Patents Represented by Attorney Paul E. Dupont

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  • Antiarrhythmic diarylamidines
    Patent number: 5286752
    Abstract: Novel diarylamidines, and compositions and methods for treating cardiac arrhythmias in mammals utilizing the novel and related known diarylamidines of formula I, II, III and IV ##STR1##
    Type: Grant
    Filed: September 10, 1991
    Date of Patent: February 15, 1994
    Assignee: Sterling Winthrop Inc.
    Inventors: Robert E. Johnson, Thomas E. D'Ambra
  • 2,5-benzodiazocine antiarrhythmic agents
    Patent number: 5268372
    Abstract: Novel 2,5-benzodiazocines of formulas II and IV, pharmaceutical compositions containing them, processes for preparing them and methods of treating cardiac arrhythmias in mammals utilizing them.
    Type: Grant
    Filed: February 17, 1993
    Date of Patent: December 7, 1993
    Assignee: Sterling Winthrop Inc.
    Inventor: Robert E. Johnson
  • 2-saccharinylmethyl aryl carboxylate
    Patent number: 5250696
    Abstract: 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl aryl carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with an arylcarboxylic acid in the presence of an acid-acceptor.
    Type: Grant
    Filed: March 30, 1992
    Date of Patent: October 5, 1993
    Assignee: Sterling Winthrop Inc.
    Inventors: Richard P. Dunlap, Neil W. Boaz, Albert J. Mura, Virendra Kumar, Chakrapani Subramanyam, Ranjit C. Desai, Dennis J. Hlasta, Manohar T. Saindane, Malcolm R. Bell, John J. Court
  • Tetrazolyl-(phenoxy and phenoxyalkyl)-piperidinylpyridazines as antiviral agents
    Patent number: 5242924
    Abstract: Compounds of the formula ##STR1## wherein: Y is a bond, or C.sub.1 -C.sub.6 alkylene;R.sub.1 is hydrogen or C.sub.1 -C.sub.3 lower-alkyl;R.sub.2 and R.sub.3 are each independently hydrogen, C.sub.1 -C.sub.3 lower-alkyl or halogen;R.sub.4 is hydrogen or C.sub.1 -C.sub.3 lower-alkyl;or pharmaceutically acceptable acid addition salts thereof are useful as antiviral agents, particularly against picornaviruses.
    Type: Grant
    Filed: July 2, 1992
    Date of Patent: September 7, 1993
    Assignee: Sterling Winthrop Inc.
    Inventor: Guy D. Diana
  • Substituted 2-azabicyclo[2.2.2]octane derivatives and compositions and method of use thereof
    Patent number: 5240935
    Abstract: Novel substituted 2-azabicyclo[2.2.2]octane derivatives, pharmaceutical compositions containing them, methods for treating central nervous system disorders utilizing them, and processes for synthesizing them.
    Type: Grant
    Filed: November 20, 1992
    Date of Patent: August 31, 1993
    Assignee: Sterling Winthrop Inc.
    Inventors: Diane L. DeHaven-Hudkins, John P. Mallamo, William F. Michne, Martha R. Heimann
  • Phenylcyclohexanol derivatives as agents for treating CNS disorders
    Patent number: 5239110
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is lower-alkanoyl or hydrogen;R.sub.2 and R.sub.3 are the same or different lower-alkyl; or pharmaceutically acceptable acid-addition salts thereof are useful in the treatment of disorders of the central nervous system.
    Type: Grant
    Filed: December 30, 1992
    Date of Patent: August 24, 1993
    Assignee: Sterling Winthrop, Inc.
