Patents Represented by Attorney Paul E. Dupont
  • Patent number: 5616584
    Abstract: A method of using 1,2,4-benzotriazine oxides, some of which are novel compounds, as radiosensitizers and selective cytotoxic agents is disclosed. These compounds are shown to specifically radiosensitize hypoxic tumor cells. Some are additionally disclosed no be useful as specific cytotoxic agents for these cells. They also show an unexpected ability to radiosensitize aerobic cells following or preceding a hypoxic incubation of the cells with the drug. This provides a basis for selective radiosensitization of tumors compared to normal cells. A novel method for preparing the 1,2,4-benzotriazine oxides is also disclosed.
    Type: Grant
    Filed: January 26, 1995
    Date of Patent: April 1, 1997
    Assignee: SRI International
    Inventors: William W. Lee, J. Martin Brown, Edward W. Grange, Abelardo P. Martinez
  • Patent number: 5614530
    Abstract: Substituted N-arylmethyl and heterocyclylmethyl-1H-pyrazolo[3,4-b]quinolin-4-amines, pharmaceutical compositions containing them and methods for a) effecting c-GMP-phosphodiesterase inhibition, b) treating heart failure and/or hypertension, c) reversing or reducing nitrate-induced tolerance and d) treating angina pectoris, congestive heart disease and myocardial infarction utilizing them.
    Type: Grant
    Filed: March 10, 1995
    Date of Patent: March 25, 1997
    Assignee: Sterling Winthrop Inc.
    Inventors: Virendra Kumar, John A. Dority, Jr.
  • Patent number: 5607933
    Abstract: 2--R.sub.2 --R.sub.4 -substituted-3--R.sub.3 --CO--1--[(C-attached-N-heteryl)-(Alk).sub.n ]--1H-indoles useful as analgesic, anti-rheumatic, anti-inflammatory or anti-glaucoma agents.
    Type: Grant
    Filed: March 16, 1994
    Date of Patent: March 4, 1997
    Assignee: Sterling Winthrop Inc.
    Inventors: Thomas E. D'Ambra, Edward R. Bacon, Malcolm R. Bell, Susan J. Ward
  • Patent number: 5604224
    Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: February 18, 1997
    Assignee: Sterling Winthrop Inc.
    Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
  • Patent number: 5602154
    Abstract: 2-(2,3,5,6-Tetrafluoro-4-pyridyl)-1,2,5-thiadiazolidin-3-one 1,1-dioxides, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: February 11, 1997
    Assignee: Sanofi Winthrop, Inc.
    Inventor: Ranjit C. Desai
  • Patent number: 5597841
    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: May 19, 1995
    Date of Patent: January 28, 1997
    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, Robert P. Farrell
  • Patent number: 5597582
    Abstract: Disclosed are anticancer tumor soft gelatin capsules comprising a 1,2,4-benzotriazine oxide and an oily excipient selected from the group consisting of soybean oil and fractionated coconut oil.
    Type: Grant
    Filed: September 12, 1995
    Date of Patent: January 28, 1997
    Assignee: Sanofi
    Inventors: Stephen Brown, Ross Blundell
  • Patent number: 5596012
    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: May 24, 1995
    Date of Patent: January 21, 1997
    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
  • Patent number: 5585486
    Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is (CR.sub.5 R.sub.6).sub.n, (CR.sub.5 R.sub.6).sub.n,-aryl, (CR.sub.5 R.sub.6).sub.n -heteroaryl, X-(CR.sub.5 R.sub.6).sub.n, X-(CR.sub.5 R.sub.6).sub.n -aryl or X-(CR.sub.5 R.sub.6).sub.n -heteroaryl wherein aryl and heteroaryl may be optionally substituted;X is 0 or NR.sub.5 ;R.sub.5 and R.sub.6 are independently H or lower alkyl;R.sub.2 is H, halo, lower alkyl or (CR.sub.5 R.sub.6).sub.n -aryl;R.sub.3 and R.sub.4 are independently H or alkyl;A is a D or L isomer of an amino acid selected from the group consisting of alanine, valine, leucine, isoleucine, proline, phenylalanine, glycine, tyrosine, methionine, asparagine, glutamine, aspartic acid, glutamic acid, lysine, arginine, histidine and .beta.-thienylalanine;Z is CH.sub.2 or O; andn is 0-4;pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1.beta.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: December 17, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: Roland E. Dolle, Todd L. Graybill, Gary J. Speier, Catherine P. Prouty, Stanley J. Schmidt
