Patents Assigned to Syntex (U.S.A.)
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Patent number: 4999285Abstract: A chromatographic device is disclosed. The device comprises in combination a housing, a strip of bibulous material non-removably confined in the housing. The strip has a length and width only slightly less than the length and width of the inner walls of the housing. The inner walls of the housing have means attached thereto for supportively confining the strip in the housing. The strip is confined so that (1) the front and back of the strip are essentially free from contact with the walls of the housing and (2) the capillary action of the strip remains substantially unchanged, and (3), where the strip is paper, the strip is allowed to expand as it is traversed by the liquid medium. The bottom end of the housing contains means for enabling contact of a portion of the strip with the liquid medium. The housing further contains means for visually observing the strip and can also contain indicating means cooperative therewith to assist in determining the result of a chromatographic test.Type: GrantFiled: November 15, 1984Date of Patent: March 12, 1991Assignee: Syntex (U.S.A.) Inc.Inventor: S. Nicholas Stiso
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Patent number: 4997846Abstract: Compounds of the formula ##STR1## wherein: R.sub.1 is cyano or nitro;R.sub.2 and R.sub.3 are independently hydrogen or lower alkyl; andR.sub.4 is alkyl; alkenyl; optionally substituted phenyl or phenyl lower alkyl; --(CH.sub.2).sub.m OR.sub.2 or --(CH.sub.2).sub.m N(R.sub.2).sub.2 ; wherein m is an integer of 1-5 and R.sub.2 is as defined above;or a pharmaceutically acceptable ester thereof; are smooth muscle relaxants, particularly useful in the treatment of hypertension.Type: GrantFiled: December 9, 1988Date of Patent: March 5, 1991Assignee: Researche Syntex France, S.A.Inventors: Gilles Genain, Henri Pinhas
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Patent number: 4997823Abstract: Infection associated with parenteral injections of parenterally suitable compounds, especially of F.sub.2.alpha. prostaglandins, is prevented by novel compositions comprising such compounds, a locally effective amount of an antibiotic, and a pharmaceutically acceptable carrier.Type: GrantFiled: July 20, 1987Date of Patent: March 5, 1991Assignee: Syntex (U.S.A.) Inc.Inventor: Richard C. Herschler
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Patent number: 4997945Abstract: The carbamate salt of 2-(2'-thienyl)-alkylamines and particularly the ethylamine and its method of synthesis are disclosed. The carbamate salt of 2-(2'-thienyl)ethylamine is a stable, easily transportable crystalline material that can be converted to 2-(2'-thienyl)ethylamine, a useful intermediate in the synthesis of 5[(2-chlorophenyl)methyl]-4,5,6,7-tetrahydrothieno-[3,2-c]pyridine hydrochloride, also known as ticlopidine hydrochloride. The synthesis is carried out by reacting an amine of formula (I): ##STR1## with CO.sub.Type: GrantFiled: January 25, 1990Date of Patent: March 5, 1991Assignee: Syntex (U.S.A.) Inc.Inventor: Hiralal N. Khatri
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Patent number: 4994368Abstract: A method is disclosed 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: GrantFiled: July 23, 1987Date of Patent: February 19, 1991Assignee: Syntex (U.S.A.) Inc.Inventors: Thomas C. Goodman, Martin Becker, Edwin F. Ullman, Samuel Rose
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Patent number: 4992467Abstract: The compounds and pharmaceutical compositions of Formula A, wherein Z is hydrogen or --C(O)R, Y is hydrogen or morpholinoethyl, and where R is lower alkyl or aryl, and the pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, particularly for treatment of allograft rejection, especially including cardiac allograft rejection, pancreatic allograft rejection and renal allograft rejection, and for treating autoimmune diabetes.Type: GrantFiled: March 28, 1990Date of Patent: February 12, 1991Assignee: Syntex (U.S.A.) Inc.Inventors: Anthony C. Allison, Elsie M. Eugui, Peter H. Nelson, Chee-Liang L. Gu, William A. Lee
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Patent number: 4988822Abstract: 5-Aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1,1-dicarboxylates of the formula ##STR1## are prepared from 2-halopyrroles. Hydrolysis and .beta.-decarboxylation of these compounds affords ketorolac and related compounds.Type: GrantFiled: July 27, 1989Date of Patent: January 29, 1991Assignee: Syntex (U.S.A.) Inc.Inventors: Joseph M. Muchowski, Robert Greenhouse
