Patents Assigned to Syntex (U.S.A.)
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Patent number: 5468647Abstract: A method is disclosed for conducting an assay for an analyte. The method comprises causing a specific binding pair member in a first aqueous medium to become bound to a first bibulous member by contacting a portion of the first bibulous member with the medium. The first bibulous member is in liquid receiving relationship with an absorbent member. The contacting is carried out under conditions wherein the first medium traverses the first bibulous member and at least a portion of the absorbent member by capillary action. The method further comprises causing the first bibulous member to come into liquid receiving relationship with a second bibulous member. A reagent in a second aqueous medium is absorbed by and preferably becomes non-diffusively bound to the second bibulous member in relation to the presence of analyte in the first medium.Type: GrantFiled: September 1, 1994Date of Patent: November 21, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Carl N. Skold, Armen B. Shanafelt, Vartan Ghazarossian, Edwin F. Ullman
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Patent number: 5466697Abstract: The disclosed 8-aryl-1,6-naphthyridin-5-ones, compounds of Formula I, ##STR1## wherein: R.sub.1 is hydrogen, alkyl, lower alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkyl lower alkyl, heterocycloalkyl lower alkyl, aralkyl or heteroaralkyl; andR.sub.2 is aryl; or a pharmaceutically acceptable salt or N-oxide thereof are useful as anti-inflammatory agents, immunosuppressive agents, anti-allograft rejection agents, anti-graft-vs-host disease agents, anti-allergic agents (e.g., asthma, rhinitis and atopic dermatitis), bronchodilation agents, anti-autoimmune agents or analgetic agents.Type: GrantFiled: July 13, 1994Date of Patent: November 14, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Robert S. Wilhelm, Bradley E. Loe
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Patent number: 5462875Abstract: An apparatus for maintaining a biological sample on a support is disclosed. The apparatus comprises a hollow chamber with internal and external surfaces and a first and second end. The first end is open and is adapted for attachment to a first closure member. The second end is either closed or open. If open, the second end is adapted for attachment to a second closure member. The apparatus provides for maintaining the support in contact with a liquid medium at all times regardless of the orientation of the apparatus. In a preferred embodiment, the apparatus provides for maintaining the original orientation of a non-integral support regardless of the orientation of the apparatus. The apparatus is useful for isolating and culturing microorganisms.Type: GrantFiled: October 11, 1994Date of Patent: October 31, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Stephen M. Barr, Paul A. Rohlf
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Patent number: 5455252Abstract: A compound of the formula ##STR1## wherein: R.sup.1 is independently selected from hydrogen, lower-alkyl, cycloalkyl, cycloalkyl lower-alkyl, lower-alkoxy, formyl, (lower-alkyl)-hydroxylmethyl, aryl, benzyl, arylmethyl, pyridylmethyl,where aryl, benzyl, arylmethyl and pyridylmethyl are unsubstituted or independently mono, di or tri substituted with hydrogen, hydroxy, thiol, amino, halo, nitro, lower-alkylthio, lower-alkoxy, mono-lower-alkylamino, di-lower-alkylamino, hydroxycarbonyl, lower-alkoxycarbonyl, hydroxysulfonyl, lower-alkoxysulfonyl, lower-alkylsulfonyl, lower-alkylsulfinyl, trifluoromethyl, cyano, tetrazoyl, carbamoyl, lower-alkylcarbamoyl, and di-lower-alkylcarbamoyl; andR.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as set forth in the specification.Type: GrantFiled: March 31, 1993Date of Patent: October 3, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Robert S. Wilhelm, Paul R. Fatheree, Ronnie L. Chin
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Patent number: 5455045Abstract: Mycophenolate mofetil and mycophenolic acid can be conveniently manufactured into high dose oral formulations by the hot melt filling of a supercooled mycophenolate mofetil or mycophenolic acid liquid into a pharmaceutical dosage form. High dose oral pharmaceutical formulations and manufacturing methods therefor are disclosed.Type: GrantFiled: May 13, 1993Date of Patent: October 3, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Glenn J. Samuels, Jung-Chung Lee, Charles Lee, Stephen Berry, Paul J. Jarosz