    Inventors: John P. Mallamo, William F. Michne, Aram Mooradian
  • Saccharin derivatives useful as proteolytic enzyme inhibitors and compositions and method of use thereof
    Patent number: 5236917
    Abstract: Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula ##STR1## wherein: L is --O--, --S--, --SO-- or --SO.sub.2 --;m and n are each independently 0 or 1;R.sub.1 is halo, lower-alkanoyl, 1-oxophenalenyl, phenyl or substituted phenyl, heterocyclyl or substituted heterocyclyl or, when L is --O-- and n is 1, cycloheptatrienon-2-yl or, when L is --S-- and n is 1, cyano or lower-alkoxythiocarbonyl or, when L is --SO.sub.2 -- and n is 1, lower-alkyl or trifluoromethyl;R.sub.2 is hydrogen, lower-alkoxycarbonyl, phenyl or phenylthio; andR.sub.3 and R.sub.4 are each hydrogen or various substituents and processes for preparation and pharmaceutical compositions and method of use thereof are disclosed.
    Type: Grant
    Filed: November 15, 1991
    Date of Patent: August 17, 1993
    Assignee: Sterling Winthrop Inc.
    Inventors: Richard P. Dunlap, Neil W. Boaz, Albert J. Mura, Dennis J. Hlasta, Ranjit C. Desai, Chakrapani Subramanyam, Lee H. Latimer, Eric P. Lodge
  • Low solubility drug-coated bead compositions
    Patent number: 5223268
    Abstract: Low solubility drug coated bead compositions, capsules filled therewith and method of preparation thereof, especially wherein the low solubility drug is an antiandrogenic steroid and most especially wherein the antiandrogenic steroid is (5.alpha.,17.alpha.)1'-(methylsulfonyl)-1'H-pregn-20-yno[3,2-c]pyrazol-17- ol, are disclosed.
    Type: Grant
    Filed: May 16, 1991
    Date of Patent: June 29, 1993
    Assignee: Sterling Drug, Inc.
    Inventors: Gregg Stetsko, Kuei-Tu Chang
  • Oral sustained-release drug compositions
    Patent number: 5213811
    Abstract: Sugar or sugar/starch beads coated with a first coating of a drug, for example 1,2-dihydro-6-(lower alkyl)-2-oxo-5-(4-pyridinyl)-nicotinonitrile (milrinone), hydroxypropyl methylcellulose or hydroxypropyl cellulose and a plasticizer selected from triacetin, diacetylated monoglycerides, glycerin, propylene glycol, polyethylene glycol, diethyl phthalate and triethyl citrate or a mixture of two or more thereof and a second coating of high-viscosity ethylcellulose, low-viscosity ethylcellulose, hydroxypropyl cellulose, polyvinyl acetate phthalate and a plasticizer selected from diacetylated monoglycerides and triacetin or a mixture thereof and optionally coated with additional first coating and capsules filled therewith and method of preparation thereof are disclosed.
    Type: Grant
    Filed: September 13, 1991
    Date of Patent: May 25, 1993
    Assignee: Sterling Drug Inc.
    Inventors: Steven E. Frisbee, Gregg Stetsko, Margaret A. Lawton
  • Selenomerocyanines and processes for preparation and methods of use and compositions thereof
    Patent number: 5208336
    Abstract: Selenomerocyanines, for example the compound having the structural formula ##STR1## a process for preparation thereof, methods of use thereof as photosensitizers for generation of singlet oxygen, virus inactivation and cancer cell inactivation, and photosensitized silver halide photographic emulsions containing them are disclosed.
    Type: Grant
    Filed: October 19, 1990
    Date of Patent: May 4, 1993
    Assignee: Sterling Drug Inc.
    Inventors: Wolfgang H. H. Gunther, Roger Searle
  • 2,5-benzodiazocine antiarrhythmic agents
    Patent number: 5206231
    Abstract: Novel 2,5-benzodiazocines of formulas II and IV, pharmaceutical compositions containing them, processes for preparing them and methods of treating cardiac arrhythmias in mammals utilizing them.
    Type: Grant
    Filed: September 10, 1991
    Date of Patent: April 27, 1993
    Assignee: Sterling Drug Inc.