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Patent number: 4983627Abstract: Compounds useful in treating or preventing gastrointestinal ulcers and 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--, trans --CH.dbd.CHCH.sub.2 -- or --CH.sub.2 CH.sub.2 --;X is lower alkyl of 1-6 carbon atoms;Y is hydrogen, exo-(lower alkyl) or endo-(lower alkyl);n is an integer from 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 trans --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.2 O-phenyl; in which each phenyl may be optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen.Type: GrantFiled: November 10, 1988Date of Patent: January 8, 1991Assignee: Syntex (U.S.A.) Inc.Inventors: Counde O'Yang, Walter Kurz, Keith A. M. Walker, Helen Y. Wu
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Patent number: 4983595Abstract: A non-stinging aqueous anti-inflammatory steroid formulation suitable for intranasal administration comprises: an anti-inflammatory steroid in an amount between about 0.01% and about 0.05% (w/v); propylene glycol in an amount between about 2% and about 10% (w/v); PEG 400 in an amount between about 10% and about 25% (w/v); polysorbate 20 in an amount between about 1% and about 4% (w/v); an effective amount of a preservative; an effective amount of a stabilizer; an effective amount of an antioxidant; water; and pH buffering agent sufficient to adjust the pH of the resulting solution to between about 3.5 and about 7.Type: GrantFiled: September 20, 1988Date of Patent: January 8, 1991Assignee: Syntex (U.S.A.) Inc.Inventors: Eric Benjamin, Shabbir Anik, Ya-Yun T. Lin
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Patent number: 4981786Abstract: A device is disclosed for conducting an assay. The device comprises a housing, means enclosed in the housing for capturing a first member of a specific binding pair (sbp) in a zone and for allowing liquid to be transported by capillary action away from the zone, first means in the housing for introducing the sample into the device, and second means in the housing other than the first means for introducing a liquid reagent other than the sample into the device. 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 are also disclosed.Type: GrantFiled: September 4, 1987Date of Patent: January 1, 1991Assignee: Syntex (U.S.A.) Inc.Inventors: Geoffrey A. Dafforn, Nurith Kurn, Martin Becker, Edwin F. Ullman
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Patent number: 4975248Abstract: Serum is passed through a column containing silica gel alkylated with lower alkyl groups. The column is then washed with dilute acid and water and the digoxin eluted with aqueous methanol at a volume less than about the volume of the serum to provide a digoxin concentrate that may be used in assay determinations. The invention also includes a kit comprising in a packaged combination for use in an assay for digoxin (a) a column containing silica gel alkylated with alkyl groups containing 1 to 2 carbon atoms and (b) an aqueous eluent solution which is 50%-70% by volume organic solvent. The organic solvent comprises from 1-4 carbon atoms and from 1-3 heteroatoms selected from the group consisting of oxygen and nitrogen.Type: GrantFiled: October 16, 1986Date of Patent: December 4, 1990Assignee: Syntex (U.S.A.) Inc.Inventors: Pyare Khanna, Roberta D. Ernst, Anne J. Stone
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Patent number: 4973591Abstract: A pharmaceutical formulation suitable for parenteral (preferably intravenous) adminstration includes an effective amount of 1-diphenylmethyl-4-[(2-(4-methylphenyl)-5-methyl-1H-imidazol-4-yl)methyl]p iperazine and a suitable amount of an acid to generate a pharmaceutically acceptable salt having a pH above about 3.0 and a solubility above about 4.0 mg/ml. The intravenous formulation optionally includes a suitable tonicifier in a quantity sufficient to achieve isotonicity with body fluids. The salt is formed in situ during the formulation process. The slat of tartaric acid is preferred; suitable salts for lower concentration dosages are the citric acid and methane sulphonic acid salts.Type: GrantFiled: October 21, 1988Date of Patent: November 27, 1990Assignee: Syntex Pharmaceuticals, Ltd.Inventors: Alastair B. Selkirk, Michael J. Dey