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Patent number: 5451517Abstract: A D-arabinitol dehydrogenase enzyme is disclosed. The enzyme is capable of catalyzing the oxidation of D-arabinitol and substantially incapable of catalyzing the oxidation of D-mannitol and is substantially free of other enzymes capable of oxidizing D-mannitol. Also disclosed are methods for determining D-arabinitol. In one embodiment the method comprises the steps of providing in combination (1) a medium suspected of containing D-arabinitol and (2) a D-arabinitol dehydrogenase enzyme and examining the medium for the product of the oxidation of the D-arabinitol. The enzyme utilized is capable of catalyzing the oxidation of D-arabinitol and substantially incapable of catalyzing the oxidation of D-mannitol. Kits for conducting the present method are also disclosed. The D-arabinitol dehydrogenase in purified form has all of the characteristics of a D-arabinitol dehydrogenase which is obtainable from Candida tropicalis ATCC 750 or Candida shehatae.Type: GrantFiled: March 3, 1995Date of Patent: September 19, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Charles G. Miyada, Arthur C. Switchenko, Melanie W. Quong, Man-Ying L. Wong
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Patent number: 5451507Abstract: 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: May 10, 1994Date of Patent: September 19, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Carl N. Skold, Armen B. Shanafelt, Vartan Ghazarossian, Edwin F. Ullman
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Patent number: 5449664Abstract: Nucleoside compounds of the formula ##STR1## wherein: B is a purine or a pyrimidine;X and X' are H, OH or F, provided that at least one is H;Y and Y' are H, OH, OCH.sub.3 or F, provided that at least one is H;Y' and Z together form a cyclic phosphate ester, provided that Y is H; orZ is ##STR2## where n is zero, one, two or three; and Z' is N.sub.3 or OCH.sub.3 ; provided that when X' and Y' are OH and Z' is N.sub.3, B is not cytosine, andwhen X' and Y' are OH and Z' is OCH.sub.3, B is not uracil, adenine or cytosine;and the pharmaceutically acceptable esters, ethers and salts thereof, have been found to have potent antiviral activity with a high therapeutic ratio.Type: GrantFiled: December 16, 1991Date of Patent: September 12, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Julien P. H. Verheyden, Hans Maag, Ernest J. Prisbe
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Patent number: 5447943Abstract: Compounds of the Formula: ##STR1## wherein: R.sup.1-7 are as defined in the specification. The compounds and salts exhibit useful pharmacological properties, including potassium channel activating properties and 5-lipoxygenase inhibiting properties, and in particular are useful as smooth muscle relaxants and bronchodilators.Type: GrantFiled: July 22, 1993Date of Patent: September 5, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Alistair W. Lochead, Michel J. Navet, Peter E. Hicks
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Patent number: 5446121Abstract: The present invention relates to processes for preparing 1-butyl-2-[2'-(2H-tetrazol-5-yl)biphenyl-4-ylmethyl]-1H-indole-3-carboxyli c acid and to intermediates useful in such processes. The present invention also relates to a process for deprotecting compounds containing a protected 2H-tetrazolyl group, which process comprises reacting a the protected compound with a Lewis acid in the presence of a thiol.Type: GrantFiled: January 17, 1995Date of Patent: August 29, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Robin D. Clark, Lawrence E. Fisher, Lee A. Flippin, Michael G. Martin, Stephen R. Stabler
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Patent number: 5446137Abstract: This invention relates to oligonucleotides having at least one nucleotide that is substituted at the 4' position of the sugar moiety with a substituent other than hydrogen. These oligonucleotides are useful in hybridization assays and as therapeutic agents.Type: GrantFiled: December 9, 1993Date of Patent: August 29, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Hans Maag, Samuel J. Rose, Beat Schmidt
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Patent number: 5445944Abstract: 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 fluorescer 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: GrantFiled: April 22, 1994Date of Patent: August 29, 1995Assignee: Syntex (U.S.A.) Inc.Inventor: Edwin F. Ullman
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Patent number: 5444072Abstract: The disclosed 6-substituted derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil.Type: GrantFiled: February 18, 1994Date of Patent: August 22, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: John W. Patterson, David Morgans, Jr., David B. Smith, Francisco X. Talamas, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fernandez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, Eric B. Sjogren, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
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Patent number: 5441953Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.Type: GrantFiled: September 23, 1994Date of Patent: August 15, 1995Assignee: Syntex (U.S.A.) Inc.Inventor: Eric B. Sjogren
