Patents by Inventor Dennis J. Hlasta

Dennis J. Hlasta has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • 2-saccharinylmethyl aryl carboxylates useful as proteolytic enzyme inhibitors and compositions and method of use thereof
    Patent number: 5512589
    Abstract: A compound having the formula: ##STR1## wherein Ar, R.sup.4 and R.sup.5 are defined herein have pharmaceutical utility as proteolytic enzyme inhibitors.
    Type: Grant
    Filed: September 3, 1993
    Date of Patent: April 30, 1996
    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
  • 2-substituted 1,2,5,-thiadiazolidin-3-one 1,1-dioxides and compositions and method of use thereof
    Patent number: 5512576
    Abstract: 2-Substituted 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: December 2, 1994
    Date of Patent: April 30, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: Ranjit C. Desai, Dennis J. Hlasta
  • 2-heterocyclyloxymethyl and 2-heterocyclylthiomethyl-1,2,5-thiadiazolidin-3-one 1,1-dioxides and compositions and method of use thereof
    Patent number: 5494925
    Abstract: 2-Heterocyclyloxymethyl and 2-heterocyclylthiomethyL-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: December 2, 1994
    Date of Patent: February 27, 1996
    Assignee: Sterling Winthrop Inc.
    Inventors: John J. Court, Ranjit C. Desai, Dennis J. Hlasta
  • 2-saccharinylmethyl heterocyclic carboxylates useful as proteolytic enzyme inhibitors and compositions and method of use thereof
    Patent number: 5488062
    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: August 9, 1994
    Date of Patent: January 30, 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
  • Saccharin derivative proteolytic enzyme inhibitors
    Patent number: 5466701
    Abstract: Compounds having the structural formula ##STR1## 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: June 22, 1994
    Date of Patent: November 14, 1995
    Assignee: Sterling Winthrop Inc.
    Inventors: Dennis J. Hlasta, James H. Ackerman, Albert J. Mura, Ranjit C. Desai
  • Saccharin derivative proteolytic enzyme inhibitors
    Patent number: 5464852
    Abstract: Compounds having the structural formula ##STR1## wherein L is N, O or SO.sub.n wherein n is 0, 1 or 2;L--R.sup.1 is a leaving group, H--L--R.sup.1 is the conjugate acid thereof and,when L is N, H--L--R.sup.1 has a pK.sub.a value less than or equal to 6, when L is O, H--L--R.sup.1 has a pK.sub.a value less than or equal to to 8, and when L is SO.sub.n, H--L--R.sup.1 has a pK.sub.a value less than or equal to 5;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.
    Type: Grant
    Filed: August 11, 1994
    Date of Patent: November 7, 1995
    Assignee: Sterling Winthrop Inc.
    Inventors: Richard P. Dunlap, Albert J. Mura, Dennis J. Hlasta, Ranjit C. Desai, Lee H. Latimer, Chakrapani Subramanyam
  • Saccharin derivative proteolytic enzyme inhibitors
    Patent number: 5380737
    Abstract: Compounds having the structural formula ##STR1## wherein L is N, O or SO.sub.n wherein n is 0, 1 or 2;L-R.sup.1 is a leaving group, H-L-R.sup.1 is the conjugate acid thereof and, when L is N, H-L-R.sup.1 has a pK.sub.a value less than or equal to 6, when L is O, H-L-R.sup.1 has a pK.sub.a value less than or equal to to 8, and when L is SO.sub.n, H-L-R.sup.1 has a pK.sub.a value less than or equal to 5;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.
    Type: Grant
    Filed: August 27, 1993
    Date of Patent: January 10, 1995
    Assignee: Sterling Winthrop Inc.
    Inventors: Richard P. Dunlap, Albert A. Mura, Dennis J. Hlasta, Ranjit C. Desai, Lee H. Latimer, Chakrapani Subramanyam
  • Saccharin derivative proteolytic enzyme inhibitors
    Patent number: 5378720
    Abstract: Compounds having the structural formula ##STR1## 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 25, 1993
    Date of Patent: January 3, 1995
    Assignee: Sterling Winthrop Inc.
    Inventors: Dennis J. Hlasta, James H. Ackerman, Albert J. Mura, Ranjit C. Desai
  • Use of saccharin derivatives as proteolytic enzyme inhibitors
    Patent number: 5371074
    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 0010wherein: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 substitued 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; and R.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, 1993
    Date of Patent: December 6, 1994
    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
  • 2-saccharinylmethyl phosphates, phosphonates and phosphinates useful as proteolytic enzyme inhibitors and compositions and method of use thereof
    Patent number: 5296496
    Abstract: 4-R.sub.1 -R.sub.2 -R.sub.3 -2-Saccharinylmethyl and 4,7-C-4,5,6,7-tetrahydro-2-saccharinylmethyl phosphates, phosphonates and phosphinates of formulas I 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 8, 1992
    Date of Patent: March 22, 1994
    Assignee: Sterling Winthrop Inc.
    Inventors: Ranjit C. Desai, John J. Court, Dennis J. Hlasta
  • 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
  • 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
  • 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
  • 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
  • Antidepressant 2-(4,5-dihydro-1H-imidazolyl)-dihydro-1H-indoles, -1,2,3,4-tetrahydroquinolines and -1H-indoles, and methods of use thereas
    Patent number: 5017584
    Abstract: 2-(4,5-Dihydro-1H-imidazol-2-yl)-2,3-dihydro-1H-indoles, 2-(4,5-dihydro-1H-imidazol-2-yl)-1,2,3,4-tetrahydroquinolines and 2-(4,5-dihydro-1H-imidazol-2-yl)-1H-indoles, useful as antidepressant agents, are prepared by reacting a respective lower-alkyl 2,3-dihydro-1H-indole-2-carboxylate 1,2,3,4-tetrahydroquinoline-2-carboxylate or 1H-indole-2-carboxylate derivative with ethylenediamine or an N-lower-alkylethylenediamine in the presence of a Lewis-type acid.
    Type: Grant
    Filed: November 27, 1985
    Date of Patent: May 21, 1991
    Assignee: Sterling Drug Inc.
    Inventor: Dennis J. Hlasta