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Patent number: 4970297Abstract: This invention is directed to compounds of the formula: ##STR1## or an optical isomer thereof, or a pharmaceutically acceptable salt thereof, wherein:n is 0, 1 or 2;p and q are independently 0, 1 or 2 and the sum of (p+q) is less than or equal to 3;X is selected from the group consisting of: halo; --OR.sup.2, --SR.sup.2, --S(O)R.sup.2, --S(O).sub.2 R.sup.2, and --S(O).sub.2 NHR.sup.2, wherein R.sup.2 is lower alkyl, mono-, di- or tri-fluoro alkyl of 2 or 3 carbon atoms, optionally substituted aryl;R is H or an N-protecting group;R.sup.1 is alkylthio, arylthio, amino, alkylamino, optionally substituted arylamino, or optionally substituted aralkylamino; and when the sum of n+p+q is greater than or equal to one, R.sup.1 is also hydroxy, alkoxy, or aralkoxy; andeach (aa) is independently an .alpha.-amino acid residue with an optionally protected amino acid side chain.Type: GrantFiled: March 13, 1987Date of Patent: November 13, 1990Assignee: Syntex (U.S.A.) Inc.Inventors: Arlindo L. Castelhano, Diana H. Pliura, Michael C. Venuti
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Patent number: 4963468Abstract: 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.Type: GrantFiled: February 12, 1987Date of Patent: October 16, 1990Assignee: Syntex (U.S.A.) Inc.Inventor: John D. Olson
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Patent number: 4962091Abstract: An active agent delivery system for the controlled administration of macromolecular polypeptides which comprises a micro-suspension of water-soluble components in a polylactide matrix.Type: GrantFiled: May 23, 1986Date of Patent: October 9, 1990Assignee: Syntex (U.S.A.) Inc.Inventors: Deborah A. Eppstein, Brian B. Schryver
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Patent number: 4960891Abstract: The invention provides a process for preparing compounds, as a single enantiomer or mixture of enantiomers, represented by the formula: ##STR1## in which: X and Y are independently hydrogen, hydroxy, lower alkyl, lower alkoxy or halo, or X and Y taken together is methylenedioxy or ethylene-1,2-dioxy, andZ is --SO.sub.2 R or --C(O)NR.sup.3 R.sup.4, in which;R is lower alkyl, optionally substituted phenyl, --(CH.sub.2).sub.m OR.sup.1 or --NR.sup.1 R.sup.2 wherein m is an integer of 1 to 6 and R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl; andR.sup.3 and R.sup.4 are independently hydrogen, alkyl, optionally substituted phenyl or phenyl lower alkyl; orR.sup.1 and R.sup.2 taken together with the nitrogen to which they are attached or R.sup.3 and R.sup.4 taken together with the nitrogen to which they are attached represent a heterocycle of the formula: ##STR2## wherein A is --CH.sub.2 --, --NR.sup.1 -- or oxygen; and novel intermediates.Type: GrantFiled: April 11, 1989Date of Patent: October 2, 1990Assignee: Syntex (U.S.A.) Inc.Inventor: Robin D. Clark
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Patent number: 4959307Abstract: A method and device for determining the presence of an analyte in a sample suspected of containing the analyte are 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 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.Type: GrantFiled: September 5, 1986Date of Patent: September 25, 1990Assignee: Syntex (U.S.A.) Inc.Inventor: John D. Olson
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Patent number: 4959217Abstract: This invention concerns novel, delayed/sustained release devices and compositions, including methods of their manufacture and use. The compositions include macromolecules, particularly polypeptide pharmaceuticals, and an initially partially-hydrated, non-biodegradable, hydrogel rate-limiting membrane.Type: GrantFiled: May 22, 1986Date of Patent: September 25, 1990Assignee: Syntex (U.S.A.) Inc.Inventors: Lynda M. Sanders, Abraham Domb
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Patent number: 4959303Abstract: Methods are disclosed for detecting an antigen in a biological sample. The methods involve providing in combination a solid support, which is substantially free of specific binding proteins, and a medium comprising an antigen from the sample and an antibody for the antigen. The combination is incubated under conditions sufficient for the antibody when bound to the antigen to bind to the support. The presence or amount of antibody on the support or in the medium is determined and is related to the presence of antigen in the sample. The methods have particular application to the detection of gram-negative bacteria.Type: GrantFiled: December 21, 1987Date of Patent: September 25, 1990Assignee: Syntex (U.S.A.) Inc.Inventors: Gary L. Milburn, Judith Rabbie, Thomas M. Houts
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Patent number: 4959387Abstract: 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, 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: GrantFiled: November 24, 1987Date of Patent: September 25, 1990Assignee: Syntex (U.S.A.) Inc.Inventors: Peter H. Nelson, Anthony C. Allison, Elsie M. Eugui, Joseph M. Muchowski