Patents Represented by Attorney Carol J. Roth
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Patent number: 5187066Abstract: This invention is to a method for detecting an amphiphilic antigen in a biological sample suspected of containing the amphiphilic antigen, which method comprises providing in combination a hydrophilic solid support modified to have a hydrophobic surface and an assay medium suspected of containing an amphiphilic antigen, incubating the combination under conditions sufficient for the amphiphilic antigen to bind to the hydrophobic surface, and determining the presence or amount of the amphiphilic antigen bound to the hydrophobic surface.Type: GrantFiled: February 14, 1990Date of Patent: February 16, 1993Assignee: Syntex (U.S.A.) Inc.Inventors: Martin Becker, Nurith Kurn, Yen P. Liu, Rajesh D. Patel, Thomas M. Houts, John D. Olson
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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: 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: 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: 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: 5108999Abstract: 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.Type: GrantFiled: December 19, 1990Date of Patent: April 28, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: John W. Patterson, Bruce H. Devens
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Patent number: 5091182Abstract: 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: GrantFiled: July 23, 1990Date of Patent: February 25, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: John T. H. Ong, Jean S. Fujiki, Wei-Cheng Liaw
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Patent number: 5055451Abstract: 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 radical; andR' is optionally substituted aryl.Type: GrantFiled: December 7, 1987Date of Patent: October 8, 1991Assignee: Syntex Inc.Inventors: Alexander Krantz, Heinz W. Pauls, Roger A. Smith, Robin W. Spencer
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Patent number: 5041442Abstract: This invention is directed to compounds of formula (I): ##STR1## wherein R.sup.1 is thiocyano, --CH.sub.2 CN, --NH.sub.2, --NHR.sup.5, or --CH.sub.2 OR.sup.5 where R.sup.5 is lower alkyl;R.sup.2 is hydrogen, halo, lower alkyl, or lower alkylthio;R.sup.3 is hydrogen, halo, lower alkyl, lower alkylthio, or thiocyano;R.sup.4 is hydrogen, halo, lower alkyl, lower alkoxy, lower alkylthio, or lower alkylsulfonyl; andY is --O--CH.sub.2 --, --S--CH.sub.2 --, --CH.dbd.CH--, or --(CH.sub.2).sub.n -- where n is 0, 1, 2, 3 or 4;or a pharmaceutically acceptable salt thereof. These compounds are useful in treating mammals having disease-states characterized by excessive gastric acid secretion.Type: GrantFiled: July 31, 1990Date of Patent: August 20, 1991Assignee: Syntex (U.S.A.) Inc.Inventors: Ruth S. Romero, Fidencio Franco, Armando C. Castaneda, Joseph M. Muchowski
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Patent number: 5035891Abstract: A sustained release, reservoir-type subcutaneous implant device for the sustained administration to a subject of a biologically active compound comprises:an effective amount of a biologically active compound;an amount of a solid hydrophilic polymer sufficient to cause swelling of the device by osmotic pressure after implantation;an effective amount of a solubilizing agent; anda sufficient amount of a non-porous rate-controlling membrane which completely encapsulates said biologically active compound, wherein said rate-controlling membrane is permeable to said biologically active compound, but is impermeable to said solubilizing agent. This device is particularly advantageous for the administration of growth promoting compounds to livestock.Type: GrantFiled: August 24, 1989Date of Patent: July 30, 1991Assignee: Syntex (U.S.A.) Inc.Inventors: Richard A. Runkel, Jung-Chung Lee
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Patent number: 5034410Abstract: This invention is directed to a method for treating helminthiasis in an animal which method comprises administering to an animal in need thereof an anthelmintically effective amount of a compound of the Formula (I): ##STR1## wherein Z is oxygen or sulfur;R.sup.1 is hydrogen or lower alkyl; andR.sup.2, R.sup.3, R.sup.4 and R.sup.5 are independently hydrogen, halo, lower haloalkyl, lower alkoxy, lower haloalkoxy, nitro, cyano, halophenoxy, haloalkylphenoxy, thiocyano or isothiocyano, provided that R.sup.2 and R.sup.3 cannot simultaneously be hydrogen and that R.sup.4 and R.sup.5 cannot simultaneously be hydrogen; or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions formulated therewith. This invention is also directed to novel anthelmintically active benzenepropanamides of Formula (I) wherein Z is oxygen.Type: GrantFiled: October 11, 1989Date of Patent: July 23, 1991Assignee: Syntex (U.S.A.) Inc.Inventors: Eric B. Sjogren, Michael A. Rider
