Patents by Inventor Michael S. Malamas

Michael S. Malamas 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).

  • Alkylidene analogs of 1'-amino-2-[(benzothiazolyl)-methyl]spiro [isoquinoline-4(1H),3'-pyrrolidine]-1,2',3,5'(2H)-tetrones useful as aldose reductase inhibitors
    Patent number: 5189167
    Abstract: This invention relates to alkylidene analogs of 1'-amino-2-[(benzothiazolyl)-methyl]spiro[isoquinoline-4(1H),3'-pyrrolidon e]-1,2',3,5'(2H)-tetrones represented by formula (I): ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen, alkyl containing 1 to 6 carbon atoms, halogen, lower alkoxy containing 1 to 6 carbon atoms, trifluoromethyl or nitro;R.sup.4 and R.sup.5 are independently hydrogen, alkyl containing 1 to 6 carbon atoms, aryl, aryl (lower alkyl) wherein aryl contains 6 to 10 carbon atoms and lower alkyl contains 1 to 6 carbon atoms, or R.sup.4 and R.sup.5 are joined to form alicyclic or heterocyclic rings selected from the group consisting of ##STR2## wherein n=1-10; ##STR3## wherein X=O, S, SO, SO.sub.2 ; ##STR4## wherein X=O, S; and ##STR5## wherein R.sup.
    Type: Grant
    Filed: November 25, 1991
    Date of Patent: February 23, 1993
    Assignee: American Home Products Corporation
    Inventor: Michael S. Malamas
  • Process and intermediates for the preparation of spiro[isoquinoline-4(1H),3-pyrrolidine]1,2,3,5 (2H)-tetrones which are useful as aldose reductase inhibitors
    Patent number: 5169948
    Abstract: This invention relates to a process for producing spiro-isoquinolinepyrrolidines. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes mellitus associated complications.
    Type: Grant
    Filed: January 2, 1992
    Date of Patent: December 8, 1992
    Assignee: American Home Products Corporation
    Inventor: Michael S. Malamas
  • Spiro-lactams and analogs thereof useful as aldose reductase inhibitors
    Patent number: 5130425
    Abstract: This invention relates to spiro-lactams and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes mellitus associated complications.
    Type: Grant
    Filed: July 12, 1991
    Date of Patent: July 14, 1992
    Assignee: American Home Products Corporation
    Inventor: Michael S. Malamas
  • Process and intermediates for the preparation of spiro(isoquinoline-4(1H), 3'-pyrrolidine)-1,2', 3,5'(2H)-tetrones which are useful as aldose reductase inhibitors
    Patent number: 5106978
    Abstract: The invention relates to a process for producing spiro-isoquinoline pyrrolidines. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes mellitus associated complications.
    Type: Grant
    Filed: May 22, 1991
    Date of Patent: April 21, 1992
    Assignee: American Home Products Corporation
    Inventor: Michael S. Malamas
  • 1'-aminospiro[isoquinoline-4(1H),3'-pyrrolidine]-1,2',3,5'(2H)-tetrones and analogs thereof useful as aldose reductase inhibitors
    Patent number: 5102886
    Abstract: This invention relates to 1'-aminospiro[isoquinoline-4(1H),3'-pyrrolidine]-1,2',3,5'(2H)-tetrones of structural formula (I) ##STR1## wherein: R.sup.1 and R.sup.2 are independently hydrogen, alkyl containing 1 to 6 carbon atoms, halogen, lower alkoxy containing 1 to 6 carbon atoms, trifluoromethyl, nitro, aryl or aryl(lower alkyl)oxy wherein aryl contains 6 to 10 carbon atoms and lower alkyl contains 1 to 6 carbon atoms;R.sup.3 is lower alkyl containing 1 to 6 carbon atoms, aryl, aryl(lower alkyl) or dihalogen substituted aryl (lower alkyl) wherein aryl contains 6 to 10 carbon atoms and lower alkyl contains 1 to 6 carbon atoms;R.sup.4 and R.sup.
    Type: Grant
    Filed: October 12, 1990
    Date of Patent: April 7, 1992
    Assignee: American Home Products Corporation
    Inventor: Michael S. Malamas
  • Spiro-isoquinoline-pyrrolidines and analogs thereof useful as aldose reductase inhibitors
    Patent number: 5093496
    Abstract: This invention relates to spiro-isoquinoline-pyrrolidines and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneificial for the prevention or treatment of diabetes mellitus associated complications.
    Type: Grant
    Filed: April 4, 1991
    Date of Patent: March 3, 1992
    Assignee: American Home Products Corporation
    Inventor: Michael S. Malamas
  • Spiro-pyridazines and analogs thereof useful as aldose reductase inhibitors
    Patent number: 5081241
    Abstract: This invention relates to spiro-pyridazines, to processes for their preparation, to methods for using the compounds, and to pharmaceutical prepartions thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes mellitus associated complications.
