under conditions for non-specific chemical binding of the magnetic particles. Thereafter, the medium is subjected to a magnetic field gradient to separate the particles from the medium. The preferred non-specific binding is achieved as the result of charge interactions between the particles usually by means of a polyionic reagent. The method of the invention has particular application to the separation of cells and microorganisms from aqueous suspensions and also to the determination of an analyte in a sample suspected of containing the analyte. The analyte is a member of a specific binding pair (sbp). The sample is combined in an assay medium with magnetic particles and a sbp member complementary to the analyte.
Type:
Grant
Filed:
June 5, 1990
Date of Patent:
December 31, 1991
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Edwin F. Ullman, Vartan E. Ghazarossian, Nurith Kurn, Litai Weng
Abstract: A method for determining the presence of a specific binding member bound to first particles in a liquid medium is disclosed. The method comprises providing in combination (1) a liquid medium suspected of containing a specific binding member bound to first particles, (2) means for agglutinating the first particles in relation to the presence of the specific binding member, and (3) second particles having the same or a different specific binding member for said means for agglutinating bound thereto, thereby providing for said means to agglutinate the second particles. Agglutination of the first and second particles are separately detectible and distinguishable by spectroscopic measurement. The medium is incubated and agglutination of each of the particles is determined spectroscopically without separating the first and second particles.
Type:
Grant
Filed:
June 23, 1988
Date of Patent:
December 10, 1991
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
John Vorpahl, Vartan Ghazarossian, Edwin F. Ullman