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Patent number: 5439793Abstract: A method is disclosed for forming a single stranded polynucleotide having two segments that are non-contiguous and hybridizable with each other. The method comprises the step of providing in combination (1) a first polynucleotide sequence having a hydroxyl at its 3'-end, (2) a second polynucleotide sequence having a hydroxyl or phosphate group at its 5'-end, and (3) a ligase, wherein at least ten consecutive bases of one of the sequences can hybridize to the other of the sequences to form a duplex. The duplex is comprised of a non-hybridized single stranded portion of one of the polynucleotide sequences containing one of the ends and at least five bases. The combination is provided under conditions for forming the duplex and ligating the ends within the duplex. The method finds particular application in the detection of polynucleotide analytes.Type: GrantFiled: July 19, 1990Date of Patent: August 8, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Samuel Rose, Linda M. Western
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Patent number: 5437983Abstract: A method for carrying out a binding assay is described wherein a member of a specific binding pair (sbp) and a sample are combined with a matrix of non-porous beads in a liquid medium under conditions such that the beads bind to the sbp member. The liquid medium is removed from the beads by aspiration using an aspiration tube having one or more orifices each of a diameter smaller than the minimum diameter of the smallest bead thereby allowing removal of the liquid medium while prohibiting aspiration of the beads.Type: GrantFiled: February 1, 1993Date of Patent: August 1, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Richard P. Watts, Mary C. Ericson, Hrair Kirakossian, Chiu C. Chang
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Patent number: 5438150Abstract: The present invention relates to a process for preparing a 5-(N-substituted)aminomethyl-1-benzocycloalkyl-1,3-dihydroimidazole-2-thio ne (wherein the N-substituent is selected from formyl, aminocarbonyl, (C.sub.1-4)alkylcarbonyl or trifluoro (C.sub.1-4)alkylcarbonyl), which process comprises reacting a benzocycloalkylamine with thiocyanic acid and dihydroxyacetone to give a corresponding 5-hydroxymethyl-1-benzocycloalkyl-1,3-dihydroimidazole-2-thione and then reacting the 5-hydroxymethyl-1-benzocycloalkyl-1,3-dihydroimidazole-2-thione with a compound of the formula H.sub.2 NC(0)R.sup.2 in which R.sup.2 is hydrogen, amino, (C.sub.1-4)alkyl or trifluoro(C.sub.1-4)alkyl or with an ammonium salt of the formula NH.sub.4.sup.+ - OC(0)R.sup.3 in which R.sup.3 is hydrogen, (C.sub.1-4)alkyl or trifluoro(C.sub.1-4)alkyl.Type: GrantFiled: April 26, 1994Date of Patent: August 1, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Rekha P. Bansal, Owen W. Gooding, Alexander V. Muehldorf, Counde O-Yang
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Patent number: 5436264Abstract: The present invention relates to novel N-aryloxyalkyl tryptamine .alpha..sub.1 -adrenergic receptor antagonists of the formula I: ##STR1## in which n is 2, 3 or 4; q is 1, 2 or 3; t is 0, 1, 2 or 3; z is 0, 1, 2 or 3; each R.sup.1 and R.sup.2 are independently hydroxy, halogen, cyano, (C.sub.1-8)alkyl, (C.sub.1-8)alkyloxy or trifluoromethyl; and R.sup.2 is hydrogen, (C.sub.1-4)alkyl, fluoro(C.sub.1-4)alkyl, difluoro(C.sub.1-4)alkyl, trifluoro(C.sub.1-4)alkyl, (C.sub.1-4)alkyloxy(C.sub.1-4)alkyl, oxo(C.sub.1-4)alkyl, (C.sub.1-8)cycloalkyl, (C.sub.1-8)cycloalkylmethyl or allyl or phenyl(C.sub.1-4)alkyl or heterocyclo(C.sub.1-8)alkyl (optionally substituted with one to two substituents independently selected from (C.sub.1-4)alkyl, (C.sub.1-4)alkyloxy, trifluoromethyl and halogen); R.sup.3 and R.sup.4 are independently hydrogen, (C.sub.1-4)alkyl, (C.sub.1-8)cycloalkyl, (C.sub.1-8)cycloalkylmethyl or allyl; and R.sup.5 is hydrogen, (C.sub.1-4)alkyl, (C.sub.1-8)cycloalkyl, (C.sub.1-8)cycloalkylmethyl, allyl, (C.Type: GrantFiled: August 19, 1993Date of Patent: July 25, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Jurg R. Pfister, David E. Clarke
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Patent number: 5416214Abstract: 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: GrantFiled: March 29, 1994Date of Patent: May 16, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: John Pease, Thomas L. Tarnowski, Donald Berger, Chiu C. Chang, Chun-Hua Chuang
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Patent number: 5414011Abstract: Stable, clear, antimicrobially effective, ophthalmic formulations are disclosed which provide an antimicrobially effective preservative. The formulations include an ophthalmologically effective amount of a drug, which is a --COOH group-containing non-steroidal anti-inflammatory drug (NSAID) alone or in combination with an antibiotic drug, and a preservative system formed of a quaternary ammonium preservative and a nonionic polyoxyethylated octylphenol surfactant, all in an aqueous vehicle. The preservative system can be used with other formulations which require the preservative to be ophthamologically acceptable and antimicrobially effective. These formulations are useful for treating diseases and/or conditions 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: GrantFiled: March 28, 1989Date of Patent: May 9, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Cherng-Chyi R. Fu, Deborah M. Lidgate