  • Patent number: 5585357
    Abstract: Compounds which inhibit interleukin-1.beta. protease activity, pharmaceutical compositions containing the compounds and methods using the compounds are provided. The compounds have the formula ##STR1## wherein n is 0-2; each AA is independently L-valine or L-alanine; R.sub.1 is selected from the group consisting of N-[4-(N,N-dimethylaminomethyl)]benzoyl, N-benzyloxycarbonyl, N-methyl-N-[4-(pyridyl)methyl], N-[4-(pyridyl)methyl]carbonyl, N-3-(piperidinopropionyl), N-[4-(morpholinoethoxy)benzoyl, N-2-(quinuclidinyl)carbonyl, N-(3-pyridyl)methoxy carbonyl, N-(2-pyridyl)methoxy carbonyl, N-methyl-N-benzyl carbonyl, N-methyl-N-[2-(4-pyridyl)ethyl]carbonyl, and N-(N-phenylpiperazino)carbonyl; and R.sub.8, R.sub.9, R.sub.10 are each independently hydrogen, lower alkyl, halo substituted methyl, carbalkoxy, benzyl, phenyl, or phenyl mono or disubstituted with fluoro, nitro, methoxy, chloro, trifluoromethyl or methanesulfonyl.
    Type: Grant
    Filed: January 29, 1996
    Date of Patent: December 17, 1996
    Assignee: Sanofi Winthrop Inc.
    Inventors: Roland E. Dolle, Jasbir Singh, David A. Whipple, Catherine Prouty, Prasad V. Chaturvedula, Stanley J. Schmidt, Mohamed M. A. Awad, Denton W. Hoyer, Tina M. Ross
  • Patent number: 5578623
    Abstract: Compounds having the structural formula ##STR1## wherein L is O;L-R.sup.1 is a leaving group, H-L-R.sup.1 is the conjugate acid thereof and H-L-R.sup.1 has a pK.sub.a value less than or equal to to 8;R.sup.2 is primary or secondary alkyl of two to four carbon atoms, primary alkylamino of one to three carbon atoms, primary alkylmethylamino of two to four carbon atoms, diethylamino or primary alkoxy of one to three carbon atoms; andR.sup.3 is from one to three of a variety of substituents at any or all of the 5-, 6- and 7-positions;or a pharmaceutically acceptable acid addition salt thereof if the compound has a basic functional group or a pharmaceutically acceptable acid addition salt thereof if the compound has an acidic functional group,which inhibit the enzymatic activity of proteolytic enzymes, and processes for preparation thereof, method of use thereof in treatment of degenerative diseases and pharmaceutical compositions thereof are disclosed.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: November 26, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: Richard P. Dunlap, Albert J. Mura, Dennis J. Hlasta, Ranjit C. Desai, Lee H. Latimer, Chakrapani Subramanyam
  • Patent number: 5578601
    Abstract: Disclosed are nonpeptides having bradykinin antagonist activity of the formulae (I) and (II) ##STR1## or a pharmaceutically acceptable salt thereof therefor.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: November 26, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: Peter R. Seoane, Joseph M. Salvino, Brent D. Douty, Mohamed M. A. Awad, Roland E. Dolle, David G. Sawutz, David M. Faunce, Wayne T. Houck
  • Patent number: 5576427
    Abstract: Compounds of formula I; ##STR1## wherein R.sup.1 is hydrogen, or a blocking group that is compatible with oligonucleotide synthesis;R.sup.2 is hydrogen, nitro, lower alkyl amino, diloweralkyl amino or methyl;R.sup.3 is hydrogen or --P(R.sup.4)OR.sup.5 ;R.sup.4 is chlorine, 4-nitroimidazole, imidazole, tetrazole, triazole or di(lower-alkyl)amino-;R.sup.5 is methyl, 2-cyanoethyl or 2,2,2-trichloroethyl;n is from 0 to 2X is oxygen, sulfur, or --NR.sup.6 ;R.sup.6 is hydrogen or lower alkyl;Q is chosen from the group consisting of ##STR2## R.sup.7 is lower-alkyl or loweralkyloxy methylene; and R.sup.8 is hydrogen, benzoyl, anisoyl, or lower-alkyl carbonyland its pharmaceutically acceptable addition salts are nucleotide analogs. Modified oligonucleotides containing the nucleoside analogs of formula I are stable to nuclease degradation and are useful in inhibiting gene expression, in sequencing, and in mutagenesis.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: November 19, 1996
    Assignee: Sterling Winthrop, Inc.