    Inventor: Robert E. Johnson
  • 2-saccharinylmethyl and 4,5,6,7-tetrahydro-2-saccharinylmethyl phosphates, phosphonates and phosphinates useful as proteolytic enzyme inhibitors and compositions and method of use thereof
    Patent number: 5187173
    Abstract: 4-R.sub.1 -R.sub.2 -R.sub.3 -2-Saccharinylmethyl, 4-R.sub.4 -4-R.sub.5 -6-R.sub.6 -4,5,6,7-tetrahydro-2-saccharinylmethyl and 4,7-C-4,5,6,7-tetrahydro-2-saccharinylmethyl phosphates, phosphonates and phosphinates of formulas I, II and IIA respectively herein, useful in the treatment of degenerative diseases, and compositions containing them, methods for using them to treat degenerative diseases, and processes for their preparation by reaction of the corresponding 2-halomethylsaccharins with a phosphate, phosphonate or phosphinic acid of formula III herein in the presence of an acid-acceptor.
    Type: Grant
    Filed: December 27, 1991
    Date of Patent: February 16, 1993
    Assignee: Sterling Winthrop Inc.
    Inventors: Ranjit C. Desai, John J. Court, Dennis J. Hlasta, Chakrapani Subramanyam
  • 1,2,4-oxadiazolyl-phenoxyalkylisoxazoles and their use as antiviral agents
    Patent number: 5175177
    Abstract: Compounds of the formula ##STR1## wherein: Y is alkylene of 3 to 9 carbon atoms;R.sub.1 is lower-alkyl, lower-alkoxy-(C.sub.1-3 -alkyl), lower-alkoxycarbonyl, cyclopropyl or trifluoromethyl;R.sub.2 and R.sub.3 independently are hydrogen, lower-alkyl, halogen, lower-alkoxy, nitro, trifluoromethyl or hydroxy; andR.sub.4 is hydrogen or lower-alkyl; where lower-alkyl and lower-alkoxy, each occurrence, have from 1-5 carbon atoms;with the proviso that when R.sub.1 is lower-alkyl, at least one of R.sub.2 and R.sub.3 is hydroxy; or pharmaceutically acceptable acid-addition salts thereof are useful as antiviral agents, particularly against picornaviruses, including numerous strains of rhinovirus.
    Type: Grant
    Filed: July 17, 1991
    Date of Patent: December 29, 1992
    Assignee: Sterling Drug Inc.
    Inventors: Guy D. Diana, Thomas R. Bailey
  • Win 49596-finasteride method of use and compositions
    Patent number: 5175155
    Abstract: The method of use of a combination of the antiandrogen (5.alpha.,17.alpha.)-1'-(methylsulfonyl)-1'H-pregn-20-yno[3,2-c]pyrazol-17 -ol (Win 49596) and the 5.alpha.-reductase inhibitor (5.alpha.,17.beta.)-N-(1,1-dimethylethyl)-3-oxo-4-azaandrost-1-ene-17-carb oxamide (finasteride) for treating prostate disease in a male mammal and pharmaceutical compositions thereof are disclosed.
    Type: Grant
    Filed: October 7, 1991
    Date of Patent: December 29, 1992
    Assignee: Sterling Winthrop Inc.
    Inventors: Paul E. Juniewicz, Bruce M. Berger
  • 1,2,4-oxadiazolyl-phenoxyalkylisoxazoles and their use as antiviral agents
    Patent number: 5175178
    Abstract: Compounds of the formulas ##STR1## wherein: Y is an alkylene bridge of 3-9 carbon atoms;R' is lower-alkyl or hydroxy-lower-alkyl of 1-5 carbon atoms;R.sub.1 and R.sub.2 are hydrogen, halogen, lower-alkyl, lower-alkoxy, nitro, lower-alkoxycarbonyl or trifluoromethyl; andR.sub.8 is hydrogen or lower-alkyl of 1-5 carbon atoms, with the proviso that when R.sub.8 is hydrogen R' is hydroxy-lower-alkyl,are useful as antiviral agents, particularly against picornaviruses, including numerous strains of rhinovirus.