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Patent number: 5001124Abstract: 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.Type: GrantFiled: February 2, 1990Date of Patent: March 19, 1991Assignee: Syntex (U.S.A.) Inc.Inventors: John W. Patterson, Bruce H. Devens
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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: 4951684Abstract: A device for collecting biological material is disclosed. The device comprises a shaft with a loop-like collection structure at one end. The collection structure provides a non-cutting, scraping edge to allow collection of the material without cutting. In a preferred embodiment, the collection means retains the material by diverting it into the interior portion of the collection means. The biological material is released from the device by rotation of the shaft or by elution in an appropriate solvent.Type: GrantFiled: March 20, 1989Date of Patent: August 28, 1990Assignee: Syntex (U.S.A.) Inc.Inventor: William A. McMillan
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Patent number: 4946845Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are the same and are lower alkoxy or optionally substituted phenoxy,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(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and m is 1 and n is 0, 1 or 2;at least one of X or Y is C(O)W and the other X or Y is different and is hydrogen, C(O)W or R.sup.Type: GrantFiled: November 25, 1988Date of Patent: August 7, 1990Assignee: Syntex (U.S.A.) Inc.Inventors: D. V. Krishna Murthy, Michael C. Venuti, John M. Young
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Patent number: 4933179Abstract: A vaccine for immunizing animals against Feline Leukemia Virus (FeLV) infections contains an FeLV antigen emulsified with a polyoxypropylene-polyoxyethylene block polymer, a glycol ether-based surfactant, an immunopotentiating amount of an immunostimulating glycopeptide, and, optionally, a metabolizable non-toxic oil.Type: GrantFiled: February 21, 1985Date of Patent: June 12, 1990Assignee: Syntex (U.S.A.) Inc.Inventors: Anthony C. Allison, Noelene E. Byars
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Patent number: 4889866Abstract: Novel arylsulfonyl-dihydropyridine derivatives which are useful as calcium entry-blocker cardiovascular agents have the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is hydrogen, lower alkyl, or lower alkoxyalkyl;R.sup.2 is hydrogen or chloro; andR.sup.3 is hydrogen, lower alkyl, or lower alkoxyethyl.A novel process using chiral sulfoxide reagents efficiently produces single isomers of these and other sulfonyl dihydropyridines.Type: GrantFiled: June 11, 1987Date of Patent: December 26, 1989Assignee: Syntex (U.S.A.) Inc.Inventors: Jurg R. Pfister, Roman Davis, Chi-Ho Lee
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Patent number: 4857318Abstract: A vaccine derived from Bordetalla bronchiseptica effective against Bordetella pertussis infection is disclosed herein.Type: GrantFiled: March 25, 1985Date of Patent: August 15, 1989Assignee: Syntex (U.S.A.) Inc.Inventor: Simon W. Lee
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Patent number: 4840965Abstract: Naphthalenes of the formula: ##STR1## wherein: m is 1 or 2;n is 1, 2, or 3;R.sup.1 is alkyl of one to seven carbon atoms or an optionally substituted phenyl;R.sup.2 is hydrogen, lower alkyl, lower alkoxy, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl, optionally substituted phenyl-lower-alkoxy, amino, lower alkylamino, lower dialkylamino, halo, cyano, hydroxy, or lower alkylthio are useful in relieving psoriasis.Type: GrantFiled: July 7, 1987Date of Patent: June 20, 1989Assignee: Syntex (U.S.A.) Inc.Inventors: Gordon H. Jones, Michael C. Venuti, John M. Young
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Patent number: 4792556Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are the same and are lower alkoxy or optionally substituted phenoxy,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(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and m is 1 and n is 0, 1 or 2;at least one of X or Y is C(O)W and the other X or Y is different and is hydrogen, C(O)W or R.sup.Type: GrantFiled: April 28, 1986Date of Patent: December 20, 1988Assignee: Syntex (U.S.A.) Inc.Inventors: D. V. K. Murthy, Michael C. Venuti, John M. Young