    Inventors: Philip D. Cook, Daniel J. Delecki, Charles Guinosso
  • Patent number: 5573514
    Abstract: This invention relates to a holder for use in combination with a pre-filled cartridge-needle unit, the holder comprising a hollow body sized for housing the cartridge-needle unit therein, and means for permitting the body to move axially relative to the cartridge-needle unit. In one preferred embodiment, the distal end of the body is elliptical in cross section and the proximal end of the body is circular in cross section. In another preferred embodiment, the body comprises a pair of cam slots at the distal end and a pair or retaining slots at the proximal end, the slots being sized to accept a circumferential ring on the cartridge-needle unit and positioned to hold the cartridge-needle units in use and safe positions. The holder is easier to use and manufacture and reduces the susceptibility of health care workers to accidental needle strikes.
    Type: Grant
    Filed: March 4, 1996
    Date of Patent: November 12, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: Mark A. Stiehl, William A. Bergstresser, John J. Niedospial
  • Patent number: 5569655
    Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.
    Type: Grant
    Filed: July 29, 1994
    Date of Patent: October 29, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
  • Patent number: 5567810
    Abstract: Compounds, compositions and methods for inhibiting gene expression are disclosed. The compounds comprise oligonucleotide sequences of from about 9 to about 200 bases having a diol at either or both termini. Preferred diols are polyalkyleneglycols, preferably polyethyleneglycols. Pharmaceutical compositions comprising the compounds and a physiologically acceptable carrier and methods of inhibiting gene expression in mammals comprising administering such compounds are also provided. Methods for inhibiting nuclease cleavage of compounds are also provided.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: October 22, 1996
    Assignee: Sterling Drug, Inc.
    Inventors: Alexander L. Weis, Fred T. Oakes, Frederick H. Hausheer, Paul F. Cavanaugh, Jr., Patricia S. Moskwa
  • Patent number: 5567719
    Abstract: The invention pertains to heterocycle substituted phenoxyalkylheterocycles of the formula ##STR1## wherein Thi, Y, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification, or a pharmaceutically acceptable salt thereof which are effective antipicornaviral agents.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 22, 1996
    Assignee: Sterling Winthrop, Inc.
    Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Theodore J. Nitz
  • Patent number: 5567717
    Abstract: A compound of the formula ##STR1## wherein Y, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined in the specification.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: October 22, 1996
    Assignee: Sterling Winthrop, Inc.
    Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Theodore J. Nitz
  • Patent number: 5565430
    Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukinprotease activity. The compounds, .alpha.-substituted acetamides a ##STR1## wherein: R.sub.2 =H or alkyl;R.sup.3 =halo, O(CO).sub.0-1 aryl, OPOR.sup.4 R.sup.5 ; ##STR2## where R.sup.4 and R.sup.5 =aryl;R.sup.6 =H, aryl or aralkyl;R.sup.7 =independently selected from R.sup.6, CF.sub.3 and CF.sub.2 CF.sub.3 ;R.sup.1 =R.sup.6 -CO, heteroaryl-CO, heteroaralkyl-CO and amino acid.
    Type: Grant
    Filed: August 2, 1994
    Date of Patent: October 15, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: Roland E. Dolle, Todd L. Graybill
  • Patent number: 5563163
    Abstract: 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl heterocyclic carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with either a heterocyclic carboxylic acid in the presence of an acid-acceptor or the alkali metal salt of a heterocyclic carboxylic acid.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: October 8, 1996
    Assignee: Sterling Winthrop, Inc.
    Inventors: Richard P. Dunlap, Dennis J. Hlasta, Ranjit C. Desai, Lee H. Latimer, Chakrapani Subramanyam, John J. Court, Malcolm R. Bell, Virendra Kumar