    Type: Grant
    Filed: June 4, 1990
    Date of Patent: December 29, 1992
    Assignee: Sterling Drug Inc.
    Inventors: Guy D. Diana, Thomas R. Bailey
  • Pyridinyl-quinolone compounds, their preparation and use
    Patent number: 5169853
    Abstract: Fluorinated 1- cyclopropyl-7-(substituted-pyridinyl)-1,4-dihydro-4-oxo-3-quinolinecarboxy lic acids of the formula ##STR1## wherein R is hydrogen, R' and R" are hydrogen or fluoro, and Z is 3- or 4-pyridinyl substituted by alkyl groups or substituted alkyl groups, are superior antibacterial agents. They are prepared via a coupling reaction between the corresponding esters (R=alkyl) having a halo group in the 7-position and a substituted (trialkylstannyl)-pyridine.
    Type: Grant
    Filed: September 9, 1991
    Date of Patent: December 8, 1992
    Assignee: Sterling Drug Inc.
    Inventors: George Y. Lesher, Baldev Singh, Michael Reuman, Sol J. Daum
  • 5-Quinolinylpyridinones, cardiotonic compositions and methods
    Patent number: 5141931
    Abstract: 6-Alkyl-5-(6, or 7-quinolinyl)-3-(substituted)-2(1H)-pyridinones useful as cardiotonics are synthesized by reaction of trialkylquinolinylstannanes with 6-alky-5-halo-3-(substituted)-2(1H)-pyridinones. Compositions containing these pyridinones and methods of using them to treat congestive heart failure are provided.
    Type: Grant
    Filed: January 3, 1991
    Date of Patent: August 25, 1992
    Assignee: Sterling Winthrop Inc.
    Inventor: Edward R. Bacon
  • Proteolytic enzyme inhibition method
    Patent number: 5128339
    Abstract: 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl aryl carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with an arylcarboxylic acid in the presence of an acid-acceptor.
    Type: Grant
    Filed: October 24, 1991
    Date of Patent: July 7, 1992
    Assignee: Sterling Winthrop Inc.
    Inventors: Richard P. Dunlap, Neil W. Boaz, Albert J. Mura, Virendra Kumar, Chakrapani Subramanyam, Ranjit C. Desai, Dennis J. Hlasta, Manohar T. Saindane, Malcolm R. Bell, John J. Court
  • Anti-glaucoma compositions containing 2- and 3-aminomethyl-6-arylcarbonyl- or 6-phenylthio-2,3-dihydropyrrolo-(1,2,3-de)-1,4-benzoxazines and method of use thereof
    Patent number: 5112820
    Abstract: Antiglaucoma compositions containing 2- and 3-aminomethyl-6-arylcarbonyl- or 6-phenylthio-2,3-dihydropyrrolo-[1,2,3-de]-1,4-benzoxazines as the active component thereof and the method of use thereof in the treatment of glaucoma.
    Type: Grant
    Filed: March 5, 1990
    Date of Patent: May 12, 1992
    Assignee: Sterling Drug Inc.
    Inventor: Susan J. Ward
  • 1,3,4-oxadiazolyl-phenoxyalkylisoxazoles and their use as antiviral agents
    Patent number: 5110821
    Abstract: Compounds of the formula ##STR1## wherein: Y is an alkylene bridge of 3-9 carbon atoms;R' is lower-alkyl or hydroxy-lower-alkyl or 1-5 carbon atoms;R.sub.1 and R.sub.2 are hydrogen, halogen, lower-alkyl, lower-alkoxy, nitro, lower-alkoxycarbonyl or trifluoromethyl; andR.sub.8 is hydrogen or lower-alkyl of 1-5 carbon atoms, with the proviso that when R.sub.8 is hydrogen R' is hydroxy-lower-alkyl,are useful as antiviral agents, particularly against picornaviruses, including numerous strains of rhinovirus.
    Type: Grant
    Filed: June 7, 1990
    Date of Patent: May 5, 1992
    Assignee: Sterling Drug Inc.
    Inventor: Guy D. Diana