    Type: Grant
    Filed: October 11, 1990
    Date of Patent: January 14, 1992
    Assignee: American Home Products Corporation
    Inventor: Michael S. Malamas
  • Alkylidene analogs of 1'-aminospiro[isoquinoline-4(1H),3'-pyrrolidine]-1,2',3,5'(2H)-tetrones useful as aldose reductase inhibitors
    Patent number: 5068332
    Abstract: This invention relates to alkylidene analogs of 1'-aminospiro[isoquinoline-4(1H),3'-pyrrolidine]-1,2',3,5'(2H)-tetrones, represented by formula (I): ##STR1## to processes for the preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes mellitus associated complications.
    Type: Grant
    Filed: October 11, 1990
    Date of Patent: November 26, 1991
    Assignee: American Home Products Corporation
    Inventor: Michael S. Malamas
  • N'-alkyl-spiro-isoquinoline-pyrrolidine tetrones and analogs thereof useful as aldose reductase inhibitors
    Patent number: 5045544
    Abstract: This invention relates to N'-alkyl-spiro-isoquinoline-pyrrolidine tetrones and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical perparations thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes melitus associated complications.
    Type: Grant
    Filed: May 21, 1990
    Date of Patent: September 3, 1991
    Assignee: American Home Products Corporation
    Inventor: Michael S. Malamas
  • Spiro-isoquinoline-pyrrolidines and analogs thereof useful as aldose reductase inhibitors
    Patent number: 5037831
    Abstract: This invention relates to spiro-isoquinoline-pyrrolidines and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes mellitus associated complications.
    Type: Grant
    Filed: May 21, 1990
    Date of Patent: August 6, 1991
    Assignee: American Home Products Corporation
    Inventor: Michael S. Malamas
  • N-[[6 -methoxy-5-(trifluoromethyl)-1-naphthalenyl]-thioxomethyl]-N-methylglycin e S-oxide and the amide thereof
    Patent number: 4994381
    Abstract: Disclosed herein are N-[[6-methoxy-5-(trifluoromethyl)-1-naphthalenyl]-thioxmethyl]-N-methylgly cine S-oxide (tolrestat S-oxide) and the amine thereof and methods of their preparation. The S-oxides are new aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.
    Type: Grant
    Filed: March 20, 1989
    Date of Patent: February 19, 1991
    Assignee: American Home Products Corporation
    Inventors: Eckhardt S. Ferdinandi, Michael S. Malamas, Kazimir Sestanj, Surendra N. Sehgal
  • Isoquinoline acetic acids and acetyl carbamates useful as aldose reductase inhibitors
    Patent number: 4983613
    Abstract: This invention relates to isoquinoline acetic acids and acetyl carbamates and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the treatment of diabetes mellitus and associated conditions.
    Type: Grant
    Filed: April 21, 1989
    Date of Patent: January 8, 1991
    Assignee: American Home Products Corporation
    Inventor: Michael S. Malamas
  • Spiro-isoquinoline-pyrrolidine tetrones and analogs thereof useful as aldose reductase inhibitors
    Patent number: 4927831
    Abstract: This invention relates to spiro-isoquinoline-pyrrolidine tetrones and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention of diabetes mellitus associated complications.
    Type: Grant
    Filed: May 26, 1989
    Date of Patent: May 22, 1990
    Assignee: American Home Products
    Inventor: Michael S. Malamas
  • N-[[6-methoxy-5-(trifluoromethyl)-1-naphthalenyl]-thioxomethyl]-N-methylg lycine S-oxide and the amide thereof
    Patent number: 4853484
    Abstract: Disclosed herein are N-[[6-methoxy-5-(trifluoromethyl)-1-naphthalenyl]thioxomethyl]-N-methylgly cine S-oxide (tolrestat S-oxide) and the amide thereof and methods of their preparation. The S-oxides are new aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.
    Type: Grant
    Filed: October 28, 1987
    Date of Patent: August 1, 1989
    Assignee: American Home Products Corporation
    Inventors: Eckhardt S. Ferdinandi, Michael S. Malamas, Kazimir Sestanj, Surendra N. Sehgal
  • Naphthalenylsulfonylimidazolidinediones and their thioxo analogs useful as aldose reductase inhibitors
    Patent number: 4743611
    Abstract: Disclosed herein are naphthalenylsulfonylimidazolidinediones and their thioxo analogs and methods for their preparation. The compounds are new aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.
    Type: Grant
    Filed: February 9, 1987
    Date of Patent: May 10, 1988
    Assignee: American Home Products Corp.
    Inventors: Michael S. Malamas, Kazimir Sestanj
  • N-[[6-methoxy-5-(trifluoromethyl)-1-naphthalenyl]-thioxome thyl]-N-methylglycine S-oxide and the amide thereof
    Patent number: 4734435
    Abstract: Disclosed herein are N-[[6-methoxy-5-(trifluoromethyl)-1-naphthalenyl]-thioxomethyl]-N-methylgl ycine S-oxide (tolrestat S-oxide) and the amide thereof and methods of their preparation. The S-oxides are new aldose reductase inhibitors useful for the treatment of prevention of diabetic complications.
    Type: Grant
    Filed: November 25, 1986
    Date of Patent: March 29, 1988
    Assignee: American Home Products Corp.
    Inventors: Eckhardt S. Ferdinandi, Michael S. Malamas, Kazimir Sestanj, Surendra N. Sehgal